RU2017114346A - АНТАГОНИСТЫ ИНТЕГРИНА ανβ6 - Google Patents
АНТАГОНИСТЫ ИНТЕГРИНА ανβ6 Download PDFInfo
- Publication number
- RU2017114346A RU2017114346A RU2017114346A RU2017114346A RU2017114346A RU 2017114346 A RU2017114346 A RU 2017114346A RU 2017114346 A RU2017114346 A RU 2017114346A RU 2017114346 A RU2017114346 A RU 2017114346A RU 2017114346 A RU2017114346 A RU 2017114346A
- Authority
- RU
- Russia
- Prior art keywords
- compound according
- pharmaceutically acceptable
- acceptable salt
- fluoro
- humans
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 16
- 241000282412 Homo Species 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 3
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 3
- 230000008485 antagonism Effects 0.000 claims 2
- 230000003176 fibrotic effect Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 229940044551 receptor antagonist Drugs 0.000 claims 2
- BUAYFDWYSYICGP-PIKZIKFNSA-N (3S)-3-(2-fluoro-5-morpholin-4-ylphenyl)-4-[(3S)-3-fluoro-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid Chemical compound OC(=O)C[C@H](CN1CC[C@@](F)(CCC2=CC=C3CCCNC3=N2)C1)C1=C(F)C=CC(=C1)N1CCOCC1 BUAYFDWYSYICGP-PIKZIKFNSA-N 0.000 claims 1
- HKDUWRRLEDNORE-LXFBAYGMSA-N (3S)-4-[(3S)-3-fluoro-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]-3-(3-morpholin-4-ylphenyl)butanoic acid Chemical compound OC(=O)C[C@H](CN1CC[C@@](F)(CCC2=CC=C3CCCNC3=N2)C1)C1=CC(=CC=C1)N1CCOCC1 HKDUWRRLEDNORE-LXFBAYGMSA-N 0.000 claims 1
- BUAYFDWYSYICGP-UHFFFAOYSA-N OC(=O)CC(CN1CCC(F)(CCC2=CC=C3CCCNC3=N2)C1)C1=C(F)C=CC(=C1)N1CCOCC1 Chemical compound OC(=O)CC(CN1CCC(F)(CCC2=CC=C3CCCNC3=N2)C1)C1=C(F)C=CC(=C1)N1CCOCC1 BUAYFDWYSYICGP-UHFFFAOYSA-N 0.000 claims 1
- HKDUWRRLEDNORE-UHFFFAOYSA-N OC(=O)CC(CN1CCC(F)(CCC2=CC=C3CCCNC3=N2)C1)C1=CC(=CC=C1)N1CCOCC1 Chemical compound OC(=O)CC(CN1CCC(F)(CCC2=CC=C3CCCNC3=N2)C1)C1=CC(=CC=C1)N1CCOCC1 HKDUWRRLEDNORE-UHFFFAOYSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 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
- A61K31/4375—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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pyrrole Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1417011.2A GB201417011D0 (en) | 2014-09-26 | 2014-09-26 | Novel compounds |
| GB1417011.2 | 2014-09-26 | ||
| PCT/EP2015/071777 WO2016046226A1 (en) | 2014-09-26 | 2015-09-22 | Novel compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2017114346A true RU2017114346A (ru) | 2018-11-02 |
Family
ID=51901167
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017114346A RU2017114346A (ru) | 2014-09-26 | 2015-09-22 | АНТАГОНИСТЫ ИНТЕГРИНА ανβ6 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10000489B2 (https=) |
| EP (1) | EP3197893B1 (https=) |
| JP (1) | JP6665169B2 (https=) |
| KR (1) | KR20170063590A (https=) |
| CN (1) | CN107074849A (https=) |
| AR (1) | AR101995A1 (https=) |
| AU (1) | AU2015320859A1 (https=) |
| BR (1) | BR112017006253A2 (https=) |
| CA (1) | CA2962326A1 (https=) |
| ES (1) | ES2704525T3 (https=) |
| GB (1) | GB201417011D0 (https=) |
| RU (1) | RU2017114346A (https=) |
| TW (1) | TW201629057A (https=) |
| UY (1) | UY36315A (https=) |
| WO (1) | WO2016046226A1 (https=) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201305668D0 (en) | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| GB201417002D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201417094D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417018D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201604681D0 (en) * | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| BR112019009245A2 (pt) | 2016-11-08 | 2019-07-16 | Bristol-Myers Squibb Company | azol amidas e aminas como inibidores de alfav integrina |
