CN112703037B - 作为jak抑制剂的5至7元杂环酰胺 - Google Patents

作为jak抑制剂的5至7元杂环酰胺 Download PDF

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Publication number
CN112703037B
CN112703037B CN201980057601.7A CN201980057601A CN112703037B CN 112703037 B CN112703037 B CN 112703037B CN 201980057601 A CN201980057601 A CN 201980057601A CN 112703037 B CN112703037 B CN 112703037B
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compound
pharmaceutically acceptable
acceptable salt
lung
mmol
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CN112703037A (zh
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丹尼尔·D·朗
C·史密斯
C·汤普森
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Theravance Biopharma R&D IP LLC
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Theravance Biopharma R&D IP LLC
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    • 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201980057601.7A 2018-09-04 2019-09-03 作为jak抑制剂的5至7元杂环酰胺 Active CN112703037B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862726583P 2018-09-04 2018-09-04
US62/726,583 2018-09-04
PCT/US2019/049342 WO2020051139A1 (en) 2018-09-04 2019-09-03 5 to 7 membered heterocyclic amides as jak inhibitors

Publications (2)

Publication Number Publication Date
CN112703037A CN112703037A (zh) 2021-04-23
CN112703037B true CN112703037B (zh) 2023-10-20

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CN201980057601.7A Active CN112703037B (zh) 2018-09-04 2019-09-03 作为jak抑制剂的5至7元杂环酰胺

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US (2) US10836763B2 (https=)
EP (1) EP3837010B1 (https=)
JP (1) JP7383696B2 (https=)
KR (1) KR20210056380A (https=)
CN (1) CN112703037B (https=)
AR (1) AR116114A1 (https=)
AU (1) AU2019335200A1 (https=)
BR (1) BR112021004063A2 (https=)
CL (1) CL2021000515A1 (https=)
CO (1) CO2021002976A2 (https=)
EA (1) EA202190686A1 (https=)
ES (1) ES2955717T3 (https=)
IL (1) IL281150B2 (https=)
MX (1) MX2021002484A (https=)
PH (1) PH12021550324A1 (https=)
SG (1) SG11202101751XA (https=)
TW (1) TWI793365B (https=)
UA (1) UA127328C2 (https=)
WO (1) WO2020051139A1 (https=)
ZA (1) ZA202100990B (https=)

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WO2016004079A1 (en) 2014-06-30 2016-01-07 Black & Decker Inc. Battery pack for a cordless power tools
HK1252685A1 (zh) 2015-11-03 2019-05-31 Theravance Biopharma R&D Ip, Llc 用於治疗呼吸疾病的jak激酶抑制剂化合物
BR112019018648A2 (pt) 2017-03-09 2020-06-16 Theravance Biopharma R&D Ip, Llc Inibidores de jak contendo uma amida heterocíclica com 4 membros
PT3837258T (pt) 2018-09-04 2024-06-20 Theravance Biopharma R&D Ip Llc Amidas de dimetil amino azetidina como inibidores de jak
CA3108848A1 (en) 2018-09-04 2020-03-12 Theravance Biopharma R&D Ip, Llc Process for preparing jak inhibitors and intermediates thereof
WO2020051139A1 (en) * 2018-09-04 2020-03-12 Theravance Biopharma R&D Ip, Llc 5 to 7 membered heterocyclic amides as jak inhibitors
TW202144343A (zh) 2020-03-02 2021-12-01 美商施萬生物製藥研發 Ip有限責任公司 Jak抑制劑化合物之結晶水合物
WO2022081872A1 (en) * 2020-10-16 2022-04-21 Gb008, Inc. Janus kinase inhibitors
TW202317550A (zh) 2021-06-25 2023-05-01 美商施萬生物製藥研發 Ip有限責任公司 作為jak抑制劑之咪唑吲唑化合物
JP7644873B2 (ja) * 2021-12-17 2025-03-12 デウン ファーマシューティカル カンパニー リミテッド （２Ｒ，３Ｓ）－２－（３－（４，５－ジクロロ－１Ｈ－ベンゾ［ｄ］イミダゾール－１－イル）プロピル）ピペリジン－３－オールの新規な酸付加塩および結晶形
WO2025172431A1 (en) * 2024-02-14 2025-08-21 Almirall, S.A. Stat6 inhibitors and methods of use thereof

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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
WO2017079205A1 (en) * 2015-11-03 2017-05-11 Theravance Biopharma R&D Ip, Llc Jak kinase inhibitor compounds for treatment of respiratory disease
WO2018011681A1 (en) * 2016-07-14 2018-01-18 Pfizer Inc. Novel pyrimidine carboxamides as inhibitors of vanin-1 enzyme
WO2018165395A1 (en) * 2017-03-09 2018-09-13 Theravance Biopharma R&D Ip, Llc Fused imidazo-piperidine jak inhibitors

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BRPI0909945A2 (pt) 2008-06-20 2015-07-28 Genentech Inc "composto, composição farmacêutica, método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak2 quinase em um paciente, kit para o tratamento de uma doença ou distúrbio responsivo à inibição da jak quinase"
JP2010111624A (ja) 2008-11-06 2010-05-20 Shionogi & Co Ltd Ｔｔｋ阻害作用を有するインダゾール誘導体
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PT3837258T (pt) 2018-09-04 2024-06-20 Theravance Biopharma R&D Ip Llc Amidas de dimetil amino azetidina como inibidores de jak
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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
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WO2017079205A1 (en) * 2015-11-03 2017-05-11 Theravance Biopharma R&D Ip, Llc Jak kinase inhibitor compounds for treatment of respiratory disease
WO2018011681A1 (en) * 2016-07-14 2018-01-18 Pfizer Inc. Novel pyrimidine carboxamides as inhibitors of vanin-1 enzyme
WO2018165395A1 (en) * 2017-03-09 2018-09-13 Theravance Biopharma R&D Ip, Llc Fused imidazo-piperidine jak inhibitors

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Publication number Publication date
WO2020051139A1 (en) 2020-03-12
KR20210056380A (ko) 2021-05-18
UA127328C2 (uk) 2023-07-19
ZA202100990B (en) 2024-09-25
JP2021535174A (ja) 2021-12-16
EA202190686A1 (ru) 2021-07-23
EP3837010A1 (en) 2021-06-23
CN112703037A (zh) 2021-04-23
EP3837010B1 (en) 2023-07-05
SG11202101751XA (en) 2021-03-30
CO2021002976A2 (es) 2021-05-31
IL281150B2 (en) 2024-03-01
ES2955717T3 (es) 2023-12-05
MX2021002484A (es) 2021-05-12
PH12021550324A1 (en) 2021-10-04
TW202024075A (zh) 2020-07-01
BR112021004063A2 (pt) 2021-05-25
US11713315B2 (en) 2023-08-01
US10836763B2 (en) 2020-11-17
JP7383696B2 (ja) 2023-11-20
TWI793365B (zh) 2023-02-21
IL281150B1 (en) 2023-11-01
IL281150A (en) 2021-04-29
US20200071325A1 (en) 2020-03-05
US20210024517A1 (en) 2021-01-28
AR116114A1 (es) 2021-03-31
AU2019335200A1 (en) 2021-03-11
EP3837010C0 (en) 2023-07-05
CL2021000515A1 (es) 2021-07-23

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