JP6585158B2 - ヤヌスキナーゼの阻害に有用なピロロ[2,3−d]ピリミジン誘導体 - Google Patents

ヤヌスキナーゼの阻害に有用なピロロ[2,3−d]ピリミジン誘導体 Download PDF

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JP6585158B2
JP6585158B2 JP2017507009A JP2017507009A JP6585158B2 JP 6585158 B2 JP6585158 B2 JP 6585158B2 JP 2017507009 A JP2017507009 A JP 2017507009A JP 2017507009 A JP2017507009 A JP 2017507009A JP 6585158 B2 JP6585158 B2 JP 6585158B2
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methyl
pyrrolo
cyclobutyl
cis
pyrimidin
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JP2017524007A (ja
JP2017524007A5 (pt-PT
Inventor
ジェイ.コフマン カレン
ジェイ.コフマン カレン
エム.デュール ジェームズ
エム.デュール ジェームズ
カイラ ニール
カイラ ニール
ディ. パリーク ミヒール
ディ. パリーク ミヒール
アール.リース マシュー
アール.リース マシュー
サマド タレク
サマド タレク
スャボラ シモーネ
スャボラ シモーネ
ビー.タトル ジャミソン
ビー.タトル ジャミソン
エル. ヴァズケズ マイケル
エル. ヴァズケズ マイケル
ロバート ヴァーホスト パトリック
ロバート ヴァーホスト パトリック
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ファイザー・インク
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    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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JP2017507009A 2014-08-12 2015-07-31 ヤヌスキナーゼの阻害に有用なピロロ[2,3−d]ピリミジン誘導体 Expired - Fee Related JP6585158B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462036276P 2014-08-12 2014-08-12
US62/036,276 2014-08-12
US201562189347P 2015-07-07 2015-07-07
US62/189,347 2015-07-07
PCT/IB2015/055823 WO2016024185A1 (en) 2014-08-12 2015-07-31 Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase

Publications (3)

Publication Number Publication Date
JP2017524007A JP2017524007A (ja) 2017-08-24
JP2017524007A5 JP2017524007A5 (pt-PT) 2018-07-19
JP6585158B2 true JP6585158B2 (ja) 2019-10-02

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US (1) US10966980B2 (pt-PT)
EP (1) EP3180344B1 (pt-PT)
JP (1) JP6585158B2 (pt-PT)
CA (1) CA2899888A1 (pt-PT)
ES (1) ES2750655T3 (pt-PT)
TW (1) TW201619159A (pt-PT)
UY (1) UY36265A (pt-PT)
WO (1) WO2016024185A1 (pt-PT)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA38347A1 (fr) 2013-02-22 2017-10-31 Pfizer Dérivés de pyrrolo[2,3-d]pyrimidine en tant qu'inhibiteurs de janus kinases (jak)
WO2016024185A1 (en) 2014-08-12 2016-02-18 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase
MX2018013413A (es) * 2016-05-26 2019-06-06 Zeno Royalties & Milestones Llc Compuestos inhibidores de egfr.
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
WO2018053190A1 (en) 2016-09-14 2018-03-22 Gilead Sciences, Inc. Syk inhibitors
EP3543241B8 (en) * 2016-11-23 2022-10-12 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Preparation method for and intermediate of pyrrolo six-membered heteroaromatic ring derivative
WO2018195471A1 (en) 2017-04-21 2018-10-25 Gilead Sciences, Inc. Syk inhibitors in combination with hypomethylating agents
US20220040197A1 (en) * 2017-12-21 2022-02-10 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising a dementia
WO2019182924A1 (en) * 2018-03-21 2019-09-26 Xibin Liao Jak inhibitors
AU2019299666B2 (en) * 2018-07-06 2024-07-11 Pfizer Inc. Manufacturing process and intermediates for a pyrrolo(2,3- d)pyrimidine compound and use thereof
KR20210072125A (ko) * 2018-11-05 2021-06-16 아비스타 파마 솔루션즈, 아이엔씨. 화합물
AU2020256166A1 (en) 2019-04-02 2021-10-14 Aligos Therapeutics, Inc. Compounds targeting PRMT5
WO2020232470A1 (en) 2019-05-13 2020-11-19 Boragen, Inc. Chemical compounds
CN110483338A (zh) * 2019-08-14 2019-11-22 苏州汉德创宏生化科技有限公司 一种大环类抑制剂中间体环庚烷基磺酰氯的合成方法
US20230219963A1 (en) * 2020-05-28 2023-07-13 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives
CN112697912B (zh) * 2020-12-14 2021-09-21 上海博悦生物科技有限公司 一种检测枸橼酸托法替布中间体及其相关杂质的方法

