CN107074818B - 作为nik抑制剂的吡唑衍生物 - Google Patents

作为nik抑制剂的吡唑衍生物 Download PDF

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Publication number
CN107074818B
CN107074818B CN201580057462.XA CN201580057462A CN107074818B CN 107074818 B CN107074818 B CN 107074818B CN 201580057462 A CN201580057462 A CN 201580057462A CN 107074818 B CN107074818 B CN 107074818B
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hydrogen
alkyl
substituted
het
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Chinese (zh)
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CN107074818A (zh
Inventor
G.海恩德
P.蒂斯塞里
J.J.库拉戈维斯
C.马勒奥德
S.E.曼恩
J.G.蒙塔纳
S.C.普里塞
F.J.G.劳斯塞
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Janssen Pharmaceutica NV
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201580057462.XA 2014-10-23 2015-10-22 作为nik抑制剂的吡唑衍生物 Expired - Fee Related CN107074818B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14190072 2014-10-23
EP14190072.0 2014-10-23
PCT/EP2015/074433 WO2016062791A1 (en) 2014-10-23 2015-10-22 New pyrazole derivatives as nik inhibitors

Publications (2)

Publication Number Publication Date
CN107074818A CN107074818A (zh) 2017-08-18
CN107074818B true CN107074818B (zh) 2020-04-17

Family

ID=51865980

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580057462.XA Expired - Fee Related CN107074818B (zh) 2014-10-23 2015-10-22 作为nik抑制剂的吡唑衍生物

Country Status (13)

Country Link
US (1) US9981962B2 (enExample)
EP (1) EP3209654B1 (enExample)
JP (1) JP6616411B2 (enExample)
KR (1) KR102499862B1 (enExample)
CN (1) CN107074818B (enExample)
AU (1) AU2015334916B2 (enExample)
BR (1) BR112017008039B1 (enExample)
CA (1) CA2960335C (enExample)
EA (1) EA033236B1 (enExample)
ES (1) ES2704749T3 (enExample)
IL (1) IL251777B (enExample)
MX (1) MX371150B (enExample)
WO (1) WO2016062791A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI663166B (zh) 2013-04-24 2019-06-21 健生藥品公司 新化合物
TWI627173B (zh) 2013-09-26 2018-06-21 比利時商健生藥品公司 作為ＮＩＫ抑制劑的新穎３－（１Ｈ－吡唑－４－基）－１Ｈ－吡咯并［２，３－ｃ］吡啶衍生物
TWI704146B (zh) 2013-09-26 2020-09-11 比利時商健生藥品公司 用作ＮＩＫ抑制劑之新的1-(４-嘧啶基)-１Ｈ-吡唑並[３,２-ｃ]吡啶衍生物
CA2960335C (en) 2014-10-23 2023-09-19 Janssen Pharmaceutica Nv New pyrazole derivatives as nik inhibitors
EA030908B1 (ru) 2014-10-23 2018-10-31 Янссен Фармацевтика Нв Соединения в качестве ингибиторов nik
MX371151B (es) 2014-10-23 2020-01-20 Janssen Pharmaceutica Nv NUEVOS DERIVADOS DE TIENOPIRIMIDINA EN CALIDAD DE INHIBIDORES DE LA CINASA INDUCTORA DE NF-kB (NIK).
ES2715104T3 (es) 2014-10-23 2019-05-31 Janssen Pharmaceutica Nv Nuevos derivados de pirazolopirimidina como inhibidores de nik
EP4455145A3 (en) * 2015-12-02 2025-03-12 Astraea Therapeutics, LLC Piperidinyl nociceptin receptor compounds
US10112924B2 (en) 2015-12-02 2018-10-30 Astraea Therapeutics, Inc. Piperdinyl nociceptin receptor compounds
CA3012031C (en) * 2016-01-22 2024-03-26 Janssen Pharmaceutica Nv 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors
MX2021014679A (es) 2019-05-31 2022-04-06 Janssen Pharmaceutica Nv Inhibidores de molécula pequeña de quinasa inductora de nf-kb.
TW202402269A (zh) * 2022-05-26 2024-01-16 大陸商迪哲（江蘇）醫藥股份有限公司 ＲＯＣＫ（Ｒｈｏ相關激酶）抑制劑及其用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009158011A1 (en) * 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors
CN103476768A (zh) * 2011-03-16 2013-12-25 弗·哈夫曼-拉罗切有限公司 6,5-杂环炔丙醇化合物及其用途

