DK2207791T4 - Krystallinske peptidepoxyketon-proteasehæmmere og syntese af aminosyreketoepoxider - Google Patents

Krystallinske peptidepoxyketon-proteasehæmmere og syntese af aminosyreketoepoxider Download PDF

Info

Publication number
DK2207791T4
DK2207791T4 DK08834964.2T DK08834964T DK2207791T4 DK 2207791 T4 DK2207791 T4 DK 2207791T4 DK 08834964 T DK08834964 T DK 08834964T DK 2207791 T4 DK2207791 T4 DK 2207791T4
Authority
DK
Denmark
Prior art keywords
poxyketon
crystallinic
peptide
synthesis
amino acid
Prior art date
Application number
DK08834964.2T
Other languages
English (en)
Other versions
DK2207791T3 (da
Inventor
Pasit Phiasivongsa
Louis C Sehl
William Dean Fuller
Guy J Laidig
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=39941499&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DK2207791(T4) "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
Application granted granted Critical
Publication of DK2207791T3 publication Critical patent/DK2207791T3/da
Publication of DK2207791T4 publication Critical patent/DK2207791T4/da

Links

Classifications

    • 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
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1016Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A62LIFE-SAVING; FIRE-FIGHTING
    • A62CFIRE-FIGHTING
    • A62C3/00Fire prevention, containment or extinguishing specially adapted for particular objects or places
    • A62C3/002Fire prevention, containment or extinguishing specially adapted for particular objects or places for warehouses, storage areas or other installations for storing goods
    • A62C3/004Fire prevention, containment or extinguishing specially adapted for particular objects or places for warehouses, storage areas or other installations for storing goods for freezing warehouses and storages
    • AHUMAN NECESSITIES
    • A62LIFE-SAVING; FIRE-FIGHTING
    • A62CFIRE-FIGHTING
    • A62C35/00Permanently-installed equipment
    • A62C35/58Pipe-line systems
    • A62C35/68Details, e.g. of pipes or valve systems
    • AHUMAN NECESSITIES
    • A62LIFE-SAVING; FIRE-FIGHTING
    • A62CFIRE-FIGHTING
    • A62C37/00Control of fire-fighting equipment
    • A62C37/08Control of fire-fighting equipment comprising an outlet device containing a sensor, or itself being the sensor, i.e. self-contained sprinklers
    • A62C37/10Releasing means, e.g. electrically released
    • A62C37/11Releasing means, e.g. electrically released heat-sensitive
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41Preparation of salts of carboxylic acids
    • C07C51/412Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/15Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
    • C07C53/16Halogenated acetic acids
    • C07C53/18Halogenated acetic acids containing fluorine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D301/00Preparation of oxiranes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D301/00Preparation of oxiranes
    • C07D301/02Synthesis of the oxirane ring
    • C07D301/03Synthesis of the oxirane ring by oxidation of unsaturated compounds, or of mixtures of unsaturated and saturated compounds
    • 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
    • C07D303/36Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1075General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of amino acids or peptide residues
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14Extraction; Separation; Purification
    • C07K1/30Extraction; Separation; Purification by precipitation
    • C07K1/306Extraction; Separation; Purification by precipitation by crystallization
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1005Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • AHUMAN NECESSITIES
    • A62LIFE-SAVING; FIRE-FIGHTING
    • A62CFIRE-FIGHTING
    • A62C35/00Permanently-installed equipment
    • A62C35/58Pipe-line systems
    • A62C35/60Pipe-line systems wet, i.e. containing extinguishing material even when not in use
    • AHUMAN NECESSITIES
    • A62LIFE-SAVING; FIRE-FIGHTING
    • A62CFIRE-FIGHTING
    • A62C35/00Permanently-installed equipment
    • A62C35/58Pipe-line systems
    • A62C35/62Pipe-line systems dry, i.e. empty of extinguishing material when not in use
    • AHUMAN NECESSITIES
    • A62LIFE-SAVING; FIRE-FIGHTING
    • A62CFIRE-FIGHTING
    • A62C37/00Control of fire-fighting equipment
    • A62C37/08Control of fire-fighting equipment comprising an outlet device containing a sensor, or itself being the sensor, i.e. self-contained sprinklers
    • A62C37/10Releasing means, e.g. electrically released
    • A62C37/11Releasing means, e.g. electrically released heat-sensitive
    • A62C37/14Releasing means, e.g. electrically released heat-sensitive with frangible vessels