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3037980A (en) 1955-08-18 1962-06-05 Burroughs Wellcome Co Pyrrolopyrimidine vasodilators and method of making them
RU2124015C1 (ru) 1992-12-17 1998-12-27 Пфайзер Инк. Производные пирроло [2,3-d] пиримидинов, фармацевтическая композиция, пирроло [2,3-d] пиримидины, производные пиррола
JPH06329675A (ja) 1993-05-20 1994-11-29 Teijin Ltd 4―置換アルキルアミノ―ピロロ[2,3―d]ピリミジン誘導体
JPH06329674A (ja) 1993-05-20 1994-11-29 Teijin Ltd 4―置換シクロヘキシルアミノ―ピロロ[2,3―d]ピリミジン
JPH08134068A (ja) 1994-11-02 1996-05-28 Teijin Ltd 4―置換アルキルアミノ―ピロロ[2,3―d]ピリミジン誘導体
US6051578A (en) 1996-02-12 2000-04-18 Pfizer Inc. Pyrazolopyrimidines for treatment of CNS disorders
US6686366B1 (en) 1998-06-02 2004-02-03 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
ID26698A (id) 1998-06-19 2001-02-01 Pfizer Prod Inc SENYAWA-SENYAWA PIROLO [2,3-d] PIRIMIDINA
CZ27399A3 (cs) 1999-01-26 2000-08-16 Ústav Experimentální Botaniky Av Čr Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv
EP1040831A3 (en) 1999-04-02 2003-05-02 Pfizer Products Inc. Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death
WO2000066585A1 (en) 1999-04-30 2000-11-09 Neurogen Corporation 9H-PYRIMIDO[4,5-b]INDOLE DERIVATIVES: CRF1 SPECIFIC LIGANDS
US6664252B2 (en) 1999-12-02 2003-12-16 Osi Pharmaceuticals, Inc. 4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof
SK287188B6 (sk) 1999-12-10 2010-02-08 Pfizer Products Inc. Pyrolo [2,3-d]pyrimidínová zlúčenina, jej použitie a farmaceutická kompozícia alebo kombinácia s jej obsahom
DE60118521T2 (de) 2000-01-07 2006-10-12 Universitaire Instelling Antwerpen Purin derivate, ihre herstellung und verwendung
SI1294724T1 (sl) 2000-06-26 2006-08-31 Pfizer Prod Inc Pirolo(2,3-d)primidinske spojine kot imunosupresivna sredstva
US6673802B2 (en) 2000-12-01 2004-01-06 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
US6680324B2 (en) 2000-12-01 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
WO2003048120A2 (en) 2001-11-30 2003-06-12 Osi Pharmaceuticals, Inc. 2-aryl pyrrologpyrimidines for a1 and a3 receptors
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
AU2003299901A1 (en) 2002-10-04 2004-05-04 Merck And Co., Inc. Thrombin inhibitors
AU2003278529A1 (en) 2002-11-21 2004-06-15 Pfizer Products Inc. 3-amino-piperidine derivatives and processes for their preparation
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
SI1913000T1 (sl) 2005-07-29 2012-02-29 Pfizer Prod Inc Derivati pirolo(2,3-d)pirimidina; njihovi intermediati in sinteza
JP2007091649A (ja) 2005-09-29 2007-04-12 Taisho Pharmaceut Co Ltd ピリミジン誘導体及びその使用に関連する治療方法
EA200870385A1 (ru) 2006-03-29 2009-04-28 Фолдркс Фармасьютикалз, Инк. Ингибирование токсичности альфа-синуклеина
