TWI726094B - 作為jak激酶抑制劑之嘧啶化合物 - Google Patents

作為jak激酶抑制劑之嘧啶化合物 Download PDF

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Publication number
TWI726094B
TWI726094B TW106114033A TW106114033A TWI726094B TW I726094 B TWI726094 B TW I726094B TW 106114033 A TW106114033 A TW 106114033A TW 106114033 A TW106114033 A TW 106114033A TW I726094 B TWI726094 B TW I726094B
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Taiwan
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amino
methyl
azabicyclo
pyrazol
compound
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TW106114033A
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Chinese (zh)
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TW201739747A (zh
Inventor
雷恩 修森
珍妮佛 柯薩克
梅莉沙 佛羅瑞
保羅 R 費瑟里
安－瑪莉 柏索里爾
丹提 D 沛戴斯妥
小軍 黃
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美商施萬生物製藥研發Ｉｐ有限責任公司
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    • 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
    • A61K31/495—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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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)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW106114033A 2016-04-28 2017-04-27 作為jak激酶抑制劑之嘧啶化合物 TWI726094B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662328737P 2016-04-28 2016-04-28
US62/328,737 2016-04-28

Publications (2)

Publication Number Publication Date
TW201739747A TW201739747A (zh) 2017-11-16
TWI726094B true TWI726094B (zh) 2021-05-01

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US (3) US10028960B2 (enExample)
EP (1) EP3433253B1 (enExample)
JP (1) JP6881879B2 (enExample)
KR (1) KR102244257B1 (enExample)
CN (1) CN109071529B (enExample)
AU (1) AU2017258186B2 (enExample)
BR (1) BR112018072168A2 (enExample)
CA (1) CA3020506A1 (enExample)
CL (1) CL2018003060A1 (enExample)
CO (1) CO2018011408A2 (enExample)
DK (1) DK3433253T3 (enExample)
EA (1) EA035226B1 (enExample)
ES (1) ES2779880T3 (enExample)
IL (1) IL262386B (enExample)
MX (1) MX377180B (enExample)
PT (1) PT3433253T (enExample)
SG (1) SG11201809342YA (enExample)
TW (1) TWI726094B (enExample)
WO (1) WO2017189822A1 (enExample)
ZA (1) ZA201807179B (enExample)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20180011272A (ko) 2015-05-28 2018-01-31 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 키나제 저해제로서 나프티리딘 화합물
DK3712152T3 (da) 2015-11-03 2021-03-22 Topivert Pharma Ltd 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridin og 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepinderivater som janus kinase-inhibitorer
EP3371185B1 (en) 2015-11-03 2020-09-30 Topivert Pharma Limited 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors
CA3020506A1 (en) 2016-04-28 2017-11-02 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as jak kinase inhibitors
GEP20227344B (en) 2017-10-27 2022-01-25 Theravance Biopharma R&D Ip Llc Pyrimidine compound as jak kinase inhibitor
US12171764B2 (en) 2018-06-20 2024-12-24 Biora Therapeutics, Inc. Treatment of a disease of the gastrointestinal tract with a JAK or other kinase inhibitor
CN111601804B (zh) * 2018-11-27 2024-06-04 江苏豪森药业集团有限公司 含氮杂芳类衍生物调节剂、其制备方法和应用
CN115925705B (zh) * 2018-11-30 2024-12-31 江苏豪森药业集团有限公司 杂芳类衍生物调节剂、其制备方法和应用
TW202106681A (zh) * 2019-04-24 2021-02-16 美商施萬生物製藥研發Ｉｐ有限責任公司 用於治療皮膚疾病之嘧啶jak抑制劑
TW202106682A (zh) 2019-04-24 2021-02-16 美商施萬生物製藥研發Ｉｐ有限責任公司 作為jak激酶抑制劑之酯類及碳酸酯類嘧啶化合物
EP4149462A4 (en) * 2020-05-14 2024-04-24 Theravance Biopharma R&D IP, LLC Administration of gut-selective jak3 inhibitor
UY39454A (es) * 2020-10-09 2022-04-29 Janssen Biotech Inc Procesos para preparar un inhibidor de pan-jak y compuestos intermedios relacionados
CN116390922B (zh) * 2020-10-21 2025-07-18 珠海联邦制药股份有限公司 硒杂环类化合物及其应用
WO2023011359A1 (zh) * 2021-08-05 2023-02-09 南京明德新药研发有限公司 桥环类化合物及其应用
CN113883920B (zh) * 2021-10-25 2024-01-23 安徽华铂再生资源科技有限公司 一种降低空分装置空冷塔出口温度的方法
WO2023202706A1 (zh) * 2022-04-21 2023-10-26 南京明德新药研发有限公司 硒杂环类化合物的盐型和晶型及其应用
WO2025040148A1 (zh) * 2023-08-22 2025-02-27 北京普祺医药科技股份有限公司 一种用于jak抑制剂的外用凝胶及其用途
TW202515852A (zh) * 2023-09-15 2025-04-16 美商莫菲克醫療股份有限公司 抑制人類整合素α４β７

