TWI746178B - 製備作為jak激酶抑制劑之萘啶化合物之方法 - Google Patents

製備作為jak激酶抑制劑之萘啶化合物之方法 Download PDF

Info

Publication number
TWI746178B
TWI746178B TW109132390A TW109132390A TWI746178B TW I746178 B TWI746178 B TW I746178B TW 109132390 A TW109132390 A TW 109132390A TW 109132390 A TW109132390 A TW 109132390A TW I746178 B TWI746178 B TW I746178B
Authority
TW
Taiwan
Prior art keywords
mmol
compound
amino
methyl
azabicyclo
Prior art date
Application number
TW109132390A
Other languages
English (en)
Chinese (zh)
Other versions
TW202108593A (zh
Inventor
雷恩 修森
珍妮佛 柯薩克
保羅 R 費瑟里
丹提 D 沛戴斯妥
蓋瑞 E L 布蘭德
梅莉沙 佛羅瑞
安－瑪莉 柏索里爾
小軍 黃
凡凱特 R 泰拉狄
Original Assignee
美商施萬生物製藥研發 Ip有限責任公司
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 美商施萬生物製藥研發 Ip有限責任公司 filed Critical 美商施萬生物製藥研發 Ip有限責任公司
Publication of TW202108593A publication Critical patent/TW202108593A/zh
Application granted granted Critical
Publication of TWI746178B publication Critical patent/TWI746178B/zh

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/06—Peri-condensed systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW109132390A 2015-05-28 2016-05-27 製備作為jak激酶抑制劑之萘啶化合物之方法 TWI746178B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562167694P 2015-05-28 2015-05-28
US62/167,694 2015-05-28
US201662312273P 2016-03-23 2016-03-23
US62/312,273 2016-03-23

Publications (2)

Publication Number Publication Date
TW202108593A TW202108593A (zh) 2021-03-01
TWI746178B true TWI746178B (zh) 2021-11-11

Family

ID=56118022

Family Applications (2)

Application Number Title Priority Date Filing Date
TW109132390A TWI746178B (zh) 2015-05-28 2016-05-27 製備作為jak激酶抑制劑之萘啶化合物之方法
TW105116751A TWI704152B (zh) 2015-05-28 2016-05-27 作為ｊａｋ激酶抑制劑之萘啶化合物

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW105116751A TWI704152B (zh) 2015-05-28 2016-05-27 作為ｊａｋ激酶抑制劑之萘啶化合物

Country Status (31)