US8008307B2 (en) * 2006-08-08 2011-08-30 Millennium Pharmaceuticals, Inc. Heteroaryl compounds useful as inhibitors of E1 activating enzymes
WO2008089310A2 (en) 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of obesity
WO2008089307A2 (en) 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer
AU2008323694A1 (en) 2007-11-07 2009-05-14 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
WO2009060278A1 (en) 2007-11-08 2009-05-14 Pfizer Inc. Cyclobutyl carboxylic acid derivatives
US8946239B2 (en) 2008-07-10 2015-02-03 Duquesne University Of The Holy Spirit Substituted pyrrolo, -furano, and cyclopentylpyrimidines having antimitotic and/or antitumor activity and methods of use thereof
DK2384326T3 (da) 2008-08-20 2014-05-05 Zoetis Llc Pyrrolo[2,3-d]pyrimidinforbindelser
EP2350017A1 (en) 2008-09-18 2011-08-03 Pfizer Limited Amide compounds useful in therapy
FR2948066B1 (fr) 2009-07-17 2012-01-20 Skf Ab Dispositif de butee de suspension et jambe de force.
JP5629324B2 (ja) 2009-10-15 2014-11-19 ファイザー・インク ピロロ[2,3−d]ピリミジン化合物
CR20170159A (es) 2009-12-01 2017-06-26 Abbvie Inc Nuevos compuestos tricíclicos
ES2461967T3 (es) 2009-12-18 2014-05-21 Pfizer Inc. Compuestos de pirrolo[2,3-d]pirimidina
RU2012132278A (ru) 2010-01-12 2014-02-20 Ф. Хоффманн-Ля Рош Аг Трициклические гетероциклические соединения, содержащие их композиции и способы их применения
CN104224737A (zh) 2010-02-24 2014-12-24 硕腾有限责任公司 兽医组合物
MX342951B (es) 2010-07-16 2016-10-18 Agios Pharmaceuticals Inc * Composiciones terapeuticamente activas y su metodo de uso.
US9050334B2 (en) 2010-07-16 2015-06-09 Innov88 Llc MIF inhibitors and their uses
CN103391939B (zh) 2010-12-03 2016-03-09 Epizyme股份有限公司 作为表观遗传酶调节剂的经取代的嘌呤和7-氮杂嘌呤化合物
US8987307B2 (en) 2011-03-03 2015-03-24 Hoffmann-La Roche Inc. 3-amino-pyridines as GPBAR1 agonists
EP2718283A4 (en) 2011-06-07 2014-10-29 Sumitomo Dainippon Pharma Co Ltd INDAZOLE AND PYRROLOPYRIDINE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
JP2013010719A (ja) 2011-06-30 2013-01-17 Dainippon Sumitomo Pharma Co Ltd ベンズイミダゾロンおよびオキシインドール誘導体ならびにそれらの医薬用途
US20140018361A1 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
IN2015DN00370A (pt-PT) 2012-07-20 2015-06-12 Zoetis Llc
JP2014133739A (ja) 2012-12-12 2014-07-24 Dainippon Sumitomo Pharma Co Ltd インダゾール誘導体またはピロロピリジン誘導体からなる医薬
MA38347A1 (fr) * 2013-02-22 2017-10-31 Pfizer Dérivés de pyrrolo[2,3-d]pyrimidine en tant qu'inhibiteurs de janus kinases (jak)
WO2016024185A1 (en) 2014-08-12 2016-02-18 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase

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US10966980B2 (en) 2021-04-06
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