KR102244257B1 - Jak 키나제 저해제로서 피리미딘 화합물 - Google Patents

Jak 키나제 저해제로서 피리미딘 화합물 Download PDF

Info

Publication number
KR102244257B1
KR102244257B1 KR1020187034319A KR20187034319A KR102244257B1 KR 102244257 B1 KR102244257 B1 KR 102244257B1 KR 1020187034319 A KR1020187034319 A KR 1020187034319A KR 20187034319 A KR20187034319 A KR 20187034319A KR 102244257 B1 KR102244257 B1 KR 102244257B1
Authority
KR
South Korea
Prior art keywords
amino
azabicyclo
pyrazol
methyl
nonan
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
KR1020187034319A
Other languages
English (en)
Korean (ko)
Other versions
KR20190002591A (ko
Inventor
라이언 허드슨
제니퍼 코작
멜리사 플레리
폴 알. 파더리
앤-마리 보솔레이
단테 디. 포데스토
샤오준 후앙
Original Assignee
세라밴스 바이오파마 알앤디 아이피, 엘엘씨
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 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 filed Critical 세라밴스 바이오파마 알앤디 아이피, 엘엘씨
Publication of KR20190002591A publication Critical patent/KR20190002591A/ko
Application granted granted Critical
Publication of KR102244257B1 publication Critical patent/KR102244257B1/ko
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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

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)
KR1020187034319A 2016-04-28 2017-04-27 Jak 키나제 저해제로서 피리미딘 화합물 Expired - Fee Related KR102244257B1 (ko)

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 (2)

Publication Number Publication Date
KR20190002591A KR20190002591A (ko) 2019-01-08
KR102244257B1 true KR102244257B1 (ko) 2021-04-26

Family

ID=58672793

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020187034319A Expired - Fee Related KR102244257B1 (ko) 2016-04-28 2017-04-27 Jak 키나제 저해제로서 피리미딘 화합물

Country Status (20)

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

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3303348T3 (da) 2015-05-28 2019-11-11 Theravance Biopharma R&D Ip Llc Naphthyridinforbindelser som JAK-kinaseinhibitorer
WO2017077288A1 (en) 2015-11-03 2017-05-11 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
EP3712152B1 (en) 2015-11-03 2021-01-13 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
AU2017258186B2 (en) * 2016-04-28 2020-09-17 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as JAK kinase inhibitors
AU2018354370B2 (en) 2017-10-27 2023-04-27 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
MX2021006283A (es) * 2018-11-30 2021-10-22 Jiangsu Hansoh Pharmaceutical Group Co Ltd Derivados heteroaromáticos para uso como regulador, método de preparación de los mismos y uso de los mismos.
HRP20241053T1 (hr) * 2019-04-24 2024-11-08 Theravance Biopharma R&D Ip, Llc Pirimidinski inhibitori jak, namijenjeni liječenju kožnih bolesti
AR118768A1 (es) 2019-04-24 2021-10-27 Theravance Biopharma R&D Ip Llc Derivados de pirimidina como inhibidores de las cinasas jak
TW202207918A (zh) * 2020-05-14 2022-03-01 美商施萬生物製藥研發Ｉｐ有限責任公司 腸道選擇性ｊａｋ３抑制劑的投與
EP4225754A1 (en) * 2020-10-09 2023-08-16 Theravance Biopharma R&D IP, LLC Processes for preparing a pan-jak inhibitor and related intermediate compounds
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ATE354573T1 (de) 2000-12-21 2007-03-15 Vertex Pharma ßPYRAZOLVERBINDUNGEN, DIE SICH ALS PROTEINKINASEINHIBITOREN EIGNENß
EP1841760B1 (en) * 2004-12-30 2011-08-10 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
CA2629781A1 (en) 2005-11-16 2007-05-24 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
UY30444A1 (es) 2006-06-30 2008-01-31 Astrazeneca Ab Derivados de pirimidina, procesos para su preparacinn, composiciones farmaccuticos y usos de los mismos.
CA2656290A1 (en) 2006-07-05 2008-01-10 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
WO2013092940A1 (en) 2011-12-22 2013-06-27 F. Hoffmann-La Roche Ag 2, 4-diamine-pyrimidine derivative as serine/threonine kinase inhibitors
DK3303348T3 (da) 2015-05-28 2019-11-11 Theravance Biopharma R&D Ip Llc Naphthyridinforbindelser som JAK-kinaseinhibitorer
AU2017258186B2 (en) * 2016-04-28 2020-09-17 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as JAK kinase inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Also Published As

Publication number Publication date
EA035226B1 (ru) 2020-05-19
MX377180B (es) 2025-03-07
CL2018003060A1 (es) 2018-12-14
US11110095B2 (en) 2021-09-07
ZA201807179B (en) 2019-08-28
CA3020506A1 (en) 2017-11-02
MX2018013191A (es) 2019-02-13
EP3433253A1 (en) 2019-01-30
ES2779880T3 (es) 2020-08-20
DK3433253T3 (da) 2020-04-06
IL262386A (en) 2018-11-29
US10485803B2 (en) 2019-11-26
TW201739747A (zh) 2017-11-16
BR112018072168A2 (pt) 2019-02-12
US20170312280A1 (en) 2017-11-02
KR20190002591A (ko) 2019-01-08
IL262386B (en) 2021-08-31
JP6881879B2 (ja) 2021-06-02
CO2018011408A2 (es) 2018-11-13
SG11201809342YA (en) 2018-11-29
US20180303836A1 (en) 2018-10-25
AU2017258186A1 (en) 2018-11-15
EA201892436A1 (ru) 2019-04-30
CN109071529B (zh) 2021-08-06
CN109071529A (zh) 2018-12-21
PT3433253T (pt) 2020-04-30
TWI726094B (zh) 2021-05-01
US10028960B2 (en) 2018-07-24
JP2019514903A (ja) 2019-06-06
WO2017189822A1 (en) 2017-11-02
US20200046709A1 (en) 2020-02-13
AU2017258186B2 (en) 2020-09-17
EP3433253B1 (en) 2020-02-12

Similar Documents

Publication Publication Date Title
KR102244257B1 (ko) Jak 키나제 저해제로서 피리미딘 화합물
JP6942853B2 (ja) Ｊａｋキナーゼ阻害剤としてのナフチリジン化合物
WO2019027960A1 (en) BICYCLIC PYRAZOLO AND TRIAZOLO COMPOUNDS AS JAK KINASE INHIBITORS
HK40003022B (en) Pyrimidine compounds as jak kinase inhibitors
HK40003022A (en) Pyrimidine compounds as jak kinase inhibitors
HK40014855A (en) Process and intermediates for the preparation of naphthyridine compounds as jak kinase inhibitors
HK1245771B (en) Naphthyridine compounds as jak kinase inhibitors

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20240421

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20240421