EA201491531A1 - C-3 циклоалкенил тритерпеноиды, ингибирующие созревание вич - Google Patents
C-3 циклоалкенил тритерпеноиды, ингибирующие созревание вичInfo
- Publication number
- EA201491531A1 EA201491531A1 EA201491531A EA201491531A EA201491531A1 EA 201491531 A1 EA201491531 A1 EA 201491531A1 EA 201491531 A EA201491531 A EA 201491531A EA 201491531 A EA201491531 A EA 201491531A EA 201491531 A1 EA201491531 A1 EA 201491531A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- cycloalkenyl
- compounds
- hiv maturation
- inhibiting hiv
- triterpenoids
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
- C07J53/002—Carbocyclic rings fused
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
- C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Описаны соединения, имеющие лекарственную и биологическую активность, их фармацевтические композиции и способы их применения. В частности, предусмотрены С-3 циклоалкенил тритерпеноиды, которые обладают уникальной противовирусной активностью в качестве ингибиторов созревания ВИЧ, представленные соединениями формул I, II, III и IVгде X может представлять собой Cциклоалкил, Cциклоалкенил, Сспироциклоалкил, Сспироциклоалкенил, Cоксациклоалкил, Сдиоксациклоалкил, Cоксациклоалкенил, Cдиоксациклоалкенил, Cциклодиалкенил, Cоксациклодиалкенил, Cоксаспироциклоалкил и Cоксаспироциклоалкенил. Указанные соединения полезны для лечения ВИЧ и СПИД.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261599040P | 2012-02-15 | 2012-02-15 | |
US13/760,726 US8906889B2 (en) | 2012-02-15 | 2013-02-06 | C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity |
PCT/US2013/025897 WO2013123019A1 (en) | 2012-02-15 | 2013-02-13 | C-3 cycloalkenyl triterpenoids with hiv maturation inhibitory activity |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201491531A1 true EA201491531A1 (ru) | 2014-11-28 |
EA024361B1 EA024361B1 (ru) | 2016-09-30 |
Family
ID=48946098
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201491531A EA024361B1 (ru) | 2012-02-15 | 2013-02-13 | C-3 циклоалкенил тритерпеноиды, ингибирующие созревание вич |
Country Status (26)
Country | Link |
---|---|
US (1) | US8906889B2 (ru) |
EP (1) | EP2814834B1 (ru) |
JP (1) | JP6155285B2 (ru) |
KR (1) | KR20140123584A (ru) |
CN (2) | CN106046106A (ru) |
AR (1) | AR089996A1 (ru) |
AU (1) | AU2013221725B2 (ru) |
BR (1) | BR112014019672A8 (ru) |
CA (1) | CA2864656A1 (ru) |
CL (1) | CL2014002141A1 (ru) |
CO (1) | CO7061077A2 (ru) |
EA (1) | EA024361B1 (ru) |
ES (1) | ES2656984T3 (ru) |
HK (1) | HK1204608A1 (ru) |
IL (1) | IL234077A (ru) |
MX (1) | MX2014009235A (ru) |
MY (1) | MY166793A (ru) |
NZ (1) | NZ631408A (ru) |
PE (1) | PE20142315A1 (ru) |
PH (1) | PH12014501816A1 (ru) |
PT (1) | PT2814834T (ru) |
SG (1) | SG11201404748XA (ru) |
TW (1) | TW201336863A (ru) |
UY (1) | UY34627A (ru) |
WO (1) | WO2013123019A1 (ru) |
ZA (1) | ZA201406724B (ru) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8889854B2 (en) | 2012-05-07 | 2014-11-18 | Bristol-Myers Squibb Company | C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity |
SG11201505639SA (en) | 2013-02-06 | 2015-08-28 | Bristol Myers Squibb Co | C-19 modified triterpenoids with hiv maturation inhibitory activity |
BR112016023414B1 (pt) * | 2014-04-11 | 2022-09-13 | ViiV Healthcare UK (No.4) Limited | Composto, composição farmacêutica, e, uso do composto |
US9920090B2 (en) | 2014-06-19 | 2018-03-20 | VIIV Healthcare UK (No.5) Limited | Betulinic acid derivatives with HIV maturation inhibitory activity |
AU2015346314B2 (en) * | 2014-11-14 | 2018-04-12 | VIIV Healthcare UK (No.5) Limited | Extended betulinic acid analogs |
KR20170092581A (ko) | 2014-11-14 | 2017-08-11 | 비브 헬스케어 유케이 (넘버5) 리미티드 | C17-아릴 치환된 베툴린산 유사체 |
