BR112018072168A2 - compostos derivados da pirimidina como inibidores da quinase jak - Google Patents

compostos derivados da pirimidina como inibidores da quinase jak

Info

Publication number
BR112018072168A2
BR112018072168A2 BR112018072168-9A BR112018072168A BR112018072168A2 BR 112018072168 A2 BR112018072168 A2 BR 112018072168A2 BR 112018072168 A BR112018072168 A BR 112018072168A BR 112018072168 A2 BR112018072168 A2 BR 112018072168A2
Authority
BR
Brazil
Prior art keywords
compounds
kinase inhibitors
pyrimidine derivatives
jak kinase
inhibitors
Prior art date
Application number
BR112018072168-9A
Other languages
English (en)
Inventor
Hudson Ryan
Kozak Jennifer
Fleury Melissa
R. Fatheree Paul
Beausoleil Anne-Marie
D. PODESTO Dante
Huang Xiaojun
Original Assignee
Theravance Biopharma R&D Ip, Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Theravance Biopharma R&D Ip, Llc filed Critical Theravance Biopharma R&D Ip, Llc
Publication of BR112018072168A2 publication Critical patent/BR112018072168A2/pt

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Classifications

    • 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
    • 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
    • C07D451/14—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

Landscapes

  • 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)

Abstract

a invenção fornece compostos de fórmula (i): onde as variáveis estão definidas na especificação, ou um sal aceitável do ponto de vista farmacêutico, portanto, que são inibidores de jak quinases. a invenção também fornece composições farmacêuticas que incluem tais compostos, métodos de uso de tais compostos para tratar doenças gastrintestinais inflamatórias e outras doenças inflamatórias e processos e intermediários úteis para preparar tais compostos.
BR112018072168-9A 2016-04-28 2017-04-27 compostos derivados da pirimidina como inibidores da quinase jak BR112018072168A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662328737P 2016-04-28 2016-04-28
US62/328,737 2016-04-28
PCT/US2017/029796 WO2017189822A1 (en) 2016-04-28 2017-04-27 Pyrimidine compounds as jak kinase inhibitors

Publications (1)

Publication Number Publication Date
BR112018072168A2 true BR112018072168A2 (pt) 2019-02-12

Family

ID=58672793

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018072168-9A BR112018072168A2 (pt) 2016-04-28 2017-04-27 compostos derivados da pirimidina como inibidores da quinase jak

Country Status (20)

Country Link
US (3) US10028960B2 (pt)
EP (1) EP3433253B1 (pt)
JP (1) JP6881879B2 (pt)
KR (1) KR102244257B1 (pt)
CN (1) CN109071529B (pt)
AU (1) AU2017258186B2 (pt)
BR (1) BR112018072168A2 (pt)
CA (1) CA3020506A1 (pt)
CL (1) CL2018003060A1 (pt)
CO (1) CO2018011408A2 (pt)
DK (1) DK3433253T3 (pt)
EA (1) EA035226B1 (pt)
ES (1) ES2779880T3 (pt)
IL (1) IL262386B (pt)
MX (1) MX2018013191A (pt)
PT (1) PT3433253T (pt)
SG (1) SG11201809342YA (pt)
TW (1) TWI726094B (pt)
WO (1) WO2017189822A1 (pt)
ZA (1) ZA201807179B (pt)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2016267141B2 (en) 2015-05-28 2020-04-16 Theravance Biopharma R&D Ip, Llc Naphthyridine compounds as jak kinase inhibitors
EP3865481A1 (en) 2015-11-03 2021-08-18 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
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
ES2779880T3 (es) * 2016-04-28 2020-08-20 Theravance Biopharma R&D Ip Llc Compuestos de pirimidina como inhibidores de la cinasa JAK
BR112020008015A2 (pt) 2017-10-27 2020-10-27 Theravance Biopharma R&D Ip, Llc composto derivado da pirimidina como inibidor da quinase jak
US20220257600A1 (en) 2018-06-20 2022-08-18 Progenity, 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
KR20210099611A (ko) * 2018-11-30 2021-08-12 장쑤 한서 파마슈티칼 그룹 캄파니 리미티드 헤테로 방향족 유도체 조절제, 이의 제조방법 및 용도
AR118767A1 (es) 2019-04-24 2021-10-27 Theravance Biopharma R&D Ip Llc Pirimidinas sustituidas como inhibidores de jak y su uso para el tratamiento de enfermedades inflamatorias o autoinmunes cutáneas
EP3958969B1 (en) 2019-04-24 2024-01-10 Theravance Biopharma R&D IP, LLC Ester and carbonate pyrimidine compounds as jak kinase inhibitors
WO2021231272A1 (en) * 2020-05-14 2021-11-18 Theravance Biopharma R&D Ip, Llc Administration of gut-selective jak3 inhibitor
WO2022083687A1 (zh) * 2020-10-21 2022-04-28 南京明德新药研发有限公司 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

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US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
KR100909665B1 (ko) 2000-12-21 2009-07-29 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 피라졸 화합물 및 이를 포함하는 약제학적 조성물
ATE519759T1 (de) * 2004-12-30 2011-08-15 Exelixis Inc Pyrimidinderivate als kinasemodulatoren und anwendungsverfahren
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
TW200817391A (en) 2006-06-30 2008-04-16 Astrazeneca Ab Novel compounds
EP2043651A2 (en) 2006-07-05 2009-04-08 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
BR112014015549A8 (pt) 2011-12-22 2017-07-04 Hoffmann La Roche composto, método de inibição da atividade pak1, método para o tratamento, processo, composição, utilização de um composto e invenção
WO2015094803A1 (en) * 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
NO2721710T3 (pt) * 2014-08-21 2018-03-31
AU2016267141B2 (en) 2015-05-28 2020-04-16 Theravance Biopharma R&D Ip, Llc Naphthyridine compounds as jak kinase inhibitors
ES2779880T3 (es) 2016-04-28 2020-08-20 Theravance Biopharma R&D Ip Llc Compuestos de pirimidina como inhibidores de la cinasa JAK

Also Published As

Publication number Publication date
WO2017189822A1 (en) 2017-11-02
US20180303836A1 (en) 2018-10-25
US10028960B2 (en) 2018-07-24
IL262386B (en) 2021-08-31
ES2779880T3 (es) 2020-08-20
US20200046709A1 (en) 2020-02-13
CN109071529A (zh) 2018-12-21
EP3433253A1 (en) 2019-01-30
CN109071529B (zh) 2021-08-06
DK3433253T3 (da) 2020-04-06
MX2018013191A (es) 2019-02-13
EA035226B1 (ru) 2020-05-19
SG11201809342YA (en) 2018-11-29
CL2018003060A1 (es) 2018-12-14
KR20190002591A (ko) 2019-01-08
JP2019514903A (ja) 2019-06-06
AU2017258186B2 (en) 2020-09-17
KR102244257B1 (ko) 2021-04-26
US20170312280A1 (en) 2017-11-02
EA201892436A1 (ru) 2019-04-30
CA3020506A1 (en) 2017-11-02
CO2018011408A2 (es) 2018-11-13
PT3433253T (pt) 2020-04-30
TW201739747A (zh) 2017-11-16
US11110095B2 (en) 2021-09-07
US10485803B2 (en) 2019-11-26
ZA201807179B (en) 2019-08-28
AU2017258186A1 (en) 2018-11-15
TWI726094B (zh) 2021-05-01
EP3433253B1 (en) 2020-02-12
JP6881879B2 (ja) 2021-06-02
IL262386A (en) 2018-11-29

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements