AP3513A - Crystalline tripeptide epoxy ketone protease inhibitors - Google Patents

Crystalline tripeptide epoxy ketone protease inhibitors

Info

Publication number
AP3513A
AP3513A AP2013007137A AP2013007137A AP3513A AP 3513 A AP3513 A AP 3513A AP 2013007137 A AP2013007137 A AP 2013007137A AP 2013007137 A AP2013007137 A AP 2013007137A AP 3513 A AP3513 A AP 3513A
Authority
AP
ARIPO
Prior art keywords
protease inhibitors
epoxy ketone
ketone protease
tripeptide epoxy
crystalline tripeptide
Prior art date
Application number
AP2013007137A
Other languages
English (en)
Other versions
AP2013007137A0 (en
Inventor
Pasit Phiasivongsa
Louis C Sehl
Original Assignee
Onyx Therapeutics Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42738216&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AP3513(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Onyx Therapeutics Inc filed Critical Onyx Therapeutics Inc
Publication of AP2013007137A0 publication Critical patent/AP2013007137A0/xx
Application granted granted Critical
Publication of AP3513A publication Critical patent/AP3513A/xx

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/02—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
    • C07K1/026—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution by fragment condensation in solution
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Analytical Chemistry (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
AP2013007137A 2009-03-20 2010-03-22 Crystalline tripeptide epoxy ketone protease inhibitors AP3513A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US16219609P 2009-03-20 2009-03-20
US18056109P 2009-05-22 2009-05-22
PCT/US2010/028126 WO2010108172A1 (en) 2009-03-20 2010-03-22 Crystalline tripeptide epoxy ketone protease inhibitors

Publications (2)

Publication Number Publication Date
AP2013007137A0 AP2013007137A0 (en) 2013-09-30
AP3513A true AP3513A (en) 2016-01-05

Family

ID=42738216

Family Applications (1)

Application Number Title Priority Date Filing Date
AP2013007137A AP3513A (en) 2009-03-20 2010-03-22 Crystalline tripeptide epoxy ketone protease inhibitors

Country Status (44)

