BR112018077390A2 - sais cristalinos de peptídeo epoxicentona inibidor de imunoproteassoma - Google Patents

sais cristalinos de peptídeo epoxicentona inibidor de imunoproteassoma

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Publication number
BR112018077390A2
BR112018077390A2 BR112018077390-5A BR112018077390A BR112018077390A2 BR 112018077390 A2 BR112018077390 A2 BR 112018077390A2 BR 112018077390 A BR112018077390 A BR 112018077390A BR 112018077390 A2 BR112018077390 A2 BR 112018077390A2
Authority
BR
Brazil
Prior art keywords
peptide
epoxicentone
crystalline salts
immunoproteasome inhibitor
immunoproteasome
Prior art date
Application number
BR112018077390-5A
Other languages
English (en)
Inventor
Johnson Henry
Lewis Evan
Dalziel Sean
Mcminn Dustin
Original Assignee
Kezar Life Sciences
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Kezar Life Sciences filed Critical Kezar Life Sciences
Publication of BR112018077390A2 publication Critical patent/BR112018077390A2/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D303/00Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02Compounds containing oxirane rings
    • C07D303/12Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/32Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/336Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

trata-se de um peptídeo epoxicetona inibidor de imunoproteassoma que tem uma estrutura: fórmula (i) em que x- é um contraíon, formas de cristal, sais e processos para fabricar os mesmos, e formulações dos mesmos.
BR112018077390-5A 2016-06-29 2017-06-29 sais cristalinos de peptídeo epoxicentona inibidor de imunoproteassoma BR112018077390A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662356287P 2016-06-29 2016-06-29
US62/356,287 2016-06-29
PCT/US2017/039961 WO2018005772A1 (en) 2016-06-29 2017-06-29 Crystalline salts of peptide epoxyketone immunoproteasome inhibitor

Publications (1)

Publication Number Publication Date
BR112018077390A2 true BR112018077390A2 (pt) 2019-04-09

Family

ID=59351084

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018077390-5A BR112018077390A2 (pt) 2016-06-29 2017-06-29 sais cristalinos de peptídeo epoxicentona inibidor de imunoproteassoma

Country Status (25)

Country Link
US (3) US10836756B2 (pt)
EP (1) EP3478670B1 (pt)
JP (2) JP7132855B2 (pt)
KR (2) KR102655020B1 (pt)
CN (1) CN109863141B (pt)
AU (1) AU2017290139B2 (pt)
BR (1) BR112018077390A2 (pt)
CA (1) CA3029032A1 (pt)
CL (1) CL2018003872A1 (pt)
DK (1) DK3478670T3 (pt)
EA (1) EA201990154A1 (pt)
ES (1) ES2944958T3 (pt)
FI (1) FI3478670T3 (pt)
HR (1) HRP20230533T1 (pt)
HU (1) HUE062106T2 (pt)
IL (1) IL263738B2 (pt)
LT (1) LT3478670T (pt)
MX (1) MX2018016387A (pt)
PL (1) PL3478670T3 (pt)
PT (1) PT3478670T (pt)
RS (1) RS64286B1 (pt)
SG (1) SG11201811507YA (pt)
SI (1) SI3478670T1 (pt)
TW (1) TWI751178B (pt)
WO (1) WO2018005772A1 (pt)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10071079B2 (en) 2016-06-29 2018-09-11 Bristol-Myers Squibb Company [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds
AU2019355041A1 (en) * 2018-10-04 2021-04-15 Kezar Life Sciences Immunoproteasome inhibitor formulation

Family Cites Families (23)

