ES2046237T3 - Acidos boronicos peptidos inhibidores de proteasas de tipo tripsinico. - Google Patents

Acidos boronicos peptidos inhibidores de proteasas de tipo tripsinico.

Info

Publication number
ES2046237T3
ES2046237T3 ES198888108817T ES88108817T ES2046237T3 ES 2046237 T3 ES2046237 T3 ES 2046237T3 ES 198888108817 T ES198888108817 T ES 198888108817T ES 88108817 T ES88108817 T ES 88108817T ES 2046237 T3 ES2046237 T3 ES 2046237T3
Authority
ES
Spain
Prior art keywords
peptides
tripsinic
boronic
protease inhibiting
protease
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES198888108817T
Other languages
English (en)
Inventor
Charles Adrian Kettner
Ashokkumar Bhikkappa Shenvi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Pharma Co
Original Assignee
DuPont Merck Pharmaceutical Co
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 DuPont Merck Pharmaceutical Co filed Critical DuPont Merck Pharmaceutical Co
Application granted granted Critical
Publication of ES2046237T3 publication Critical patent/ES2046237T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • C07K5/10—Tetrapeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

LOS PEPTIDOS QUE CONTIENEN ACIDO BORONICO C-TERMINAL DERIVADOS DE LISINA, ORNITINA Y ARGININA, HOMOARGININA Y SUS CORRESPONDIENTES ANALOGOS DE ISOTIOURONIO, SON INHIBIDORES REVERSIBLES DE PROTEASAS SERINAS DE TIPO TRIPSINA TAL COMO TROMBINA, CALICREINA DEL PLASMA Y PLASMINA.
ES198888108817T 1987-06-05 1988-06-01 Acidos boronicos peptidos inhibidores de proteasas de tipo tripsinico. Expired - Lifetime ES2046237T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US5967087A 1987-06-05 1987-06-05
US07/178,368 US5187157A (en) 1987-06-05 1988-04-06 Peptide boronic acid inhibitors of trypsin-like proteases

Publications (1)

Publication Number Publication Date
ES2046237T3 true ES2046237T3 (es) 1994-02-01

Family

ID=26739035

Family Applications (1)

Application Number Title Priority Date Filing Date
ES198888108817T Expired - Lifetime ES2046237T3 (es) 1987-06-05 1988-06-01 Acidos boronicos peptidos inhibidores de proteasas de tipo tripsinico.

Country Status (16)

Country Link
US (1) US5187157A (es)
EP (1) EP0293881B1 (es)
JP (1) JPH0730090B2 (es)
KR (1) KR910003619B1 (es)
AU (1) AU623592B2 (es)
CA (1) CA1328332C (es)
DE (1) DE3878991T2 (es)
DK (1) DK304488A (es)
ES (1) ES2046237T3 (es)
FI (1) FI97297C (es)
HU (1) HU205141B (es)
IE (1) IE64787B1 (es)
IL (1) IL86613A (es)
NO (1) NO882472L (es)
NZ (1) NZ224903A (es)
PT (1) PT87652B (es)

