AR076694A1 - Benzoxazepinas como inhibidores de pi3k/m/tor, su uso en el tratamiento del cancer y su preparacion - Google Patents
Benzoxazepinas como inhibidores de pi3k/m/tor, su uso en el tratamiento del cancer y su preparacionInfo
- Publication number
- AR076694A1 AR076694A1 ARP100101771A ARP100101771A AR076694A1 AR 076694 A1 AR076694 A1 AR 076694A1 AR P100101771 A ARP100101771 A AR P100101771A AR P100101771 A ARP100101771 A AR P100101771A AR 076694 A1 AR076694 A1 AR 076694A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- alkyl
- hydroxyalkyl
- haloalkyl
- independently
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se preveen composiciones farmacéuticas que comprenden métodos para preparar y uso de los compuestos en el tratamiento del cáncer. Reivindicacion 1: Un compuesto de la formula 1: o uno de sus estereoisomeros individuales o una mezcla de estereoisomeros y además, opcionalmente como una de sus sales farmacéuticamente aceptables, en donde R1es fenilo opcionalmente sustituido con uno, dos o tres grupos R6 o R1 es heteroarilo opcionalmente sustituido con uno, dos o tres R7 R2 es heteroarilo sustituido con R3, R3a, R3b, R3c y R3d; R3, R3a, R3b, R3c y R3d son, de modo independiente, hidrogeno, ciano, alquilo, alquenilo, halo, haloalquilo, hidroxialquilo, alcoxialquilo, cianoalquilo, -SR12, -S(O) 2R20, -C(O)OR4, halocarbonilo, -NR11R11a, -OR11a fenilo opcionalmente sustituido, fenilalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heterocicloalquilalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroarilalquilo opcionalmente sustituido o alquilo sustituido con uno o dos R16 o dos de R3, R3a, R3b, R3c y R3d cuando se unen con el mismo carbono, forman un cicloalquilo opcionalmente sustituido o un heterocicloalquilo opcionalmente sustituido; y el otro de R3, R3a, R3b, R3c y R3d son, de modo independiente, hidrogeno, ciano, alquilo, alquenilo, halo, haloalquilo, hidroxialquilo, alcoxialquilo, cianoalquilo, -SR12, -S(O)2R20, -C(O)OR4, halocarbonilo, -NR11R11a, -OR11a, fenilo opcionalmente sustituido, fenilalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heterocicloalquilalquilo opcionalmente sustituido, heteroarilo opcionalmente, heteroarilalquilo opcionalmente sustituido o alquilo sustituido con uno o dos R16 R4 es alquilo, alquenilo, alquinilo, hidroxialquilo, alcoxialquilo, haloalquilo, bencilo o heterocicloalquilalquilo opcionalmente sustituido; R5a y R5c son, de modo independiente, hidrogeno o alquilo; R5h es hidrogeno o halo; R5b es hidrogeno, amino o halo; R5d, R5e, R5f y R5g son hidrogeno; cada R6, cuando R6 está presente, es, de modo independiente, nitro; ciano; halo; alquilo; alquenilo; alquinilo; haloalquilo; -OR8a; -NR8R8a; -C(O)NR8R8a; - S(O)2R8, -NR8C(O)OR9, -NR8C(O)R9, -NR8S(O)2R8a;. -NR8C(O)NR8aR9 carboxi, -C(O)OR9 halocarbonilo; alquilcarbonilo; alquilo sustituido con uno o dos -C(O)NR8R8a; heteroarilo opcionalmente sustituido con 1, 2 o 3 R14; o heterocicloalquilo opcionalmente sustituido; cada R7, cuando R7 está presente, es, de modo