RU2021107754A - ТЕТРАГИДРО-1H-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА - Google Patents
ТЕТРАГИДРО-1H-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА Download PDFInfo
- Publication number
- RU2021107754A RU2021107754A RU2021107754A RU2021107754A RU2021107754A RU 2021107754 A RU2021107754 A RU 2021107754A RU 2021107754 A RU2021107754 A RU 2021107754A RU 2021107754 A RU2021107754 A RU 2021107754A RU 2021107754 A RU2021107754 A RU 2021107754A
- Authority
- RU
- Russia
- Prior art keywords
- compound
- cancer
- hydrogen
- pharmaceutically acceptable
- acceptable salt
- Prior art date
Links
- 230000001833 anti-estrogenic effect Effects 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- 239000000328 estrogen antagonist Substances 0.000 title 1
- 238000000034 method Methods 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 238000001356 surgical procedure Methods 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 229940122815 Aromatase inhibitor Drugs 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 239000003886 aromatase inhibitor Substances 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 238000009261 endocrine therapy Methods 0.000 claims 1
- 229940034984 endocrine therapy antineoplastic and immunomodulating agent Drugs 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 206010046885 vaginal cancer Diseases 0.000 claims 1
- 208000013139 vaginal neoplasm Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/475—Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (39)
1. Способ предотвращения рецидива рака у пациента, включающий введение пациенту соединения Формулы I:
I
или его фармацевтически приемлемой соли,
где
X является -O-;
каждый R1 и R2 является водородом;
каждый R3 и R4 независимо выбран из водорода и галогена, и когда один из R3 или R4 является галогеном, другой из R3 или R4 является водородом;
R5 является C1-C6алкилом или C1-C6галогеналкилом;
R6 является C1-C6галогеналкилом; и
каждый R7 и R8 независимо выбран из водорода и C1-C6алкила.
2. Способ по п. 1, где рак выбран из рака молочной железы, рака яичника, рака эндометрия, рака влагалища, рака легкого, рака кости, рака матки и эндометриоза.
3. Способ по п. 1, где соединение вводят в качестве вспомогательной терапии после или вместо химиотерапии, радиации или хирургии.
4. Способ по п. 3, где соединение вводят после хирургии.
5. Способ по п. 1, где соединение вводят до хирургии.
6. Способ по п. 2, где раком является рак молочной железы.
7. Способ по п. 6, где рак молочной железы прогрессировал в присутствии эндокринной терапии или терапии ингибитором ароматазы.
10. Способ по п. 1, где соединение является соединением Формулы I(a):
I(a)
или его фармацевтически приемлемой солью.
11. Способ по п. 10, где каждый R1, R2, R3 и R4 является водородом.
12. Способ по п. 1, где соединение является соединением Формулы I(c):
I(c)
или его фармацевтически приемлемой солью.
13. Способ по п. 12, где каждый R1, R2, R3 и R4 является водородом.
14. Способ по п. 1, где соединение представляет собой:
или его фармацевтически приемлемую соль.
15. Способ по п. 1, где соединение представляет собой:
или его фармацевтически приемлемую соль.