Families Citing this family (177)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0315574A3 (de) * 1987-11-05 1990-08-22 Hoechst Aktiengesellschaft Renin-Inhibitoren
US5023236A (en) * 1988-04-07 1991-06-11 Corvas, Inc. Factor VII/VIIA active site inhibitors
US5574014A (en) * 1988-04-28 1996-11-12 Thrombosis Research Institute Inhibitors of trypsin-like enzymes
US6313096B1 (en) 1988-04-28 2001-11-06 Trigen Limited Inhibitors of trypsin-like enzymes
EP0341661A3 (en) * 1988-05-11 1991-05-02 The Du Pont Merck Pharmaceutical Company Peptide-drug compositions containing alpha-aminoboronic acid derivatives
DE3827340A1 (de) * 1988-08-12 1990-02-15 Hoechst Ag Verwendung von (alpha)-aminoboronsaeure-derivaten zur prophylaxe und behandlung von viruserkrankungen
US5580560A (en) * 1989-11-13 1996-12-03 Novo Nordisk A/S Modified factor VII/VIIa
US5252463A (en) * 1990-06-22 1993-10-12 The Du Pont Merck Pharmaceutical Company Clipsin, a chymotrypsin-like protease and method of using same
GB9017694D0 (en) * 1990-08-13 1990-09-26 Sandoz Ltd Improvements in or relating to organic chemistry
GB9024129D0 (en) * 1990-11-06 1990-12-19 Thrombosis Research Trust Inhibitors and substrates of thrombin
DE69206795T2 (de) * 1991-04-30 1996-09-05 Procter & Gamble ARYLBORONSäURE ENTHALTENDE FLüSSIGWASCHMITTEL
US5635477A (en) * 1991-09-30 1997-06-03 The Dupont Merck Pharmaceutical Company Cyclic compounds useful as inhibitors of platelet glycoprotein IIB/IIIA
US6825169B1 (en) 1991-10-22 2004-11-30 Trustees Of Tufts College Inhibitors of dipeptidyl-aminopeptidase type IV
SE9103612D0 (sv) * 1991-12-04 1991-12-04 Astra Ab New peptide derivatives
CA2124788C (en) * 1991-12-04 1998-02-10 Stanton L. Boyer Liquid laundry detergents with citric acid, cellulase, and boric-diol complex to inhibit proteolytic enzyme
US5442100A (en) * 1992-08-14 1995-08-15 The Procter & Gamble Company β-aminoalkyl and β-N-peptidylaminoalkyl boronic acids
US5576283A (en) * 1992-08-14 1996-11-19 The Procter & Gamble Company Liquid detergents containing a peptide aldehyde
US5582762A (en) * 1992-08-14 1996-12-10 The Procter & Gamble Company Liquid detergents containing a peptide trifluoromethyl ketone
EP0583534B1 (en) * 1992-08-14 1997-03-05 The Procter & Gamble Company Liquid detergents containing a peptide aldehyde
EP0583536B1 (en) * 1992-08-14 1997-03-05 The Procter & Gamble Company Liquid detergents containing an alpha-amino boronic acid
US5354491A (en) * 1992-08-14 1994-10-11 The Procter & Gamble Company Liquid detergent compositions containing protease and certain β-aminoalkylboronic acids and esters
JPH08504769A (ja) * 1992-12-15 1996-05-21 コルバス・インターナショナル、インコーポレイテッド 因子Ｘａの新規インヒビター
IL108031A0 (en) * 1992-12-22 1994-04-12 Procter & Gamble Difluoro pentapeptide derivatives and pharmaceutical compositions containing them
FR2701951B1 (fr) * 1993-02-24 1995-06-09 Adir Nouveaux derives peptidiques de l'acide boronique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
DK0688336T3 (da) * 1993-03-03 1997-10-20 Sandoz Ltd Peptidboronsyrederivater med proteaseinhiberende aktivitet
WO1994021650A1 (en) * 1993-03-24 1994-09-29 The Du Pont Merck Pharmaceutical Company Boronic acid and ester inhibitors of thrombin
US5384410A (en) * 1993-03-24 1995-01-24 The Du Pont Merck Pharmaceutical Company Removal of boronic acid protecting groups by transesterification
US5563127A (en) * 1993-03-24 1996-10-08 The Dupont Merck Pharmaceutical Company Boronic acid and ester inhibitors of thrombin
US5656600A (en) * 1993-03-25 1997-08-12 Corvas International, Inc. α-ketoamide derivatives as inhibitors of thrombosis
US5658885A (en) * 1993-04-27 1997-08-19 The Dupont Merck Pharmaceutical Company Amidino and guanidino substituted boronic acid inhibitors of trypsin-like enzymes