independiente, oxo; nitro; ciano; alquilo; alquenilo; alquinilo; halo; haloalquilo; hidroxialquilo; alcoxialquilo; -OR8a; -SR13 -S(O)R13a, -S(O)2R13a; -NR8R8a; -C(O)NR8R8a, -NR8C(O)OR9, -NR8C(O)R9; -NR8S(O)2R8a; -NR8C(O)NR8aR9, -C(O)OR9 halocarbonilo; alquilcarbonilo; -S(O)2NR8R9 alquilsulfonilalquilo; alquilo sustituido con uno o dos -NR8R8a; alquilo sustituido con uno o dos -NR8C(O)R8a; alquilo sustituido, con uno o dos -NR8C(O)OR9 alquilo sustituido con uno o dos -S(O)2R13a; cicloalquilo opcionalmente sustituido; cicloalquilalquilo opcionalmente sustituido; heterocicloalquilo opcionalmente sustituido; heterocicloalquilalquilo opcionalmente sustituido; fenilo opcionalmente sustituido; fenilalquilo opcionalmente sustituido; heteroarilo opcionalmente sustituido; o heteroarilalquilo opcionalmente sustituido; cada R8, R11, R15, R17 y R18 es, de modo independiente, hidrogeno, alquilo, alquenilo, alquinilo, hidroxialquilo, alcoxialquilo o haloalquilo; cada R8a, R11a , R15a es, de modo independiente, hidrogeno, alquilo, alquenilo, alquinilo, haloalquilo, hidroxialquilo, cianoalquilo, aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, alcoxialquilo, carboxialquilo, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heterocicloalquilalquilo opcionalmente sustituido, fenilo opcionalmente sustituido, fenilalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido o heteroarilalquilo opcionalmente sustituido; R9 es hidrogeno; alquilo; alquenilo; alquinilo; hidroxialquilo; alcoxialquilo; aminoalquilo; alquilaminoalquilo; dialquilaminoalquilo; haloalquilo; hidroxialquilo sustituido con uno, dos o tres grupos que son, de modo independiente, halo, amino, alquilamino o dialquilamino; alquilo sustituido con uno o dos aminocarbonilo; fenilo opcionalmente sustituido; fenilalquilo opcionalmente sustituido; cicloalquilo opcionalmente sustituido; cicloalquilalquilo opcionalmente sustituido; heteroarilo opcionalmente sustituido; heteroarilalquilo opcionalmente sustituido; heterocicloalquilo opcionalmente sustituido; o heterocicloalquilalquilo opcionalmente sustituido; R12 es alquilo o fenilalquilo opcionalmente sustituido; R13 es alquilo, hidroxialquilo o haloalquilo; y R13a es hidroxi, alquilo, haloalquilo, hidroxialquilo o heterocicloalquilo opcionalmente sustituido con uno o dos grupos que son, de modo independiente, halo, amino, alquilamino, dialquilamino, hidroxi, alquilo o hidroxialquilo; cada R14, cuando R14 está presente, es, de modo independiente, amino, alquilamino, dialquilamino, acilamino, halo, hidroxi, alquilo, haloalquilo, hidroxialquilo, aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, alcoxicarbonilo, aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo o fenilo opcionalmente sustituido; cada R16 es, de modo independiente, -NR11R12a, -NR15S(O)R15a, -OC(O)R17 u -OR18 y R20 es alquilo, haloalquilo, hidroxialquilo, amino, alquilamino, dialquilamino o heterocicloalquilo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US21698009P | 2009-05-22 | 2009-05-22 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR076694A1 true AR076694A1 (es) | 2011-06-29 |