16. Способ по п. 1, где соединение представляет собой:
или его фармацевтически приемлемую соль.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562235900P | 2015-10-01 | 2015-10-01 | |
US62/235,900 | 2015-10-01 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2018115696A Division RU2745742C1 (ru) | 2015-10-01 | 2016-09-29 | ТЕТРАГИДРО-1Н-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА |
Publications (1)
Publication Number | Publication Date |
---|---|
RU2021107754A true RU2021107754A (ru) | 2021-04-01 |
Family
ID=58427985
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2018115696A RU2745742C1 (ru) | 2015-10-01 | 2016-09-29 | ТЕТРАГИДРО-1Н-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА |
RU2021107754A RU2021107754A (ru) | 2015-10-01 | 2016-09-29 | ТЕТРАГИДРО-1H-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2018115696A RU2745742C1 (ru) | 2015-10-01 | 2016-09-29 | ТЕТРАГИДРО-1Н-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА |
Country Status (26)
Country | Link |
---|---|
US (5) | US10292971B2 (ru) |
EP (2) | EP3355884B1 (ru) |
JP (3) | JP6776348B2 (ru) |
KR (2) | KR102710603B1 (ru) |
CN (2) | CN113248494A (ru) |
AU (3) | AU2016331065B2 (ru) |
BR (2) | BR112018006121B1 (ru) |
CA (1) | CA3000410A1 (ru) |
CL (1) | CL2018000827A1 (ru) |
CY (1) | CY1124669T1 (ru) |
DK (1) | DK3355884T3 (ru) |
ES (1) | ES2881398T3 (ru) |
HR (1) | HRP20211124T1 (ru) |
HU (1) | HUE055321T2 (ru) |
IL (3) | IL286518B2 (ru) |
LT (1) | LT3355884T (ru) |
MX (2) | MX2018003929A (ru) |
NZ (2) | NZ741130A (ru) |
PL (1) | PL3355884T3 (ru) |
PT (1) | PT3355884T (ru) |
RS (1) | RS62133B1 (ru) |
RU (2) | RU2745742C1 (ru) |
SI (1) | SI3355884T1 (ru) |
SM (1) | SMT202100433T1 (ru) |
UA (1) | UA122346C2 (ru) |
WO (1) | WO2017059139A1 (ru) |
Families Citing this family (35)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DK3233852T3 (da) | 2014-12-18 | 2020-09-14 | Hoffmann La Roche | Tetrahydro-pyrido[3,4-b]indoler som østrogenreceptormodulatorer og anvendelser deraf |
KR102710603B1 (ko) | 2015-10-01 | 2024-09-27 | 올레마 파마슈티컬스 인코포레이티드 | 테트라히드로-1H-피리도[3,4-b]인돌 항에스트로겐 약물 |
DK3386500T3 (da) | 2015-12-09 | 2022-12-12 | Univ Illinois | Benzothiophen-baserede selektive østrogenreceptor ned-regulatorer |
DK3411034T3 (da) * | 2016-02-05 | 2021-01-11 | Inventisbio Inc | Selektiv østrogenreceptornedbrydere og anvendelser deraf |
US10125135B2 (en) | 2016-04-20 | 2018-11-13 | Astrazeneca Ab | Chemical compounds |
US10149839B2 (en) | 2016-07-25 | 2018-12-11 | Astrazeneca Ab | Chemical compounds |
WO2018049042A1 (en) * | 2016-09-07 | 2018-03-15 | The Wistar Institute Of Anatomy And Biology | Methods and compositions for treating cancers by inhibiting estrogen signaling in myeloid-derived suppressor cells |
WO2018081168A2 (en) | 2016-10-24 | 2018-05-03 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective mixed estrogen receptor downregulators |
UA125824C2 (uk) | 2016-10-24 | 2022-06-15 | Астразенека Аб | 6,7,8,9-ТЕТРАГІДРО-3H-ПІРАЗОЛО[4,3-f]ІЗОХІНОЛІНОВІ ПОХІДНІ, ЗАСТОСОВНІ В ЛІКУВАННІ РАКУ |
NZ754865A (en) | 2017-01-06 | 2023-07-28 | G1 Therapeutics Inc | Combination therapy for the treatment of cancer |
AU2018211495B2 (en) | 2017-01-30 | 2020-05-21 | Astrazeneca Ab | Estrogen receptor modulators |