Country Link
US (5) US8604215B2 (da)
EP (2) EP2408758B1 (da)
JP (1) JP5723357B2 (da)
KR (1) KR101729344B1 (da)
CN (1) CN102428075B (da)
AP (1) AP3513A (da)
AR (1) AR075899A1 (da)
AU (1) AU2010226410B2 (da)
BR (1) BRPI1009369A2 (da)
CA (1) CA2755971C (da)
CL (1) CL2011002326A1 (da)
CO (1) CO6430433A2 (da)
CR (1) CR20110491A (da)
CU (1) CU20110176A7 (da)
CY (1) CY1118359T1 (da)
DK (2) DK2408758T3 (da)
DO (1) DOP2011000286A (da)
EA (2) EA020973B1 (da)
EC (1) ECSP11011341A (da)
ES (2) ES2527619T3 (da)
GE (1) GEP20156392B (da)
HN (1) HN2011002459A (da)
HR (2) HRP20150014T1 (da)
HU (1) HUE032430T2 (da)
IL (1) IL215174A (da)
LT (1) LT2813241T (da)
MA (1) MA33197B1 (da)
ME (1) ME01277B (da)
MX (2) MX343562B (da)
MY (1) MY156522A (da)
NI (1) NI201100170A (da)
NZ (2) NZ595847A (da)
PE (1) PE20120645A1 (da)
PL (2) PL2813241T3 (da)
PT (2) PT2813241T (da)
RS (2) RS53746B1 (da)
SA (2) SA114350283B1 (da)
SG (2) SG174446A1 (da)
SI (2) SI2813241T1 (da)
SM (3) SMT201700068T1 (da)
TN (1) TN2011000470A1 (da)
TW (1) TWI504598B (da)
WO (1) WO2010108172A1 (da)
ZA (2) ZA201106826B (da)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5436860B2 (ja) * 2005-11-09 2014-03-05 オニキス セラピューティクス， インク． 酵素阻害のための化合物
NZ573759A (en) 2006-06-19 2012-03-30 Proteolix Inc Peptide epoxyketones for proteasome inhibition
EA018973B1 (ru) 2007-10-04 2013-12-30 Оникс Терапьютикс, Инк. Кристаллические пептидные кето-эпоксидные ингибиторы протеаз и синтез кето-эпоксидов аминокислот
BRPI0919668A2 (pt) 2008-10-21 2018-05-29 Onyx Therapeutics, Inc. terapia de combinação com epóxi-cetonas de peptídeo
AR075899A1 (es) 2009-03-20 2011-05-04 Onyx Therapeutics Inc Tripeptidos epoxicetonas cristalinos inhibidores de proteasa
HUE042624T2 (hu) 2009-10-07 2019-07-29 Dow Agrosciences Llc Szinergetikus fungicid keverékek gombák kontrollálására gabonafélékben
EP2498793B1 (en) 2009-11-13 2019-07-10 Onyx Therapeutics, Inc. Oprozomib for use in metastasis suppression
PH12012501719A1 (en) 2010-03-01 2012-11-12 Onyx Therapeutics Inc Compounds for immunoproteasome inhibition
US8697646B2 (en) 2010-04-07 2014-04-15 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
US9309283B2 (en) 2012-07-09 2016-04-12 Onyx Therapeutics, Inc. Prodrugs of peptide epoxy ketone protease inhibitors
MY169137A (en) * 2012-08-10 2019-02-18 Ajinomoto Kk Method for producing ?-gamma-glutamyl-valyl-glycine crystal
UY35091A (es) * 2012-10-24 2014-05-30 Onyx Therapeutics Inc Formulaciones de liberacion modificada para oprozomib
LT2938191T (lt) 2012-12-28 2018-05-10 Dow Agrosciences Llc Sinergistiniai fungicidiniai mišiniai, skirti grybelių kontrolei javuose
WO2015100184A1 (en) 2013-12-26 2015-07-02 Dow Agrosciences Llc Use of macrocyclic picolinamides as fungicides
CN104945470B (zh) * 2014-03-30 2020-08-11 浙江大学 杂环构建的三肽环氧酮类化合物及制备和应用
CN104974221B (zh) * 2014-04-03 2020-10-23 中国医学科学院药物研究所 二肽及三肽类蛋白酶体抑制剂及其制法和药物用途
