EA201991122A1 - 3-ЗАМЕЩЕННЫЕ ПРОПАНОВЫЕ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ИНТЕГРИНА αV - Google Patents
3-ЗАМЕЩЕННЫЕ ПРОПАНОВЫЕ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ИНТЕГРИНА αVInfo
- Publication number
- EA201991122A1 EA201991122A1 EA201991122A EA201991122A EA201991122A1 EA 201991122 A1 EA201991122 A1 EA 201991122A1 EA 201991122 A EA201991122 A EA 201991122A EA 201991122 A EA201991122 A EA 201991122A EA 201991122 A1 EA201991122 A1 EA 201991122A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compounds
- propanic
- acids
- substituted
- integrin inhibitors
- Prior art date
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- 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
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- 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
- A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—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
Abstract
Настоящее изобретение относится к соединениям формулы (I)или их стереоизомерам, таутомерам или фармацевтически приемлемым солям или сольватам, где все переменные являются такими, как определено в настоящем документе. Эти соединения являются антагонистами к αv-содержащим интегринам. Данное изобретение также относится к фармацевтическим композициям, содержащим эти соединения, и способам лечения заболевания, расстройства или состояния, связанного с нарушением регуляции αv-содержащих интегринов, таких как патологический фиброз, отторжение трансплантата, рак, остеопороз и воспалительные расстройства, с применением соединений и фармацевтических композиций.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662418848P | 2016-11-08 | 2016-11-08 | |
| PCT/US2017/060376 WO2018089353A1 (en) | 2016-11-08 | 2017-11-07 | 3-substituted propionic acids as alpha v integrin inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201991122A1 true EA201991122A1 (ru) | 2019-10-31 |
| EA038164B1 EA038164B1 (ru) | 2021-07-16 |
Family
ID=60409432
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201991122A EA038164B1 (ru) | 2016-11-08 | 2017-11-07 | 3-замещенные пропановые кислоты в качестве ингибиторов интегрина v |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US10968219B2 (ru) |
| EP (1) | EP3538525B1 (ru) |
| JP (1) | JP7097358B2 (ru) |
| KR (1) | KR102505629B1 (ru) |
| CN (1) | CN110167935B (ru) |
| AR (1) | AR110153A1 (ru) |
| AU (1) | AU2017359023B2 (ru) |
| CA (1) | CA3042707A1 (ru) |
| CL (1) | CL2019001264A1 (ru) |
| CO (1) | CO2019005824A2 (ru) |
| DK (1) | DK3538525T3 (ru) |
| EA (1) | EA038164B1 (ru) |
| ES (1) | ES2925173T3 (ru) |
| HR (1) | HRP20220990T1 (ru) |
| HU (1) | HUE059708T2 (ru) |
| IL (1) | IL266473B (ru) |
| LT (1) | LT3538525T (ru) |
| MA (1) | MA46743A (ru) |
| MX (1) | MX2019005244A (ru) |
| MY (1) | MY199931A (ru) |
| PE (1) | PE20191647A1 (ru) |
| PL (1) | PL3538525T3 (ru) |
| PT (1) | PT3538525T (ru) |
| RS (1) | RS63483B1 (ru) |
| SI (1) | SI3538525T1 (ru) |
| TW (1) | TWI763733B (ru) |
| WO (1) | WO2018089353A1 (ru) |
| ZA (1) | ZA201903665B (ru) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201823208A (zh) | 2016-09-07 | 2018-07-01 | 美商普萊恩醫療公司 | N－醯基胺基酸化合物及其使用方法 |
| CA3042684A1 (en) * | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | Azole amides and amines as .alpha.v integrin inhibitors |
