TW201619159A - 吡咯并[2,3-d]嘧啶衍生物 - Google Patents

吡咯并[2,3-d]嘧啶衍生物 Download PDF

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Publication number
TW201619159A
TW201619159A TW104125949A TW104125949A TW201619159A TW 201619159 A TW201619159 A TW 201619159A TW 104125949 A TW104125949 A TW 104125949A TW 104125949 A TW104125949 A TW 104125949A TW 201619159 A TW201619159 A TW 201619159A
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Taiwan
Prior art keywords
methyl
cis
pyrrolo
cyclobutyl
pyrimidin
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TW104125949A
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Chinese (zh)
Inventor
凱倫 考夫曼
詹姆士 杜爾
尼路 凱拉
米海爾 派瑞克
馬修 瑞斯
泰瑞克 薩瑪德
西蒙 夏波拉
傑明森 塔爾特
麥可 凡奎茲
派崔克 佛赫斯特
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輝瑞股份有限公司
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Publication of TW201619159A publication Critical patent/TW201619159A/zh

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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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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    • A61K31/53751,4-Oxazines, e.g. morpholine
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TW104125949A 2014-08-12 2015-08-10 吡咯并[2,3-d]嘧啶衍生物 TW201619159A (zh)

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US201462036276P 2014-08-12 2014-08-12
US201562189347P 2015-07-07 2015-07-07

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TW201619159A true TW201619159A (zh) 2016-06-01

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US (1) US10966980B2 (cg-RX-API-DMAC10.html)
EP (1) EP3180344B1 (cg-RX-API-DMAC10.html)
JP (1) JP6585158B2 (cg-RX-API-DMAC10.html)
CA (1) CA2899888A1 (cg-RX-API-DMAC10.html)
ES (1) ES2750655T3 (cg-RX-API-DMAC10.html)
TW (1) TW201619159A (cg-RX-API-DMAC10.html)
UY (1) UY36265A (cg-RX-API-DMAC10.html)
WO (1) WO2016024185A1 (cg-RX-API-DMAC10.html)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI771342B (zh) * 2016-11-23 2022-07-21 大陸商江蘇恆瑞醫藥股份有限公司 吡咯并六員雜芳環類衍生物的製備方法及中間體

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS56503B1 (sr) 2013-02-22 2018-02-28 Pfizer Derivati pirolo [2,3-d] pirimidina kao inhibitori janus kinaza (jak)
EP3180344B1 (en) 2014-08-12 2019-09-18 Pfizer Inc Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase
SG11201809751XA (en) 2016-05-26 2018-12-28 Zeno Royalties & Milestones Llc Egfr inhibitor compounds
CA3036384A1 (en) 2016-09-14 2018-03-22 Gilead Sciences, Inc. Syk inhibitors
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
WO2018195471A1 (en) 2017-04-21 2018-10-25 Gilead Sciences, Inc. Syk inhibitors in combination with hypomethylating agents
US12274703B2 (en) * 2017-12-21 2025-04-15 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising a dementia
US12310967B2 (en) 2017-12-21 2025-05-27 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising motor neuron diseases
US11365188B2 (en) 2018-03-21 2022-06-21 Xibin Liao JAK inhibitors
HRP20251339T1 (hr) 2018-07-06 2025-12-19 Pfizer Inc. Postupak proizvodnje i međuprodukti pirolo[2,3-d]pirimidinskog spoja i njegova upotreba
US10744136B2 (en) 2018-11-05 2020-08-18 Avista Pharma Solutions, Inc. Sulfonamide derivatives as JAK inhibitors
WO2020132378A2 (en) 2018-12-22 2020-06-25 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising depression
US11198699B2 (en) 2019-04-02 2021-12-14 Aligos Therapeutics, Inc. Compounds targeting PRMT5
EP3969458A4 (en) 2019-05-13 2023-05-17 Borah, 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
IL298450A (en) * 2020-05-28 2023-01-01 Pfizer Pyrrolo[2,3-d]pyrimidine derivatives
AU2021341899A1 (en) * 2020-09-11 2023-05-25 Galderma Holding SA Novel jak inhibitor compounds, method for synthesizing same and use thereof
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
CA3206106A1 (en) 2021-02-10 2022-08-18 Bhaskar Chaudhuri Methods for ophthalmic delivery of roflumilast
AU2022353032A1 (en) 2021-09-22 2024-03-28 Iolyx Therapeutics, Inc. Methods of treating ocular inflammatory diseases
CN119013261A (zh) 2022-02-14 2024-11-22 雅瑞斯医疗公司 Parg的抑制剂
WO2024173234A1 (en) * 2023-02-13 2024-08-22 Arase Therapeutics Inc. Inhibitors of parg

