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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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)
- Pyrrole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1417011.2 | 2014-09-26 | ||
| GBGB1417011.2A GB201417011D0 (en) | 2014-09-26 | 2014-09-26 | Novel compounds |
| 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 (enExample) |
| EP (1) | EP3197893B1 (enExample) |
| JP (1) | JP6665169B2 (enExample) |
| KR (1) | KR20170063590A (enExample) |
| CN (1) | CN107074849A (enExample) |
| AR (1) | AR101995A1 (enExample) |
| AU (1) | AU2015320859A1 (enExample) |
| BR (1) | BR112017006253A2 (enExample) |
| CA (1) | CA2962326A1 (enExample) |
| ES (1) | ES2704525T3 (enExample) |
| GB (1) | GB201417011D0 (enExample) |
| RU (1) | RU2017114346A (enExample) |
| TW (1) | TW201629057A (enExample) |
| UY (1) | UY36315A (enExample) |
| WO (1) | WO2016046226A1 (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201305668D0 (en) | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| GB201417018D0 (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 |
| GB201417094D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| 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 |
| BR112019009245A2 (pt) | 2016-11-08 | 2019-07-16 | Bristol-Myers Squibb Company | azol amidas e aminas como inibidores de alfav integrina |
| CA3042710A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | Cyclobutane- and azetidine-containing mono and spirocyclic compounds as .alpha.v integrin inhibitors |
| WO2018089353A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | 3-substituted propionic acids as alpha v integrin inhibitors |
| EA201991123A1 (ru) | 2016-11-08 | 2019-11-29 | ИНДАЗОЛОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ АНТАГОНИСТОВ ИНТЕГРИНА αV | |
| PL3538528T3 (pl) * | 2016-11-08 | 2021-05-31 | Bristol-Myers Squibb Company | Amidy pirolu jako inhibitory integryny alfa v |
| EP3558303A4 (en) | 2016-12-23 | 2020-07-29 | Pliant Therapeutics, Inc. | AMINO ACID COMPOUNDS AND PROCESSES FOR USE |
| IL316954A (en) | 2017-02-28 | 2025-01-01 | Morphic Therapeutic Inc | (Alpha-V)(beta-6)integrin inhibitors |
| EP3760202A1 (en) | 2017-02-28 | 2021-01-06 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| 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 |
| BR112020008893A2 (pt) | 2017-11-07 | 2020-10-13 | Bristol-Myers Squibb Company | derivados de pirrolopirazina como inibidores de alfa v integrina |
| 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 |
| UY38352A (es) * | 2018-08-29 | 2020-03-31 | Morphic Therapeutic Inc | Inhibidores de integrina alfavbeta6 |
| UY38353A (es) | 2018-08-29 | 2020-03-31 | Morphic Therapeutic Inc | Inhibición de integrina alfavbeta6 |
| 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 |
| 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 |
| MX2021006544A (es) * | 2018-12-04 | 2021-07-07 | Sumitomo Pharma Oncology Inc | Inhibidores de cinasa dependiente de ciclina 9 (cdk9) y polimorfos de los mismos para uso como agentes para el tratamiento de cancer. |
| EP4525866A1 (en) * | 2022-05-18 | 2025-03-26 | Pliant Therapeutics, Inc. | Stabilization of integrin inhibitors |
| WO2024129931A1 (en) | 2022-12-14 | 2024-06-20 | Alnylam Pharmaceuticals, Inc. | ALPHA-V BETA-6(ανβ6) INTEGRIN LIGANDS 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 |
| WO2025259743A1 (en) | 2024-06-12 | 2025-12-18 | Alnylam Pharmaceuticals, Inc. | Dual conjugate compounds for extrahepatic delivery |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1047425A4 (en) | 1997-12-17 | 2009-04-22 | Merck & Co Inc | INTEGRIN RECEPTOR ANTAGONISTS |