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Emergency Management (AREA)
  • Business, Economics & Management (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Analytical Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Operations Research (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
DK08834964.2T 2007-10-04 2008-10-03 Krystallinske peptidepoxyketon-proteasehæmmere og syntese af aminosyreketoepoxider DK2207791T4 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US99761307P 2007-10-04 2007-10-04
US898707P 2007-12-20 2007-12-20
PCT/US2008/011443 WO2009045497A1 (en) 2007-10-04 2008-10-03 Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides

Publications (2)

Publication Number Publication Date
DK2207791T3 DK2207791T3 (da) 2016-07-25
DK2207791T4 true DK2207791T4 (da) 2019-10-07

Family

ID=39941499

Family Applications (1)

Application Number Title Priority Date Filing Date
DK08834964.2T DK2207791T4 (da) 2007-10-04 2008-10-03 Krystallinske peptidepoxyketon-proteasehæmmere og syntese af aminosyreketoepoxider

Country Status (36)

Country Link
US (3) US8367617B2 (da)
EP (3) EP2207791B2 (da)
JP (2) JP5734656B2 (da)
KR (5) KR20170125413A (da)
CN (1) CN101883779B (da)
AR (1) AR068681A1 (da)
AU (1) AU2008307510A1 (da)
CA (1) CA2701778C (da)
CL (2) CL2008002966A1 (da)
CO (1) CO6270366A2 (da)
CR (1) CR11364A (da)
CY (1) CY1117710T1 (da)
DK (1) DK2207791T4 (da)
DO (1) DOP2010000095A (da)
EA (2) EA018973B1 (da)
EC (1) ECSP10010103A (da)
ES (2) ES2684340T3 (da)
HK (1) HK1149573A1 (da)
HR (1) HRP20160808T4 (da)
HU (1) HUE029665T2 (da)
IL (5) IL204890A0 (da)
MA (1) MA31831B1 (da)
ME (1) ME02462B (da)
MX (1) MX2010003732A (da)
MY (2) MY173938A (da)
NZ (2) NZ598436A (da)
PH (1) PH12013501377A1 (da)
PL (1) PL2207791T5 (da)
PT (1) PT2207791T (da)
RS (1) RS54847B2 (da)
SA (1) SA08290624B1 (da)
SG (2) SG10201902704TA (da)
SI (1) SI2207791T2 (da)
TW (1) TWI501773B (da)
WO (1) WO2009045497A1 (da)
ZA (1) ZA201002770B (da)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8198270B2 (en) * 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
CN103554222A (zh) 2004-04-15 2014-02-05 欧尼斯治疗公司 用于抑制蛋白酶体酶的化合物
JP5108509B2 (ja) 2004-05-10 2012-12-26 プロテオリックス, インコーポレイテッド 酵素阻害のための化合物
NZ595196A (en) 2005-11-09 2013-03-28 Proteolix Inc Peptide-based compounds for enzyme inhibition
PL2041158T3 (pl) 2006-06-19 2013-08-30 Onyx Therapeutics Inc Peptydowe epoksyketony do hamowania proteasomu
PL2207791T5 (pl) 2007-10-04 2020-07-27 Onyx Therapeutics, Inc. Krystaliczne peptydo- epoksy ketonowe inhibitory proteazy i synteza keto-epoksydów Aminokwasowych
US7635773B2 (en) 2008-04-28 2009-12-22 Cydex Pharmaceuticals, Inc. Sulfoalkyl ether cyclodextrin compositions
