BR112021016751B8 - Compostos, composições farmacêuticas e usos dos compostos - Google Patents

Compostos, composições farmacêuticas e usos dos compostos

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Publication number
BR112021016751B8
BR112021016751B8 BR112021016751A BR112021016751A BR112021016751B8 BR 112021016751 B8 BR112021016751 B8 BR 112021016751B8 BR 112021016751 A BR112021016751 A BR 112021016751A BR 112021016751 A BR112021016751 A BR 112021016751A BR 112021016751 B8 BR112021016751 B8 BR 112021016751B8
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Brazil
Prior art keywords
compounds
pharmaceutical compositions
present
relates
tautomer
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BR112021016751A
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English (en)
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BR112021016751A2 (pt
BR112021016751B1 (pt
Inventor
Hai Huang
Jixuan Zhang
Liang Lu
Longzheng Zhang
Saisai Zhao
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Henan Medinno Pharmaceutical Tech Co Ltd
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Publication of BR112021016751A2 publication Critical patent/BR112021016751A2/pt
Publication of BR112021016751B1 publication Critical patent/BR112021016751B1/pt
Publication of BR112021016751B8 publication Critical patent/BR112021016751B8/pt

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    • 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
    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
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    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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    • 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
    • C07D487/10—Spiro-condensed systems
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    • 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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)

Abstract

compostos, composições farmacêuticas e usos dos compostos. a presente invenção se refere a uma classe de compostos inibidores de jak e seus usos. de forma específica, a presente invenção divulga um composto representado pela fórmula (g), composto marcado de forma isotópica do mesmo, ou um isômero ótico do mesmo, um isômero geométrico do mesmo, um tautômero do mesmo, ou uma mistura de vários isômeros ou um sal farmaceuticamente aceitável do mesmo, ou um pró-fármaco do mesmo, ou um metabólito do mesmo. a presente invenção também se refere à aplicação dos compostos na medicina.
BR112021016751A 2019-02-25 2020-02-21 Compostos, composições farmacêuticas e usos dos compostos BR112021016751B8 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201910137984 2019-02-25
CN201910137984.0 2019-02-25
CN201910877661 2019-09-17
CN201910877661.5 2019-09-17
PCT/CN2020/076231 WO2020173400A1 (zh) 2019-02-25 2020-02-21 Jak抑制剂化合物及其用途

Publications (3)

Publication Number Publication Date
BR112021016751A2 BR112021016751A2 (pt) 2021-10-19
BR112021016751B1 BR112021016751B1 (pt) 2023-11-07
BR112021016751B8 true BR112021016751B8 (pt) 2023-11-21

Family

ID=72205292

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021016751A BR112021016751B8 (pt) 2019-02-25 2020-02-21 Compostos, composições farmacêuticas e usos dos compostos

Country Status (14)

Country Link
US (2) US11629148B2 (pt)
EP (1) EP3932919A4 (pt)
JP (1) JP2022523274A (pt)
KR (1) KR20210132666A (pt)
CN (2) CN113563345A (pt)
AU (1) AU2020228799A1 (pt)
BR (1) BR112021016751B8 (pt)
CA (1) CA3131293A1 (pt)
CL (1) CL2021002244A1 (pt)
IL (1) IL285783A (pt)
MX (1) MX2021010242A (pt)
PE (1) PE20212069A1 (pt)
WO (1) WO2020173400A1 (pt)
ZA (1) ZA202106511B (pt)

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IL281150B2 (en) 2018-09-04 2024-03-01 Theravance Biopharma R& D Ip Llc Heterocyclic amides with 5 to 7 atoms as JAK inhibitors
KR20210056382A (ko) 2018-09-04 2021-05-18 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 억제제 및 이의 중간체를 제조하는 방법
EP3837258B1 (en) 2018-09-04 2024-04-24 Theravance Biopharma R&D IP, LLC Dimethyl amino azetidine amides as jak inhibitors
US10968222B2 (en) 2018-10-29 2021-04-06 Theravance Biopharma R&D Ip, Llc 2-azabicyclo hexane JAK inhibitor compound
CN114075199A (zh) * 2020-08-14 2022-02-22 河南迈英诺医药科技有限公司 Jak抑制剂化合物及其用途
CN114075200A (zh) * 2020-08-14 2022-02-22 河南迈英诺医药科技有限公司 用于治疗重症肺炎的jak抑制剂化合物
CN113563345A (zh) * 2019-02-25 2021-10-29 河南迈英诺医药科技有限公司 Jak抑制剂化合物及其用途
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
EP4261213A1 (en) * 2021-01-15 2023-10-18 Shenzhen Kangsu Pharmaceutical Technology Co., Ltd. Fgfr inhibitor compound and use thereof
WO2022178215A1 (en) 2021-02-19 2022-08-25 Theravance Biopharma R&D Ip, Llc Amino amide tetrahydro imidazo pyridines as jak inhibitors
WO2022268080A1 (zh) * 2021-06-21 2022-12-29 河南迈英诺医药科技有限公司 Trk激酶抑制剂化合物及其用途
CN117343063A (zh) * 2022-07-04 2024-01-05 河南迈英诺医药科技有限公司 作为trk抑制剂和/或ret抑制剂的化合物及其用途
CN117534686A (zh) * 2022-08-08 2024-02-09 河南迈英诺医药科技有限公司 TGF-β抑制剂化合物及其用途

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EP3932919A4 (en) 2022-12-14
ZA202106511B (en) 2022-08-31
AU2020228799A1 (en) 2021-10-07
CN111606908B (zh) 2021-08-24
EP3932919A1 (en) 2022-01-05
US20220073524A1 (en) 2022-03-10
CA3131293A1 (en) 2020-09-03
JP2022523274A (ja) 2022-04-21
WO2020173400A1 (zh) 2020-09-03
KR20210132666A (ko) 2021-11-04
CN113563345A (zh) 2021-10-29
CL2021002244A1 (es) 2022-03-18
US20230192711A1 (en) 2023-06-22
IL285783A (en) 2021-10-31
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