AU2018217809A1 (en) | 2017-02-10 | 2019-08-22 | G1 Therapeutics, Inc. | Benzothiophene estrogen receptor modulators |
CN110343101B (zh) * | 2018-04-04 | 2022-07-12 | 青岛福沃药业有限公司 | 用于治疗乳腺癌的雌激素受体降解剂 |
LT3810283T (lt) | 2018-06-21 | 2023-08-25 | F. Hoffmann-La Roche Ag | 3-((1r,3r)-1-(2,6-difluor-4-((1-(3-fluorpropil)azetidin-3- il)amino) fenil)-3-metil-1,3,4,9-tetrahidro-2h-pirido[3,4-b]indol-2-il)- 2,2- difluorpropan-1-olio tartrato druskos kietosios formos, jų paruošimo procesas ir jų naudojimo būdai vėžiui gydyti |
JP7524506B2 (ja) | 2018-10-15 | 2024-07-30 | トーヨーカネツ株式会社 | 搬送情報システム、プログラム、及び記録媒体 |
MX2021007687A (es) | 2018-12-24 | 2021-10-13 | Inventisbio Co Ltd | Sales novedosas de degradadores selectivos de receptores de estrogeno. |
JP2022532342A (ja) * | 2019-05-14 | 2022-07-14 | ニューベイション・バイオ・インコーポレイテッド | 抗がん核内ホルモン受容体標的化化合物 |
CA3144791A1 (en) * | 2019-07-07 | 2021-01-14 | Olema Pharmaceuticals, Inc. | Regimens of estrogen receptor antagonists |
EP4058464A1 (en) | 2019-11-13 | 2022-09-21 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
KR20220151616A (ko) | 2020-03-06 | 2022-11-15 | 올레마 파마슈티컬스 인코포레이티드 | 에스트로겐 수용체-연관 질환의 치료 방법 |
US11848549B2 (en) * | 2020-09-15 | 2023-12-19 | Easy Solar Products, Inc. | Junction box with flashing for a tile surface |
WO2022140744A1 (en) | 2020-12-23 | 2022-06-30 | Recurium Ip Holdings, Llc | Estrogen receptor modulators |
WO2022166983A1 (zh) * | 2021-02-08 | 2022-08-11 | 贝达药业股份有限公司 | 杂芳基并哌啶类衍生物及其药物组合物和应用 |
WO2022235585A1 (en) | 2021-05-03 | 2022-11-10 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
AU2022305957A1 (en) * | 2021-07-08 | 2024-01-25 | Olema Pharmaceuticals, Inc. | Methods of treating estrogen receptor-associated diseases |
WO2023091550A1 (en) * | 2021-11-18 | 2023-05-25 | Olema Pharmaceuticals, Inc. | Methods of treating estrogen receptor-associated diseases |
WO2023221123A1 (en) * | 2022-05-20 | 2023-11-23 | Olema Pharmaceuticals, Inc. | Crystalline forms of an estrogen receptor antagonist |
WO2023221122A1 (en) * | 2022-05-20 | 2023-11-23 | Olema Pharmaceuticals, Inc. | Salts and solid forms of an estrogen receptor antagonist |
WO2024033513A1 (en) | 2022-08-11 | 2024-02-15 | Diaccurate | Compounds for treating cancer |
AU2023324854A1 (en) | 2022-08-19 | 2025-01-30 | Olema Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
WO2024039860A1 (en) | 2022-08-19 | 2024-02-22 | Olema Pharmaceuticals, Inc. | 2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole derivatives as estrogen receptor modulators for the treatment of cancer |
AU2023324857A1 (en) | 2022-08-19 | 2025-01-30 | Olema Pharmaceuticals, Inc. | 2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole derivatives as estrogen receptor modulators for the treatment of cancer |
WO2024076626A1 (en) * | 2022-10-05 | 2024-04-11 | Olema Pharmaceuticals, Inc. | Methods of treating estrogen receptor-mediated disorders |
WO2024076633A1 (en) * | 2022-10-05 | 2024-04-11 | Olema Pharmaceuticals, Inc. | Methods of treating estrogen receptor-mediated disorders |
WO2024124182A1 (en) * | 2022-12-09 | 2024-06-13 | Olema Pharmaceuticals, Inc. | Dosage forms of an estrogen receptor antagonist |
Family Cites Families (69)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4418068A (en) | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
GB8327256D0 (en) | 1983-10-12 | 1983-11-16 | Ici Plc | Steroid derivatives |
