PE134099A1 - Un proceso para la preparacion de intermediarios de epotilona de anillo abierto utiles para la preparacion de analogos de epotilona - Google Patents

Un proceso para la preparacion de intermediarios de epotilona de anillo abierto utiles para la preparacion de analogos de epotilona

Info

Publication number
PE134099A1
PE134099A1 PE1998001181A PE00118198A PE134099A1 PE 134099 A1 PE134099 A1 PE 134099A1 PE 1998001181 A PE1998001181 A PE 1998001181A PE 00118198 A PE00118198 A PE 00118198A PE 134099 A1 PE134099 A1 PE 134099A1
Authority
PE
Peru
Prior art keywords
epotilone
optionally replaced
preparation
rent
methyl
Prior art date
Application number
PE1998001181A
Other languages
English (en)
Inventor
Soong-Hoon Kim
Robert M Borzilleri
Original Assignee
Bristol Myers Squibb 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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of PE134099A1 publication Critical patent/PE134099A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/38—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • 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
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • A61P7/06—Antianaemics
    • 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
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • AIDS & HIV (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)

Abstract

SE REFIERE A UN INTERMEDIARIO PARA LA PREPARACION DE ANALOGOS DE EPOTILONA DE FORMULA I, DONDE X ES N3, NR7R8, N(COR11)COR12, NR9SO2R10; Q ES UN GRUPO a, b, c, ENTRE OTROS; R1, R2, R3, R4, R5, R13, R14, R15 SON H, ALQUILO OPCIONALMENTE SUSTITUIDO, ARILO; O R1 Y R2 SON ALQUILO O JUNTOS FORMAN CICLOALQUILO; R8 ES H, ALQUILO OPCIONALMENTE SUSTITUIDO, ARILO OPCIONALMENTE SUSTITUIDO, O-ALQUILO OPCIONALMENTE SUSTITUIDO; R6, R7, R9 SON H, ALQUILO OPCIONALMENTE SUSTITUIDO, ARILO, CICLOALQUILO, HETEROCICLO; R10, R11, R12 SON ALQUILO OPCIONALMENTE SUSTITUIDO, ARILO OPCIONALMENTE SUSTITUIDO O R11 Y R12 FORMAN JUNTOS UN ANILLO CON NITROGENO. SON COMPUESTOS PREFERIDOS ACIDO (3S,6R,7S,8S,12R,13S,15S)-15-AMINO-12,13-EPOXI-4,4,6,8,12,16-HEXAMETIL-7-HIDROXI-17-(2-METIL-4-TIAZOLIL)-5-OXO-16-HEPTADECENOICO, [1S-[1R*,3R*(E),7R*,10R*,11S*,12R*,16S*]]-7,11-DIHIDROXI-8,8,10,12,16-PENTAMETIL-3-[1-METIL-2-(2-METIL-4-TIAZOLIL)ETENIL]-4-AZA-17-OXABICICLO[14.1.0]HEPTADECANO-5,9-DIONA. LA EPOTILONA ES UN AGENTE ESTABILIZADOR MICROTUBULAR O INHIBIDOR DE LA ANGIOGENESIS DEL TUMOR O INHIBIDOR DE LA APOPTOSIS Y PUEDE SER UTIL PARA EL TRATAMIENTO DE CANCER Y OTRAS ENFERMEDADES PROLIFERATIVAS ANORMALES TALES COMO CARCINOMAS, TUMORES HEMATOPOYETICOS DE LINAJE LINFOIDEO, MIELOIDE, TUMORES DE ORIGEN MESENQUIMAL, TUMORES DEL SISTEMA NERVIOSO CENTRAL
PE1998001181A 1997-12-04 1998-12-04 Un proceso para la preparacion de intermediarios de epotilona de anillo abierto utiles para la preparacion de analogos de epotilona PE134099A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US6755097P 1997-12-04 1997-12-04

Publications (1)

Publication Number Publication Date
PE134099A1 true PE134099A1 (es) 2000-03-29

Family

ID=22076753

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1998001181A PE134099A1 (es) 1997-12-04 1998-12-04 Un proceso para la preparacion de intermediarios de epotilona de anillo abierto utiles para la preparacion de analogos de epotilona