WO2016077561A1 (en) | 2014-11-14 | 2016-05-19 | Bristol-Myers Squibb Company | Oxolupene derivatives |
CA2981056A1 (en) * | 2015-04-14 | 2016-10-20 | ViiV Healthcare UK (No.4) Limited | Methods of producing an hiv maturation inhibitor |
JP2018521093A (ja) | 2015-07-28 | 2018-08-02 | グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited | Hiv感染を予防または治療するためのベツイン誘導体 |
AU2016298667A1 (en) | 2015-07-28 | 2018-02-22 | Glaxosmithkline Intellectual Property (No.2) Limited | Betuin derivatives for preventing or treating HIV infections |
EP3353158A1 (en) | 2015-09-24 | 2018-08-01 | Glaxosmithkline Intellectual Property (No. 2) Limited | Compounds with hiv maturation inhibitory activity |
KR20180098675A (ko) * | 2016-01-20 | 2018-09-04 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | Hiv 성숙 억제 활성을 갖는 루판의 아민 유도체 |
AR107512A1 (es) | 2016-02-04 | 2018-05-09 | VIIV HEALTHCARE UK Nº 5 LTD | Triterpenoides modificados en c-3 y c-17 como inhibidores del vih-1 |
CN106905264B (zh) * | 2017-04-12 | 2019-06-07 | 连云港杰瑞药业有限公司 | 一种合成阿扎拉韦中间体的方法 |
JP2020533377A (ja) * | 2017-09-13 | 2020-11-19 | エミオン インコーポレイテッドEmmyon, Inc. | ウルソール酸モルホリン塩及びジエタノールアミン塩 |
US20210347813A1 (en) | 2018-04-24 | 2021-11-11 | Viiv Healthcare Uk (No. 5) Limited | Compounds with hiv maturation inhibitory activity |
CN109705189B (zh) * | 2018-12-29 | 2020-06-05 | 中国医学科学院药用植物研究所 | 具有式i所示结构的三萜衍生物及其制备方法和应用 |
EP4248960A3 (en) | 2019-02-11 | 2024-01-03 | Hetero Labs Limited | Novel triterpene derivatives as hiv inhibitors |
WO2020229398A1 (de) | 2019-05-14 | 2020-11-19 | Bayer Aktiengesellschaft | (1-alkenyl)-substituierte pyrazole und triazole als schädlingsbekämpfungsmittel |
Family Cites Families (25)
Publication number | Priority date | Publication date | Assignee | Title |
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US5413999A (en) | 1991-11-08 | 1995-05-09 | Merck & Co., Inc. | HIV protease inhibitors useful for the treatment of AIDS |
US5869535A (en) | 1995-03-21 | 1999-02-09 | The Board Of Trustees Of The University Of Illinois | Method and composition for selectively inhibiting melanoma |
US5962527A (en) | 1995-03-21 | 1999-10-05 | The Board Of Trustees Of The University Of Illinois | Method and composition for treating cancers |
US5679828A (en) | 1995-06-05 | 1997-10-21 | Biotech Research Labs, Inc. | Betulinic acid and dihydrobetulinic acid derivatives and uses therefor |
US20040110785A1 (en) | 2001-02-02 | 2004-06-10 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
US7365221B2 (en) | 2002-09-26 | 2008-04-29 | Panacos Pharmaceuticals, Inc. | Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof |
WO2004089357A2 (en) | 2003-04-02 | 2004-10-21 | Regents Of The University Of Minnesota | Anti-fungal formulation of triterpene and essential oil |
US7745625B2 (en) | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
JP2007529544A (ja) | 2004-03-17 | 2007-10-25 | パナコス ファーマシューティカルズ, インコーポレイテッド | 3−o−(3’,3’−ジメチルスクシニル)ベツリン酸の製薬的な塩 |
TW200628161A (en) | 2004-11-12 | 2006-08-16 | Panacos Pharmaceuticals Inc | Novel betulin derivatives, preparation thereof and use thereof |
WO2008127364A2 (en) | 2006-10-13 | 2008-10-23 | Myriad Genetics, Inc. | Antiviral compounds and use thereof |
US20090105203A1 (en) | 2006-10-16 | 2009-04-23 | Myriad Genetics, Incorporated | Compounds for treating viral infections |
US20090062243A1 (en) | 2007-08-03 | 2009-03-05 | Advanced Life Sciences, Inc. | Lupane-Type Triterpenoids Modified at 30-Position and Analogues Thereof |
CN101981047A (zh) * | 2008-01-03 | 2011-02-23 | Viro化学制药公司 | 新的羽扇烷衍生物 |
WO2009100532A1 (en) | 2008-02-14 | 2009-08-20 | Virochem Pharma Inc. | NOVEL 17ß LUPANE DERIVATIVES |