AP2011005690A0 (en) 2008-10-21 2011-06-30 Onyx Therapeutics Inc Combination therapy with peptide epoxyketones.
TWI504598B (zh) 2009-03-20 2015-10-21 Onyx Therapeutics Inc 結晶性三肽環氧酮蛋白酶抑制劑
JP5919196B2 (ja) 2009-11-13 2016-05-18 オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. 転移抑制のためのペプチドエポキシケトンの使用
BR112012022060A2 (pt) 2010-03-01 2018-05-08 Onyx Therapeutics Inc composto para a inibição de imunoproteassoma
NZ602872A (en) * 2010-04-07 2014-05-30 Onyx Therapeutics Inc Crystalline peptide epoxyketone immunoproteasome inhibitor
JO3283B1 (ar) 2011-04-26 2018-09-16 Sanofi Sa تركيب يتضمن أفليبيرسيبت, حمض فولينيك, 5- فلورويوراسيل (5- Fu) وإرينوسيتان (FOLFIRI)
US9751957B2 (en) 2012-02-15 2017-09-05 Cydex Pharmaceuticals, Inc. Manufacturing process for cyclodextrin derivatives
CN104704007A (zh) 2012-02-28 2015-06-10 锡德克斯药物公司 烷基化环糊精组合物及其制备和使用方法
KR20190137963A (ko) * 2012-05-08 2019-12-11 오닉스 세라퓨틱스, 인크. 펩티드 프로테아좀 억제제 제제화를 위한 사이클로덱스트린 복합체화 방법
KR20150007361A (ko) * 2012-05-08 2015-01-21 오닉스 세라퓨틱스, 인크. 펩티드 프로테아좀 억제제 제제화를 위한 사이클로덱스트린 복합체화 방법
EP2867202B1 (en) 2012-06-29 2017-08-09 Nissan Chemical Industries, Ltd. Method for producing stereoselective epoxyketone compound
JP2015524394A (ja) 2012-07-09 2015-08-24 オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. ペプチドエポキシケトンプロテアーゼ阻害剤のプロドラッグ
WO2014018807A1 (en) * 2012-07-26 2014-01-30 Centrax International, Inc. Peptide epoxyketone compounds
CN109180780B (zh) * 2012-07-26 2022-03-18 圣特莱国际公司 多肽环氧酮化合物
US9636376B2 (en) * 2012-09-11 2017-05-02 Innopharma, Inc. Stable compositions of peptide epoxy ketones
KR102112119B1 (ko) 2012-10-22 2020-05-19 사이덱스 파마슈티칼스, 인크. 알킬화된 시클로덱스트린 조성물 및 이의 제조 및 사용 방법
TW201422255A (zh) * 2012-10-24 2014-06-16 Onyx Therapeutics Inc 用於蛋白酶體抑制劑之調整釋放製劑
US8906853B2 (en) 2012-11-28 2014-12-09 Enanta Pharmaceuticals, Inc. [N-Me-4-hydroxyleucine]-9-cyclosporin analogues for treatment and prevention of hepatitis C infection
US9795638B1 (en) * 2013-03-16 2017-10-24 BioDlogics, LLC Cardiothoracic construct and methods of use
EP3021862B1 (en) 2013-07-19 2017-08-30 Onyx Therapeutics, Inc. Peptide epoxyketone proteasome inhibitors in combination with pim kinase inhibitors for treatment of cancers
CN103360348B (zh) * 2013-07-25 2015-06-24 苏州鹏旭医药科技有限公司 一种Carfilzomib中间体及其制备方法和制备Carfilzomib的方法
WO2015032622A1 (en) * 2013-09-06 2015-03-12 Sandoz Ag Stereoselective synthesis of diols and triols by mannich reaction and their use in the synthesis of carfilzomib
EP3041856A1 (en) * 2013-09-06 2016-07-13 Sandoz AG Synthesis of peptide epoxy ketones
WO2015121769A1 (en) 2014-02-13 2015-08-20 Ranbaxy Laboratories Limited Process for the preparation of methyl n-[(benzyloxy)-carbonyl]-l-leucyl-l-phenylalaninate
EP3170005B1 (en) 2014-07-18 2019-04-10 Sanofi Method for predicting the outcome of a treatment with aflibercept of a patient suspected to suffer from a cancer
CN104230857A (zh) * 2014-08-19 2014-12-24 上海皓元生物医药科技有限公司 卡非佐米(Carfilzomib)的中间体化合物的制备方法及其中间体化合物
WO2016029179A1 (en) 2014-08-22 2016-02-25 Cydex Pharmaceuticals, Inc. Fractionated alkylated cyclodextrin compositions and processes for preparing and using the same
US10329325B2 (en) * 2014-09-24 2019-06-25 Biophore India Pharmaceuticals Pvt. Ltd Process for the preparation of (S)-4-methyl-N-((S)-1-(((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxo-pentan-2-yl) amino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido) pentanamide
US20160115198A1 (en) 2014-10-27 2016-04-28 Apicore Us Llc Methods of making carfilzomib and intermediates thereof
CN107548400A (zh) * 2014-12-02 2018-01-05 费森尤斯卡比肿瘤学有限公司 卡非佐米的纯化方法
EP3240575A4 (en) 2014-12-31 2018-07-25 Dr. Reddy's Laboratories Ltd. Co-crystal of carfilzomib with maleic acid and process for the preparation of pure carfilzomib
CN105985408B (zh) * 2015-02-12 2020-06-26 正大天晴药业集团股份有限公司 一种卡非佐米的纯化方法
CN104844540A (zh) * 2015-05-18 2015-08-19 上海凯欣生物医药科技有限公司 一种(2s)-2-氨基-4-甲基-1-[(2r)-2-甲基环氧乙烷基]-1-戊酮三氟乙酸盐的新晶型及其制备方法
WO2016185450A1 (en) * 2015-05-21 2016-11-24 Laurus Labs Private Limited An improved processes for the preparation of carfilzomib or pharmaceutically acceptable salts thereof
CN104961799B (zh) * 2015-06-19 2021-05-11 重庆医药工业研究院有限责任公司 一种卡非佐米晶型a及其制备方法
CN105017181B (zh) * 2015-07-02 2017-10-10 南京师范大学 卡非佐米关键中间体及其衍生物的制备方法
CN105294501B (zh) * 2015-08-21 2017-09-29 上海应用技术学院 一种卡非佐米中间体化合物的制备方法
WO2017098532A1 (en) 2015-12-11 2017-06-15 Mylan Laboratories Limited Crystalline and amorphous forms of carfilzomib
TWI759301B (zh) 2016-05-24 2022-04-01 美商安美基公司 聚乙二醇化卡非佐米化合物
PL3478670T3 (pl) 2016-06-29 2023-07-24 Kezar Life Sciences Krystaliczne sole peptydowego epoksyketonowego inhibitora immunoproteasomu
MX2018016386A (es) 2016-06-29 2019-09-09 Kezar Life Sciences Proceso de preparacion de un inhibidor de inmunoproteasoma de peptido epoxicetona, y precursores del mismo.
WO2018024645A1 (en) 2016-08-02 2018-02-08 Synthon B.V. Process for making carfilzomib
SI3494108T1 (sl) 2016-08-05 2021-02-26 Amgen Inc., Sinteza spojine (S)-2-amino-4-metil-1-((R)-2-metiloksiran-2-il)-pentan-1-on in njenih farmacevtsko sprejemljivih soli
EP3330260A1 (en) 2016-12-01 2018-06-06 Enantia, S.L. Process for the preparation of an intermediate for the synthesis of i.a. carfilzomib
MX2020004936A (es) 2017-11-16 2020-08-27 Amgen Inc Composiciones estables de compuestos de carfilzomib pegilado.
CN114195741A (zh) * 2021-12-28 2022-03-18 南京格亚医药科技有限公司 一种卡非佐米关键中间体异构体的制备方法
CN116023347A (zh) * 2022-10-09 2023-04-28 无锡紫杉药业股份有限公司 一种卡非佐米侧链的异构体制备方法

