CA3081805A1 - Pyrrolopyrazine derivatives as alpha v integrin inhibitors - Google Patents
Pyrrolopyrazine derivatives as alpha v integrin inhibitors Download PDFInfo
- Publication number
- CA3081805A1 CA3081805A1 CA3081805A CA3081805A CA3081805A1 CA 3081805 A1 CA3081805 A1 CA 3081805A1 CA 3081805 A CA3081805 A CA 3081805A CA 3081805 A CA3081805 A CA 3081805A CA 3081805 A1 CA3081805 A1 CA 3081805A1
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- Prior art keywords
- hydrogen
- amino
- mmol
- lcms
- alkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
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- 108010044426 integrins Proteins 0.000 title abstract description 29
- 239000003112 inhibitor Substances 0.000 title description 18
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Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
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- Health & Medical Sciences (AREA)
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- General Chemical & Material Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762582693P | 2017-11-07 | 2017-11-07 | |
| US62/582,693 | 2017-11-07 | ||
| PCT/US2018/059157 WO2019094319A1 (en) | 2017-11-07 | 2018-11-05 | Pyrrolopyrazine derivatives as alpha v integrin inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3081805A1 true CA3081805A1 (en) | 2019-05-16 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3081805A Abandoned CA3081805A1 (en) | 2017-11-07 | 2018-11-05 | Pyrrolopyrazine derivatives as alpha v integrin inhibitors |
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| US (1) | US11292802B2 (https=) |
| EP (1) | EP3707142B1 (https=) |
| JP (1) | JP7291696B2 (https=) |
| KR (1) | KR102700471B1 (https=) |
| CN (1) | CN111433207B (https=) |
| AU (1) | AU2018365793A1 (https=) |
| BR (1) | BR112020008893A2 (https=) |
| CA (1) | CA3081805A1 (https=) |
| EA (1) | EA202091136A1 (https=) |
| ES (1) | ES2904645T3 (https=) |
| IL (1) | IL274425A (https=) |
| MX (1) | MX2020004455A (https=) |
| SG (1) | SG11202004077WA (https=) |
| WO (1) | WO2019094319A1 (https=) |
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| KR102700471B1 (ko) * | 2017-11-07 | 2024-08-28 | 브리스톨-마이어스 스큅 컴퍼니 | 알파 v 인테그린 억제제로서의 피롤로피라진 유도체 |
| FI3873884T3 (fi) | 2018-10-30 | 2025-02-24 | Gilead Sciences Inc | 3-(kinolin-8-yyli)-1,4-dihydropyrido[3,4-d]pyrimidiini-2,4-dionijohdannaisia alfa-4-beta-7-integriinin estäjinä tulehdussairauksien hoidossa |
| JP7189368B2 (ja) | 2018-10-30 | 2022-12-13 | ギリアード サイエンシーズ， インコーポレイテッド | アルファ４ベータ７インテグリンの阻害のための化合物 |
| ES3013256T3 (en) | 2018-10-30 | 2025-04-11 | Gilead Sciences Inc | Imidazo[1,2-a]pyridine derivatives as alpha4beta7 integrin inhibitors for the treatment of inflammatory diseases |
| EP3873605B1 (en) | 2018-10-30 | 2024-10-23 | Gilead Sciences, Inc. | Compounds for inhibition of alpha4beta7 integrin |
| WO2021030438A1 (en) | 2019-08-14 | 2021-02-18 | Gilead Sciences, Inc. | Compounds for inhibition of alpha 4 beta 7 integrin |
| US20230060422A1 (en) * | 2019-12-20 | 2023-03-02 | Novartis Ag | Combination treatment of liver diseases using integrin inhibitors |
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| 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 |
| CA2309204A1 (en) | 1997-11-26 | 1999-06-03 | Dupont Pharmaceuticals Company | 1,3,4-thiadiazoles and 1,3,4-oxadiazoles as .alpha.v.beta.3 antagonists |
| CA2315370A1 (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 |
| JP2004521079A (ja) | 2000-08-29 | 2004-07-15 | ファルマシア・コーポレーション | アルファーｖベータ３アンタゴニストとして有用な二環式環系を含有する化合物 |
| CA2436130A1 (en) * | 2001-01-29 | 2002-08-08 | Ortho-Mcneil Pharmaceutical, Inc. | Substituted indoles and their use as integrin antagonists |
| EP1592421A1 (en) | 2002-12-20 | 2005-11-09 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| US7365209B2 (en) | 2003-02-11 | 2008-04-29 | Pharmacopeia, Inc. | Nitrogen heterocycle biaryls for osteoporosis and other diseases |
| TW200526626A (en) | 2003-09-13 | 2005-08-16 | Astrazeneca Ab | Chemical compounds |
| WO2006108040A1 (en) | 2005-04-05 | 2006-10-12 | Janssen Pharmaceutica, N.V. | Substituted indoles and their use as integrin antagonists |
| 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 |
| JP2011184298A (ja) | 2008-06-02 | 2011-09-22 | Sanwa Kagaku Kenkyusho Co Ltd | 新規化合物及びその医薬用途 |
| 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. |
| US8969349B2 (en) | 2010-05-26 | 2015-03-03 | Sunovion Pharmaceuticals Inc. | Substituted quinoxalines and quinoxalinones as PDE-10 inhibitors |
| 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 |
| 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 |
| GB201417011D0 (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 |
| KR102700471B1 (ko) * | 2017-11-07 | 2024-08-28 | 브리스톨-마이어스 스큅 컴퍼니 | 알파 v 인테그린 억제제로서의 피롤로피라진 유도체 |
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2018
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- 2018-11-05 EA EA202091136A patent/EA202091136A1/ru unknown
- 2018-11-05 JP JP2020524801A patent/JP7291696B2/ja active Active
- 2018-11-05 WO PCT/US2018/059157 patent/WO2019094319A1/en not_active Ceased
- 2018-11-05 BR BR112020008893-5A patent/BR112020008893A2/pt not_active Application Discontinuation
- 2018-11-05 ES ES18804882T patent/ES2904645T3/es active Active
- 2018-11-05 SG SG11202004077WA patent/SG11202004077WA/en unknown
- 2018-11-05 CN CN201880071717.1A patent/CN111433207B/zh active Active
- 2018-11-05 MX MX2020004455A patent/MX2020004455A/es unknown
- 2018-11-05 EP EP18804882.1A patent/EP3707142B1/en active Active
- 2018-11-05 AU AU2018365793A patent/AU2018365793A1/en not_active Abandoned
- 2018-11-05 CA CA3081805A patent/CA3081805A1/en not_active Abandoned
- 2018-11-05 US US16/761,286 patent/US11292802B2/en active Active
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2020
- 2020-05-04 IL IL274425A patent/IL274425A/en unknown
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| SG11202004077WA (en) | 2020-05-28 |
| AU2018365793A1 (en) | 2020-06-18 |
| ES2904645T3 (es) | 2022-04-05 |
| WO2019094319A1 (en) | 2019-05-16 |
| CN111433207B (zh) | 2023-07-25 |
| EA202091136A1 (ru) | 2020-07-29 |
| BR112020008893A2 (pt) | 2020-10-13 |
| US20210163501A1 (en) | 2021-06-03 |
| JP7291696B2 (ja) | 2023-06-15 |
| EP3707142A1 (en) | 2020-09-16 |
| EP3707142B1 (en) | 2021-12-08 |
| MX2020004455A (es) | 2020-07-24 |
| CN111433207A (zh) | 2020-07-17 |
| IL274425A (en) | 2020-06-30 |
| KR102700471B1 (ko) | 2024-08-28 |
| US11292802B2 (en) | 2022-04-05 |
| JP2021502358A (ja) | 2021-01-28 |
| KR20200084879A (ko) | 2020-07-13 |
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| Date | Code | Title | Description |
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| FZDE | Discontinued |
Effective date: 20230505 |