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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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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  • Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Psychology (AREA)
TW104125949A 2014-08-12 2015-08-10 吡咯并［２，３－ｄ］嘧啶衍生物 TW201619159A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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 (enExample)
EP (1) EP3180344B1 (enExample)
JP (1) JP6585158B2 (enExample)
CA (1) CA2899888A1 (enExample)
ES (1) ES2750655T3 (enExample)
TW (1) TW201619159A (enExample)
UY (1) UY36265A (enExample)
WO (1) WO2016024185A1 (enExample)

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
JP6145179B2 (ja) 2013-02-22 2017-06-07 ファイザー・インク ヤヌス関連キナーゼ（ＪＡＫ）の阻害剤としてのピロロ［２，３−ｄ］ピリミジン誘導体
ES2750655T3 (es) 2014-08-12 2020-03-26 Pfizer Derivados de pirrolo[2,3-d]pirimidina útiles para inhibir la Janus cinasa
KR102444835B1 (ko) * 2016-05-26 2022-09-19 리커리엄 아이피 홀딩스, 엘엘씨 Egfr 억제제 화합물
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
US10111882B2 (en) 2016-09-14 2018-10-30 Gilead Sciences, Inc. SYK inhibitors
WO2018195471A1 (en) 2017-04-21 2018-10-25 Gilead Sciences, Inc. Syk inhibitors in combination with hypomethylating agents
US12310967B2 (en) 2017-12-21 2025-05-27 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising motor neuron diseases
US12274703B2 (en) * 2017-12-21 2025-04-15 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising a dementia
JP7462951B2 (ja) 2018-03-21 2024-04-08 リャオ，シビン Ｊａｋ阻害剤
TWI709562B (zh) * 2018-07-06 2020-11-11 美商輝瑞股份有限公司 吡咯并〔２，３-ｄ〕嘧啶化合物的製造方法與中間產物及其用途
KR20210072125A (ko) * 2018-11-05 2021-06-16 아비스타 파마 솔루션즈, 아이엔씨. 화합물
WO2020132378A2 (en) 2018-12-22 2020-06-25 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising depression
BR112021019465A8 (pt) 2019-04-02 2022-06-07 Aligos Therapeutics Inc Compostos que têm como alvo 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
CN115667263A (zh) * 2020-05-28 2023-01-31 辉瑞公司 吡咯并[2,3-d]嘧啶衍生物
CA3191598A1 (en) * 2020-09-11 2022-03-17 Gilles Ouvry 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
EP4405048A4 (en) 2021-09-22 2025-08-06 Iolyx Therapeutics Inc METHODS OF TREATMENT OF INFLAMMATORY EYE DISEASES
WO2023154913A1 (en) 2022-02-14 2023-08-17 Arase Therapeutics Inc. Inhibitors of parg
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
DE69323768T2 (de) 1992-12-17 1999-07-01 Pfizer Inc., New York, N.Y. Pyrrolopyrimidine als crf antagonisten
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
DK1087970T3 (da) 1998-06-19 2004-08-02 Pfizer Prod Inc Pyrrol[2,3-d]pyrimidin forbindelser
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [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
US6284766B1 (en) 1999-04-30 2001-09-04 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
AU777911B2 (en) 1999-12-10 2004-11-04 Pfizer Products Inc. Pyrrolo(2,3-d)pyrimidine compounds
CZ20022353A3 (cs) 2000-01-07 2003-02-12 Universitaire Instelling Antwerpen Deriváty purinu, způsob jejich přípravy a jejich použití
AP1911A (en) 2000-06-26 2008-10-30 Pfizer Prod Inc Pyrrolo[2,3-d]pyrimidine compounds.
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
EP2050751A1 (en) 2001-11-30 2009-04-22 OSI Pharmaceuticals, Inc. Compounds specific to adenosine A1 and A3 receptors and uses thereof
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
RS20050380A (sr) 2002-11-21 2007-11-15 Pfizer Products Inc., Derivati 3-aminopiperidina i postupci njihove proizvodnje
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.
DK1913000T3 (da) 2005-07-29 2012-03-12 Pfizer Prod Inc Pyrrolo[2,3-D]pyrimidinderivater; deres mellemprodukter og syntese
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
CA2647543A1 (en) 2006-03-29 2007-11-08 Foldrx Pharmaceuticals, Inc. Inhibition of alpha-synuclein toxicity
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
WO2008089307A2 (en) 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer
WO2009062118A2 (en) 2007-11-07 2009-05-14 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
JP2011503046A (ja) 2007-11-08 2011-01-27 ファイザー・インク シクロブチルカルボン酸誘導体
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
RS53382B (sr) 2008-08-20 2014-10-31 Zoetis Llc Jedinjenja pirol [2,3-d]pirimidina
AU2009294290B2 (en) 2008-09-18 2012-08-30 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.
EP2488524B1 (en) 2009-10-15 2013-07-03 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine compounds
HRP20171175T1 (hr) 2009-12-01 2017-10-06 Abbvie Inc. Novi triciklički spojevi
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
MX2012008049A (es) 2010-01-12 2012-08-01 Hoffmann La Roche Compuestos heterociclicos triciclicos, composiciones y metodos de uso de los mismos,.
KR101484382B1 (ko) 2010-02-24 2015-01-19 조에티스 엘엘씨 수의학적 조성물
WO2012009678A1 (en) 2010-07-16 2012-01-19 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their method of use
US9050334B2 (en) 2010-07-16 2015-06-09 Innov88 Llc MIF inhibitors and their uses
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
JP2014510708A (ja) 2011-06-07 2014-05-01 大日本住友製薬株式会社 インダゾール誘導体およびピロロピリジン誘導体ならびにその医薬用途
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
NZ703152A (en) 2012-07-20 2016-03-31 Zoetis Llc Dosing regimen for janus kinase (jak) inhibitors
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
JP6145179B2 (ja) * 2013-02-22 2017-06-07 ファイザー・インク ヤヌス関連キナーゼ（ＪＡＫ）の阻害剤としてのピロロ［２，３−ｄ］ピリミジン誘導体
ES2750655T3 (es) 2014-08-12 2020-03-26 Pfizer Derivados de pirrolo[2,3-d]pirimidina útiles para inhibir la Janus cinasa

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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