KR102700471B1 - 알파 v 인테그린 억제제로서의 피롤로피라진 유도체 - Google Patents

알파 v 인테그린 억제제로서의 피롤로피라진 유도체 Download PDF

Info

Publication number
KR102700471B1
KR102700471B1 KR1020207015957A KR20207015957A KR102700471B1 KR 102700471 B1 KR102700471 B1 KR 102700471B1 KR 1020207015957 A KR1020207015957 A KR 1020207015957A KR 20207015957 A KR20207015957 A KR 20207015957A KR 102700471 B1 KR102700471 B1 KR 102700471B1
Authority
KR
South Korea
Prior art keywords
hydrogen
amino
mmol
compound
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.)
Active
Application number
KR1020207015957A
Other languages
English (en)
Korean (ko)
Other versions
KR20200084879A (ko
Inventor
궈후아 자오
제임스 미그논
Original Assignee
브리스톨-마이어스 스큅 컴퍼니
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by 브리스톨-마이어스 스큅 컴퍼니 filed Critical 브리스톨-마이어스 스큅 컴퍼니
Publication of KR20200084879A publication Critical patent/KR20200084879A/ko
Application granted granted Critical
Publication of KR102700471B1 publication Critical patent/KR102700471B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/495—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
    • 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
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020207015957A 2017-11-07 2018-11-05 알파 v 인테그린 억제제로서의 피롤로피라진 유도체 Active KR102700471B1 (ko)

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 (2)

Publication Number Publication Date
KR20200084879A KR20200084879A (ko) 2020-07-13
KR102700471B1 true KR102700471B1 (ko) 2024-08-28

Family

ID=64362756

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020207015957A Active KR102700471B1 (ko) 2017-11-07 2018-11-05 알파 v 인테그린 억제제로서의 피롤로피라진 유도체

Country Status (14)

Country Link
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=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2904645T3 (es) * 2017-11-07 2022-04-05 Bristol Myers Squibb Co Derivados de pirrolopirazina como inhibidores de integrina alfa v
KR102659859B1 (ko) 2018-10-30 2024-04-25 길리애드 사이언시즈, 인코포레이티드 알파4β7 인테그린의 억제를 위한 화합물
AU2019373242B2 (en) 2018-10-30 2023-07-13 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin
EP4541422A3 (en) 2018-10-30 2025-06-25 Gilead Sciences, Inc. Quinoline derivatives as alpha4beta7 integrin inhibitors
CN112969700B (zh) 2018-10-30 2024-08-20 吉利德科学公司 作为α4β7整合素抑制剂的咪唑并吡啶衍生物
KR102908219B1 (ko) 2019-08-14 2026-01-08 길리애드 사이언시즈, 인코포레이티드 알파 4 베타 7 인테그린의 저해용 화합물
KR20220119424A (ko) * 2019-12-20 2022-08-29 노파르티스 아게 인테그린 억제제를 사용한 간 질환의 조합 치료

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002508323A (ja) 1997-12-17 2002-03-19 メルク エンド カムパニー インコーポレーテッド インテグリン受容体拮抗薬

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP1049693A1 (en) 1997-11-26 2000-11-08 Du Pont Pharmaceuticals Company 1,3,4-THIADIAZOLES AND 1,3,4-OXADIAZOLES AS $g(a) v?$g(b) 3? ANTAGONISTS
WO2000009503A1 (en) 1998-08-13 2000-02-24 Merck & Co., Inc. Integrin receptor antagonists
US20020072518A1 (en) * 2000-08-29 2002-06-13 Khanna Ish Kumar Bicyclic alphavbeta3 antagonists
NZ539682A (en) * 2001-01-29 2006-03-31 Dimensional Pharm Inc Substituted indoles and their use as integrin antagonists
BR0317600A (pt) * 2002-12-20 2005-11-29 Pharmacia Corp ácidos heteroarilalcanóicos como derivados de antagonistas de receptor de integrina
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
EP2049490A1 (en) 2006-06-09 2009-04-22 Astra Zeneca AB N-(benzoyl)-o- [2- (pyridin- 2 -ylamino) ethyl]-l-tyrosine derivatives and related compounds as a5b1 antagonists for the treatment of solid tumors
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.
NZ603789A (en) 2010-05-26 2015-03-27 Sunovion Pharmaceuticals Inc Heteroaryl compounds and methods of use thereof
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
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
GB201417018D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
KR102647026B1 (ko) 2015-02-19 2024-03-12 사이플루어 라이프 사이언시즈, 인크 플루오르화 테트라히드로나프티리디닐 노난산 유도체 및 이의 용도
CA2981371A1 (en) 2015-03-10 2016-09-15 The Regents Of The University Of California Anti-alphavbeta1 integrin inhibitors and methods of use
ES2904645T3 (es) * 2017-11-07 2022-04-05 Bristol Myers Squibb Co Derivados de pirrolopirazina como inhibidores de integrina alfa v

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002508323A (ja) 1997-12-17 2002-03-19 メルク エンド カムパニー インコーポレーテッド インテグリン受容体拮抗薬

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Bioorganic & Medicinal Chemistry Letters, 1995, Vol. 5, pp.475-480.

Also Published As

Publication number Publication date
AU2018365793A1 (en) 2020-06-18
CN111433207B (zh) 2023-07-25
BR112020008893A2 (pt) 2020-10-13
IL274425A (en) 2020-06-30
JP7291696B2 (ja) 2023-06-15
EA202091136A1 (ru) 2020-07-29
US11292802B2 (en) 2022-04-05
ES2904645T3 (es) 2022-04-05
US20210163501A1 (en) 2021-06-03
EP3707142A1 (en) 2020-09-16
MX2020004455A (es) 2020-07-24
CN111433207A (zh) 2020-07-17
WO2019094319A1 (en) 2019-05-16
KR20200084879A (ko) 2020-07-13
SG11202004077WA (en) 2020-05-28
CA3081805A1 (en) 2019-05-16
JP2021502358A (ja) 2021-01-28
EP3707142B1 (en) 2021-12-08

Similar Documents

Publication Publication Date Title
KR102700471B1 (ko) 알파 v 인테그린 억제제로서의 피롤로피라진 유도체
US11639353B2 (en) Cyclobutanes- and azetidine-containing mono and spirocyclic compounds as αV integrin inhibitors
KR102785137B1 (ko) Rip1 억제 화합물 및 그를 제조 및 사용하는 방법
KR102506327B1 (ko) αV 인테그린 길항제로서의 인다졸 유도체
US10717736B2 (en) Pyrrole amides as alpha V integrin inhibitors
KR102505629B1 (ko) 알파 v 인테그린 억제제로서의 3-치환된 프로피온산
KR102913125B1 (ko) Lpa 수용체 길항제 및 이의 용도
JP2020505327A5 (https=)
US11980609B2 (en) LPA receptor antagonists and uses thereof
CN106852142A (zh) 作为醛固酮合酶抑制剂的螺二胺衍生物
JP2019537603A (ja) アルファｖインテグリン阻害剤としてのアゾールアミドおよびアミン
JP7365332B2 (ja) Ｃｄｋ８／１９阻害薬としての新規ヘテロ環式化合物
TW202122382A (zh) 乙內醯脲衍生物
WO2026048766A1 (ja) 多環性化合物

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20200603

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20211105

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20240122

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20240527

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20240826

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20240826

End annual number: 3

Start annual number: 1

PG1601 Publication of registration