RU2017114352A - АНТАГОНИСТЫ ИНТЕГРИНА ανβ6 - Google Patents
АНТАГОНИСТЫ ИНТЕГРИНА ανβ6 Download PDFInfo
- Publication number
- RU2017114352A RU2017114352A RU2017114352A RU2017114352A RU2017114352A RU 2017114352 A RU2017114352 A RU 2017114352A RU 2017114352 A RU2017114352 A RU 2017114352A RU 2017114352 A RU2017114352 A RU 2017114352A RU 2017114352 A RU2017114352 A RU 2017114352A
- Authority
- RU
- Russia
- Prior art keywords
- compound according
- pharmaceutically acceptable
- acceptable salt
- pyrrolidin
- tetrahydro
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 23
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims 20
- -1 3-morpholinophenyl Chemical group 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 241000282412 Homo Species 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 229940123038 Integrin antagonist Drugs 0.000 claims 2
- 230000008485 antagonism Effects 0.000 claims 2
- 230000009286 beneficial effect Effects 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000003176 fibrotic effect Effects 0.000 claims 2
- 239000012634 fragment Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 230000004060 metabolic process Effects 0.000 claims 2
- IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical class CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- SDXAWLJRERMRKF-UHFFFAOYSA-N 3,5-dimethyl-1h-pyrazole Chemical group CC=1C=C(C)NN=1 SDXAWLJRERMRKF-UHFFFAOYSA-N 0.000 claims 1
- XKVUYEYANWFIJX-UHFFFAOYSA-N 5-methyl-1h-pyrazole Chemical group CC1=CC=NN1 XKVUYEYANWFIJX-UHFFFAOYSA-N 0.000 claims 1
- NIVBRIPUAQCFIE-ZJSXRUAMSA-N OC(=O)C[C@H](CN1CC[C@@H](CCC2=CC=C3CCCNC3=N2)C1)C1=CC(=CC=C1)N1CCOCC1 Chemical compound OC(=O)C[C@H](CN1CC[C@@H](CCC2=CC=C3CCCNC3=N2)C1)C1=CC(=CC=C1)N1CCOCC1 NIVBRIPUAQCFIE-ZJSXRUAMSA-N 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 239000001273 butane Substances 0.000 claims 1
- 239000003085 diluting agent Substances 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
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- OFBQJSOFQDEBGM-UHFFFAOYSA-N n-pentane Natural products CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- 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
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- 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
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1417018.7 | 2014-09-26 | ||
| GBGB1417018.7A GB201417018D0 (en) | 2014-09-26 | 2014-09-26 | Novel compounds |
| PCT/EP2015/071798 WO2016046241A1 (en) | 2014-09-26 | 2015-09-22 | Novel compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2017114352A true RU2017114352A (ru) | 2018-10-26 |
Family
ID=51901174
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017114352A RU2017114352A (ru) | 2014-09-26 | 2015-09-22 | АНТАГОНИСТЫ ИНТЕГРИНА ανβ6 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US10004724B2 (enExample) |
| EP (1) | EP3197895B1 (enExample) |
| JP (1) | JP6672276B2 (enExample) |
| KR (1) | KR20170054413A (enExample) |
| CN (1) | CN107074850A (enExample) |
| AU (1) | AU2015320874A1 (enExample) |
| BR (1) | BR112017006240A2 (enExample) |
| CA (1) | CA2962319A1 (enExample) |
| ES (1) | ES2796235T3 (enExample) |
| GB (1) | GB201417018D0 (enExample) |
| RU (1) | RU2017114352A (enExample) |
| WO (1) | WO2016046241A1 (enExample) |
Families Citing this family (15)