Family
ID=42556812
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100101771A AR076694A1 (es) | 2009-05-22 | 2010-05-21 | Benzoxazepinas como inhibidores de pi3k/m/tor, su uso en el tratamiento del cancer y su preparacion |
Country Status (13)
Country | Link |
---|---|
US (1) | US8648066B2 (es) |
EP (1) | EP2432779A1 (es) |
JP (1) | JP2012527474A (es) |
KR (1) | KR20120034666A (es) |
CN (1) | CN102459249A (es) |
AR (1) | AR076694A1 (es) |
AU (1) | AU2010249790A1 (es) |
BR (1) | BRPI1010974A2 (es) |
CA (1) | CA2763099A1 (es) |
IL (1) | IL216472A0 (es) |
MX (1) | MX2011012345A (es) |
TW (1) | TW201111371A (es) |
WO (1) | WO2010135524A1 (es) |
Families Citing this family (58)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
NZ717410A (en) | 2008-01-04 | 2017-07-28 | Intellikine Llc | Heterocyclic containing entities, compositions and methods |
US8637499B2 (en) | 2009-05-26 | 2014-01-28 | Exelixis, Inc. | Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture |
US8765940B2 (en) * | 2009-06-25 | 2014-07-01 | Amgen Inc. | Heterocyclic compounds and their uses |
ES2693257T3 (es) | 2010-09-14 | 2018-12-10 | Exelixis, Inc. | Inhibidores de PI3K-delta y métodos para su uso y fabricación |
ME02663B (me) | 2010-10-06 | 2017-06-20 | Glaxosmithkline Llc | Derivati benzimidazola kao inhibitori pi3 kinaze |
DE102010049595A1 (de) * | 2010-10-26 | 2012-04-26 | Merck Patent Gmbh | Chinazolinderivate |
US20140066431A1 (en) * | 2010-11-15 | 2014-03-06 | Exelixis, Inc. | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture |
WO2012068096A2 (en) * | 2010-11-15 | 2012-05-24 | Exelixis, Inc. | Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture |
MX2013005826A (es) * | 2010-11-24 | 2013-08-27 | Exelixis Inc | Benzoxazepinas como inhibidores de fosfatidilinositol 3-cinasa/objetivo de rapamicina en mamiferos (p13k/mtor) y metodos de uso y fabricacion. |
JP2013544826A (ja) * | 2010-11-24 | 2013-12-19 | エクセリクシス, インク. | PI3K/mTORの阻害剤としてのベンゾオキサゼピン類ならびにそれらの使用法および製造法 |
US20140005172A1 (en) * | 2010-11-24 | 2014-01-02 | Elelixis, Inc. | Benzoxazepines as Inhibitors of PI3K/M TOR and Methods of Their Use and Manufacture |
CN103328485A (zh) * | 2010-11-24 | 2013-09-25 | 埃克塞里艾克西斯公司 | 作为mTOR抑制剂的苯并氧氮杂卓及其使用和生产方法 |
AR084824A1 (es) | 2011-01-10 | 2013-06-26 | Intellikine Inc | Procesos para preparar isoquinolinonas y formas solidas de isoquinolinonas |
KR20140032383A (ko) * | 2011-03-21 | 2014-03-14 | 에프. 호프만-라 로슈 아게 | Pi3k p110 델타에 대하여 선택적인 벤즈옥사제핀 화합물 및 이의 사용 방법 |
JP6240063B2 (ja) * | 2011-04-28 | 2017-11-29 | ザ ブロード インスティテュート, インコーポレイテッド | ヒストンデアセチラーゼ阻害剤 |
CN103732588B (zh) * | 2011-07-27 | 2016-10-12 | 南京奥昭生物科技有限公司 | 螺环分子作为蛋白激酶抑制剂 |
EA201490905A1 (ru) | 2011-11-01 | 2014-11-28 | Экселиксис, Инк. | N-(3-{[(3-{[2-хлор-5-(метокси)фенил]амино}хиноксалин-2-ил)амино]сульфонил}фенил)-2-метилаланинамид как ингибитор фосфатидилинозитол-3-киназы для лечения лимфопролиферативных злокачественных заболеваний |
JP5949070B2 (ja) * | 2012-04-03 | 2016-07-06 | Jsr株式会社 | 液晶配向剤、液晶配向膜及び液晶表示素子 |