US9067966B2 (en) | 2009-07-14 | 2015-06-30 | Hetero Research Foundation, Hetero Drugs Ltd. | Lupeol-type triterpene derivatives as antivirals |
EA022790B1 (ru) | 2009-12-17 | 2016-03-31 | Мерк Шарп Энд Домэ Корп. | Аминопиримидины в качестве syk ингибиторов |
CA2801487C (en) * | 2010-06-04 | 2017-12-05 | Bristol-Myers Squibb Company | Modified c-3 betulinic acid derivatives as hiv maturation inhibitors |
JP5755731B2 (ja) | 2010-06-04 | 2015-07-29 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Hiv成熟阻害剤としての修飾c−3ベツリン酸誘導体のc−28アミド |
SG186820A1 (en) | 2010-07-02 | 2013-02-28 | Gilead Sciences Inc | Napht- 2 -ylacetic acid derivatives to treat aids |
EP2670764B1 (en) * | 2011-01-31 | 2015-09-02 | Bristol-Myers Squibb Company | C-28 amines of c-3 modified betulinic acid derivatives as hiv maturation inhibitors |
MA34909B1 (fr) * | 2011-01-31 | 2014-02-01 | Bristol Myers Squibb Co | Triterpénoïdes modifi2s en c-17 et c-3 presentant une activité inhibitrice de la maturation du vih |
BR112014006559A2 (pt) | 2011-09-21 | 2017-03-28 | Bristol Myers Squibb Co | derivados do ácido betulínico com atividade antiviral |
US8889854B2 (en) | 2012-05-07 | 2014-11-18 | Bristol-Myers Squibb Company | C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity |
SG11201505639SA (en) * | 2013-02-06 | 2015-08-28 | Bristol Myers Squibb Co | C-19 modified triterpenoids with hiv maturation inhibitory activity |
-
2013
- 2013-02-06 US US13/760,726 patent/US8906889B2/en active Active
- 2013-02-08 TW TW102105203A patent/TW201336863A/zh unknown
- 2013-02-13 CN CN201610397768.6A patent/CN106046106A/zh active Pending
- 2013-02-13 WO PCT/US2013/025897 patent/WO2013123019A1/en active Application Filing
- 2013-02-13 PE PE2014001279A patent/PE20142315A1/es not_active Application Discontinuation
- 2013-02-13 ES ES13707493.6T patent/ES2656984T3/es active Active
- 2013-02-13 PT PT137074936T patent/PT2814834T/pt unknown
- 2013-02-13 MX MX2014009235A patent/MX2014009235A/es unknown
- 2013-02-13 CN CN201380019696.6A patent/CN104220451B/zh not_active Expired - Fee Related
- 2013-02-13 CA CA2864656A patent/CA2864656A1/en not_active Abandoned
- 2013-02-13 SG SG11201404748XA patent/SG11201404748XA/en unknown
- 2013-02-13 KR KR1020147025339A patent/KR20140123584A/ko not_active Application Discontinuation
- 2013-02-13 EA EA201491531A patent/EA024361B1/ru not_active IP Right Cessation
- 2013-02-13 JP JP2014557739A patent/JP6155285B2/ja active Active
- 2013-02-13 NZ NZ631408A patent/NZ631408A/en not_active IP Right Cessation
- 2013-02-13 BR BR112014019672A patent/BR112014019672A8/pt not_active Application Discontinuation
- 2013-02-13 MY MYPI2014702277A patent/MY166793A/en unknown
- 2013-02-13 AU AU2013221725A patent/AU2013221725B2/en not_active Ceased
- 2013-02-13 EP EP13707493.6A patent/EP2814834B1/en active Active
- 2013-02-14 UY UY0001034627A patent/UY34627A/es not_active Application Discontinuation
- 2013-02-14 AR ARP130100466A patent/AR089996A1/es unknown
-
2014
- 2014-08-12 IL IL234077A patent/IL234077A/en not_active IP Right Cessation
- 2014-08-12 PH PH12014501816A patent/PH12014501816A1/en unknown
- 2014-08-13 CL CL2014002141A patent/CL2014002141A1/es unknown
- 2014-08-28 CO CO14189685A patent/CO7061077A2/es unknown
- 2014-09-12 ZA ZA2014/06724A patent/ZA201406724B/en unknown
-
2015
- 2015-05-28 HK HK15105069.8A patent/HK1204608A1/xx unknown
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Legal Events
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MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM |
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PC4A | Registration of transfer of a eurasian patent by assignment | ||
MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |