AU2018365793A1 - Pyrrolopyrazine derivatives as alpha V integrin inhibitors - Google Patents

Pyrrolopyrazine derivatives as alpha V integrin inhibitors Download PDF

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Publication number
AU2018365793A1
AU2018365793A1 AU2018365793A AU2018365793A AU2018365793A1 AU 2018365793 A1 AU2018365793 A1 AU 2018365793A1 AU 2018365793 A AU2018365793 A AU 2018365793A AU 2018365793 A AU2018365793 A AU 2018365793A AU 2018365793 A1 AU2018365793 A1 AU 2018365793A1
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AU
Australia
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
Application number
AU2018365793A
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English (en)
Inventor
James Mignone
Guohua Zhao
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AU2018365793A1 publication Critical patent/AU2018365793A1/en
Abandoned legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

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  • 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)
AU2018365793A 2017-11-07 2018-11-05 Pyrrolopyrazine derivatives as alpha V integrin inhibitors Abandoned AU2018365793A1 (en)

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
AU2018365793A1 true AU2018365793A1 (en) 2020-06-18

Family

ID=64362756

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2018365793A Abandoned AU2018365793A1 (en) 2017-11-07 2018-11-05 Pyrrolopyrazine derivatives as alpha V integrin inhibitors

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

Family Cites Families (25)

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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
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
WO1999030709A1 (en) 1997-12-17 1999-06-24 Merck & Co., Inc. Integrin receptor 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

Also Published As

Publication number Publication date
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
KR102700471B1 (ko) 2024-08-28
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

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Legal Events

Date Code Title Description
MK1 Application lapsed section 142(2)(a) - no request for examination in relevant period