| AU2017359023B2 (en) | 2016-11-08 | 2021-12-09 | Bristol-Myers Squibb Company | 3-substituted propionic acids as alpha v integrin inhibitors |
| WO2018089357A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | INDAZOLE DERIVATIVES AS αV INTEGRIN ANTAGONISTS |
| HRP20210228T1 (hr) * | 2016-11-08 | 2021-03-19 | Bristol-Myers Squibb Company | Amidi pirola kao inhibitori alfa v integrina |
| ES2984394T3 (es) | 2016-11-08 | 2024-10-29 | Bristol Myers Squibb Co | Compuestos mono y espirocíclicos que contienen ciclobutano y azetidina como inhibidores de la integrina alfa v |
| US10696672B2 (en) | 2016-12-23 | 2020-06-30 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
| MA52117A (fr) | 2017-02-28 | 2022-04-06 | Morphic Therapeutic Inc | Inhibiteurs de l'intégrine (alpha-v) (bêta-6) |
| MX394210B (es) | 2017-02-28 | 2025-03-04 | Morphic Therapeutic Inc | INHIBIDORES DE INTEGRINA AVß6. |
| CN107823208A (zh) * | 2017-10-25 | 2018-03-23 | 南京多宝生物科技有限公司 | 吗啉类化合物在制备治疗和预防肾纤维化药物中的应用 |
| KR102700471B1 (ko) | 2017-11-07 | 2024-08-28 | 브리스톨-마이어스 스큅 컴퍼니 | 알파 v 인테그린 억제제로서의 피롤로피라진 유도체 |
| CN108208177A (zh) * | 2017-11-28 | 2018-06-29 | 上海交通大学医学院附属新华医院 | 含丁酸类化合物的组合物及其应用 |
| SI3844162T1 (sl) * | 2018-08-29 | 2025-06-30 | Morphic Therapeutic, Inc. | Zaviralci integrina alfa v beta6 |
| WO2020047239A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | INHIBITING αV β6 INTEGRIN |
| WO2020047208A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| TW202028179A (zh) | 2018-10-08 | 2020-08-01 | 美商普萊恩醫療公司 | 胺基酸化合物及使用方法 |
| US20240165195A1 (en) * | 2018-10-09 | 2024-05-23 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of alpha-v-integrin (cd51) inhibitors for the treatment of cardiac fibrosis |
| JP2022512648A (ja) * | 2018-10-09 | 2022-02-07 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 心筋線維化の処置のためのαＶ－インテグリン（ＣＤ５１）阻害剤の使用 |
| US11034710B2 (en) * | 2018-12-04 | 2021-06-15 | Sumitomo Dainippon Pharma Oncology, Inc. | CDK9 inhibitors and polymorphs thereof for use as agents for treatment of cancer |
| JP2025518533A (ja) * | 2022-05-18 | 2025-06-17 | プライアント・セラピューティクス・インコーポレイテッド | インテグリン阻害剤の安定化 |
| EP4605008A1 (en) | 2022-12-14 | 2025-08-27 | Alnylam Pharmaceuticals, Inc. | Alpha-v beta-6 integrin ligands for extrahepatic delivery |
| WO2025259743A1 (en) | 2024-06-12 | 2025-12-18 | Alnylam Pharmaceuticals, Inc. | Dual conjugate compounds for extrahepatic delivery |
| WO2025259747A2 (en) | 2024-06-12 | 2025-12-18 | Alnylam Pharmaceuticals, Inc. | Dystrophy myotonic protein kinase (dmpk) irna compositions and methods of use thereof |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2315370A1 (en) | 1997-12-17 | 1999-06-24 | Merck & Co., Inc. | Integrin receptor antagonists |
| KR20010033248A (ko) | 1997-12-17 | 2001-04-25 | 폴락 돈나 엘. | 인테그린 수용체 길항제 |
| CN1589145A (zh) | 1999-06-02 | 2005-03-02 | 麦克公司 | αv整联蛋白受体拮抗剂 |
| WO2000078317A1 (en) | 1999-06-23 | 2000-12-28 | Merck & Co., Inc. | Integrin receptor antagonists |
| EP1229910A4 (en) * | 1999-10-04 | 2003-10-01 | Merck & Co Inc | integrin |
| PL355011A1 (en) | 1999-11-08 | 2004-03-22 | Merck & Co, Inc. | Process and intermediates for the preparation of imidazolidinone alpha v integrin antagonists |
| US7119098B2 (en) | 2000-06-15 | 2006-10-10 | Pharmacia Corporation | Heteroarylakanoic acids as intergrin receptor antagonists |
| AU7793501A (en) | 2000-07-26 | 2002-02-05 | Merck & Co Inc | Alpha v integrin receptor antagonists |
| WO2002022616A2 (en) | 2000-09-14 | 2002-03-21 | Merck & Co., Inc. | Alpha v integrin receptor antagonists |