| 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 |
| 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 |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| CA3042714A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | Indazole derivatives as a .alpha.v integrin antagonists |
| BR112019009245A2 (pt) | 2016-11-08 | 2019-07-16 | Bristol-Myers Squibb Company | azol amidas e aminas como inibidores de alfav integrina |
| HRP20210228T1 (hr) | 2016-11-08 | 2021-03-19 | Bristol-Myers Squibb Company | Amidi pirola kao inhibitori alfa v integrina |
| WO2018089355A1 (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 |
| USRE50554E1 (en) | 2016-12-23 | 2025-08-26 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
| EP4147698A1 (en) | 2017-02-28 | 2023-03-15 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| US20180244648A1 (en) | 2017-02-28 | 2018-08-30 | Lazuli, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| WO2019094319A1 (en) | 2017-11-07 | 2019-05-16 | Bristol-Myers Squibb Company | Pyrrolopyrazine derivatives as alpha v integrin inhibitors |
| CR20210109A (es) | 2018-08-29 | 2021-06-24 | Morphic Therapeutic Inc | INHIBICIÓN DE LA INTEGRINA av ß6 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2241192T3 (es) | 1997-12-17 | 2005-10-16 | MERCK & CO., INC. (A NEW JERSEY CORP.) | Antagonistas del receptor de integrina. |
| EP1047425A4 (en) * | 1997-12-17 | 2009-04-22 | Merck & Co Inc | INTEGRIN RECEPTOR ANTAGONISTS |
| CN1589145A (zh) | 1999-06-02 | 2005-03-02 | 麦克公司 | αv整联蛋白受体拮抗剂 |
| AU748949B2 (en) | 1999-06-23 | 2002-06-13 | Merck & Co., Inc. | Integrin receptor antagonists |
| AU7743400A (en) * | 1999-10-04 | 2001-05-10 | Merck & Co., Inc. | Integrin receptor antagonists |
| IL149313A0 (en) | 1999-11-08 | 2002-11-10 | Merck & Co Inc | Process and intermediates for the preparation of imidazolidinone alpha v integrin antagonists |
| WO2001096334A2 (en) | 2000-06-15 | 2001-12-20 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| CA2416751A1 (en) | 2000-07-26 | 2002-01-31 | Merck & Co., Inc. | Alpha v integrin receptor antagonists |
| AU2001290772A1 (en) | 2000-09-14 | 2002-03-26 | Merck And Co., Inc. | Alpha v integrin receptor antagonists |
| WO2002053099A2 (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 |
| CA2507699A1 (en) | 2002-12-20 | 2004-07-15 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| PT2139882E (pt) | 2007-03-23 | 2014-01-30 | Amgen Inc | Derivados de quinolina ou quinoxalina 3-substituídos e sua utilização como inibidores de fosfatidilinositol 3-cinase (pi3k) |
| JP2011500823A (ja) | 2007-10-22 | 2011-01-06 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Ｐｉ３キナーゼ阻害物質としてのピリドスルホンアミド誘導体 |
| 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 |
| 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 |
| JP2018510139A (ja) | 2015-02-19 | 2018-04-12 | サイフルーア ライフ サイエンシズ インコーポレイテッド | フッ化テトラヒドロナフチリジニルノナン酸誘導体およびその使用法 |
| EP3268369A4 (en) | 2015-03-10 | 2018-08-08 | 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 |
| 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 |
-
2014
- 2014-09-26 GB GBGB1417018.7A patent/GB201417018D0/en not_active Ceased
-
2015
- 2015-09-22 ES ES15767479T patent/ES2796235T3/es active Active
- 2015-09-22 RU RU2017114352A patent/RU2017114352A/ru unknown
