BR112021020637A2 - Derivados de tetra-hidro-1h-ciclopenta[cd]indeno como inibidores de fator -2(alfa) induzível por hipóxia - Google Patents

Derivados de tetra-hidro-1h-ciclopenta[cd]indeno como inibidores de fator -2(alfa) induzível por hipóxia

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Publication number
BR112021020637A2
BR112021020637A2 BR112021020637A BR112021020637A BR112021020637A2 BR 112021020637 A2 BR112021020637 A2 BR 112021020637A2 BR 112021020637 A BR112021020637 A BR 112021020637A BR 112021020637 A BR112021020637 A BR 112021020637A BR 112021020637 A2 BR112021020637 A2 BR 112021020637A2
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Brazil
Prior art keywords
hypoxia
inhibitors
tetrahydro
inducible factor
cyclopenta
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Application number
BR112021020637A
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English (en)
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Jiping Fu
Yan Lou
Yigang He
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Nikang Therapeutics Inc
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Publication date
Application filed by Nikang Therapeutics Inc filed Critical Nikang Therapeutics Inc
Publication of BR112021020637A2 publication Critical patent/BR112021020637A2/pt

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/65—One oxygen atom attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/50—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • 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
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/54—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C313/00—Sulfinic acids; Sulfenic acids; Halides, esters or anhydrides thereof; Amides of sulfinic or sulfenic acids, i.e. compounds having singly-bound oxygen atoms of sulfinic or sulfenic groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C313/02—Sulfinic acids; Derivatives thereof
    • C07C313/06—Sulfinamides
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    • C07—ORGANIC CHEMISTRY
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/60—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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    • C07B2200/05—Isotopically modified compounds, e.g. labelled
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    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/93—Spiro compounds
    • C07C2603/95—Spiro compounds containing "not free" spiro atoms
    • C07C2603/96—Spiro compounds containing "not free" spiro atoms containing at least one ring with less than six members
    • C07C2603/97—Spiro compounds containing "not free" spiro atoms containing at least one ring with less than six members containing five-membered rings

Abstract

derivados de tetra-hidro-1hciclopenta[cd]indeno como inibidores de fator-2(alfa) induzível por hipóxia. a presente invenção refere-se a certos compostos de tetra-hidro-1h-ciclopenta[cd]indeno que são inibidores de fator 2a induzível por hipóxia (hif-2a) e são, portanto, úteis para o tratamento de doenças tratáveis por inibição de hif-2a. também são fornecidas composições farmacêuticas contendo tais compostos e processos para preparar tais compostos.
BR112021020637A 2019-04-18 2020-04-16 Derivados de tetra-hidro-1h-ciclopenta[cd]indeno como inibidores de fator -2(alfa) induzível por hipóxia BR112021020637A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962836019P 2019-04-18 2019-04-18
US201962946191P 2019-12-10 2019-12-10
PCT/US2020/028579 WO2020214853A1 (en) 2019-04-18 2020-04-16 Tetrahydro-1h-cyclopenta[cd]indene derivatives as hypoxia inducible factor-2(alpha) inhibitors

Publications (1)

Publication Number Publication Date
BR112021020637A2 true BR112021020637A2 (pt) 2022-02-15

Family

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BR112021020637A BR112021020637A2 (pt) 2019-04-18 2020-04-16 Derivados de tetra-hidro-1h-ciclopenta[cd]indeno como inibidores de fator -2(alfa) induzível por hipóxia

Country Status (13)