Country Link
US (6) US9725470B2 (enExample)
EP (2) EP3569604B1 (enExample)
JP (4) JP6692836B2 (enExample)
KR (1) KR20180011272A (enExample)
CN (2) CN111362975B (enExample)
AU (2) AU2016267141B2 (enExample)
BR (1) BR112017025542A2 (enExample)
CA (1) CA2983453A1 (enExample)
CL (1) CL2017002994A1 (enExample)
CO (1) CO2017012267A2 (enExample)
CY (1) CY1122279T1 (enExample)
DK (1) DK3303348T3 (enExample)
EA (1) EA032953B1 (enExample)
ES (2) ES2753159T3 (enExample)
HU (1) HUE046130T2 (enExample)
IL (3) IL255358B (enExample)
LT (1) LT3303348T (enExample)
ME (1) ME03610B (enExample)
MX (2) MX383074B (enExample)
PH (1) PH12017502050A1 (enExample)
PL (1) PL3303348T3 (enExample)
PT (1) PT3303348T (enExample)
RS (1) RS59522B1 (enExample)
SA (1) SA517390337B1 (enExample)
SG (1) SG10201910742VA (enExample)
SI (1) SI3303348T1 (enExample)
SM (1) SMT201900587T1 (enExample)
TW (2) TWI746178B (enExample)
UA (1) UA121138C2 (enExample)
WO (1) WO2016191524A1 (enExample)
ZA (1) ZA201707326B (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6692836B2 (ja) 2015-05-28 2020-05-13 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー Ｊａｋキナーゼ阻害剤としてのナフチリジン化合物
US10556901B2 (en) 2015-11-03 2020-02-11 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
WO2017077283A1 (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
BR112018072168A2 (pt) 2016-04-28 2019-02-12 Theravance Biopharma R&D Ip, Llc compostos derivados da pirimidina como inibidores da quinase jak
JOP20190144A1 (ar) 2016-12-16 2019-06-16 Janssen Pharmaceutica Nv إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز
MX2022004474A (es) 2016-12-16 2023-08-15 Janssen Pharmaceutica Nv Inhibidores de moléculas pequeñas de la familia de quinasas jak.
MX2020004255A (es) 2017-10-27 2020-07-29 Theravance Biopharma R&D Ip Llc Compuesto de pirimidina como inhibidor de las janocinasas.
TW202016110A (zh) 2018-06-15 2020-05-01 比利時商健生藥品公司 Ｊａｋ激酶家族之小分子抑制劑
EP3810094A1 (en) 2018-06-20 2021-04-28 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with a jak or other kinase inhibitor
TWI740288B (zh) * 2018-11-27 2021-09-21 大陸商江蘇豪森藥業集團有限公司 含氮雜芳類衍生物調節劑、其製備方法和應用
KR20210099611A (ko) * 2018-11-30 2021-08-12 장쑤 한서 파마슈티칼 그룹 캄파니 리미티드 헤테로 방향족 유도체 조절제, 이의 제조방법 및 용도
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP3958969B1 (en) 2019-04-24 2024-01-10 Theravance Biopharma R&D IP, LLC Ester and carbonate pyrimidine compounds as jak kinase inhibitors
HUE067909T2 (hu) 2019-04-24 2024-11-28 Theravance Biopharma R&D Ip Llc Pirimidin JAK-inhibitorok bõrbetegségek kezelésére
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
TW202144366A (zh) * 2020-05-25 2021-12-01 大陸商上海翰森生物醫藥科技有限公司 雜芳類衍生物的鹽、晶型及其製備方法
CN113717202B (zh) * 2020-05-25 2025-10-17 上海翰森生物医药科技有限公司 杂芳类衍生物的自由碱晶型及其制备方法
UY39454A (es) * 2020-10-09 2022-04-29 Janssen Biotech Inc Procesos para preparar un inhibidor de pan-jak y compuestos intermedios relacionados
WO2022076717A1 (en) * 2020-10-09 2022-04-14 Janssen Biotech, Inc. Solvate forms of a pan-jak inhibitor
TW202228689A (zh) * 2020-10-09 2022-08-01 美商賽若凡斯生物製藥研發智財有限責任公司 泛ｊａｋ抑制劑的調配物
WO2022076714A1 (en) * 2020-10-09 2022-04-14 Janssen Biotech, Inc. Solid forms of a pan-jak inhibitor
WO2022165529A1 (en) * 2021-02-01 2022-08-04 Janssen Biotech, Inc. Small molecule inhibitors of salt inducible kinases
EP4304590A1 (en) 2021-03-11 2024-01-17 Janssen Pharmaceutica NV Lorpucitinib for use in the treatment of jak mediated disorders
WO2022241188A1 (en) 2021-05-14 2022-11-17 Theravance Biopharma R&D Ip, Llc Enantioselective synthesis of aminotropane compound
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
WO2023102800A1 (en) 2021-12-09 2023-06-15 Theravance Biopharma R&D Ip, Llc Synthesis of 5, 7-dichloro-1, 6-naphthyridine
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
CA3261072A1 (en) 2022-07-27 2025-04-07 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Fused cyclic compound, its preparation process and its medicinal application
WO2024249568A1 (en) 2023-05-30 2024-12-05 Paragon Therapeutics, Inc. Alpha4beta7 integrin antibody compositions and methods of use

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006067614A2 (en) * 2004-12-23 2006-06-29 Pfizer Products Inc. Heteroaromatic derivatives useful as anticancer agents
WO2007071348A1 (en) * 2005-12-19 2007-06-28 F. Hoffmann-La Roche Ag Isoquinoline aminopyrazole derivatives, their manufacture and use as pharmaceutical agents for the treatment of cancer
WO2008119792A1 (en) * 2007-04-02 2008-10-09 Palau Pharma, S. A. Pyrrolopyrimidine derivatives as jak3 inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
PL210066B1 (pl) 2000-12-21 2011-11-30 Vertex Pharma Związek pirazolowy, kompozycja zawierająca ten związek i jego zastosowania
EP1595881A1 (en) * 2004-05-12 2005-11-16 Pfizer Limited Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands
US20110269740A1 (en) * 2008-07-02 2011-11-03 Ambit Biosciences Corporation Jak kinase modulating compounds and methods of use thereof
CA2732087A1 (en) 2008-08-05 2010-02-11 Boehringer Ingelheim International Gmbh Substituted naphthyridines and their use as medicaments
EP2346859A1 (en) 2008-09-30 2011-07-27 AstraZeneca AB Heterocyclic jak kinase inhibitors
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
WO2012022045A1 (en) * 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
EP2527344A1 (en) * 2011-05-25 2012-11-28 Almirall, S.A. Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases
CN105367555B (zh) 2014-08-07 2019-06-25 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
JP6692836B2 (ja) 2015-05-28 2020-05-13 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー Ｊａｋキナーゼ阻害剤としてのナフチリジン化合物
BR112018072168A2 (pt) 2016-04-28 2019-02-12 Theravance Biopharma R&D Ip, Llc compostos derivados da pirimidina como inibidores da quinase jak

