CN114641289A - 补体成分C5a受体的游离碱晶型 - Google Patents

补体成分C5a受体的游离碱晶型 Download PDF

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Publication number
CN114641289A
CN114641289A CN202080077446.8A CN202080077446A CN114641289A CN 114641289 A CN114641289 A CN 114641289A CN 202080077446 A CN202080077446 A CN 202080077446A CN 114641289 A CN114641289 A CN 114641289A
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China
Prior art keywords
disease
free base
crystalline form
compound
disorder
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Pending
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CN202080077446.8A
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English (en)
Chinese (zh)
Inventor
R·辛格
邱国
曾一斌
张朋烈
R·M·路易
A·卡拉辛斯基
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Chemocentryx Inc
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Chemocentryx Inc
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Publication of CN114641289A publication Critical patent/CN114641289A/zh
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    • 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
    • C07D211/36—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 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)
  • Materials For Medical Uses (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN202080077446.8A 2019-11-08 2020-11-06 补体成分C5a受体的游离碱晶型 Pending CN114641289A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962932652P 2019-11-08 2019-11-08
US62/932,652 2019-11-08
PCT/US2020/059287 WO2021092292A1 (en) 2019-11-08 2020-11-06 FREE BASE CRYSTALLINE FORM OF A COMPLEMENT COMPONENT C5a RECEPTOR

Publications (1)

Publication Number Publication Date
CN114641289A true CN114641289A (zh) 2022-06-17

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ID=75846182

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080077446.8A Pending CN114641289A (zh) 2019-11-08 2020-11-06 补体成分C5a受体的游离碱晶型

Country Status (13)

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US (3) US11026935B2 (https=)
EP (1) EP4054577A4 (https=)
JP (1) JP2022554019A (https=)
KR (1) KR20220098179A (https=)
CN (1) CN114641289A (https=)
AU (1) AU2020378061A1 (https=)
BR (1) BR112022007488A2 (https=)
CA (1) CA3155596A1 (https=)
CL (1) CL2022001173A1 (https=)
IL (1) IL292317A (https=)
MX (1) MX2022005403A (https=)
WO (1) WO2021092292A1 (https=)
ZA (1) ZA202305622B (https=)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114867473A (zh) 2019-11-08 2022-08-05 凯莫森特里克斯股份有限公司 补体成分c5a受体的盐形式
US11603356B2 (en) 2019-11-08 2023-03-14 Chemocentryx, Inc. Amorphous form of a complement component C5a receptor
JP2022554019A (ja) * 2019-11-08 2022-12-27 ケモセントリックス，インコーポレイティド 補体成分Ｃ５ａ受容体の遊離塩基結晶形態
WO2022078269A1 (zh) * 2020-10-16 2022-04-21 苏州科睿思制药有限公司 Avacopan的晶型及其制备方法和用途
JP7839157B2 (ja) * 2020-10-28 2026-04-01 ケモセントリックス， インコーポレイテッド 化膿性汗腺炎を処置する方法
EP4137133A1 (en) 2021-08-19 2023-02-22 Sandoz AG Crystalline form of avacopan
WO2022263263A1 (en) 2021-06-16 2022-12-22 Sandoz Ag Crystalline form of avacopan
US20260027049A1 (en) 2024-07-23 2026-01-29 Amgen Inc. Avacopan formulations

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102264227A (zh) * 2008-12-22 2011-11-30 凯莫森特里克斯股份有限公司 C5aR拮抗剂
CN103068385A (zh) * 2010-06-24 2013-04-24 凯莫森特里克斯股份有限公司 C5aR拮抗剂
CN106999481A (zh) * 2014-09-29 2017-08-01 凯莫森特里克斯股份有限公司 制备C5aR拮抗剂的方法和中间体

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4996467B2 (ja) * 2004-09-27 2012-08-08 アカディア ファーマシューティカルズ インコーポレイテッド Ｎ−（４−フルオロベンジル）−ｎ−（１−メチルピペリジン−４−イル）−ｎ’−（４−（２−メチルプロピルオキシ）フェニルメチル）カルバミド、並びにその酒石酸塩及び結晶形態の合成
US20110275639A1 (en) 2008-12-22 2011-11-10 Chemocentryx, Inc. C5aR ANTAGONISTS
CN114867473A (zh) * 2019-11-08 2022-08-05 凯莫森特里克斯股份有限公司 补体成分c5a受体的盐形式
JP2022554019A (ja) * 2019-11-08 2022-12-27 ケモセントリックス，インコーポレイティド 補体成分Ｃ５ａ受容体の遊離塩基結晶形態
WO2022078269A1 (zh) * 2020-10-16 2022-04-21 苏州科睿思制药有限公司 Avacopan的晶型及其制备方法和用途

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102264227A (zh) * 2008-12-22 2011-11-30 凯莫森特里克斯股份有限公司 C5aR拮抗剂
CN103068385A (zh) * 2010-06-24 2013-04-24 凯莫森特里克斯股份有限公司 C5aR拮抗剂
CN106999481A (zh) * 2014-09-29 2017-08-01 凯莫森特里克斯股份有限公司 制备C5aR拮抗剂的方法和中间体

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
LIU H，等: "Orthosteric and allosteric action of the C5a receptor antagonists", NAT STRUCT MOL BIOL, vol. 25, no. 6, 4 June 2018 (2018-06-04), pages 472 - 481, XP036518029, DOI: 10.1038/s41594-018-0067-z *

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Publication number Publication date
WO2021092292A1 (en) 2021-05-14
US20210137907A1 (en) 2021-05-13
BR112022007488A2 (pt) 2022-07-12
EP4054577A1 (en) 2022-09-14
AU2020378061A1 (en) 2022-05-26
US20230381167A1 (en) 2023-11-30
JP2022554019A (ja) 2022-12-27
IL292317A (en) 2022-06-01
US11026935B2 (en) 2021-06-08
CL2022001173A1 (es) 2023-02-10
EP4054577A4 (en) 2023-11-29
MX2022005403A (es) 2022-05-24
US20220096453A1 (en) 2022-03-31
ZA202305622B (en) 2024-01-31
KR20220098179A (ko) 2022-07-11
CA3155596A1 (en) 2021-05-14

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Application publication date: 20220617