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
    • 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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    • A61K31/53751,4-Oxazines, e.g. morpholine
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  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
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  • Communicable Diseases (AREA)
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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

Publications (1)

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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
RS58245B1 (sr) 2013-02-22 2019-03-29 Pfizer Kombinacija derivata pirolo[2,3-d]pirimidina sa jednim ili više dodatnih sredstava kao inhibitor janus kinaza (jak)
EP3180344B1 (en) 2014-08-12 2019-09-18 Pfizer Inc Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase
CN109311858B (zh) 2016-05-26 2021-12-03 里科瑞尔姆Ip控股有限责任公司 Egfr抑制剂化合物
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
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
CN111936144B (zh) * 2018-03-21 2023-12-22 廖细斌 Jak抑制剂
CN112384282B (zh) * 2018-07-06 2024-07-02 辉瑞公司 吡咯并[2,3-d]嘧啶化合物的制造方法与中间体及其用途
MX2021005334A (es) * 2018-11-05 2021-06-23 Avista Pharma Solutions Inc Compuestos quimicos.
WO2020132378A2 (en) 2018-12-22 2020-06-25 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising depression
CN114072407A (zh) 2019-04-02 2022-02-18 阿里戈斯治疗公司 靶向prmt5的化合物
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
KR20230015989A (ko) * 2020-05-28 2023-01-31 화이자 인코포레이티드 피롤로[2,3-d]피리미딘 유도체
EP4210828A1 (en) * 2020-09-11 2023-07-19 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
JP2024506384A (ja) 2021-02-10 2024-02-13 イオリクス セラピューティクス,インコーポレーテッド ロフルミラストの眼科的送達方法
CA3231766A1 (en) 2021-09-22 2023-03-30 Elizabeth W. JEFFORDS Methods of treating ocular inflammatory diseases
US12227484B2 (en) 2022-02-14 2025-02-18 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
US6765008B1 (en) 1992-12-17 2004-07-20 Pfizer Inc Pyrrolopyrimidines as CRF antagonists
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
TW505646B (en) 1998-06-19 2002-10-11 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine compounds
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
EP1175421A1 (en) 1999-04-30 2002-01-30 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
PT1382339E (pt) 1999-12-10 2008-02-06 Pfizer Prod Inc Composições que contêm derivados de pirrolo[2,3-d]- pirimidina
US20030187261A1 (en) 2000-01-07 2003-10-02 Libor Havlicek Purine derivatives, process for their preparation and use thereof
PL359563A1 (pl) 2000-06-26 2004-08-23 Pfizer Products Inc. Związki pirolo [2,3-d] pirymidynowe jako środki immunosupresyjne
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
JP2005529062A (ja) 2001-11-30 2005-09-29 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド アデノシンa1及びa3受容体に特異的な化合物とその使用
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
KR100678800B1 (ko) 2002-11-21 2007-02-05 화이자 프로덕츠 인코포레이티드 3-아미노-피페리딘 유도체 및 그의 제조 방법
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.
CA2614907C (en) 2005-07-29 2012-02-28 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
JP2009531443A (ja) 2006-03-29 2009-09-03 フォールドアールエックス ファーマシューティカルズ インコーポレーティッド α−シヌクレイン毒性の抑制
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
AU2008323694A1 (en) 2007-11-07 2009-05-14 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
EP2384326B1 (en) 2008-08-20 2014-04-23 Zoetis LLC Pyrrolo[2,3-d]pyrimidine compounds
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.
EA201290147A1 (ru) 2009-10-15 2012-11-30 Пфайзер Инк. Пирроло[2,3-d]пиримидиновые соединения
ME02800B (me) 2009-12-01 2018-01-20 Abbvie Inc Nova triciklična jedinjenja
WO2011075334A1 (en) 2009-12-18 2011-06-23 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine compounds
US8461328B2 (en) 2010-01-12 2013-06-11 Genentech, Inc. Tricyclic heterocyclic compounds, compositions and methods of use thereof
MX2012009798A (es) 2010-02-24 2012-09-12 Pfizer Composiciones veterinarias.
WO2012009649A1 (en) 2010-07-16 2012-01-19 Anderson Gaweco Mif inhibitors and their uses
WO2012009678A1 (en) 2010-07-16 2012-01-19 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their method of use
CA2819648C (en) 2010-12-03 2018-05-01 Epizyme, Inc. Substituted purine and 7-deazapurine compounds
US8987307B2 (en) 2011-03-03 2015-03-24 Hoffmann-La Roche Inc. 3-amino-pyridines as GPBAR1 agonists
US20140057895A1 (en) 2011-06-07 2014-02-27 Kazuhiro Mizuno 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
KR20150028299A (ko) 2012-07-20 2015-03-13 조에티스 엘엘씨 야누스 키나제 (jak) 억제제 투여요법
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
RS58245B1 (sr) * 2013-02-22 2019-03-29 Pfizer Kombinacija derivata pirolo[2,3-d]pirimidina sa jednim ili više dodatnih sredstava kao inhibitor 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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