US5780631A (en) * 1993-06-03 1998-07-14 Astra Aktiebolag Starting materials in the synthesis of thrombin and kininogenase inhibitors
US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide derivatives
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
IL111175A0 (en) * 1993-10-07 1994-12-29 Du Pont Merck Pharma Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them
WO1995009859A1 (en) * 1993-10-07 1995-04-13 The Du Pont Merck Pharmaceutical Company Boropeptide inhibitors of thrombin which contain a substituted pyrrolidine ring
IL111176A0 (en) * 1993-10-07 1994-12-29 Du Pont Merck Pharma Dipeptide boronic acid inhibitors of trypsin-like enzymes and pharmaceutical compositions containing them
US6060462A (en) * 1993-10-20 2000-05-09 Dupont Pharmaceuticals Company Electrophilic peptide analogs as inhibitors of trypsin-like enzymes
US5446056A (en) * 1993-11-24 1995-08-29 The Du Pont Merck Pharmaceutical Company Isoxazoline compounds useful as fibrinogen receptor antagonists
GB9401483D0 (en) * 1994-01-26 1994-03-23 Sandoz Ltd Organic compounds
US5484772A (en) * 1994-03-04 1996-01-16 Eli Lilly And Company Antithrombotic agents
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
CA2143533A1 (en) * 1994-03-04 1995-09-05 Kenneth D. Kurz Antithrombotic agents
US5488037A (en) * 1994-03-04 1996-01-30 Eli Lilly And Company Antithrombotic agents
US5439888A (en) * 1994-03-04 1995-08-08 Eli Lilly And Company Antithrombotic agents
ZA951618B (en) * 1994-03-04 1996-08-27 Lilly Co Eli Antithrombotic agents
US5436229A (en) * 1994-03-04 1995-07-25 Eli Lilly And Company Bisulfite adducts of arginine aldehydes
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5885967A (en) * 1994-03-04 1999-03-23 Eli Lilly And Company Antithrombotic agents
US5602101A (en) * 1994-03-04 1997-02-11 Eli Lilly And Company Antithrombotic agents
US5693617A (en) * 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
FR2718448B3 (fr) * 1994-04-12 1996-02-09 Synthelabo Dérivés d'acides aminoboroniques, leur préparation et leur utilisation comme intermédiaires de synthèse.
FR2718451B1 (fr) * 1994-04-12 1996-05-10 Synthelabo Dérivés de peptides boroniques, leur préparation et leur application en thérapeutique.
DE4421052A1 (de) 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
FR2721611B1 (fr) * 1994-06-22 1996-09-27 Adir Nouveaux dérivés peptidiques de l'acide boronique, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent .
US6083903A (en) * 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
SE9404196D0 (sv) * 1994-12-02 1994-12-02 Astra Ab New antithrombotic formulation
US6030972A (en) * 1995-02-17 2000-02-29 Basf Aktiengesellschaft Dipeptide amidines as thrombin inhibitors
US5914319A (en) * 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
US5710130A (en) * 1995-02-27 1998-01-20 Eli Lilly And Company Antithrombotic agents
US5731439A (en) * 1995-03-24 1998-03-24 The Dupont Merck Pharmaceutical Company Piperidine containing aminobornic acids
US5639739A (en) * 1995-03-24 1997-06-17 The Dupont Merck Pharmaceutical Company Imidazole containing aminoboronic acids
SA96170106A (ar) 1995-07-06 2005-12-03 أسترا أكتيبولاج مشتقات حامض أميني جديدة
ATE377006T1 (de) * 1995-11-28 2007-11-15 Cephalon Inc Aus d-aminosäuren abgeleitete cystein- und serinproteasehemmer
TWI238827B (en) 1995-12-21 2005-09-01 Astrazeneca Ab Prodrugs of thrombin inhibitors
US5760028A (en) * 1995-12-22 1998-06-02 The Dupont Merck Pharmaceutical Company Integrin receptor antagonists
US5942544A (en) * 1996-02-22 1999-08-24 Dupont Pharmaceuticals Company α-branched anilines, toluenes, and analogs thereof as factor Xa inhibitors