Family Cites Families (90)

* 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
WO1991013904A1 (en) 1990-03-05 1991-09-19 Cephalon, Inc. Chymotrypsin-like proteases and their inhibitors
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
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
WO1998010779A1 (en) 1996-09-13 1998-03-19 New York University Method for treating parasitic diseases with proteasome inhibitors
CA2268391A1 (en) * 1996-10-18 1998-04-30 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
SI0932617T1 (en) 1996-10-18 2002-06-30 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
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
US6133248A (en) * 1997-06-13 2000-10-17 Cydex, Inc. Polar drug of 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
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
US6838436B1 (en) * 1998-07-10 2005-01-04 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
US6902721B1 (en) * 1998-07-10 2005-06-07 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
EP1123412B1 (en) * 1998-10-20 2004-10-06 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
EP1477180A1 (en) 1999-10-20 2004-11-17 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone and hair growth
EP1430903A1 (de) * 2000-10-12 2004-06-23 Viromics Gmbh Verwendung von Proteasome Hemmern zur Behandlung von Virus-Infektionen
EP1360189A1 (en) 2001-01-25 2003-11-12 Millennium Pharmaceuticals, Inc. Formulation of boronic acid compounds
ES2278049T3 (es) * 2001-05-21 2007-08-01 Alcon, Inc. Uso de inhibidores de proteasoma para tratar trastornos de ojo seco.
EP1463719A2 (en) * 2002-01-08 2004-10-06 Eisai Co., Ltd Eponemycin and epoxomicin analogs and uses thereof
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
US20030224469A1 (en) * 2002-06-03 2003-12-04 Buchholz Tonia J. Methods and kits for assays utilizing fluorescence polarization
WO2003101481A1 (en) * 2002-06-03 2003-12-11 Als Therapy Development Foundation Treatment of neurodegenerative diseases using proteasome modulators
WO2004010937A2 (en) 2002-07-26 2004-02-05 Advanced Research & Technology Institute At Indiana University Method of treating cancer
US6749743B1 (en) * 2002-10-04 2004-06-15 Zabel Industries International, Ltd. Fuel diverter for a recirculating wastewater treatment system
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
PE20150676A1 (es) 2003-04-08 2015-05-17 Novartis Ag Composicion farmaceutica que contiene un agonista del receptor s1p y un alcohol de azucar
US8338180B2 (en) * 2003-06-10 2012-12-25 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
CN1976679B (zh) 2003-12-31 2011-08-31 锡德克斯药物公司 含有磺基烷基醚环糊精以及皮质甾类的吸入制剂
GB0400804D0 (en) 2004-01-14 2004-02-18 Innoscience Technology Bv Pharmaceutical compositions
CN101006098B (zh) * 2004-04-15 2014-10-29 欧尼斯治疗公司 用于抑制蛋白酶体酶的化合物
US7232818B2 (en) 2004-04-15 2007-06-19 Proteolix, Inc. Compounds for enzyme inhibition
CN103554222A (zh) 2004-04-15 2014-02-05 欧尼斯治疗公司 用于抑制蛋白酶体酶的化合物
US8198270B2 (en) * 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
JP5108509B2 (ja) * 2004-05-10 2012-12-26 プロテオリックス, インコーポレイテッド 酵素阻害のための化合物
AU2005243140A1 (en) 2004-05-10 2005-11-24 Proteolix, Inc. Synthesis of amino acid keto-epoxides
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
EP2100899A3 (en) * 2004-10-20 2009-09-30 Proteolix, Inc. Compounds for proteasome enzyme inhibition
EP2260835B1 (en) 2004-12-07 2013-03-06 Onyx Therapeutics, Inc. Composition for proteasome inhibition
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
ATE553198T1 (de) 2005-04-15 2012-04-15 Geron Corp Behandlung von krebs durch die kombinierte hemmung der proteasom- und telomeraseaktivitäten
GT200600350A (es) 2005-08-09 2007-03-28 Formulaciones líquidas
NZ595196A (en) * 2005-11-09 2013-03-28 Proteolix Inc Peptide-based compounds for enzyme inhibition
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
PL2041158T3 (pl) * 2006-06-19 2013-08-30 Onyx Therapeutics Inc Peptydowe epoksyketony do hamowania proteasomu
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
WO2008091620A2 (en) 2007-01-23 2008-07-31 Gloucester Pharmaceuticals, Inc. Combination therapy comprising romidepsin and i.a. bortezomib
WO2008140782A2 (en) 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition
WO2009020448A1 (en) 2007-08-06 2009-02-12 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
PL2207791T5 (pl) 2007-10-04 2020-07-27 Onyx Therapeutics, Inc. Krystaliczne peptydo- epoksy ketonowe inhibitory proteazy i synteza keto-epoksydów Aminokwasowych
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
US20090131367A1 (en) 2007-11-19 2009-05-21 The Regents Of The University Of Colorado Combinations of HDAC Inhibitors and Proteasome Inhibitors
EP2730579A1 (en) 2008-06-17 2014-05-14 Millennium Pharmaceuticals, Inc. Boronate ester compounds and pharmaceutical compositions thereof
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.
AP2011005690A0 (en) 2008-10-21 2011-06-30 Onyx Therapeutics Inc Combination therapy with peptide epoxyketones.
TWI504598B (zh) 2009-03-20 2015-10-21 Onyx Therapeutics Inc 結晶性三肽環氧酮蛋白酶抑制劑
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
JP5919196B2 (ja) 2009-11-13 2016-05-18 オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. 転移抑制のためのペプチドエポキシケトンの使用
BR112012022060A2 (pt) 2010-03-01 2018-05-08 Onyx Therapeutics Inc composto para a inibição de imunoproteassoma
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
NZ602872A (en) 2010-04-07 2014-05-30 Onyx Therapeutics Inc Crystalline peptide epoxyketone immunoproteasome inhibitor