US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
NZ702334A (en) * | 2012-06-13 | 2016-11-25 | Hoffmann La Roche | New diazaspirocycloalkane and azaspirocycloalkane |
US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
CA2880117C (en) | 2012-07-27 | 2021-04-06 | The Broad Institute, Inc. | Inhibitors of histone deacetylase |
UA116547C2 (uk) | 2012-09-25 | 2018-04-10 | Ф. Хоффманн-Ля Рош Аг | Біциклічні похідні |
AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
PL3074400T3 (pl) | 2013-11-26 | 2018-03-30 | F.Hoffmann-La Roche Ag | Pochodne oktahydrocyklobuta[1,2-c;3,4-c']dipirolu jako inhibitory autotaksyny |
MX2016009135A (es) | 2014-01-14 | 2016-10-05 | Millennium Pharm Inc | Heteroarilos y usos de estos. |
WO2015108881A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
DK3122750T3 (da) | 2014-03-26 | 2019-11-04 | Hoffmann La Roche | Bicykliske forbindelser som autotaxin (ATX)- og lysofosfatidsyre (LPA)-produktionshæmmere |
PE20161223A1 (es) | 2014-03-26 | 2016-11-12 | Hoffmann La Roche | Compuestos condensados de [1,4]diazepina como inhibidores de la produccion de autotaxina (atx) y acido lisofosfatidico (lpa) |
US20150320755A1 (en) | 2014-04-16 | 2015-11-12 | Infinity Pharmaceuticals, Inc. | Combination therapies |
MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
CN104910158B (zh) * | 2015-06-15 | 2017-04-12 | 河南师范大学 | 具有生物活性的5,6,7,8‑四氢吡啶并[3,4‑d]嘧啶化合物及其制备方法和应用 |
PE20180479A1 (es) | 2015-09-04 | 2018-03-07 | Hoffmann La Roche | Nuevos derivados de fenoximetilo |
MX2018001890A (es) | 2015-09-24 | 2018-06-20 | Hoffmann La Roche | Compuestos biciclicos como inhibidores de autotaxina (atx). |
JP6846414B2 (ja) | 2015-09-24 | 2021-03-24 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Atx阻害剤としての二環式化合物 |
JP6845230B2 (ja) | 2015-09-24 | 2021-03-17 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | デュアルatx/ca阻害剤としての新規な二環式化合物 |
EP3353178B1 (en) | 2015-09-24 | 2021-07-14 | F. Hoffmann-La Roche AG | Bicyclic compounds as dual atx/ca inhibitors |
US11147818B2 (en) | 2016-06-24 | 2021-10-19 | Infinity Pharmaceuticals, Inc. | Combination therapies |
EP3555104B1 (en) * | 2016-12-15 | 2021-11-24 | GlaxoSmithKline Intellectual Property Development Limited | Nrf2 compounds |
JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ.ホフマン-ラ ロシュ アーゲー | Atxインヒビターとしての新規二環式化合物 |
CR20190423A (es) | 2017-03-16 | 2019-11-01 | Hoffmann La Roche | Nuevos compuestos biciclícos como inhibidores dobles de atx/ca |
RU2707751C1 (ru) | 2017-03-20 | 2019-11-29 | Форма Терапьютикс, Инк. | Пирролопирроловые композиции в качестве активаторов пируваткиназы (pkr) |
US12128018B2 (en) | 2018-01-12 | 2024-10-29 | KDAc Therapeutics, Inc. | Combination of a selective histone deacetylase 3 (HDAC3) inhibitor and an immunotherapy agent for the treatment of cancer |
CA3089566A1 (en) | 2018-01-31 | 2019-08-08 | Deciphera Pharmaceuticals, Llc | Combination therapy for the treatment of gastrointestinal stromal tumors |
WO2019152719A1 (en) | 2018-01-31 | 2019-08-08 | Deciphera Pharmaceuticals, Llc | Combination therapy for the treatment of mastocytosis |