FR2745288B1 (fr) * 1996-02-27 1998-04-17 Adir Nouveaux derives de l'acide boronique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
SE9602263D0 (sv) 1996-06-07 1996-06-07 Astra Ab New amino acid derivatives
US5965532A (en) * 1996-06-28 1999-10-12 Trustees Of Tufts College Multivalent compounds for crosslinking receptors and uses thereof
SE9602646D0 (sv) 1996-07-04 1996-07-04 Astra Ab Pharmaceutically-useful compounds
US6004955A (en) * 1996-08-15 1999-12-21 Dupont Pharmaceuticals Company Cyclic carbamates and isoxazolidines as IIb/IIIa antagonists
US6165966A (en) * 1996-09-24 2000-12-26 The Procter & Gamble Company Liquid detergents containing proteolytic enzyme and protease inhibitors
US6180586B1 (en) 1996-09-24 2001-01-30 The Procter & Gamble Company Liquid laundry detergent compositions containing proteolytic enzyme and protease inhibitors
JP2000506931A (ja) * 1996-09-24 2000-06-06 ザ、プロクター、エンド、ギャンブル、カンパニー タンパク質分解酵素とプロテアーゼインヒビターを含有した液体洗剤
WO1998024886A1 (en) * 1996-12-04 1998-06-11 Brigham And Women's Hospital, Inc. Mast cell protease that cleaves fibrinogen
US5955431A (en) * 1997-02-05 1999-09-21 Brigham And Women's Hospital, Inc. Mast cell protease peptide inhibitors
US6100234A (en) * 1997-05-07 2000-08-08 Tufts University Treatment of HIV
US6040145A (en) 1997-05-07 2000-03-21 Tufts University Potentiation of the immune response
SK174699A3 (en) 1997-06-19 2000-08-14 Du Pont Pharm Co Inhibitors of factor xa with a neutral p1 specificity group
AR013084A1 (es) 1997-06-19 2000-12-13 Astrazeneca Ab Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados
ATE357509T1 (de) * 1997-09-29 2007-04-15 Point Therapeutics Inc Stimulierung von hämatopoietischen zellen im vitro
ZA988735B (en) * 1997-10-06 2000-03-23 Du Pont Pharm Co An efficient method for the conversion of nitriles to amidines.
US6011047A (en) * 1997-11-26 2000-01-04 Corvas International Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors
US6204384B1 (en) 1997-11-26 2001-03-20 Corvas International, Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (II)
SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
JP2002501081A (ja) 1998-01-26 2002-01-15 ビーエーエスエフ アクチェンゲゼルシャフト トロンビンインヒビター
JP2003504301A (ja) 1998-04-01 2003-02-04 ブリストル−マイヤーズ スクイブ ファーマ カンパニー インテグリンアンタゴニスト
IL139247A0 (en) 1998-05-04 2001-11-25 Point Therapeutics Inc Hematopoietic stimulation
JP2002517401A (ja) 1998-06-05 2002-06-18 ポイント セラピューティクス， インコーポレイテッド 環状ボロプロリン化合物
US6979697B1 (en) * 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
CA2348740A1 (en) 1998-12-23 2000-07-06 Ruth R. Wexler Thrombin or factor xa inhibitors
KR100639274B1 (ko) 1999-01-13 2006-10-27 아스트라제네카 아베 신규 아미디노벤질아민 유도체 및 트롬빈 억제제로서의 용도
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
US6890904B1 (en) 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
US6649593B1 (en) * 1999-10-13 2003-11-18 Tularik Inc. Modulators of SREBP processing
SE0001803D0 (sv) 2000-05-16 2000-05-16 Astrazeneca Ab New compounds i
US6433186B1 (en) 2000-08-16 2002-08-13 Astrazeneca Ab Amidino derivatives and their use as thormbin inhibitors
US7129233B2 (en) 2000-12-01 2006-10-31 Astrazeneca Ab Mandelic acid derivatives and their use as thrombin inhibitors
AR035216A1 (es) 2000-12-01 2004-05-05 Astrazeneca Ab Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios
AU2002243508A1 (en) 2001-01-10 2002-07-24 Bristol-Myers Squibb Company Patent Department Alpha-aminoboronic acids prepared by novel synthetic methods
ES2571219T3 (es) * 2001-01-25 2024-09-23 The United States Of America Represented By The Sec Dep Of Health And Human Services Formulación de compuestos de ácido borónico
AR034517A1 (es) 2001-06-21 2004-02-25 Astrazeneca Ab Formulacion farmaceutica