EP3166936A4 (en) 2014-07-08 2017-11-22 Dow AgroSciences LLC Macrocyclic picolinamides as fungicides
WO2016069479A1 (en) 2014-10-27 2016-05-06 Apicore Us Llc Methods of making carfilzomib and intermediates thereof
US20170290333A1 (en) 2014-12-30 2017-10-12 Dow Agrosciences Llc Picolinamide compounds with fungicidal activity
EP3240412A4 (en) 2014-12-30 2018-04-25 Dow Agrosciences LLC Use of picolinamide compounds with fungicidal activity
CA2972408A1 (en) 2014-12-30 2016-07-07 Dow Agrosciences Llc Use of picolinamide compounds with fungicidal activity
NZ732812A (en) 2014-12-30 2019-01-25 Dow Agrosciences Llc Use of picolinamides and other compounds as fungicides
AU2015374375B2 (en) * 2014-12-30 2019-03-21 Dow Agrosciences Llc Picolinamides with fungicidal activity
CN105949279A (zh) * 2016-04-27 2016-09-21 浙江大学 蛋白酶体抑制剂Oprozomib及其类似物的制备方法
FI3478670T3 (fi) 2016-06-29 2023-05-04 Kezar Life Sciences Peptidi-epoksiketoni-immunoproteasomi-estäjän kiteiset suolat
IL263771B2 (en) 2016-06-29 2023-09-01 Kezar Life Sciences Preparation process of immunoproteasome epoxytone peptide inhibitor and its precursors
US10334852B2 (en) 2016-08-30 2019-07-02 Dow Agrosciences Llc Pyrido-1,3-oxazine-2,4-dione compounds with fungicidal activity
WO2018045003A1 (en) 2016-08-30 2018-03-08 Dow Agrosciences Llc Picolinamide n-oxide compounds with fungicidal activity
WO2018044987A1 (en) 2016-08-30 2018-03-08 Dow Agrosciences Llc Thiopicolinamide compounds with fungicidal activity
US10214490B2 (en) 2016-08-30 2019-02-26 Dow Agrosciences Llc Picolinamides as fungicides
US20180078532A1 (en) 2016-09-21 2018-03-22 Amgen Inc. Immediate release formulations for oprozomib
US20180161279A1 (en) 2016-12-14 2018-06-14 Amgen Inc. Gastro-retentive modified release dosage forms for oprozomib and process to make thereof
BR102018000183B1 (pt) 2017-01-05 2023-04-25 Dow Agrosciences Llc Picolinamidas, composição para controle de um patógeno fúngico, e método para controle e prevenção de um ataque por fungos em uma planta
TWI774761B (zh) 2017-05-02 2022-08-21 美商科迪華農業科技有限責任公司 用於穀物中的真菌防治之協同性混合物
CN110996665B (zh) 2017-05-02 2021-10-26 陶氏益农公司 无环吡啶酰胺化合物作为针对草坪草上的真菌病害的杀真菌剂的用途
TW201842851A (zh) 2017-05-02 2018-12-16 美商陶氏農業科學公司 用於穀類中的真菌防治之協同性混合物
JP2020533382A (ja) 2017-09-14 2020-11-19 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ 癌の組合せ治療
BR102019004480B1 (pt) 2018-03-08 2023-03-28 Dow Agrosciences Llc Picolinamidas como fungicidas
US11639334B2 (en) 2018-10-15 2023-05-02 Corteva Agriscience Llc Methods for synthesis of oxypicolinamides
EP4044811A4 (en) 2019-10-18 2023-09-27 Corteva Agriscience LLC METHOD FOR SYNTHESIS OF PICOLINAMIDS
TWI869142B (zh) * 2022-12-27 2025-01-01 大陸商上海美悦生物科技發展有限公司 三肽環氧酮化合物、藥物組合物及其製備方法和用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008140782A2 (en) * 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition

Family Cites Families (94)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4733665C2 (en) 1985-11-07 2002-01-29 Expandable Grafts Partnership Expandable intraluminal graft and method and apparatus for implanting an expandable intraluminal graft
US5135919A (en) 1988-01-19 1992-08-04 Children's Medical Center Corporation Method and a pharmaceutical composition for the inhibition of angiogenesis
US5441944A (en) 1989-04-23 1995-08-15 The Trustees Of The University Of Pennsylvania Substituted cyclodextrin sulfates and their uses as growth modulating agents
US5071957A (en) 1989-08-04 1991-12-10 Bristol-Myers Company Antibiotic BU-4061T
US4990448A (en) 1989-08-04 1991-02-05 Bristol-Myers Company Bu-4061T
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
HUT62312A (en) 1990-03-05 1993-04-28 Cephalon Inc Process for producing chymotrypsin-like proteases and their inhibitors
US5561134A (en) * 1990-09-25 1996-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
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
US5866114A (en) * 1992-06-09 1999-02-02 Chiron Corporation Crystallization of M-CSFα
GB9300048D0 (en) 1993-01-04 1993-03-03 Wellcome Found Endothelin converting enzyme inhibitors
TW380137B (en) 1994-03-04 2000-01-21 Merck & Co Inc Process for making an epoxide
US5693617A (en) 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
US6660268B1 (en) 1994-03-18 2003-12-09 The President And Fellows Of Harvard College Proteasome regulation of NF-KB activity
US6506876B1 (en) 1994-10-11 2003-01-14 G.D. Searle & Co. LTA4 hydrolase inhibitor pharmaceutical compositions and methods of use
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
DE19505263A1 (de) 1995-02-16 1996-08-22 Consortium Elektrochem Ind Verfahren zur Reinigung von wasserlöslichen Cyclodextrinderivaten
US6335358B1 (en) 1995-04-12 2002-01-01 President And Fellows Of Harvard College Lactacystin analogs
US6150415A (en) 1996-08-13 2000-11-21 The Regents Of The University Of California Epoxide hydrolase complexes and methods therewith
AU4499697A (en) 1996-09-13 1998-04-02 New York University Method for treating parasitic diseases with proteasome inhibitors
EP1136498A1 (en) 1996-10-18 2001-09-26 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus NS3 protease
CZ298749B6 (cs) 1996-10-18 2008-01-16 Vertex Pharmaceuticals Incorporated Inhibitory serinových proteáz a farmaceutické prostředky s jejich obsahem
US5874418A (en) 1997-05-05 1999-02-23 Cydex, Inc. Sulfoalkyl ether cyclodextrin based solid pharmaceutical formulations and their use
US6046177A (en) 1997-05-05 2000-04-04 Cydex, Inc. Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations
WO1998056422A1 (en) 1997-06-13 1998-12-17 The University Of Kansas Polar drug or prodrug compositions with extended shelf-life storage and a method of making thereof
US6133308A (en) 1997-08-15 2000-10-17 Millennium Pharmaceuticals, Inc. Synthesis of clasto-lactacystin beta-lactone and analogs thereof
US6100282A (en) * 1998-01-02 2000-08-08 Hoffman-La Roche Inc. Thiazole derivatives
US6075150A (en) 1998-01-26 2000-06-13 Cv Therapeutics, Inc. α-ketoamide inhibitors of 20S proteasome
US6099851A (en) 1998-06-02 2000-08-08 Weisman; Kenneth M. Therapeutic uses of leuprolide acetate
US6902721B1 (en) 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6204257B1 (en) 1998-08-07 2001-03-20 Universtiy Of Kansas Water soluble prodrugs of hindered alcohols
AU762373B2 (en) 1998-10-20 2003-06-26 Millennium Pharmaceuticals, Inc. Method for monitoring proteasome inhibitor drug action