Country Status (10)

Country Link
US (1) US6365749B1 (es)
EP (1) EP1035824A4 (es)
JP (1) JP2003522722A (es)
AR (1) AR017808A1 (es)
AU (1) AU739380B2 (es)
CA (1) CA2312098C (es)
PE (1) PE134099A1 (es)
UY (1) UY25279A1 (es)
WO (1) WO1999027890A2 (es)
ZA (1) ZA9810993B (es)

Families Citing this family (89)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69734362T2 (de) * 1996-12-03 2006-07-20 Sloan-Kettering Institute For Cancer Research Synthese von epothilonen, zwischenprodukte dazu, analoga und verwendungen davon
US20050043376A1 (en) * 1996-12-03 2005-02-24 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US6204388B1 (en) 1996-12-03 2001-03-20 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US6867305B2 (en) 1996-12-03 2005-03-15 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US6605599B1 (en) 1997-07-08 2003-08-12 Bristol-Myers Squibb Company Epothilone derivatives
DE19826988A1 (de) * 1998-06-18 1999-12-23 Biotechnolog Forschung Gmbh Epothilon-Nebenkomponenten
US6410301B1 (en) 1998-11-20 2002-06-25 Kosan Biosciences, Inc. Myxococcus host cells for the production of epothilones
NZ511722A (en) 1998-11-20 2004-05-28 Kosan Biosciences Inc Recombinant methods and materials for producing epothilone and epothilone derivatives
US6780620B1 (en) * 1998-12-23 2004-08-24 Bristol-Myers Squibb Company Microbial transformation method for the preparation of an epothilone
US20020058286A1 (en) * 1999-02-24 2002-05-16 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
WO2000062778A1 (en) 1999-04-15 2000-10-26 Bristol-Myers Squibb Co. Cyclic protein tyrosine kinase inhibitors
CA2385528C (en) 1999-10-01 2013-12-10 Immunogen, Inc. Compositions and methods for treating cancer using immunoconjugates and chemotherapeutic agents
US6518421B1 (en) * 2000-03-20 2003-02-11 Bristol-Myers Squibb Company Process for the preparation of epothilone analogs
US6593115B2 (en) * 2000-03-24 2003-07-15 Bristol-Myers Squibb Co. Preparation of epothilone intermediates
US6489314B1 (en) 2001-04-03 2002-12-03 Kosan Biosciences, Inc. Epothilone derivatives and methods for making and using the same
UA75365C2 (en) * 2000-08-16 2006-04-17 Bristol Myers Squibb Co Epothilone analog polymorph modifications, a method for obtaining thereof (variants), a pharmaceutical composition based thereon
GB0029895D0 (en) * 2000-12-07 2001-01-24 Novartis Ag Organic compounds
WO2002058699A1 (en) 2001-01-25 2002-08-01 Bristol-Myers Squibb Company Pharmaceutical forms of epothilones for oral administration
NZ526870A (en) 2001-01-25 2005-11-25 Bristol Myers Squibb Co Methods of administering epothilone analogs for the treatment of cancer
MXPA03006412A (es) * 2001-01-25 2003-10-15 Bristol Myers Squibb Co Metodos para administrar analogos de epotilona para tratamiento de cancer.
SK8552003A3 (en) 2001-01-25 2004-06-08 Bristol Myers Squibb Co Parenteral formulation containing epothilone analogs
US6893859B2 (en) 2001-02-13 2005-05-17 Kosan Biosciences, Inc. Epothilone derivatives and methods for making and using the same
HUP0400041A2 (hu) 2001-02-20 2004-04-28 Bristol-Myers Squibb Co. Epotilonszármazékok alkalmazása makacs tumorok kezelésére szolgáló gyógyszerkészítmények előállítására
HUP0303175A2 (hu) 2001-02-20 2003-12-29 Bristol-Myers Squibb Co. Epotilonszármazékok alkalmazása makacs tumorok kezelésére alkalmas gyógyszerkészítmény előállítására