| EP3538526B1 (en) * | 2016-11-08 | 2024-04-10 | Bristol-Myers Squibb Company | Cyclobutane- and azetidine-containing mono and spirocyclic compounds as alpha v integrin inhibitors |
| LT3538525T (lt) * | 2016-11-08 | 2022-09-26 | Bristol-Myers Squibb Company | Propiono rūgštys, pakeistos 3 padėtyje, kaip alfa v integrino inhibitoriai |
| RU2019116820A (ru) | 2016-12-29 | 2021-01-29 | Сент-Луис Юниверсити | Антагонисты интегрина |
| US11046685B2 (en) | 2017-02-28 | 2021-06-29 | Morphic Therapeutic, Inc. | Inhibitors of (α-v)(β-6) integrin |
| US20180244648A1 (en) | 2017-02-28 | 2018-08-30 | Lazuli, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| CR20210109A (es) | 2018-08-29 | 2021-06-24 | Morphic Therapeutic Inc | INHIBICIÓN DE LA INTEGRINA av ß6 |
| CR20210213A (es) | 2018-10-30 | 2021-06-24 | Gilead Sciences Inc | Derivados de quinolina como inhibidores de la integrina alfa4beta7 |
| AU2019373242B2 (en) | 2018-10-30 | 2023-07-13 | Gilead Sciences, Inc. | Compounds for inhibition of alpha 4 beta 7 integrin |
| US11179383B2 (en) | 2018-10-30 | 2021-11-23 | Gilead Sciences, Inc. | Compounds for inhibition of α4β7 integrin |
| US11174256B2 (en) | 2018-10-30 | 2021-11-16 | Gilead Sciences, Inc. | Imidazopyridine derivatives |
| CN109824495B (zh) * | 2019-02-02 | 2022-12-09 | 盐城师范学院 | 一种新型偶联反应在制备碳-碳键结构化合物中的应用 |
| AU2020329207B2 (en) | 2019-08-14 | 2024-02-29 | Gilead Sciences, Inc. | Compounds for inhibition of alpha 4 beta 7 integrin |
| GB202010626D0 (en) | 2020-07-10 | 2020-08-26 | Univ Nottingham | Compound |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0451790A1 (de) * | 1990-04-12 | 1991-10-16 | Hoechst Aktiengesellschaft | 3,5-disubstituierte 2-Isoxazoline und Isoxazole, Verfahren zu deren Herstellung, diese enthaltende Mittel und ihre Verwendung |
| US5849736A (en) | 1993-11-24 | 1998-12-15 | The Dupont Merck Pharmaceutical Company | Isoxazoline and isoxazole fibrinogen receptor antagonists |
| ZA972195B (en) | 1996-03-15 | 1998-09-14 | Du Pont Merck Pharma | Spirocycle integrin inhibitors |
| JP2001524481A (ja) | 1997-11-26 | 2001-12-04 | デュポン ファーマシューティカルズ カンパニー | αＶβ３アンタゴニストとしての１，３，４−チアジアゾール類および１，３，４−オキサジアゾール類 |
| WO1999030709A1 (en) * | 1997-12-17 | 1999-06-24 | Merck & Co., Inc. | Integrin receptor antagonists |
| AU748621B2 (en) * | 1998-08-13 | 2002-06-06 | Merck & Co., Inc. | Integrin receptor antagonists |
| KR100854424B1 (ko) | 2001-01-29 | 2008-08-27 | 3-디멘져널 파마슈티칼즈 인코오포레이티드 | 치환된 인돌 및 인테그린 길항제로서의 이들의 용도 |
| BR0316875A (pt) * | 2002-12-20 | 2005-10-25 | Pharmacia Corp | Compostos de pirazol como derivados antagonistas receptores da integrina, sua composição farmacêutica e respectivo uso |
| JP2006518333A (ja) * | 2002-12-20 | 2006-08-10 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニストとしてのヘテロアリールアルカン酸 |
| WO2006108040A1 (en) | 2005-04-05 | 2006-10-12 | Janssen Pharmaceutica, N.V. | Substituted indoles and their use as integrin antagonists |
| TW200800999A (en) * | 2005-09-06 | 2008-01-01 | Astrazeneca Ab | Novel compounds |
| US7592461B2 (en) | 2005-12-21 | 2009-09-22 | Bristol-Myers Squibb Company | Indane modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof |
| AR059224A1 (es) | 2006-01-31 | 2008-03-19 | Jerini Ag | Compuestos para la inhibicion de integrinas y uso de estas |
| JP2009539815A (ja) * | 2006-06-09 | 2009-11-19 | アストラゼネカ アクチボラグ | 固形腫瘍の治療用のａ５ｂ１アンタゴニストとしてのＮ−（ベンゾイル）−Ｏ−［２−（ピリジン−２−イルアミノ）エチル］−Ｌ−チロシン誘導体と関連化合物 |
