CN114641288A - 补体成分C5a受体的无定形形式 - Google Patents

补体成分C5a受体的无定形形式 Download PDF

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Publication number
CN114641288A
CN114641288A CN202080077440.0A CN202080077440A CN114641288A CN 114641288 A CN114641288 A CN 114641288A CN 202080077440 A CN202080077440 A CN 202080077440A CN 114641288 A CN114641288 A CN 114641288A
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CN
China
Prior art keywords
compound
amorphous form
disease
disorder
solution
Prior art date
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Pending
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CN202080077440.0A
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English (en)
Chinese (zh)
Inventor
邱国
梁强发
R·辛格
曾一斌
张朋烈
M·R·乐乐缇
R·M·路易
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Chemocentryx Inc
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Chemocentryx Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=75846408&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN114641288(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Chemocentryx Inc filed Critical Chemocentryx Inc
Publication of CN114641288A publication Critical patent/CN114641288A/zh
Pending legal-status Critical Current

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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
    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/10—Dispersions; Emulsions
    • 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)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Dispersion Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Materials For Medical Uses (AREA)
  • Secondary Cells (AREA)
  • Soft Magnetic Materials (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN202080077440.0A 2019-11-08 2020-11-06 补体成分C5a受体的无定形形式 Pending CN114641288A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962932644P 2019-11-08 2019-11-08
US62/932,644 2019-11-08
PCT/US2020/059280 WO2021092286A1 (en) 2019-11-08 2020-11-06 Amorphous form of a complement component c5a receptor

Publications (1)

Publication Number Publication Date
CN114641288A true CN114641288A (zh) 2022-06-17

Family

ID=75846408

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080077440.0A Pending CN114641288A (zh) 2019-11-08 2020-11-06 补体成分C5a受体的无定形形式

Country Status (13)

Country Link
US (1) US11603356B2 (https=)
EP (1) EP4054576A4 (https=)
JP (2) JP2023501789A (https=)
KR (1) KR20220098754A (https=)
CN (1) CN114641288A (https=)
AU (1) AU2020378397A1 (https=)
BR (1) BR112022007489A2 (https=)
CA (1) CA3155542A1 (https=)
CL (1) CL2022001172A1 (https=)
IL (1) IL292383A (https=)
MX (1) MX2022005406A (https=)
WO (1) WO2021092286A1 (https=)
ZA (1) ZA202305624B (https=)

Families Citing this family (7)

* 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
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
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
US20250333381A1 (en) 2024-04-26 2025-10-30 Amgen Inc. Solid state forms
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 (10)

* 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
CA3078732A1 (en) 2017-10-31 2019-05-09 Chemocentryx, Inc. C5ar inhibitor reduction of urinary scd163
US11191756B2 (en) 2018-06-07 2021-12-07 Chemocentryx, Inc. Dosing and effect of C5a antagonist with ANCA-associated vasculitis
WO2020112961A1 (en) 2018-11-30 2020-06-04 Chemocentryx, Inc. Capsule formulations
IL312955B1 (en) 2019-03-11 2026-01-01 Inflarx Gmbh Fused piperidinyl bicyclic compounds and related compounds as C5a receptor modulators
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

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 (2)

* Cited by examiner, † Cited by third party
Title
ALLEGRETTI M，等: "Allosteric Modulation of Chemoattractant Receptors", FRONT IMMUNOL, vol. 7, 2 May 2016 (2016-05-02), pages 170 *
VRANIĆ E: "Amorphous pharmaceutical solids", BOSN J BASIC MED SCI, vol. 4, no. 3, 31 July 2004 (2004-07-31), pages 35 - 39 *

Also Published As

Publication number Publication date
TW202128622A (zh) 2021-08-01
US20210139426A1 (en) 2021-05-13
US11603356B2 (en) 2023-03-14
ZA202305624B (en) 2023-12-20
BR112022007489A2 (pt) 2022-07-12
CL2022001172A1 (es) 2023-02-17
KR20220098754A (ko) 2022-07-12
MX2022005406A (es) 2022-05-24
WO2021092286A1 (en) 2021-05-14
JP2023501789A (ja) 2023-01-19
EP4054576A4 (en) 2023-12-13
JP2026016449A (ja) 2026-02-03
AU2020378397A1 (en) 2022-06-23
EP4054576A1 (en) 2022-09-14
IL292383A (en) 2022-06-01
CA3155542A1 (en) 2021-05-14

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