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2564356A1 (en) 2004-04-26 2005-11-03 Pfizer Inc. Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors
AR056786A1 (es) 2005-11-10 2007-10-24 Smithkline Beecham Corp Compuesto de 1h- imidazo ( 4,5-c) piridin-2-ilo, composicion farmaceutica que lo comprende, procedimiento para preparar dicha composicion, su uso para preparar unmedicamento, uso de una combinacion que omprende al compuesto y al menos un agente antineoplasico para preparar un medicamento y dicha com
DE102008005493A1 (de) 2008-01-22 2009-07-23 Merck Patent Gmbh 4-(Pyrrolo[2,3-c] pyridine-3-yl)-pyrimidin-2-yl-amin-derivate
EP2320895A2 (en) 2008-07-03 2011-05-18 Exelixis, Inc. Cdk modulators
US20110183975A1 (en) 2008-10-07 2011-07-28 Yasuhiro Goto Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity
CN101723936B (zh) 2008-10-27 2014-01-15 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
TWI663166B (zh) 2013-04-24 2019-06-21 健生藥品公司 新化合物
TWI704146B (zh) 2013-09-26 2020-09-11 比利時商健生藥品公司 用作ＮＩＫ抑制劑之新的1-(４-嘧啶基)-１Ｈ-吡唑並[３,２-ｃ]吡啶衍生物
TWI627173B (zh) 2013-09-26 2018-06-21 比利時商健生藥品公司 作為ＮＩＫ抑制劑的新穎３－（１Ｈ－吡唑－４－基）－１Ｈ－吡咯并［２，３－ｃ］吡啶衍生物
EA030908B1 (ru) 2014-10-23 2018-10-31 Янссен Фармацевтика Нв Соединения в качестве ингибиторов nik
MX371151B (es) 2014-10-23 2020-01-20 Janssen Pharmaceutica Nv NUEVOS DERIVADOS DE TIENOPIRIMIDINA EN CALIDAD DE INHIBIDORES DE LA CINASA INDUCTORA DE NF-kB (NIK).
CA2960335C (en) 2014-10-23 2023-09-19 Janssen Pharmaceutica Nv New pyrazole derivatives as nik inhibitors
ES2715104T3 (es) 2014-10-23 2019-05-31 Janssen Pharmaceutica Nv Nuevos derivados de pirazolopirimidina como inhibidores de nik

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009158011A1 (en) * 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors
CN103476768A (zh) * 2011-03-16 2013-12-25 弗·哈夫曼-拉罗切有限公司 6,5-杂环炔丙醇化合物及其用途

Also Published As

Publication number Publication date
MX371150B (es) 2020-01-20
CA2960335C (en) 2023-09-19
EA033236B1 (ru) 2019-09-30
IL251777A0 (en) 2017-06-29
CA2960335A1 (en) 2016-04-28
CN107074818A (zh) 2017-08-18
BR112017008039A2 (pt) 2017-12-19
ES2704749T3 (es) 2019-03-19
MX2017005283A (es) 2017-08-15
BR112017008039B1 (pt) 2023-04-11
AU2015334916B2 (en) 2020-02-06
US9981962B2 (en) 2018-05-29
JP2017531677A (ja) 2017-10-26
WO2016062791A1 (en) 2016-04-28
KR102499862B1 (ko) 2023-02-13
JP6616411B2 (ja) 2019-12-04
EP3209654B1 (en) 2018-10-03
EA201790904A1 (ru) 2017-08-31
EP3209654A1 (en) 2017-08-30
KR20170068488A (ko) 2017-06-19
IL251777B (en) 2021-09-30
US20170334900A1 (en) 2017-11-23
AU2015334916A1 (en) 2017-03-23

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