US6777431B2 (en) 2001-07-13 2004-08-17 Corvas International, Inc. Non-convalent thrombin inhibitors
US20060014697A1 (en) * 2001-08-22 2006-01-19 Travis Mickle Pharmaceutical compositions for prevention of overdose or abuse
SE0201661D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab New salts
SE0201659D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab Modified release pharmaceutical formulation
WO2004004661A2 (en) * 2002-07-09 2004-01-15 Point Therapeutics, Inc. Boroproline compound combination therapy
US20060084592A1 (en) * 2002-09-09 2006-04-20 Trigen Limited Peptide boronic acid inhibitors
US20050176651A1 (en) * 2002-09-09 2005-08-11 Trigen Limited Peptide boronic acids useful in making salts thereof
US20050282757A1 (en) * 2002-09-09 2005-12-22 Trigen Limited Peptide boronic acid compounds useful in anticoagulation
US20050119226A1 (en) * 2003-09-09 2005-06-02 Trigen Limited Methods for synthesizing organoboronic compounds and products thereof
US20050288253A1 (en) * 2002-09-09 2005-12-29 Trigen Limited Boronic acid salts
US7781424B2 (en) 2003-05-27 2010-08-24 Astrazeneca Ab Modified release pharmaceutical formulation
US7223745B2 (en) * 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7576206B2 (en) 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
GB0405272D0 (en) * 2004-03-09 2004-04-21 Trigen Ltd Compounds
ME01975B (me) 2004-03-30 2015-05-20 Millennium Pharm Inc Sinteza jedinjenja estra organoborne kiseline i organoborne kiseline
US7795205B2 (en) 2004-04-12 2010-09-14 Canyon Pharmaceuticals, Inc. Methods for effecting regression of tumor mass and size in a metastasized pancreatic tumor
US20060063719A1 (en) * 2004-09-21 2006-03-23 Point Therapeutics, Inc. Methods for treating diabetes
US7468383B2 (en) * 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
TW200827336A (en) 2006-12-06 2008-07-01 Astrazeneca Ab New crystalline forms
PL2178888T3 (pl) 2007-08-06 2012-11-30 Millennium Pharm Inc Inhibitory proteasomów
HRP20160569T1 (hr) * 2007-12-03 2016-07-29 Obe Therapy Biotechnology Boropeptidni inhibitori enteropeptidaze i njihove uporabe u liječenju pretilosti, pretjerane tjelesne težine i/ili bolesti povezane s abnormalnim metabolizmom masti
US10793515B2 (en) 2008-03-19 2020-10-06 Aurimmed Pharma, Inc. Compounds advantageous in the treatment of central nervous system diseases and disorders
RU2010142655A (ru) 2008-03-19 2012-04-27 Ауриммед Фарма, Инк. (Us) Соединение, пригодное для лечения болезней и нарушений центральной нервной системы, и способ его получения
US20210130285A1 (en) 2008-03-19 2021-05-06 Aurimmed Pharma, Inc. Novel compounds advantageous in the treatment of central nervous system diseases and disorders
US9212155B2 (en) 2008-03-19 2015-12-15 Aurimmed Pharma, Inc. Compounds advantageous in the treatment of central nervous system diseases and disorders
GB0807828D0 (en) * 2008-04-29 2008-06-04 Vantia Ltd Aminopyridine derivatives
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.
EA201170527A1 (ru) * 2008-10-01 2011-10-31 Др. Редди'С Лабораторис Лтд. Фармацевтические композиции, включающие соединения бороновой кислоты
WO2011022502A1 (en) 2009-08-18 2011-02-24 Georgetown University Boronic acid compositions and methods related to cancer
GB0918924D0 (en) 2009-10-28 2009-12-16 Vantia Ltd Azaindole derivatives
GB0918923D0 (en) 2009-10-28 2009-12-16 Vantia Ltd Aminothiazole derivatives
GB0918922D0 (en) 2009-10-28 2009-12-16 Vantia Ltd Aminopyridine derivatives
AU2010341530B2 (en) 2009-12-22 2016-03-10 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
MX2012011298A (es) 2010-03-31 2012-11-06 Millennium Pharm Inc Derivados del acido 1-amino-2-ciclopropiletilboronico.