Also Published As

Publication number Publication date
AU2008307510A1 (en) 2009-04-09
NZ598436A (en) 2014-03-28
EA201201476A1 (ru) 2013-07-30
RS54847B2 (sr) 2019-09-30
SI2207791T1 (sl) 2016-07-29
EP2207791B2 (en) 2019-08-07
SG10201902704TA (en) 2019-04-29
US20090105156A1 (en) 2009-04-23
WO2009045497A1 (en) 2009-04-09
ES2578905T3 (es) 2016-08-02
AR068681A1 (es) 2009-11-25
HUE029665T2 (en) 2017-03-28
KR20150131405A (ko) 2015-11-24
MY166950A (en) 2018-07-25
HK1149573A1 (en) 2011-10-07
KR20170125413A (ko) 2017-11-14
PH12013501377A1 (en) 2014-08-27
IL204890A0 (en) 2010-11-30
MY173938A (en) 2020-02-27
IL238246A (en) 2016-05-31
EP2612856B8 (en) 2018-10-17
US8921583B2 (en) 2014-12-30
DOP2010000095A (es) 2010-06-30
ES2684340T3 (es) 2018-10-02
HRP20160808T4 (hr) 2020-05-29
TWI501773B (zh) 2015-10-01
EP2612865A3 (en) 2014-03-19
US20130150290A1 (en) 2013-06-13
CY1117710T1 (el) 2017-05-17
ES2578905T5 (es) 2020-03-18
EP2612856A2 (en) 2013-07-10
ECSP10010103A (es) 2010-06-29
IL238248A (en) 2016-12-29
PT2207791T (pt) 2016-07-12
DK2207791T3 (da) 2016-07-25
EP2612865A2 (en) 2013-07-10
CN101883779A (zh) 2010-11-10
US8921324B2 (en) 2014-12-30
IL238247A (en) 2016-05-31
US8367617B2 (en) 2013-02-05
KR20170040374A (ko) 2017-04-12
MA31831B1 (fr) 2010-11-01
EA201070429A1 (ru) 2010-10-29
KR20100088664A (ko) 2010-08-10
CL2008002966A1 (es) 2010-06-25
PL2207791T3 (pl) 2016-10-31
EP2612856A3 (en) 2014-03-26
EP2207791A1 (en) 2010-07-21
CO6270366A2 (es) 2011-04-20
JP2010540637A (ja) 2010-12-24
US20130150289A1 (en) 2013-06-13
TW200924789A (en) 2009-06-16
KR20160086980A (ko) 2016-07-20
SG185994A1 (en) 2012-12-28
SI2207791T2 (sl) 2019-09-30
ME02462B (me) 2017-02-20
EP2207791B1 (en) 2016-04-13
EP2612856B1 (en) 2018-07-18
ZA201002770B (en) 2022-03-30
CR11364A (es) 2010-07-09
JP5734656B2 (ja) 2015-06-17
EA018973B1 (ru) 2013-12-30
HRP20160808T1 (hr) 2016-08-26
SA08290624B1 (ar) 2013-08-18
CA2701778A1 (en) 2009-04-09
JP2015163619A (ja) 2015-09-10
PL2207791T5 (pl) 2020-07-27
CL2012003441A1 (es) 2013-12-13
RS54847B1 (sr) 2016-10-31
MX2010003732A (es) 2010-08-09
NZ584814A (en) 2012-03-30
IL223698A0 (en) 2013-02-03
CN101883779B (zh) 2014-08-06
CA2701778C (en) 2018-09-11
EA024437B1 (ru) 2016-09-30