TW366342B (en) | 1992-07-28 | 1999-08-11 | Lilly Co Eli | The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss |
US5478847A (en) | 1994-03-02 | 1995-12-26 | Eli Lilly And Company | Methods of use for inhibiting bone loss and lowering serum cholesterol |
ES2204932T3 (es) * | 1994-09-12 | 2004-05-01 | Eli Lilly And Company Limited | Moduladores serotonergicos. |
US5780497A (en) | 1996-04-19 | 1998-07-14 | American Home Products Corporation | 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents |
US5998402A (en) | 1996-04-19 | 1999-12-07 | American Home Products Corporation | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents |
US5880137A (en) | 1996-04-19 | 1999-03-09 | American Home Products Corporation | 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents |
TW397821B (en) | 1996-04-19 | 2000-07-11 | American Home Produits Corp | 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof |
US6005102A (en) | 1997-10-15 | 1999-12-21 | American Home Products Corporation | Aryloxy-alkyl-dialkylamines |
ID24568A (id) | 1997-11-06 | 2000-07-27 | American Home Prod | Kontrasepsi oral yang mengandung anti-estrogen plus progestin |
US6326392B1 (en) | 1997-11-06 | 2001-12-04 | American Home Products Corporation | Anti-estrogen plus progestin containing oral contraceptives |
US6479535B1 (en) | 1998-05-15 | 2002-11-12 | Wyeth | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations |
US6583170B1 (en) | 1998-05-15 | 2003-06-24 | Wyeth | 2-Phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol and estrogen formulations |
GB0000313D0 (en) | 2000-01-10 | 2000-03-01 | Astrazeneca Uk Ltd | Formulation |
CO5271709A1 (es) | 2000-01-12 | 2003-04-30 | Pfizer Prod Inc | Composiciones y procedimientos para el y tratamiento de afecciones que responden a estrogenos |
CO5271696A1 (es) | 2000-01-12 | 2003-04-30 | Pfizer Prod Inc | Procedimiento para reducir la morbilidad y el riesgo de mortalidad |
CO5271697A1 (es) | 2000-01-12 | 2003-04-30 | Pfizer Prod Inc | Composiciones y procedimientos para el tratamiento de afecciones que responden a un aumento de testosterona |
CO5251465A1 (es) | 2000-01-26 | 2003-02-28 | Pfizer Prod Inc | Composiciones y procedimientos para tratar la osteoporosis y reducir el colesterol |
US20020013327A1 (en) | 2000-04-18 | 2002-01-31 | Lee Andrew G. | Compositions and methods for treating female sexual dysfunction |
AU2001273144A1 (en) | 2000-07-06 | 2002-01-21 | Wyeth | Use of substituted indole compounds for treating neuropeptide y-related conditions |
BR0112365A (pt) | 2000-07-06 | 2003-05-13 | Wyeth Corp | Combinações de estatinas, agentes estrogênicos e opcionalmente estrogênios |
WO2002003976A2 (en) | 2000-07-06 | 2002-01-17 | Wyeth | Combinations of bisphosphonates, estrogenic agents and optionally estrogens |
AU7178301A (en) | 2000-07-06 | 2002-01-21 | American Home Prod | Methods for increasing nitric oxide synthase activity |
AR030064A1 (es) | 2000-07-06 | 2003-08-13 | Wyeth Corp | Metodos para inhibir los efectos uterotroficos de los agentes estrogenicos |
WO2002003986A2 (en) | 2000-07-06 | 2002-01-17 | Wyeth | Use of substituted indole compounds for treating breast disorders |
WO2002003990A2 (en) | 2000-07-06 | 2002-01-17 | Wyeth | Use of substituted insole compounds for treating excessive intraocular pressure |