US6492333B1 (en) 1999-04-09 2002-12-10 Osteoscreen, Inc. Treatment of myeloma bone disease with proteasomal and NF-κB activity inhibitors
US6831099B1 (en) * 1999-05-12 2004-12-14 Yale University Enzyme inhibition
US6114365A (en) * 1999-08-12 2000-09-05 Pharmacia & Upjohn S.P.A. Arylmethyl-carbonylamino-thiazole derivatives, process for their preparation, and their use as antitumor agents
EP1477180A1 (en) 1999-10-20 2004-11-17 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone and hair growth
US20040106539A1 (en) 2000-10-12 2004-06-03 Ulrich Schubert Agents for the treatment of viral infections
GB0114185D0 (en) * 2001-06-12 2001-08-01 Protherics Molecular Design Lt Compounds
PT3078667T (pt) 2001-01-25 2018-12-28 The United States Of America Represented By The Sec Dep Of Health And Human Services Formulação de compostos de ácido borónico
ATE353667T1 (de) 2001-05-21 2007-03-15 Alcon Inc Verwendung von proteasom-inhibitoren zur behandlung des trockenen auges
JP4412586B2 (ja) 2002-01-08 2010-02-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 エポネマイシンおよびエポキソマイシン類似物およびそれらの用途
US20040116329A1 (en) 2002-01-29 2004-06-17 Epstein Stephen E. Inhibition of proteasomes to prevent restenosis
EP1496916A2 (en) 2002-04-09 2005-01-19 Greenville Hospital System Metastasis modulating activity of highly sulfated oligosaccharides
US7968569B2 (en) 2002-05-17 2011-06-28 Celgene Corporation Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione
US7902185B2 (en) 2002-06-03 2011-03-08 Als Therapy Development Foundation, Inc. Treatment of neurodegenerative diseases using proteasome modulators
US20030224469A1 (en) 2002-06-03 2003-12-04 Buchholz Tonia J. Methods and kits for assays utilizing fluorescence polarization
US20040167139A1 (en) 2002-07-26 2004-08-26 Potter David A. Methods of treating cancer
US7189740B2 (en) 2002-10-15 2007-03-13 Celgene Corporation Methods of using 3-(4-amino-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myelodysplastic syndromes
TW200418791A (en) 2003-01-23 2004-10-01 Bristol Myers Squibb Co Pharmaceutical compositions for inhibiting proteasome
DE202004021680U1 (de) 2003-04-08 2010-04-22 Novartis Ag Feste pharmazeutische Zusammensetzung
AU2004255564A1 (en) 2003-06-10 2005-01-20 The J. David Gladstone Institutes Methods for treating lentivirus infections
US7012063B2 (en) 2003-06-13 2006-03-14 Children's Medical Center Corporation Reducing axon degeneration with proteasome inhibitors
BRPI0418276B8 (pt) 2003-12-31 2021-05-25 Cydex Pharmaceuticals Inc formulação líquida inalável compreeendendo budesonida
GB0400804D0 (en) 2004-01-14 2004-02-18 Innoscience Technology Bv Pharmaceutical compositions
US20050228031A1 (en) * 2004-04-13 2005-10-13 Bilodeau Mark T Tyrosine kinase inhibitors
US8198270B2 (en) * 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
US7232818B2 (en) 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
JP5616569B2 (ja) 2004-04-15 2014-10-29 オニキス セラピューティクス， インク．Ｏｎｙｘ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． 酵素阻害のための化合物
US20050256324A1 (en) 2004-05-10 2005-11-17 Proteolix, Inc. Synthesis of amino acid keto-epoxides
BRPI0510802A (pt) * 2004-05-10 2007-11-06 Proteolix Inc compostos para inibição de enzima
CN101044157B (zh) * 2004-08-06 2011-07-13 普罗特奥里克斯公司 用于抑制蛋白酶体的化合物
EP1805208A2 (en) 2004-10-20 2007-07-11 Proteolix, Inc. Labeled compounds for proteasome inhibition
CN101180071A (zh) 2004-12-07 2008-05-14 普罗特奥里克斯公司 抑制蛋白酶体的组合物
