AU2015320863B2 - Naphthyridine derivatives as alpha v beta 6 integrin antagonists for the treatment of e.g. fibrotic diseases - Google Patents

Naphthyridine derivatives as alpha v beta 6 integrin antagonists for the treatment of e.g. fibrotic diseases Download PDF

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Publication number
AU2015320863B2
AU2015320863B2 AU2015320863A AU2015320863A AU2015320863B2 AU 2015320863 B2 AU2015320863 B2 AU 2015320863B2 AU 2015320863 A AU2015320863 A AU 2015320863A AU 2015320863 A AU2015320863 A AU 2015320863A AU 2015320863 B2 AU2015320863 B2 AU 2015320863B2
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Australia
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methyl
mmol
pyrazol
compound
pharmaceutically acceptable
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Ceased
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AU2015320863A
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AU2015320863A1 (en
Inventor
Niall Andrew ANDERSON
Ian Baxter Campbell
Matthew Howard James CAMPBELL-CRAWFORD
Ashley Paul Hancock
Seble LEMMA
Simon John Fawcett Macdonald
John Martin Pritchard
Panayiotis Alexandrou Procopiou
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GlaxoSmithKline Intellectual Property Development Ltd
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GlaxoSmithKline Intellectual Property Development Ltd
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    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2015320863A 2014-09-26 2015-09-22 Naphthyridine derivatives as alpha v beta 6 integrin antagonists for the treatment of e.g. fibrotic diseases Ceased AU2015320863B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1417094.8 2014-09-26
GBGB1417094.8A GB201417094D0 (en) 2014-09-26 2014-09-26 Novel compounds
PCT/EP2015/071782 WO2016046230A1 (en) 2014-09-26 2015-09-22 Naphthyridine derivatives as alpha v beta 6 integrin antagonists for the treatment of e.g. fibrotic diseases

Publications (2)

Publication Number Publication Date
AU2015320863A1 AU2015320863A1 (en) 2017-03-09
AU2015320863B2 true AU2015320863B2 (en) 2018-09-06

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AU2015320863A Ceased AU2015320863B2 (en) 2014-09-26 2015-09-22 Naphthyridine derivatives as alpha v beta 6 integrin antagonists for the treatment of e.g. fibrotic diseases

Country Status (12)

Country Link
US (2) US10144733B2 (OSRAM)
EP (1) EP3197894B1 (OSRAM)
JP (1) JP6657196B2 (OSRAM)
KR (1) KR20170053638A (OSRAM)
CN (1) CN107074851B (OSRAM)
AU (1) AU2015320863B2 (OSRAM)
BR (1) BR112017006242A2 (OSRAM)
CA (1) CA2962321A1 (OSRAM)
ES (1) ES2811119T3 (OSRAM)
GB (1) GB201417094D0 (OSRAM)
RU (1) RU2692775C2 (OSRAM)
WO (1) WO2016046230A1 (OSRAM)

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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
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
US20190144547A1 (en) * 2015-11-23 2019-05-16 Merck Patent Gmbh Anti-alpha-v integrin antibody for the treatment of fibrosis and/or fibrotic disorders
WO2017157735A1 (de) 2016-03-15 2017-09-21 Bayer Cropscience Aktiengesellschaft Substituierte sulfonylamide zur bekämpfung tierischer schädlinge
GB201604680D0 (en) 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds
ES2886650T3 (es) 2016-11-08 2021-12-20 Bristol Myers Squibb Co Derivados de indazol como antagonistas de integrina alfaV
WO2018089360A1 (en) * 2016-11-08 2018-05-17 Bristol-Myers Squibb Company Pyrrole amides as alpha v integrin inhibitors
EP3538525B1 (en) 2016-11-08 2022-06-22 Bristol-Myers Squibb Company 3-substituted propionic acids as alpha v integrin inhibitors
EP3538527B1 (en) 2016-11-08 2021-10-13 Bristol-Myers Squibb Company Azole amides and amines as alpha v integrin inhibitors
TW201819378A (zh) * 2016-11-08 2018-06-01 美商必治妥美雅史谷比公司 作為αｖ整合素抑制劑之含環丁烷及氮雜環丁烷之單及螺環化合物
WO2018119087A1 (en) 2016-12-23 2018-06-28 Pliant Therapeutics, Inc. Amino acid compounds and methods of use
MA52117A (fr) 2017-02-28 2022-04-06 Morphic Therapeutic Inc Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
TW201835078A (zh) 2017-02-28 2018-10-01 美商萊築理公司 αvβ6整合蛋白之抑制劑
SG11202004077WA (en) 2017-11-07 2020-05-28 Bristol Myers Squibb Co Pyrrolopyrazine derivatives as alpha v integrin inhibitors
MX2021002181A (es) 2018-08-29 2021-07-15 Morphic Therapeutic Inc Inhibicion de la integrina alfa v beta 6.
TWI835840B (zh) * 2018-08-29 2024-03-21 美商莫菲克醫療股份有限公司 αvβ6整合素之抑制劑
GB202010626D0 (en) 2020-07-10 2020-08-26 Univ Nottingham Compound
CA3244889A1 (en) 2022-03-08 2023-09-14 Equashield Medical Ltd FLUID TRANSFER STATION IN A ROBOTIC PHARMACEUTICAL PREPARATION SYSTEM
AU2023399039A1 (en) 2022-12-14 2025-05-22 Alnylam Pharmaceuticals, Inc. ALPHA-V BETA-6(ανβ6) INTEGRIN LIGANDS FOR EXTRAHEPATIC DELIVERY
WO2025259743A1 (en) 2024-06-12 2025-12-18 Alnylam Pharmaceuticals, Inc. Dual conjugate compounds 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