- 2015-09-22 BR BR112017006240A patent/BR112017006240A2/pt not_active Application Discontinuation
- 2015-09-22 CN CN201580052202.3A patent/CN107074850A/zh active Pending
- 2015-09-22 EP EP15767479.7A patent/EP3197895B1/en active Active
- 2015-09-22 KR KR1020177007735A patent/KR20170054413A/ko not_active Withdrawn
- 2015-09-22 US US15/514,414 patent/US10004724B2/en not_active Expired - Fee Related
- 2015-09-22 AU AU2015320874A patent/AU2015320874A1/en not_active Abandoned
- 2015-09-22 CA CA2962319A patent/CA2962319A1/en active Pending
- 2015-09-22 JP JP2017516386A patent/JP6672276B2/ja not_active Expired - Fee Related
- 2015-09-22 WO PCT/EP2015/071798 patent/WO2016046241A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| ES2796235T3 (es) | 2020-11-26 |
| JP6672276B2 (ja) | 2020-03-25 |
| AU2015320874A1 (en) | 2017-03-09 |
| US10004724B2 (en) | 2018-06-26 |
| EP3197895B1 (en) | 2020-03-11 |
| EP3197895A1 (en) | 2017-08-02 |
| WO2016046241A1 (en) | 2016-03-31 |
| CA2962319A1 (en) | 2016-03-31 |
| BR112017006240A2 (pt) | 2017-12-12 |
| JP2017528506A (ja) | 2017-09-28 |
| US20170290818A1 (en) | 2017-10-12 |
| GB201417018D0 (en) | 2014-11-12 |
| KR20170054413A (ko) | 2017-05-17 |
| CN107074850A (zh) | 2017-08-18 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2017114352A (ru) | АНТАГОНИСТЫ ИНТЕГРИНА ανβ6 | |
| RU2017114346A (ru) | АНТАГОНИСТЫ ИНТЕГРИНА ανβ6 | |
| WO2014205229A8 (en) | Use of high dose pridopidine for treating huntington's disease | |
| RU2017114355A (ru) | Производные нафтиридина в качестве антагонистов альфа v бета 6 интегрина для лечения, в частности, фиброзных заболеваний | |
| CA2925624C (en) | Substituted nicotinimide inhibitors of btk and their preparation and use in the treatment of cancer, inflammation and autoimmune disease | |
| MX2021002321A (es) | Nuevos metodos. | |
| MX393855B (es) | Terapia de combinación que comprende un inhibidor de raf y trametinib | |
| JP2017528506A5 (enExample) | ||
| JP2017528507A5 (enExample) | ||
| MX2021002322A (es) | Nuevos metodos. | |
| RU2017105353A (ru) | Соединения | |
| JP2016106150A5 (enExample) | ||
| MD20140059A2 (en) | Substituted 4-phenyl-pyridines for the treatment of NK-1 receptor related diseases | |
| ME02841B (me) | Supstituirani piperidil-etil-pirimidin kao inhibitor grelin-o-acil-transferaze | |
| NZ600544A (en) | Compositions and methods for the treatment of angiogenesis-related eye diseases | |
| PH12020500543A1 (en) | Nonracemic mixtures and uses thereof | |
| RU2018136580A (ru) | Цитратная соль (s)-4-((s)-3-фтор-3-(2-(5,6,7,8-тетрагидро-1,8-нафтиридин-2-ил)этил)пирролидин-1-ил)-3-(3-(2-метоксиэтокси)фенил)бутановой кислоты | |
| JP2016510326A5 (enExample) | ||
| JP2015505564A5 (enExample) | ||
| WO2015116856A3 (en) | Farnesoid x receptor antagonists | |
| MA37455A1 (fr) | Utilisation d'un dérivé de pyrazole dans le traitement d'exacerbations aigues d'une maladie pulmonaire obstructive chronique | |
| WO2016168553A8 (en) | Deuterated obeticholic acid | |
| HRP20201187T1 (hr) | Derivat triazolopirazinona koristan kao inhibitor ljudskog pde1 | |
| RU2020120156A (ru) | Лечение приливов и потери костной ткани, вызванных андрогенной депривационной терапией с применением цис-кломифена | |
| CR20210043A (es) | Forma de dosificación farmacèutica administrable por vía oral con liberación modificada |