WO2002003975A2 (en) | 2000-07-06 | 2002-01-17 | Wyeth | Combinations of ssri and estrogenic agents |
AU2001271781A1 (en) | 2000-07-06 | 2002-01-21 | Wyeth | Use of substituted indole compounds for treating sphincter incontinence |
AU2001271784A1 (en) | 2000-07-06 | 2002-01-21 | Wyeth | Therapy for prosthesis-related bone degeneration |
EP1177787A3 (en) | 2000-07-28 | 2003-09-10 | Pfizer Products Inc. | Use of an estrogen agonist/antagonist for treating cataracts |
JP2004507465A (ja) | 2000-08-11 | 2004-03-11 | ワイス | エストロゲン受容体陽性癌腫の治療方法 |
EP1192945A3 (en) | 2000-09-21 | 2004-03-03 | Pfizer Products Inc. | Use of an estrogen agonist/antagonist for treating osteoarthritis |
IL145838A (en) | 2000-10-16 | 2008-11-03 | Pfizer Prod Inc | Use of an estrogen agonist / antagonist to produce a drug for the treatment of vaginitis |
AU781168B2 (en) | 2001-01-26 | 2005-05-12 | Pfizer Products Inc. | Method of treating certain cancers using an estrogen agonist/antagonist |
HUP0500573A2 (hu) | 2001-08-11 | 2005-11-28 | Bristol-Myers Squibb Pharma Company | Trifenil-etilén származékok, mint szelektív ösztrogén receptor modulátorok és ezeket tartalmazó gyógyszerkészítmények |
WO2005080380A1 (en) | 2004-02-03 | 2005-09-01 | Eli Lilly And Company | Kinase inhibitors |
US8076352B2 (en) | 2004-03-15 | 2011-12-13 | Ptc Therapeutics, Inc. | Administration of carboline derivatives useful in the treatment of cancer and other diseases |
US7767689B2 (en) * | 2004-03-15 | 2010-08-03 | Ptc Therapeutics, Inc. | Carboline derivatives useful in the treatment of cancer |
JP4857452B2 (ja) * | 2004-03-15 | 2012-01-18 | ピーティーシー セラピューティクス,インコーポレーテッド | 血管新生の抑制に有用なカルボリン誘導体 |
US7745625B2 (en) | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
JP2008528496A (ja) | 2005-01-21 | 2008-07-31 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | エストロゲン受容体のモジュレーターとして有用な新規な複素環式ベンゾ[c]クロメン誘導体 |
RU58668U1 (ru) | 2006-06-05 | 2006-11-27 | Открытое акционерное общество "Нижегородский машиностроительный завод" | Водогрейный котел |
US20120157401A1 (en) | 2009-05-27 | 2012-06-21 | Ptc Therapeutics, Inc. | Methods for treating neurofibromatosis |
WO2010138706A1 (en) | 2009-05-27 | 2010-12-02 | Ptc Therapeutics, Inc. | Methods for treating breast cancer |
EP2434891B9 (en) | 2009-05-27 | 2021-05-05 | PTC Therapeutics, Inc. | Methods for treating cancer and non-neoplastic conditions |
PH12012502419A1 (en) | 2010-06-10 | 2022-03-21 | Seragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
US8853423B2 (en) | 2010-06-17 | 2014-10-07 | Seragon Pharmaceuticals, Inc. | Indane estrogen receptor modulators and uses thereof |
GB2483736B (en) | 2010-09-16 | 2012-08-29 | Aragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
CA2819299A1 (en) * | 2010-12-24 | 2012-06-28 | Merck Sharp & Dohme B.V. | N-substituted azetidine derivatives |
JP2015500346A (ja) | 2011-12-14 | 2015-01-05 | セラゴン ファーマシューティカルズ,インク. | エストロゲン受容体モジュレーターおよびその使用 |
BR112014014767A2 (pt) | 2011-12-16 | 2017-06-13 | Olema Pharmaceuticals Inc | novos compostos de benzopirano, composições e usos dos mesmos |
BR112015029455A8 (pt) | 2013-05-28 | 2020-03-17 | Astrazeneca Ab | compostos químicos, uso, métodos e composições para prevenção ou tratamento de câncer |