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Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5340736A (en) 1991-05-13 1994-08-23 The President & Fellows Of Harvard College ATP-dependent protease and use of inhibitors for same in the treatment of cachexia and muscle wasting
WO1998010779A1 (en) 1996-09-13 1998-03-19 New York University Method for treating parasitic diseases with proteasome inhibitors
ES2421516T3 (es) 2002-11-06 2013-09-03 Dana Farber Cancer Inst Inc Composiciones para tratar el cáncer usando el inhibidor de proteasomas PS-341
PL2623113T3 (pl) 2005-11-09 2018-05-30 Onyx Therapeutics, Inc. Związek do hamowania enzymu
EP2484688B1 (en) 2006-06-19 2016-06-08 Onyx Therapeutics, Inc. Peptide epoxyketones for proteasome inhibition
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US8367617B2 (en) 2007-10-04 2013-02-05 Onyx Therapeutics, Inc. Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides
CN101525370A (zh) 2008-03-06 2009-09-09 海南建邦制药科技有限公司 一种新型高效多肽合成缩合剂
EP3090737A1 (en) 2008-10-21 2016-11-09 Onyx Therapeutics, Inc. Combination therapy with peptide epoxyketones
AR075899A1 (es) 2009-03-20 2011-05-04 Onyx Therapeutics Inc Tripeptidos epoxicetonas cristalinos inhibidores de proteasa
US8853147B2 (en) 2009-11-13 2014-10-07 Onyx Therapeutics, Inc. Use of peptide epoxyketones for metastasis suppression
EP2555621A4 (en) 2010-04-07 2014-07-02 Onyx Therapeutics Inc CRYSTALLINE EPOXYCETONE PEPTIDE IMMUNOPROTEASOME INHIBITOR
US8609610B2 (en) 2011-02-18 2013-12-17 Trustees Of Dartmouth College Inhibitors of the trypsin-like site of the proteasome and methods of use thereof
JP2014513123A (ja) 2011-05-02 2014-05-29 ギリアード サイエンシーズ, インコーポレイテッド 無定形固体の塩
KR20190137963A (ko) 2012-05-08 2019-12-11 오닉스 세라퓨틱스, 인크. 펩티드 프로테아좀 억제제 제제화를 위한 사이클로덱스트린 복합체화 방법
US9187442B2 (en) 2012-06-29 2015-11-17 Nissan Chemical Industies, Ltd. Method for producing stereoselective epoxyketone compound
KR20150065885A (ko) 2012-10-11 2015-06-15 에프. 호프만-라 로슈 아게 케토아마이드 이뮤노프로테아좀 억제제
CA2892370A1 (en) 2012-10-12 2014-04-17 F. Hoffmann-La Roche Ag Macrocyclic ketoamide immunoproteasome inhibitors
AU2014240122B2 (en) 2013-03-14 2019-02-14 Onyx Therapeutics, Inc. Dipeptide and tripeptide epoxy ketone protease inhibitors
AR095426A1 (es) * 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
KR102365509B1 (ko) * 2013-03-14 2022-02-21 오닉스 세라퓨틱스, 인크. 트리펩타이드 에폭시 케톤 프로테이스 억제제
CN104710507B (zh) 2013-12-11 2018-08-14 深圳翰宇药业股份有限公司 一种卡非佐米的制备方法

Also Published As

Publication number Publication date
JP2022106971A (ja) 2022-07-20
FI3478670T3 (fi) 2023-05-04
US20210032232A1 (en) 2021-02-04
AU2017290139B2 (en) 2021-09-16
PL3478670T3 (pl) 2023-07-24
TWI751178B (zh) 2022-01-01
US20190308961A1 (en) 2019-10-10
HUE062106T2 (hu) 2023-09-28
IL263738A (en) 2019-01-31
IL263738B1 (en) 2023-05-01
CL2018003872A1 (es) 2019-07-19
SG11201811507YA (en) 2019-01-30
DK3478670T3 (da) 2023-05-15
SI3478670T1 (sl) 2023-06-30
TW201800398A (zh) 2018-01-01
MX2018016387A (es) 2019-09-09
EP3478670A1 (en) 2019-05-08
LT3478670T (lt) 2023-05-25
PT3478670T (pt) 2023-05-24
IL263738B2 (en) 2023-09-01
HRP20230533T1 (hr) 2023-08-04
KR20240046315A (ko) 2024-04-08
EP3478670B1 (en) 2023-04-05
US11891383B2 (en) 2024-02-06
RS64286B1 (sr) 2023-07-31
US20230106656A1 (en) 2023-04-06
CN109863141A (zh) 2019-06-07
US11479548B2 (en) 2022-10-25
KR20190026797A (ko) 2019-03-13
CA3029032A1 (en) 2018-01-04
JP7132855B2 (ja) 2022-09-07
JP2019527205A (ja) 2019-09-26
ES2944958T3 (es) 2023-06-27
KR102655020B1 (ko) 2024-04-04
AU2017290139A1 (en) 2019-01-17
CN109863141B (zh) 2023-09-15
EA201990154A1 (ru) 2019-06-28
WO2018005772A1 (en) 2018-01-04
US10836756B2 (en) 2020-11-17

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