| WO2008125811A1 (en) * | 2007-04-11 | 2008-10-23 | Astrazeneca Ab | N-[HETEROARYLCARBONYL]-S-THIENYL-L-ALANINE DERIVATIVES AS α5β1 ANTAGONISTS |
| EP2473485B1 (en) | 2009-09-04 | 2014-04-23 | Basf Se | Process for preparing 1-phenylpyrazoles |
| US9556201B2 (en) | 2009-10-29 | 2017-01-31 | Glaxosmithkline Llc | Bicyclic pyridines and analogs as sirtuin modulators |
| ITFI20100019A1 (it) | 2010-02-12 | 2011-08-13 | Univ Firenze | Inibitori peptidomimetici di integrine basati sull'1,2,3-triazolo per la diagnosi e terapia dei tumori. |
| GB201305668D0 (en) | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| TWI667233B (zh) | 2013-12-19 | 2019-08-01 | 德商拜耳製藥公司 | 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途 |
| GB201417011D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417094D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417002D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201417018D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| AU2016219906B2 (en) | 2015-02-19 | 2020-10-01 | Scifluor Life Sciences, Inc. | Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof |
| CA2981371A1 (en) | 2015-03-10 | 2016-09-15 | The Regents Of The University Of California | Anti-alphavbeta1 integrin inhibitors and methods of use |
| LT3538525T (lt) * | 2016-11-08 | 2022-09-26 | Bristol-Myers Squibb Company | Propiono rūgštys, pakeistos 3 padėtyje, kaip alfa v integrino inhibitoriai |
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2017
- 2017-11-07 LT LTEPPCT/US2017/060376T patent/LT3538525T/lt unknown
- 2017-11-07 SI SI201731195T patent/SI3538525T1/sl unknown
- 2017-11-07 HU HUE17801230A patent/HUE059708T2/hu unknown
- 2017-11-07 PT PT178012308T patent/PT3538525T/pt unknown
- 2017-11-07 AU AU2017359023A patent/AU2017359023B2/en active Active
- 2017-11-07 MY MYPI2019002576A patent/MY199931A/en unknown
- 2017-11-07 US US16/347,844 patent/US10968219B2/en active Active
- 2017-11-07 WO PCT/US2017/060376 patent/WO2018089353A1/en unknown
- 2017-11-07 PL PL17801230.8T patent/PL3538525T3/pl unknown
- 2017-11-07 KR KR1020197016082A patent/KR102505629B1/ko active IP Right Grant
- 2017-11-07 EP EP17801230.8A patent/EP3538525B1/en active Active
- 2017-11-07 RS RS20220759A patent/RS63483B1/sr unknown
- 2017-11-07 PE PE2019000940A patent/PE20191647A1/es unknown
- 2017-11-07 HR HRP20220990TT patent/HRP20220990T1/hr unknown
- 2017-11-07 CN CN201780082473.2A patent/CN110167935B/zh active Active
- 2017-11-07 ES ES17801230T patent/ES2925173T3/es active Active
- 2017-11-07 CA CA3042707A patent/CA3042707A1/en active Pending
- 2017-11-07 DK DK17801230.8T patent/DK3538525T3/da active
- 2017-11-07 MX MX2019005244A patent/MX2019005244A/es unknown
- 2017-11-07 MA MA046743A patent/MA46743A/fr unknown
- 2017-11-07 JP JP2019523576A patent/JP7097358B2/ja active Active
- 2017-11-07 EA EA201991122A patent/EA038164B1/ru unknown
- 2017-11-08 TW TW106138533A patent/TWI763733B/zh active
- 2017-11-08 AR ARP170103105A patent/AR110153A1/es unknown
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2019
- 2019-05-06 IL IL266473A patent/IL266473B/en unknown
- 2019-05-08 CL CL2019001264A patent/CL2019001264A1/es unknown
- 2019-06-04 CO CONC2019/0005824A patent/CO2019005824A2/es unknown
- 2019-06-07 ZA ZA2019/03665A patent/ZA201903665B/en unknown
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2021
- 2021-02-24 US US17/184,179 patent/US11884661B2/en active Active
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