WO2014203129A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Combinations of benzopyran compounds, compositions and uses thereof |
MX2015017655A (es) | 2013-06-19 | 2016-04-15 | Seragon Pharmaceuticals Inc | Modulador de receptores de estrogeno y uso del mismo. |
WO2014203132A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Substituted benzopyran compounds, compositions and uses thereof |
KR20160021281A (ko) | 2013-06-19 | 2016-02-24 | 세라곤 파마슈티컬스, 인크. | 아제티딘 에스트로겐 수용체 조절제 및 이의 용도 |
BR112017008410A2 (pt) * | 2014-10-23 | 2017-12-19 | Oy Mtg Meltron Ltd | aparelho de iluminação para áreas perigosas |
CN107018652B (zh) * | 2014-10-31 | 2019-06-14 | 卡斯腾制造公司 | 高尔夫球杆头的沟槽和制作高尔夫球杆头的沟槽的方法 |
WO2016097073A1 (en) | 2014-12-18 | 2016-06-23 | F. Hoffmann-La Roche Ag | Derivatives of 2,3-diphenylchromene useful for the treatment of cancer |
DK3233852T3 (da) * | 2014-12-18 | 2020-09-14 | Hoffmann La Roche | Tetrahydro-pyrido[3,4-b]indoler som østrogenreceptormodulatorer og anvendelser deraf |
WO2016097071A1 (en) | 2014-12-18 | 2016-06-23 | F. Hoffmann-La Roche Ag | Estrogen receptor modulators and uses thereof |
WO2016174551A1 (en) | 2015-04-27 | 2016-11-03 | Pfizer Inc. | Anti-estrogenic compounds |
KR102710603B1 (ko) | 2015-10-01 | 2024-09-27 | 올레마 파마슈티컬스 인코포레이티드 | 테트라히드로-1H-피리도[3,4-b]인돌 항에스트로겐 약물 |
US20180002344A1 (en) | 2016-06-16 | 2018-01-04 | Genentech, Inc. | Heteroaryl estrogen receptor modulators and uses thereof |
US20170362228A1 (en) | 2016-06-16 | 2017-12-21 | Genentech, Inc. | TETRAHYDRO-PYRIDO[3,4-b]INDOLE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF |
UA125824C2 (uk) | 2016-10-24 | 2022-06-15 | Астразенека Аб | 6,7,8,9-ТЕТРАГІДРО-3H-ПІРАЗОЛО[4,3-f]ІЗОХІНОЛІНОВІ ПОХІДНІ, ЗАСТОСОВНІ В ЛІКУВАННІ РАКУ |
EP3820874B1 (en) | 2018-07-12 | 2022-11-30 | Eli Lilly and Company | Selective estrogen receptor degraders |
TWI702219B (zh) | 2018-07-12 | 2020-08-21 | 美商美國禮來大藥廠 | 選擇性雌激素受體降解劑 |
-
2016
- 2016-09-29 KR KR1020187011902A patent/KR102710603B1/ko active IP Right Grant
- 2016-09-29 SM SM20210433T patent/SMT202100433T1/it unknown
- 2016-09-29 NZ NZ741130A patent/NZ741130A/en unknown
- 2016-09-29 IL IL286518A patent/IL286518B2/en unknown
- 2016-09-29 JP JP2018516524A patent/JP6776348B2/ja active Active
- 2016-09-29 RU RU2018115696A patent/RU2745742C1/ru active
- 2016-09-29 US US15/764,988 patent/US10292971B2/en active Active
- 2016-09-29 WO PCT/US2016/054549 patent/WO2017059139A1/en active Application Filing
- 2016-09-29 EP EP16852640.8A patent/EP3355884B1/en active Active
- 2016-09-29 PT PT168526408T patent/PT3355884T/pt unknown
- 2016-09-29 LT LTEP16852640.8T patent/LT3355884T/lt unknown
- 2016-09-29 RS RS20210924A patent/RS62133B1/sr unknown
- 2016-09-29 NZ NZ779654A patent/NZ779654A/en unknown
- 2016-09-29 CA CA3000410A patent/CA3000410A1/en active Pending
- 2016-09-29 CN CN202110308336.4A patent/CN113248494A/zh active Pending
- 2016-09-29 DK DK16852640.8T patent/DK3355884T3/da active
- 2016-09-29 PL PL16852640T patent/PL3355884T3/pl unknown
- 2016-09-29 RU RU2021107754A patent/RU2021107754A/ru unknown
- 2016-09-29 UA UAA201804591A patent/UA122346C2/uk unknown
- 2016-09-29 BR BR112018006121-2A patent/BR112018006121B1/pt active IP Right Grant
- 2016-09-29 CN CN201680067297.0A patent/CN108366996B/zh active Active
- 2016-09-29 EP EP21164199.8A patent/EP3912680A1/en active Pending