CN113166060B (zh) | 2018-09-19 | 2024-01-09 | 诺沃挪第克健康护理股份公司 | 用丙酮酸激酶激活化合物治疗镰状细胞病 |
CN113226356A (zh) | 2018-09-19 | 2021-08-06 | 福马治疗股份有限公司 | 活化丙酮酸激酶r |
WO2021030405A1 (en) | 2019-08-12 | 2021-02-18 | Deciphera Pharmaceuticals, Llc | Ripretinib for treating gastrointestinal stromal tumors |
AU2020329956B2 (en) | 2019-08-12 | 2023-11-16 | Deciphera Pharmaceuticals, Llc. | Ripretinib for treating gastrointestinal stromal tumors |
IL293864A (en) | 2019-12-30 | 2022-08-01 | Deciphera Pharmaceuticals Llc | Preparations of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3- phenylurea |
HRP20231699T1 (hr) | 2019-12-30 | 2024-05-10 | Deciphera Pharmaceuticals, Llc | Formulacije inhibitora amorfne kinaze i postupci njihove primjene |
AU2021251341A1 (en) | 2020-04-07 | 2022-11-03 | Bayer Aktiengesellschaft | Substituted thiazolopyridines, salts thereof and their use as herbicidally active substances |
US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
TW202328151A (zh) | 2021-09-07 | 2023-07-16 | 德商拜耳廠股份有限公司 | 經取代之2,3-二氫[1,3]噻唑并[4,5-b]吡啶、其鹽及其作為除草活性物質之用途 |
TW202328150A (zh) | 2021-09-07 | 2023-07-16 | 德商拜耳廠股份有限公司 | 經取代之噻唑并吡啶、其鹽及其作為除草活性物質之用途 |
US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
WO2024145259A2 (en) * | 2022-12-28 | 2024-07-04 | Reservoir Neuroscience, Inc. | Ep2 antagonist compounds |
Family Cites Families (27)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE4102103A1 (de) | 1991-01-25 | 1992-08-20 | Bayer Ag | Substituierte benzoxazepine und benzthiazepine, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln |
US5272158A (en) | 1991-10-29 | 1993-12-21 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
KR19990076876A (ko) | 1995-12-29 | 1999-10-25 | 스티븐 베네티아너 | 비트로넥틴 수용체 길항제 |
CZ203898A3 (cs) | 1995-12-29 | 1999-03-17 | Smithkline Beecham Corporation | Antagonista vitronektinového receptoru, farmaceutický přípravek s jeho obsahem, způsob a použití |
SE9701681D0 (sv) * | 1997-05-05 | 1997-05-05 | Astra Ab | New compounds |
AU747503B2 (en) | 1999-02-03 | 2002-05-16 | Merck & Co., Inc. | Benzazepine derivatives as alpha-V integrin receptor antagonists |
JP2003508581A (ja) | 1999-08-27 | 2003-03-04 | ザ、プロクター、エンド、ギャンブル、カンパニー | 処方成分の制御された有効化法、それを使用する組成物および洗濯方法 |
CN1384867A (zh) | 1999-08-27 | 2002-12-11 | 宝洁公司 | 稳定性提高的配制组分、使用该组分的组合物和洗衣方法 |
JP2003508586A (ja) | 1999-08-27 | 2003-03-04 | ザ、プロクター、エンド、ギャンブル、カンパニー | 迅速に作用する処方成分、それらの成分を使用する組成物および洗濯方法 |
MXPA02002128A (es) | 1999-08-27 | 2002-09-02 | Procter & Gamble | Componentes para formulacion estable, composiciones y metodos para lavanderia que los emplean. |
US6723752B2 (en) * | 1999-09-23 | 2004-04-20 | Pharmacia Corporation | (R)-chiral halogenated substituted n-benzyl-n-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity |
US20030114448A1 (en) | 2001-05-31 | 2003-06-19 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
AU2003219652A1 (en) | 2002-01-08 | 2003-07-30 | Eisai Co. Ltd. | Eponemycin and epoxomicin analogs and uses thereof |
US7196108B2 (en) | 2002-03-08 | 2007-03-27 | Incyte San Diego Inc. | Bicyclic heterocycles for the treatment of diabetes and other diseases |
CL2004000409A1 (es) * | 2003-03-03 | 2005-01-07 | Vertex Pharma | Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu |
US7521457B2 (en) * | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
HUE031979T2 (en) | 2005-05-17 | 2017-08-28 | Sarcode Bioscience Inc | Preparations and methods for treating eye disorders |
CN101258136A (zh) * | 2005-07-05 | 2008-09-03 | 阿斯利康(瑞典)有限公司 | 新化合物、其制备方法、中间体、药物组合物和其在治疗5-ht6介导的疾病例如阿尔茨海默病、认知障碍、精神分裂症相关的认知缺损、肥胖和帕金森病中的用途 |
WO2008109599A1 (en) * | 2007-03-05 | 2008-09-12 | Wyeth | Pyrimido [5,4-c] quinoline-2, 4-diamine derivatives and methods of use thereof |
CA2680312A1 (en) * | 2007-03-07 | 2008-09-12 | Alantos Pharmaceuticals Holding, Inc. | Metalloprotease inhibitors containing a heterocyclic moiety |
WO2008108445A1 (ja) * | 2007-03-07 | 2008-09-12 | Takeda Pharmaceutical Company Limited | ベンゾオキサゼピン誘導体およびその用途 |
WO2008144483A2 (en) | 2007-05-18 | 2008-11-27 | Armgo Pharma, Inc. | Agents for treating disorders involving modulation of ryanodine receptors |
US20110263569A1 (en) | 2007-08-22 | 2011-10-27 | President And Fellows Of Harvard College | Ryanodine channel binders and uses thereof |
US20100197657A1 (en) * | 2007-09-25 | 2010-08-05 | Chang Ronald K | 2-aryl or heteroaryl indole derivatives |
JP5650540B2 (ja) | 2007-12-12 | 2015-01-07 | ライジェル ファーマシューティカルズ, インコーポレイテッド | 代謝障害のためのカルボキサミド、スルホンアミド、およびアミン化合物 |
CN101497612A (zh) | 2009-03-03 | 2009-08-05 | 北京华禧联合科技发展有限公司 | 一类新喹诺酮类化合物及其制备与用途 |
US8637499B2 (en) * | 2009-05-26 | 2014-01-28 | Exelixis, Inc. | Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture |
-
2010
- 2010-05-20 KR KR1020117030799A patent/KR20120034666A/ko not_active Application Discontinuation
- 2010-05-20 MX MX2011012345A patent/MX2011012345A/es active IP Right Grant
- 2010-05-20 CN CN2010800329112A patent/CN102459249A/zh active Pending
- 2010-05-20 BR BRPI1010974A patent/BRPI1010974A2/pt not_active IP Right Cessation
- 2010-05-20 US US12/784,254 patent/US8648066B2/en not_active Expired - Fee Related
- 2010-05-20 JP JP2012512029A patent/JP2012527474A/ja active Pending
- 2010-05-20 AU AU2010249790A patent/AU2010249790A1/en not_active Abandoned
- 2010-05-20 EP EP10731844A patent/EP2432779A1/en not_active Withdrawn
- 2010-05-20 CA CA2763099A patent/CA2763099A1/en not_active Abandoned
- 2010-05-20 WO PCT/US2010/035565 patent/WO2010135524A1/en active Application Filing
- 2010-05-21 AR ARP100101771A patent/AR076694A1/es not_active Application Discontinuation
- 2010-05-21 TW TW099116315A patent/TW201111371A/zh unknown
-
2011
- 2011-11-20 IL IL216472A patent/IL216472A0/en unknown
Also Published As
Publication number | Publication date |
---|---|
CN102459249A (zh) | 2012-05-16 |
WO2010135524A1 (en) | 2010-11-25 |
TW201111371A (en) | 2011-04-01 |
WO2010135524A8 (en) | 2012-01-12 |
US20100298290A1 (en) | 2010-11-25 |
JP2012527474A (ja) | 2012-11-08 |
US8648066B2 (en) | 2014-02-11 |
KR20120034666A (ko) | 2012-04-12 |