Country Link
US (5) US20200361855A1 (pt)
EP (1) EP3956299A1 (pt)
JP (1) JP2022529166A (pt)
KR (1) KR20210154191A (pt)
CN (1) CN113874350A (pt)
AU (1) AU2020260130A1 (pt)
BR (1) BR112021020637A2 (pt)
CA (1) CA3136650A1 (pt)
IL (1) IL287258A (pt)
MX (1) MX2021012549A (pt)
SG (1) SG11202111118YA (pt)
TW (1) TW202104174A (pt)
WO (1) WO2020214853A1 (pt)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20200361855A1 (en) 2019-04-18 2020-11-19 Nikang Therapeutics, Inc. Tetrahydro-1h-cyclopenta[cd]indene derivatives as hypoxia inducible factor-2(alpha) inhibitors
WO2021016280A1 (en) * 2019-07-22 2021-01-28 Nikang Therapeutics, Inc. Tricyclic derivatives as hypoxia inducible factor-2(alpha) inhibitors
BR112022018600A2 (pt) 2020-03-19 2022-11-08 Arcus Biosciences Inc Compostos, composição farmacêutica, método de tratamento de uma doença e combinação
AU2021256998A1 (en) * 2020-04-16 2022-10-20 Nikang Therapeutics, Inc. Hypoxia Inducible Factor-2(alpha) inhibitors and their use in the treatment of diseases
US11420936B2 (en) 2020-04-16 2022-08-23 Nikang Therapeutics, Inc. Hypoxia inducible factor-2(alpha) inhibitors and their use in the treatment of diseases
CN114315552A (zh) * 2020-09-30 2022-04-12 江西济民可信集团有限公司 三并环类化合物及其制备方法和应用
WO2022082329A1 (en) 2020-10-19 2022-04-28 Nikang Therapeutics, Inc. Processes of preparing 3-fluoro-5- ( ( (1s, 2ar) -1, 3, 3, 4, 4-pentafluoro-2a-hydroxy-2, 2a, 3, 4-tetrahydro-1h-cyclopenta [cd] inden-7-yl) oxy) -benzonitrile
WO2022082337A1 (en) * 2020-10-19 2022-04-28 Nikang Therapeutics, Inc. Process of preparing 3-fluoro-5 ( ( (1r, 2ar) -3, 3, 4, 4-tetrafluoro-1, 2a-dihydroxy-2, 2a, 3, 4-tetrahydro-1h-cyclopenta [cd] inden-7-yl) oxy) benzonitrile
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EP4299570A1 (en) * 2021-02-23 2024-01-03 Shanghai Jemincare Pharmaceuticals Co., Ltd. Tricyclic compound as hif2a inhibitor, preparation method therefor and application thereof
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WO2023060431A1 (en) * 2021-10-12 2023-04-20 Nikang Therapeutics, Inc. Processes of making 3-fluoro-5- ( ( (1s, 2ar) -1, 3, 3, 4, 4-pentafluoro-2a-hydroxy-2, 2a, 3, 4-tetrahydro-1h-cyclopenta [cd] inden-7-yl) oxy) -benzonitrile and polymorphs thereof
CA3235013A1 (en) * 2021-10-18 2023-04-27 Jing Lu Hypoxia inducible factor-2(alpha) inhibitors for the treatment of bladder cancer
WO2023070483A1 (en) 2021-10-29 2023-05-04 Nikang Therapeutics, Inc. PROCESSES OF MAKING 3-FLUORO-5- ( ( (1R, 2S, 2aS) -1, 2, 3, 3, 4, 4-HEXAFLUORO-2A-HYDROXY-2, 2A, 3, 4-TETRAHYDRO-1H-CYCLOPENTA [CD] INDEN-7-YL) -OXY) -BENZONITRILE AND POLYMORPHS THEREOF

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SG11202111118YA (en) 2021-11-29
CN113874350A (zh) 2021-12-31
MX2021012549A (es) 2022-01-18
US20220162158A1 (en) 2022-05-26
TW202104174A (zh) 2021-02-01
AU2020260130A1 (en) 2021-11-04
US20230373909A1 (en) 2023-11-23
US20210347729A1 (en) 2021-11-11
US11753366B2 (en) 2023-09-12
EP3956299A1 (en) 2022-02-23
US11267782B2 (en) 2022-03-08
US20200361855A1 (en) 2020-11-19
WO2020214853A1 (en) 2020-10-22
CA3136650A1 (en) 2020-10-22
KR20210154191A (ko) 2021-12-20
IL287258A (en) 2021-12-01
JP2022529166A (ja) 2022-06-17
US20210246102A1 (en) 2021-08-12

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