- 2016-09-29 AU AU2016331065A patent/AU2016331065B2/en active Active
- 2016-09-29 MX MX2018003929A patent/MX2018003929A/es unknown
- 2016-09-29 IL IL310489A patent/IL310489A/en unknown
- 2016-09-29 HU HUE16852640A patent/HUE055321T2/hu unknown
- 2016-09-29 BR BR122023020677-0A patent/BR122023020677A2/pt not_active Application Discontinuation
- 2016-09-29 SI SI201631280T patent/SI3355884T1/sl unknown
- 2016-09-29 ES ES16852640T patent/ES2881398T3/es active Active
- 2016-09-29 KR KR1020247031670A patent/KR20240142622A/ko active Search and Examination
-
2018
- 2018-03-26 IL IL258363A patent/IL258363B/en unknown
- 2018-03-28 MX MX2021005214A patent/MX2021005214A/es unknown
- 2018-03-29 CL CL2018000827A patent/CL2018000827A1/es unknown
-
2019
- 2019-04-23 US US16/391,686 patent/US10624878B2/en active Active
-
2020
- 2020-04-17 US US16/852,272 patent/US11229630B2/en active Active
- 2020-10-07 JP JP2020169604A patent/JP7277424B2/ja active Active
-
2021
- 2021-07-14 HR HRP20211124TT patent/HRP20211124T1/hr unknown
- 2021-07-22 AU AU2021206861A patent/AU2021206861B2/en active Active
- 2021-07-22 CY CY20211100665T patent/CY1124669T1/el unknown
- 2021-12-06 US US17/542,908 patent/US11672785B2/en active Active
-
2023
- 2023-04-28 AU AU2023202620A patent/AU2023202620A1/en active Pending
- 2023-05-02 US US18/142,068 patent/US20240226073A9/en active Pending
- 2023-05-08 JP JP2023076673A patent/JP2023087106A/ja active Pending
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
RU2021107754A (ru) | ТЕТРАГИДРО-1H-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА | |
RU2015125307A (ru) | Комбинированная терапия | |
JP2016501221A5 (ru) | ||
PH12020551717A1 (en) | Dual atm and dna-pk inhibitors for use in anti-tumor therapy | |
CY1123627T1 (el) | Παραγωγα διυδροϊμιδαζοπυραζινονης χρησιμα στη θεραπευτικη αντιμετωπιση του καρκινου | |
CY1123475T1 (el) | Αναστολεις της ειδικης για λυσινη απομεθυλασης-1 | |
EA201892395A1 (ru) | Лекарственные составы ингибитора lsd1 | |
CY1119227T1 (el) | Παραγωγα πυριδινης ως ηπιοι αναστολεις της rock | |
EA201591296A1 (ru) | Фталазиноны и изохинолиноны в качестве ингибиторов rock | |
MX2021005463A (es) | Derivados de espiro-sulfonamida como inhibidores de la proteina de leucemia de celula mieloide 1 (mcl-1). | |
RU2016108667A (ru) | Комбинированная терапия для лечения рака | |
RU2018113718A (ru) | Новые соединения | |
JP2016530283A5 (ru) | ||
JP2016528246A5 (ru) | ||
MX2016014574A (es) | El uso de compuestos de tienotriazolodiazepina para el tratamiento de cancer de mama triple-negativo. | |
EA201591781A1 (ru) | Химические соединения | |
PH12021550825A1 (en) | Quinoline derivatives as alpha4beta7 integrin inhibitors | |
EA201791289A1 (ru) | Ингибиторы клеточного некроза и связанные с ними способы | |
RU2018102963A (ru) | Производные анилинпиримидина и их применения | |
MX2018007844A (es) | Derivado de benzopiperidina, metodo de preparacion del mismo y su uso medico del mismo. | |
EA201590222A1 (ru) | Способ усовершенствованного синтеза опиоидов | |
MX2020010942A (es) | Inhibidores dobles de atm y adn-pk para uso en terapias antitumorales. | |
EA201692481A1 (ru) | Комбинация, содержащая глюкокортикоид и edo-s101 | |
JP2018062523A5 (ru) | ||
BR112015022385A2 (pt) | droga para uma doença respiratória |