BRPI1010974A2 (pt) | 2019-09-24 |
IL216472A0 (en) | 2012-01-31 |
MX2011012345A (es) | 2012-01-31 |
EP2432779A1 (en) | 2012-03-28 |
AU2010249790A1 (en) | 2011-12-08 |
CA2763099A1 (en) | 2010-11-25 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR076694A1 (es) | Benzoxazepinas como inhibidores de pi3k/m/tor, su uso en el tratamiento del cancer y su preparacion | |
AR076271A1 (es) | Inhibidores de mtor, composiciones farmaceuticas, metodo de fabricacion y su uso en el tratamiento de cancer | |
AR076922A1 (es) | Benzodiazepinas como inhibidores de pi3k/mtor, una composicion farmaceutica que las comprende, metodos para su fabricacion y su uso en el tratamiento del cancer. | |
AR083953A1 (es) | Compuestos para tratar enfermedades neurodegenerativas | |
AR083199A1 (es) | Compuestos de n-heteroarilo con unidad de puente ciclico | |
AR084849A1 (es) | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos | |
AR092108A1 (es) | Piridazina 1,4 disustituida, analogos de la misma y metodos para tratar las enfermedades relacionadas con deficiencia del smn | |
AR083169A1 (es) | Compuestos para tratar enfermedades neurodegenerativas | |
NI201400023A (es) | Derivados de pirrolopirimidina y purina | |
AR077328A1 (es) | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos | |
CR20140091A (es) | Nuevos derivados dihidroquinolina-2-ona | |
AR072906A1 (es) | Nucleosidos modificados utiles como antivirales | |
AR063912A1 (es) | Derivados de 1,2,4 oxadiazol. composiciones farmaceuticas. | |
CO6140024A2 (es) | Uso de compuestos inhibidores de quinaxolina de pi3k-alfa para el tratamiento del cancer | |
AR067757A1 (es) | Derivados de imidazo[4,5-c]piridin-2-ona, composiciones farmaceuticas que los contienen, procedimiento para su preparacion y uso de los mismos como agentes antivirales. | |
AR081075A1 (es) | Derivados de imidazo[1,2-c]pirimidina, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos en el tratamiento de enfermedades autoinmunes e inflamatorias. | |
AR086972A1 (es) | Procesos para preparar compuestos heterociclicos, que incluyen trans-7-oxo-6-(sulfooxi)-1,6-diazabiciclo[3,2,1]octano-2-carboxamida y sales de la misma | |
ES2531274T3 (es) | Indazoles sustituidos con oxazol como inhibidores de PI3-cinasas | |
RU2015121431A (ru) | Замещенные производные индол-5-ола и их терапевтическое применение | |
AR079224A1 (es) | Compuestos insecticidas basados en derivados de isoxazolina | |
AR066153A1 (es) | Derivados de piperidina / piperazina | |
AR089776A1 (es) | 5,8-dihidro-6h-pirazolo[3,4-h]quinazolinas como inhibidores de igf-1r/ir | |
AR079553A1 (es) | Derivados de diaza-espiro-[5,5]-undecanos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de trastornos del snc, tales como trastornos del sueno y de la dependencia,entre otros. | |
AR069364A1 (es) | Derivados heterociclicos que modulan la miosina del musculo liso y/o la miosina no muscular y composiciones farmaceuticas que los contienen | |
UY35845A (es) | ?derivados de purina?. |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA | Abandonment or withdrawal |