| CA2432504A1 (en) | 2001-01-03 | 2002-07-11 | Merck & Co., Inc. | Methods and compositions for treating periodontal disease |
| DE10112771A1 (de) | 2001-03-16 | 2002-09-26 | Merck Patent Gmbh | Inhibitoren des Integrins alpha¶v¶beta¶6¶ |
| US20040224986A1 (en) * | 2002-08-16 | 2004-11-11 | Bart De Corte | Piperidinyl targeting compounds that selectively bind integrins |
| EP1592421A1 (en) | 2002-12-20 | 2005-11-09 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| US6932865B2 (en) | 2003-04-11 | 2005-08-23 | Lockheed Martin Corporation | System and method of making single-crystal structures through free-form fabrication techniques |
| EP2139882B1 (en) | 2007-03-23 | 2013-12-25 | Amgen Inc. | 3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors |
| EP2211615A4 (en) | 2007-10-22 | 2010-10-13 | Glaxosmithkline Llc | PYRIDOSULFONAMIDE DERIVATIVES AS PI3 KINASE INHIBITORS |
| WO2011111880A1 (ko) | 2010-03-08 | 2011-09-15 | 주식회사 메디젠텍 | 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물 |
| GB201305668D0 (en) * | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| WO2015048819A1 (en) | 2013-09-30 | 2015-04-02 | The Regents Of The University Of California | Anti-alphavbeta1 integrin compounds and methods |
| 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 |
| GB201417094D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| US9790222B2 (en) | 2015-02-19 | 2017-10-17 | Scifluor Life Sciences, Inc. | Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof |
| WO2016145258A1 (en) | 2015-03-10 | 2016-09-15 | The Regents Of The University Of California | Anti-alphavbeta1 integrin inhibitors and methods of use |
| GB201604589D0 (en) | 2016-03-18 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical compound |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| GB201604681D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
-
2014
- 2014-09-26 GB GBGB1417011.2A patent/GB201417011D0/en not_active Ceased
-
2015
- 2015-09-22 UY UY0001036315A patent/UY36315A/es not_active Application Discontinuation
- 2015-09-22 ES ES15767476T patent/ES2704525T3/es active Active
- 2015-09-22 AR ARP150103048A patent/AR101995A1/es unknown
- 2015-09-22 CN CN201580051539.2A patent/CN107074849A/zh active Pending
- 2015-09-22 US US15/514,407 patent/US10000489B2/en not_active Expired - Fee Related
- 2015-09-22 RU RU2017114346A patent/RU2017114346A/ru unknown
- 2015-09-22 JP JP2017516365A patent/JP6665169B2/ja not_active Expired - Fee Related
- 2015-09-22 KR KR1020177007734A patent/KR20170063590A/ko not_active Withdrawn
- 2015-09-22 WO PCT/EP2015/071777 patent/WO2016046226A1/en not_active Ceased
- 2015-09-22 TW TW104131367A patent/TW201629057A/zh unknown
- 2015-09-22 BR BR112017006253A patent/BR112017006253A2/pt not_active Application Discontinuation
- 2015-09-22 EP EP15767476.3A patent/EP3197893B1/en active Active
- 2015-09-22 CA CA2962326A patent/CA2962326A1/en active Pending
- 2015-09-22 AU AU2015320859A patent/AU2015320859A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2016046226A1 (en) | 2016-03-31 |
| CN107074849A (zh) | 2017-08-18 |
| US20170298063A1 (en) | 2017-10-19 |
| AR101995A1 (es) | 2017-01-25 |
| TW201629057A (zh) | 2016-08-16 |
| JP6665169B2 (ja) | 2020-03-13 |
| JP2017528503A (ja) | 2017-09-28 |
| CA2962326A1 (en) | 2016-03-31 |
| EP3197893A1 (en) | 2017-08-02 |
| BR112017006253A2 (pt) | 2017-12-12 |
| GB201417011D0 (en) | 2014-11-12 |
| KR20170063590A (ko) | 2017-06-08 |
| ES2704525T3 (es) | 2019-03-18 |
| AU2015320859A1 (en) | 2017-03-09 |
| UY36315A (es) | 2016-04-29 |
| EP3197893B1 (en) | 2018-10-24 |
| US10000489B2 (en) | 2018-06-19 |
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