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006067614A2 (en) * 2004-12-23 2006-06-29 Pfizer Products Inc. Heteroaromatic derivatives useful as anticancer agents
WO2007071348A1 (en) * 2005-12-19 2007-06-28 F. Hoffmann-La Roche Ag Isoquinoline aminopyrazole derivatives, their manufacture and use as pharmaceutical agents for the treatment of cancer
WO2008119792A1 (en) * 2007-04-02 2008-10-09 Palau Pharma, S. A. Pyrrolopyrimidine derivatives as jak3 inhibitors

Also Published As

Publication number Publication date
DK3303348T3 (da) 2019-11-11
RS59522B1 (sr) 2019-12-31
AU2020202181A1 (en) 2020-04-16
CO2017012267A2 (es) 2018-03-28
IL255358B (en) 2020-01-30
US20240132520A1 (en) 2024-04-25
IL272057B (en) 2020-09-30
EP3569604A1 (en) 2019-11-20
TWI704152B (zh) 2020-09-11
PT3303348T (pt) 2019-11-15
ME03610B (me) 2020-07-20
JP6942853B2 (ja) 2021-09-29
TW201716416A (zh) 2017-05-16
IL276677A (en) 2020-09-30
TW202108593A (zh) 2021-03-01
EP3569604B1 (en) 2022-07-06
MX2020011774A (es) 2021-06-01
CN111362975B (zh) 2022-04-05
SG10201910742VA (en) 2020-01-30
IL255358A0 (en) 2017-12-31
IL276677B (en) 2021-05-31
HUE046130T2 (hu) 2020-02-28
CN111362975A (zh) 2020-07-03
US20180354974A1 (en) 2018-12-13
US12358931B2 (en) 2025-07-15
AU2020202181B2 (en) 2021-07-01
CY1122279T1 (el) 2020-10-14
JP2020111593A (ja) 2020-07-27
PL3303348T3 (pl) 2020-02-28
JP2021001196A (ja) 2021-01-07
ZA201707326B (en) 2018-11-28
MX2017015211A (es) 2018-04-13
US10494382B2 (en) 2019-12-03
ES2924698T3 (es) 2022-10-10
JP6850922B2 (ja) 2021-03-31
US10947254B2 (en) 2021-03-16
JP2021098757A (ja) 2021-07-01
SA517390337B1 (ar) 2021-03-31
CL2017002994A1 (es) 2018-03-09
EA032953B1 (ru) 2019-08-30
EA201792619A1 (ru) 2018-04-30
SI3303348T1 (sl) 2019-12-31
CA2983453A1 (en) 2016-12-01
US20160347772A1 (en) 2016-12-01
CN107667108B (zh) 2020-05-12
PH12017502050B1 (en) 2018-04-23
ES2753159T3 (es) 2020-04-07
WO2016191524A1 (en) 2016-12-01
PH12017502050A1 (en) 2018-04-23
EP3303348B1 (en) 2019-08-07
US20200040010A1 (en) 2020-02-06
US20170305934A1 (en) 2017-10-26
AU2016267141A1 (en) 2017-11-16
BR112017025542A2 (pt) 2018-08-07
US10072026B2 (en) 2018-09-11
MX383074B (es) 2025-03-13
HK1245771A1 (en) 2018-08-31
SMT201900587T1 (it) 2019-11-13
KR20180011272A (ko) 2018-01-31
US9725470B2 (en) 2017-08-08
UA121138C2 (uk) 2020-04-10
JP2018515581A (ja) 2018-06-14
EP3303348A1 (en) 2018-04-11
JP6692836B2 (ja) 2020-05-13
US20210179637A1 (en) 2021-06-17
AU2016267141B2 (en) 2020-04-16
US11780852B2 (en) 2023-10-10
CN107667108A (zh) 2018-02-06
LT3303348T (lt) 2019-11-25
IL272057A (en) 2020-02-27
MX378963B (es) 2025-03-10

Similar Documents

Publication Publication Date Title
TWI746178B (zh) 製備作為jak激酶抑制劑之萘啶化合物之方法
JP6881879B2 (ja) Ｊａｋキナーゼ阻害剤としてのピリミジン化合物
TW201920150A (zh) 作為jak激酶抑制劑之吡唑并及三唑并雙環化合物
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
MM4A Annulment or lapse of patent due to non-payment of fees