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006074057A2 (en) * 2004-12-30 2006-07-13 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
WO2015094803A1 (en) * 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
US20160052930A1 (en) * 2014-08-21 2016-02-25 Pfizer Inc. Aminopyrimidinyl compounds

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US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CA2432799C (en) 2000-12-21 2008-08-19 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CN101360740A (zh) 2005-11-16 2009-02-04 沃泰克斯药物股份有限公司 可用作激酶抑制剂的氨基嘧啶
UY30444A1 (es) 2006-06-30 2008-01-31 Astrazeneca Ab Derivados de pirimidina, procesos para su preparacinn, composiciones farmaccuticos y usos de los mismos.
EP2043651A2 (en) 2006-07-05 2009-04-08 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
RU2014129740A (ru) 2011-12-22 2016-02-10 Ф.Хоффманн-Ля Рош Аг Производные 2,4-диаминопиримидина в качестве ингибиторов серин/треонин киназы
KR20180011272A (ko) 2015-05-28 2018-01-31 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 키나제 저해제로서 나프티리딘 화합물
CA3020506A1 (en) * 2016-04-28 2017-11-02 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as jak kinase inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006074057A2 (en) * 2004-12-30 2006-07-13 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
WO2015094803A1 (en) * 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
US20160052930A1 (en) * 2014-08-21 2016-02-25 Pfizer Inc. Aminopyrimidinyl compounds

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Publication number Publication date
US10485803B2 (en) 2019-11-26
CA3020506A1 (en) 2017-11-02
CN109071529A (zh) 2018-12-21
KR20190002591A (ko) 2019-01-08
EA035226B1 (ru) 2020-05-19
ES2779880T3 (es) 2020-08-20
JP6881879B2 (ja) 2021-06-02
ZA201807179B (en) 2019-08-28
EP3433253A1 (en) 2019-01-30
MX2018013191A (es) 2019-02-13
EP3433253B1 (en) 2020-02-12
TW201739747A (zh) 2017-11-16
CL2018003060A1 (es) 2018-12-14
US10028960B2 (en) 2018-07-24
CN109071529B (zh) 2021-08-06
EA201892436A1 (ru) 2019-04-30
KR102244257B1 (ko) 2021-04-26
JP2019514903A (ja) 2019-06-06
US11110095B2 (en) 2021-09-07
SG11201809342YA (en) 2018-11-29
US20180303836A1 (en) 2018-10-25
BR112018072168A2 (pt) 2019-02-12
IL262386A (en) 2018-11-29
AU2017258186A1 (en) 2018-11-15
PT3433253T (pt) 2020-04-30
US20170312280A1 (en) 2017-11-02
IL262386B (en) 2021-08-31
AU2017258186B2 (en) 2020-09-17
CO2018011408A2 (es) 2018-11-13
US20200046709A1 (en) 2020-02-13
MX377180B (es) 2025-03-07
WO2017189822A1 (en) 2017-11-02
DK3433253T3 (da) 2020-04-06

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