Similar Documents

Publication Publication Date Title
DK2207791T4 (da) Krystallinske peptidepoxyketon-proteasehæmmere og syntese af aminosyreketoepoxider
DK2035554T3 (da) Celle-fri syntese af proteiner indeholdende ikke-naturlige aminosyrer
LTPA2017010I1 (lt) Proteazomos inhibitoriai
DK2526962T3 (da) Therapeutic application of Kazal-type serine protease inhibitors
DE602005019971D1 (de) Inhibitoren von cysteinprotease
DK1940839T3 (da) Pyridopyrimidione Inhibitors of P13Ka
CY2014011I2 (el) Χορηγηση αναστολεων διπεπτιδυλοπεπτιδασης
DK1912636T3 (da) N-(arylamino)-sulfonamid-inhibitorer af mek
DK1848694T3 (da) Heterocykliske substituerede phenylmethanoner som inhibitorer af glycintransporter
DK2408758T3 (da) Krystallin tripeptid-epoxy-keton-protease-inhibitorer
DK1877379T3 (da) Hydroxybenzamidderivater og anvendelse heraf som inhibitorer af hsp90
DK3385267T3 (da) Syntese af boronestere og syreforbindelser
BRPI0807547A2 (pt) Inibidores de aspartil protease hetercíclicos
DK2021466T3 (da) Kloning og ekspression af en hidtil ukendt phytase
ATE538092T1 (de) Asparaginsäureproteaseinhibitoren
DK2035451T3 (da) Insulinoptrop peptidsyntese
DK2032535T3 (da) Spiro-cycliske nitriler som protease-inhibitorer
DK1999133T3 (da) Fremgangsmåde til fremstilling af HIV-proteaseinhibitorer
IL195782A0 (en) Epoxide inhibitors of cysteine proteases
DK1803732T3 (da) Peptider og derivater af APL-TYPE af HSP60 og famaceutiske sammensætninger
DE602005012550D1 (de) Inhibitoren des glycintransports
DE602005025521D1 (de) Synthese von aminosäure-n-carboxyanhydriden
BRPI0922283A2 (pt) inibidores da cistéina protease
DK3366686T3 (da) Inhibitorer af diacylglycerol-o-acyltransferase 1 (dgat-1) og anvendelser deraf
DK2032593T3 (da) Aminoderivater af B-homoandrostaner og B-heteroandrostaner