EP2624818B1 (en) 2010-10-05 2017-04-05 Fresenius Kabi USA, LLC Bortezomib formulations stabilised with boric acid
GB2494851A (en) 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
EP2819673B1 (en) 2012-03-02 2016-09-07 Dr. Reddy's Laboratories Ltd. Pharmaceutical compositions comprising boronic acid compounds
GB201212081D0 (en) 2012-07-06 2012-08-22 Kalvista Pharmaceuticals Ltd New polymorph
GB201300304D0 (en) 2013-01-08 2013-02-20 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
PH12015501492B1 (en) 2013-01-08 2015-09-28 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
GB2510407A (en) 2013-02-04 2014-08-06 Kalvista Pharmaceuticals Ltd Aqueous suspensions of kallikrein inhibitors for parenteral administration
CA2909519A1 (en) 2013-04-16 2014-10-23 Cipla Limited Process for the preparation of bortezomib mannitol ester
EP2999697B1 (en) 2013-05-23 2017-04-19 Kalvista Pharmaceuticals Limited Heterocyclic derivates
WO2015003146A1 (en) 2013-07-03 2015-01-08 Georgetown University Boronic acid derivatives of resveratrol for activating deacetylase enzymes
HUE14755117T2 (hu) 2013-08-14 2018-12-28 Kalvista Pharmaceuticals Ltd Plazma-kallikrein inhibitorok
GB2517908A (en) 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
TWI636047B (zh) 2013-08-14 2018-09-21 英商卡爾維斯塔製藥有限公司 雜環衍生物
CN111116622A (zh) 2014-02-03 2020-05-08 俄亥俄州创新基金会 硼酸酯和其药物制剂
MA39964A (fr) 2014-05-20 2015-11-26 Millennium Pharm Inc Inhibiteurs du protéasome contenant du bore destinés à être utilisés après une thérapie contre le cancer primaire
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
GB201421088D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
MA41505A (fr) 2015-02-11 2017-12-19 Millennium Pharm Inc Nouvelle forme cristalline d'un inhibiteur de protéasome
EP3270891A1 (en) 2015-03-17 2018-01-24 Leon-Nanodrugs GmbH Nanoparticles comprising a stabilized boronic acid compound
DK3464271T3 (da) 2016-05-31 2020-06-15 Kalvista Pharmaceuticals Ltd Pyrazolderivater som plasma-kallikreininhibitorer
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
GB201609603D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
PT3716952T (pt) 2017-11-29 2022-04-14 Kalvista Pharmaceuticals Ltd Formas de administração que incluem um inibidor de calicreína plasmática
GB201910125D0 (en) 2019-07-15 2019-08-28 Kalvista Pharmaceuticals Ltd Treatments of angioedema
GB201910116D0 (en) 2019-07-15 2019-08-28 Kalvista Pharmaceuticals Ltd Treatments of hereditary angioedema
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
GB2591730A (en) 2019-12-09 2021-08-11 Kalvista Pharmaceuticals Ltd New polymorphs
GB201918994D0 (en) 2019-12-20 2020-02-05 Kalvista Pharmaceuticals Ltd Treatments of diabetic macular edema and impaired visual acuity
WO2022079446A1 (en) 2020-10-15 2022-04-21 Kalvista Pharmaceuticals Limited Treatments of angioedema
EP4232031A1 (en) 2020-10-23 2023-08-30 Kalvista Pharmaceuticals Limited Treatments of angioedema
JP2024505596A (ja) 2021-02-09 2024-02-06 カルビスタ・ファーマシューティカルズ・リミテッド 遺伝性血管性浮腫の治療
WO2023002219A1 (en) 2021-07-23 2023-01-26 Kalvista Pharmaceuticals Limited Treatments of hereditary angioedema
EP4480545A3 (en) 2022-04-27 2025-02-26 Kalvista Pharmaceuticals Limited Formulations of a plasma kallikrein inhibitor
WO2024180100A1 (en) 2023-02-27 2024-09-06 Kalvista Pharmaceuticals Limited New solid form of a plasma kallikrein inhibitor
WO2025172692A1 (en) 2024-02-13 2025-08-21 Kalvista Pharmaceuticals Limited Oral sebetralstat for the treatment of an attack of hereditary angioedema
WO2025172693A1 (en) 2024-02-13 2025-08-21 Kalvista Pharmaceuticals Limited Oral sebetralstat for the treatment of an attack of hereditary angioedema