Citations (3)

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WO2001024797A1 (en) * 1999-10-04 2001-04-12 Merck & Co., Inc. Integrin receptor antagonists
WO2005082889A1 (en) * 2004-02-18 2005-09-09 Janssen Pharmaceutica N.V. Piperidinyl targeting compounds that selectively bind integrins
WO2014154725A1 (en) * 2013-03-28 2014-10-02 Glaxosmithkline Intellectual Property Development Limited Naphthyridine derivatives useful as alpha-v-beta-6 integrin antagonists

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EA002822B1 (ru) 1997-12-17 2002-10-31 Мерк Энд Ко., Инк. Антагонисты рецептора интегрина
WO1999030709A1 (en) 1997-12-17 1999-06-24 Merck & Co., Inc. Integrin receptor antagonists
IL146378A0 (en) 1999-06-02 2002-07-25 Merck & Co Inc Alpha v integrin receptor antagonists
WO2000078317A1 (en) 1999-06-23 2000-12-28 Merck & Co., Inc. Integrin receptor antagonists
PL355011A1 (en) 1999-11-08 2004-03-22 Merck & Co, Inc. Process and intermediates for the preparation of imidazolidinone alpha v integrin antagonists
US6933304B2 (en) * 2000-06-15 2005-08-23 Pharmacia Corporation Heteroarylalkanoic acids as integrin receptor antagonists
ATE353219T1 (de) 2000-07-26 2007-02-15 Merck & Co Inc Alpha v integrin-rezeptor-antagonisten
AU2001290772A1 (en) 2000-09-14 2002-03-26 Merck And Co., Inc. Alpha v integrin receptor antagonists
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MY130622A (en) * 2001-11-05 2007-07-31 Novartis Ag Naphthyridine derivatives, their preparation and their use as phosphodiesterase isoenzyme 4 (pde4) inhibitors
CA2507699A1 (en) 2002-12-20 2004-07-15 Pharmacia Corporation Heteroarylalkanoic acids as integrin receptor antagonists
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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
WO2015048819A1 (en) 2013-09-30 2015-04-02 The Regents Of The University Of California Anti-alphavbeta1 integrin compounds and methods
GB201417094D0 (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
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
CN114805342A (zh) 2015-02-19 2022-07-29 赛弗卢尔生命科学公司 氟化四氢萘啶基壬酸衍生物及其用途
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001024797A1 (en) * 1999-10-04 2001-04-12 Merck & Co., Inc. Integrin receptor antagonists
WO2005082889A1 (en) * 2004-02-18 2005-09-09 Janssen Pharmaceutica N.V. Piperidinyl targeting compounds that selectively bind integrins
WO2014154725A1 (en) * 2013-03-28 2014-10-02 Glaxosmithkline Intellectual Property Development Limited Naphthyridine derivatives useful as alpha-v-beta-6 integrin antagonists

Also Published As

Publication number Publication date
EP3197894A1 (en) 2017-08-02
JP2017528504A (ja) 2017-09-28
GB201417094D0 (en) 2014-11-12
US10144733B2 (en) 2018-12-04
US10513517B2 (en) 2019-12-24
US20190048005A1 (en) 2019-02-14
EP3197894B1 (en) 2020-06-03
RU2692775C2 (ru) 2019-06-27
ES2811119T3 (es) 2021-03-10
RU2017114355A3 (OSRAM) 2019-01-14
RU2017114355A (ru) 2018-10-29
CN107074851A (zh) 2017-08-18
KR20170053638A (ko) 2017-05-16
CN107074851B (zh) 2020-01-10
US20170291899A1 (en) 2017-10-12
WO2016046230A1 (en) 2016-03-31
JP6657196B2 (ja) 2020-03-04
BR112017006242A2 (pt) 2017-12-12
CA2962321A1 (en) 2016-03-31
AU2015320863A1 (en) 2017-03-09

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