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
WO2006099261A2 (en) 2005-03-11 2006-09-21 The University Of North Carolina At Chapel Hill Potent and specific immunoproteasome inhibitors
WO2006113470A2 (en) 2005-04-15 2006-10-26 Geron Corporation Cancer treatment by combined inhibition of proteasome and telomerase activities
GT200600350A (es) 2005-08-09 2007-03-28 Formulaciones líquidas
JP5436860B2 (ja) 2005-11-09 2014-03-05 オニキス セラピューティクス， インク． 酵素阻害のための化合物
AR057227A1 (es) 2005-12-09 2007-11-21 Centocor Inc Metodo para usar antagonistas de il6 con inhibidores del proteasoma
US20070207950A1 (en) 2005-12-21 2007-09-06 Duke University Methods and compositions for regulating HDAC6 activity
WO2007122686A1 (ja) 2006-04-14 2007-11-01 Eisai R & D Management Co., Ltd. ベンズイミダゾール化合物
DE102006026464A1 (de) 2006-06-01 2007-12-06 Virologik Gmbh Innovationszentrum Medizintechnik Und Pharma Pharmazeutische Zusammensetzung zur Behandlung von Virusinfektionen und / oder Tumorerkrankungen durch Inhibition der Proteinfaltung und des Proteinabbaus
NZ573759A (en) 2006-06-19 2012-03-30 Proteolix Inc Peptide epoxyketones for proteasome inhibition
WO2008033807A2 (en) 2006-09-13 2008-03-20 The Arizona Board Of Regents On Behalf Of The University Of Arizona Synergistic combinations of antineoplastic thiol-binding mitochondrial oxidants and antineoplastic proteasome inhibitors for the treatment of cancer
US8601054B2 (en) * 2006-12-07 2013-12-03 International Business Machines Corporation Project-related communications
MX2009007777A (es) 2007-01-23 2009-12-16 Gloucester Pharmaceuticals Inc Terapia de combinacion que comprende romidepsina y bortezomib.
EP2178888B1 (en) 2007-08-06 2012-07-04 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
EA018973B1 (ru) 2007-10-04 2013-12-30 Оникс Терапьютикс, Инк. Кристаллические пептидные кето-эпоксидные ингибиторы протеаз и синтез кето-эпоксидов аминокислот
JP5600595B2 (ja) 2007-10-16 2014-10-01 ミレニアム ファーマシューティカルズ， インコーポレイテッド プロテアソーム阻害剤
US7838673B2 (en) 2007-10-16 2010-11-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
WO2009067453A1 (en) 2007-11-19 2009-05-28 Syndax Pharmaceuticals, Inc. Combinations of hdac inhibitors and proteasome inhibitors
HRP20150592T4 (hr) 2008-06-17 2025-02-14 Millennium Pharmaceuticals, Inc Organoborni esterski spojevi i njihove farmaceutske kompozicije
AR075090A1 (es) 2008-09-29 2011-03-09 Millennium Pharm Inc Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.
BRPI0919668A2 (pt) 2008-10-21 2018-05-29 Onyx Therapeutics, Inc. terapia de combinação com epóxi-cetonas de peptídeo
AR075899A1 (es) 2009-03-20 2011-05-04 Onyx Therapeutics Inc Tripeptidos epoxicetonas cristalinos inhibidores de proteasa
CN101928329B (zh) 2009-06-19 2013-07-17 北京大学 三肽硼酸(酯)类化合物、其制备方法和应用
EP2498793B1 (en) 2009-11-13 2019-07-10 Onyx Therapeutics, Inc. Oprozomib for use in metastasis suppression
PH12012501719A1 (en) 2010-03-01 2012-11-12 Onyx Therapeutics Inc Compounds for immunoproteasome inhibition
JP5933523B2 (ja) 2010-03-31 2016-06-08 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． １−アミノ−２−シクロプロピルエチルボロン酸の誘導体
US8697646B2 (en) 2010-04-07 2014-04-15 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008140782A2 (en) * 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
GROLL M. et al. "Crystal Structure of Epoxomicin:20S Proteasome Reveals a Molecular Basis for Selectivity of alpha',beta'-Epoxyketone Proteasome Inhibitors", J. Am. Chem. Soc., 2000, 122, 1237-1238. See whole document; figures 1&2 *