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
DK0674641T3 (da) 1992-12-17 1999-09-27 Pfizer Pyrrolopyrimidiner som CRF-antagonister
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
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
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
AU3951899A (en) 1998-06-19 2000-01-05 Pfizer Products Inc. Pyrrolo(2,3-d)pyrimidine compounds
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
AU4808300A (en) 1999-04-30 2000-11-17 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
ATE380031T1 (de) 1999-12-10 2007-12-15 Pfizer Prod Inc Pyrrolo 2,3-d pyrimidinderivate enthaltende zusammensetzungen
WO2001049688A1 (en) 2000-01-07 2001-07-12 Universitaire Instelling Antwerpen Purine derivatives, process for their preparation and use thereof
CA2412560C (en) 2000-06-26 2008-12-30 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine compounds as immunosuppressive agents
US6680324B2 (en) 2000-12-01 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
US6673802B2 (en) 2000-12-01 2004-01-06 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor 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
WO2004032834A2 (en) 2002-10-04 2004-04-22 Merck & Co., Inc. Thrombin inhibitors
PL377791A1 (pl) 2002-11-21 2006-02-20 Pfizer Products Inc. Pochodne 3-aminopiperydyny i sposoby ich wytwarzania
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.
EP1913000B1 (en) 2005-07-29 2012-01-11 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
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
US20080200458A1 (en) 2007-01-18 2008-08-21 Joseph Barbosa Methods and compositions for the treatment of body composition disorders
US20080194557A1 (en) 2007-01-18 2008-08-14 Joseph Barbosa Methods and compositions for the treatment of pain, inflammation and cancer
EP2217239A2 (en) 2007-11-07 2010-08-18 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
EP2209771A1 (en) 2007-11-08 2010-07-28 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
BRPI0918935A2 (pt) 2008-09-18 2015-12-01 Pfizer Ltd compostos amida úteis em terapia
FR2948066B1 (fr) 2009-07-17 2012-01-20 Skf Ab Dispositif de butee de suspension et jambe de force.
KR20120083452A (ko) 2009-10-15 2012-07-25 화이자 인코포레이티드 피롤로[2,3-d]피리미딘 화합물
DK2506716T3 (en) 2009-12-01 2017-09-04 Abbvie Inc HIS UNKNOWN TRICYCLIC RELATIONS
JP5739446B2 (ja) * 2009-12-18 2015-06-24 ファイザー・インク ピロロ[2,3−d]ピリミジン化合物
EP2523957A1 (en) 2010-01-12 2012-11-21 F. Hoffmann-La Roche AG Tricyclic heterocyclic compounds, compositions and methods of use thereof
AU2011219452B2 (en) 2010-02-24 2014-05-29 Zoetis Llc Veterinary compositions
US9050334B2 (en) 2010-07-16 2015-06-09 Innov88 Llc MIF inhibitors and their uses
CN103097340B (zh) 2010-07-16 2018-03-16 安吉奥斯医药品有限公司 治疗活性组合物及其使用方法
BR112013013659B8 (pt) 2010-12-03 2024-02-27 Epizyme Inc Compostos moduladores de enzimas epigenéticas, composição farmacêutica compreendendo ditos compostos e usos da dita composição farmacêutica para tratar câncer, câncer hematológico ou leucemia
US8987307B2 (en) 2011-03-03 2015-03-24 Hoffmann-La Roche Inc. 3-amino-pyridines as GPBAR1 agonists
WO2012169649A1 (en) 2011-06-07 2012-12-13 Dainippon Sumitomo 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
WO2014011911A2 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
SMT201900044T1 (it) 2012-07-20 2019-02-28 Zoetis Services Llc Regime posologico per gli inibitori delle janus chinasi (jak)
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
RS56503B1 (sr) 2013-02-22 2018-02-28 Pfizer Derivati pirolo [2,3-d] pirimidina kao inhibitori janus kinaza (jak)
EP3180344B1 (en) 2014-08-12 2019-09-18 Pfizer Inc Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI771342B (zh) * 2016-11-23 2022-07-21 大陸商江蘇恆瑞醫藥股份有限公司 吡咯并六員雜芳環類衍生物的製備方法及中間體

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