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4318904A (en) * 1980-04-25 1982-03-09 Research Corporation Peptide affinity labels for thrombin and other trypsin-like proteases
US4537773A (en) * 1983-12-05 1985-08-27 E. I. Du Pont De Nemours And Company α-Aminoboronic acid derivatives
US4499082A (en) * 1983-12-05 1985-02-12 E. I. Du Pont De Nemours And Company α-Aminoboronic acid peptides
JPS61112018A (ja) * 1984-11-06 1986-05-30 Mitsubishi Chem Ind Ltd 線溶増強剤
NZ223148A (en) * 1987-01-16 1989-10-27 Merrell Dow Pharma Peptide derivatives having peptidase inhibition activity

Also Published As

Publication number Publication date
PT87652A (pt) 1988-07-01
HU205141B (en) 1992-03-30
FI882638L (fi) 1988-12-06
FI97297C (fi) 1996-11-25
KR910003619B1 (ko) 1991-06-07
IE64787B1 (en) 1995-09-06
EP0293881A2 (en) 1988-12-07
DE3878991D1 (de) 1993-04-15
US5187157A (en) 1993-02-16
EP0293881A3 (en) 1990-05-30
DK304488A (da) 1988-12-06
DK304488D0 (da) 1988-06-03
IL86613A0 (en) 1988-11-30
PT87652B (pt) 1992-09-30
FI882638A0 (fi) 1988-06-03
NO882472L (no) 1988-12-06
EP0293881B1 (en) 1993-03-10
HUT49629A (en) 1989-10-30
IL86613A (en) 1993-04-04
CA1328332C (en) 1994-04-05
NZ224903A (en) 1990-02-26
DE3878991T2 (de) 1993-07-15
AU1733288A (en) 1988-12-08
NO882472D0 (no) 1988-06-03
JPH0730090B2 (ja) 1995-04-05
IE881666L (en) 1988-12-05
AU623592B2 (en) 1992-05-21
FI97297B (fi) 1996-08-15
JPS6463583A (en) 1989-03-09
KR890000514A (ko) 1989-03-15

Similar Documents

Publication Publication Date Title
ES2046237T3 (es) Acidos boronicos peptidos inhibidores de proteasas de tipo tripsinico.
CO4600683A1 (es) Bikunina humana
ES2056817T3 (es) Transformacion de trichoderma.
CO5700784A2 (es) Polipeptidos de virus de papiloma humano y composiciones in- munogenas
JPS5690047A (en) Cyclic hexapeptide of somatostatin analogue
ES8801930A1 (es) Procedimiento para la preparacion de dipeptidos de n,n'-dialquilguanidino
DK0654078T3 (da) Thrombinblodfraktion til anvendelse i en medicinsk procedure
ES2078907T3 (es) Metodo para radiomarcar proteinas.
DK289285D0 (da) Thymopentin analoge
ES444622A1 (es) Procedimiento para la preparacion de derivados peptidicos delos acidos fosfonico y fosfinico.
ES2059356T3 (es) Inhibidor de la tripsina pancreatico secretor, preparado mediante tecnologia genetica y sus variantes.
ATE253920T1 (de) Phosphor enthaltende hemmer von cystein- und serin-proteasen
FI961044A0 (fi) Kininogeeni-inhibiittorit
EP0082568A3 (en) Retro-inverso analogues of c-terminal penta and hexapeptides of substance p.
EP0192988A3 (en) Process for solubilization, purification and characterization of protein from insoluble protein aggregates or complexes and compositions of matter therefrom
ES2196088T3 (es) Analogos del factor de crecimiento de los queratinocitos.
CH406524A (de) Verfahren zur Herstellung von hoch gereinigten Kallikrein-Präparaten
ES2092751T3 (es) Nuevos 2-sacarinilmetil aril carboxilatos utiles como inhibidores de enzimas proteoliticos y composiciones y metodos de empleo de los mismos.
ES2060123T3 (es) Aminoacidos protegidos y procedimientos para su fabricacion.
GB1109086A (en) Polypeptides
ZA902054B (en) Production and use of anthelmintic agents and protective immunogens
DK495786D0 (da) Fremgangsmaade til fremstilling af halogen-magnesium-alanat og alanatets anvendelse
ATE78872T1 (de) Herstellung von polypeptiden.
ES2062006T3 (es) Un psti humano modificado.
ES2032812T3 (es) Vacuna.

Legal Events

Date Code Title Description
FG2A Definitive protection

Ref document number: 293881

Country of ref document: ES