Also Published As

Publication number Publication date
GEP20156392B (en) 2015-11-10
US9403868B2 (en) 2016-08-02
DK2813241T3 (da) 2017-01-16
HN2011002459A (es) 2015-03-16
MX2011009777A (es) 2011-10-17
SMT201700068T1 (it) 2017-03-08
RS55431B1 (sr) 2017-04-28
US20140024804A1 (en) 2014-01-23
ZA201106826B (en) 2018-11-28
CU20110176A7 (es) 2012-04-15
TW201043623A (en) 2010-12-16
HRP20150014T1 (hr) 2015-02-27
US8604215B2 (en) 2013-12-10
HK1204952A1 (en) 2015-12-11
CN102428075B (zh) 2016-05-11
AR075899A1 (es) 2011-05-04
AU2010226410A1 (en) 2011-11-03
KR20110132577A (ko) 2011-12-08
SA114350283B1 (ar) 2016-06-08
PL2408758T3 (pl) 2015-03-31
PE20120645A1 (es) 2012-06-07
NI201100170A (es) 2012-02-21
EA024672B1 (ru) 2016-10-31
US20120088903A1 (en) 2012-04-12
IL215174A (en) 2016-03-31
EP2408758B1 (en) 2014-10-22
ME01277B (me) 2010-03-22
SG2014011373A (en) 2014-05-29
ZA201601686B (en) 2016-11-30
ES2614557T3 (es) 2017-05-31
CA2755971C (en) 2017-05-16
US8822512B2 (en) 2014-09-02
LT2813241T (lt) 2017-01-10
CL2011002326A1 (es) 2012-03-23
CA2755971A1 (en) 2010-09-23
AP2013007137A0 (en) 2013-09-30
NZ595847A (en) 2013-12-20
CO6430433A2 (es) 2012-04-30
MY156522A (en) 2016-02-26
JP5723357B2 (ja) 2015-05-27
CY1118359T1 (el) 2017-06-28
US20150175656A1 (en) 2015-06-25
EP2813241B1 (en) 2016-11-16
EP2813241A1 (en) 2014-12-17
WO2010108172A1 (en) 2010-09-23
SI2813241T1 (sl) 2017-03-31
SI2408758T1 (sl) 2015-01-30
CR20110491A (es) 2012-01-19
CN102428075A (zh) 2012-04-25
EA020973B1 (ru) 2015-03-31
PT2408758E (pt) 2014-11-04
EP2408758A1 (en) 2012-01-25
TWI504598B (zh) 2015-10-21
MA33197B1 (fr) 2012-04-02
JP2012521363A (ja) 2012-09-13
NZ618432A (en) 2015-04-24
EA201300860A1 (ru) 2014-04-30
ES2527619T3 (es) 2015-01-27
BRPI1009369A2 (pt) 2016-10-11
IL215174A0 (en) 2011-12-29
US20120077855A1 (en) 2012-03-29
HK1162476A1 (en) 2012-08-31
KR101729344B1 (ko) 2017-04-21
ECSP11011341A (es) 2011-10-31
SG174446A1 (en) 2011-10-28
SMT201700068B (it) 2017-03-08
EA201171151A1 (ru) 2012-04-30
SMT201500009B (it) 2015-03-05
AU2010226410B2 (en) 2015-09-17
RS53746B1 (sr) 2015-06-30
PL2813241T3 (pl) 2017-04-28
PT2813241T (pt) 2016-12-23
HUE032430T2 (en) 2017-09-28
TN2011000470A1 (en) 2013-03-27
HRP20161654T1 (hr) 2017-01-27
MX343562B (es) 2016-11-09
SA110310221B1 (ar) 2014-04-28
DK2408758T3 (da) 2014-12-01
US9051353B2 (en) 2015-06-09
DOP2011000286A (es) 2011-10-15
EP2408758A4 (en) 2012-09-05
US20100240903A1 (en) 2010-09-23

Similar Documents

Publication Publication Date Title
ZA201601686B (en) Crystalline tripeptide epoxy ketone protease inhibitors
ZA201202631B (en) Hcv protease inhibitors
ZA201008988B (en) Hcv protease inhibitors
IL215506A0 (en) Protease inhibitors
IL222330A0 (en) Crystalline peptide epoxyketone immunoproteasome inhibitor
EP2509956A4 (en) INHIBITORS OF CYSTEINE PROTEASES
EP2313426A4 (en) NEW PROTEASE INHIBITORS
IL215161A0 (en) 5-alkynyl-pyridines
ZA201102179B (en) Protease inhibitors
ZA201200811B (en) Cathepsin c inhibitors
AP2912A (en) Crystalline tripeptide epoxy protease inhibitors
GB0817425D0 (en) Protease inhibitors
SG2014011258A (en) Hcv protease inhibitors
AU2009902963A0 (en) Novel protease inhibitors
HK1175945A (en) Crystalline peptide epoxyketone immunoproteasome inhibitor
TWM379488U (en) Improved screwdriver stem
GB0915927D0 (en) Novel inhibitors
GB0903650D0 (en) Glyoalase inhibitors
GB0902661D0 (en) Inhibitors
GB0914739D0 (en) Enzyme inhibition