| BR9813769A (pt) | 1997-12-17 | 2000-10-10 | Merck & Co Inc | Composto, composição farmacêutica, e, processos para fabricar a mesma, para evocar um efeito antagonizante do receptor da integrina em um mamìfero em necessidade deste, para tratar ou prevenir uma condição mediada pelo antagonismo de um receptor da integrina em um mamìfero em necessidade deste, para inibir a reabsorção óssea em um mamìfero em necessidade deste, e para tratar o desenvolvimento tumoral em um mamìfero em necessidade deste. |
| DZ3263A1 (fr) | 1999-06-02 | 2000-12-07 | Merck & Co Inc | Antagonistes du recepteur de l'alpha v integrine |
| AU748949B2 (en) | 1999-06-23 | 2002-06-13 | Merck & Co., Inc. | Integrin receptor antagonists |
| WO2001024797A1 (en) * | 1999-10-04 | 2001-04-12 | Merck & Co., Inc. | Integrin receptor antagonists |
| CN1414966A (zh) | 1999-11-08 | 2003-04-30 | 麦克公司 | 用于制备咪唑烷酮αu蛋白拮抗剂的方法和中间体 |
| US7119098B2 (en) | 2000-06-15 | 2006-10-10 | Pharmacia Corporation | Heteroarylakanoic acids as intergrin receptor antagonists |
| US7056909B2 (en) | 2000-07-26 | 2006-06-06 | Merck & Co., Inc. | Alpha v integrin receptor antagonists |
| WO2002022616A2 (en) | 2000-09-14 | 2002-03-21 | Merck & Co., Inc. | Alpha v integrin receptor antagonists |
| EP1349548A4 (en) | 2001-01-03 | 2004-06-02 | Merck & Co Inc | METHOD AND COMPOSITIONS FOR TREATING PERIODONTOSIS |
| 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 |
| BR0317600A (pt) | 2002-12-20 | 2005-11-29 | Pharmacia Corp | ácidos heteroarilalcanóicos como derivados de antagonistas de receptor de integrina |
| US6932865B2 (en) | 2003-04-11 | 2005-08-23 | Lockheed Martin Corporation | System and method of making single-crystal structures through free-form fabrication techniques |
| US7705018B2 (en) | 2007-03-23 | 2010-04-27 | Amgen Inc. | Substituted quinolines and their uses in treatment of inflammatory and related conditions |
| 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 |
| GB201417018D0 (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 |
| GB201417094D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| EP3925959A1 (en) | 2015-02-19 | 2021-12-22 | OcuTerra Therapeutics, Inc. | Fluorinated derivatives of 3-(2-oxo-3-(3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl)imidazolidin-1-yl)propanoic acid 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 |
| 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 WO PCT/EP2015/071777 patent/WO2016046226A1/en not_active Ceased
- 2015-09-22 ES ES15767476T patent/ES2704525T3/es active Active
- 2015-09-22 CN CN201580051539.2A patent/CN107074849A/zh active Pending
- 2015-09-22 RU RU2017114346A patent/RU2017114346A/ru unknown
- 2015-09-22 EP EP15767476.3A patent/EP3197893B1/en active Active
- 2015-09-22 US US15/514,407 patent/US10000489B2/en not_active Expired - Fee Related
- 2015-09-22 JP JP2017516365A patent/JP6665169B2/ja not_active Expired - Fee Related
- 2015-09-22 UY UY0001036315A patent/UY36315A/es not_active Application Discontinuation
- 2015-09-22 BR BR112017006253A patent/BR112017006253A2/pt not_active Application Discontinuation
- 2015-09-22 TW TW104131367A patent/TW201629057A/zh unknown
- 2015-09-22 AU AU2015320859A patent/AU2015320859A1/en not_active Abandoned
- 2015-09-22 AR ARP150103048A patent/AR101995A1/es unknown
- 2015-09-22 CA CA2962326A patent/CA2962326A1/en active Pending
- 2015-09-22 KR KR1020177007734A patent/KR20170063590A/ko not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| CA2962326A1 (en) | 2016-03-31 |
| US20170298063A1 (en) | 2017-10-19 |
| EP3197893B1 (en) | 2018-10-24 |
| EP3197893A1 (en) | 2017-08-02 |
| KR20170063590A (ko) | 2017-06-08 |
| WO2016046226A1 (en) | 2016-03-31 |
| US10000489B2 (en) | 2018-06-19 |
| UY36315A (es) | 2016-04-29 |
| AU2015320859A1 (en) | 2017-03-09 |
| AR101995A1 (es) | 2017-01-25 |
| BR112017006253A2 (pt) | 2017-12-12 |
| CN107074849A (zh) | 2017-08-18 |
| GB201417011D0 (en) | 2014-11-12 |
| ES2704525T3 (es) | 2019-03-18 |
| TW201629057A (zh) | 2016-08-16 |
| JP6665169B2 (ja) | 2020-03-13 |
| JP2017528503A (ja) | 2017-09-28 |
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