MXPA03007466A (es) 2001-02-27 2003-12-08 Gbf Ges F R Biotechnologische Degradacion de epotilonas y epotilonas substituidas con etileno.
CA2440555A1 (en) * 2001-03-14 2002-09-19 Bristol-Myers Squibb Company Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases
JP2004532888A (ja) 2001-06-01 2004-10-28 ブリストル−マイヤーズ　スクイブ　カンパニー エポチロン誘導体
WO2003077903A1 (en) * 2002-03-12 2003-09-25 Bristol-Myers Squibb Company C12-cyano epothilone derivatives
DK1483251T3 (da) 2002-03-12 2010-04-12 Bristol Myers Squibb Co C3-cyano-epothilon-derivater
TW200403994A (en) * 2002-04-04 2004-03-16 Bristol Myers Squibb Co Oral administration of EPOTHILONES
TW200400191A (en) * 2002-05-15 2004-01-01 Bristol Myers Squibb Co Pharmaceutical compositions and methods of using C-21 modified epothilone derivatives
US7405234B2 (en) 2002-05-17 2008-07-29 Bristol-Myers Squibb Company Bicyclic modulators of androgen receptor function
WO2003105828A1 (en) * 2002-06-14 2003-12-24 Bristol-Myers Squibb Company Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases
US6921769B2 (en) 2002-08-23 2005-07-26 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
ES2281692T3 (es) * 2002-08-23 2007-10-01 Sloan-Kettering Institute For Cancer Research Sintesis de epotilones, sus intermediarios, sus analogos y sus usos.
TWI291464B (en) 2002-09-23 2007-12-21 Bristol Myers Squibb Co Methods for the preparation, isolation and purification of epothilone B, and X-ray crystal structures of epothilone B
EP1567487A4 (en) 2002-11-15 2005-11-16 Bristol Myers Squibb Co OPEN-CHAINED, PROLYL-FROSTED MODULATORS OF ANDROGEN RECEPTOR FUNCTION
US20050171167A1 (en) * 2003-11-04 2005-08-04 Haby Thomas A. Process and formulation containing epothilones and analogs thereof
US7820702B2 (en) 2004-02-04 2010-10-26 Bristol-Myers Squibb Company Sulfonylpyrrolidine modulators of androgen receptor function and method
US7378426B2 (en) 2004-03-01 2008-05-27 Bristol-Myers Squibb Company Fused heterotricyclic compounds as inhibitors of 17β-hydroxysteroid dehydrogenase 3
US7696241B2 (en) 2004-03-04 2010-04-13 Bristol-Myers Squibb Company Bicyclic compounds as modulators of androgen receptor function and method
US7625923B2 (en) 2004-03-04 2009-12-01 Bristol-Myers Squibb Company Bicyclic modulators of androgen receptor function
US20090004277A1 (en) * 2004-05-18 2009-01-01 Franchini Miriam K Nanoparticle dispersion containing lactam compound
US10675326B2 (en) 2004-10-07 2020-06-09 The Board Of Trustees Of The University Of Illinois Compositions comprising cupredoxins for treating cancer
KR20070084325A (ko) 2004-11-18 2007-08-24 브리스톨-마이어스 스큅 컴퍼니 익사베필론을 포함하는 장용성 코팅된 비드 및 그의 제조방법
JP2008536479A (ja) 2005-02-11 2008-09-11 ユニバーシティ オブ サザン カリフォルニア ジスルフィド架橋を有するタンパク質の発現法
US8008256B2 (en) * 2006-05-01 2011-08-30 University Of Southern California Combination therapy for treatment of cancer
US8463852B2 (en) * 2006-10-06 2013-06-11 Oracle International Corporation Groupware portlets for integrating a portal with groupware systems
BRPI0718360A2 (pt) 2006-12-04 2013-11-12 Univ Illinois "composições e métodos para o tratamento do câncer com cupredoxinas e dna rico em cpg"
JP2010518123A (ja) 2007-02-08 2010-05-27 ザ・ボード・オブ・トラスティーズ・オブ・ザ・ユニバーシティ・オブ・イリノイ 癌をキュプレドキシンで予防するための組成物および方法
CN101519404B (zh) 2008-02-29 2016-01-20 唐莉 15环噻酮衍生物及其制备方法与应用
US8802394B2 (en) 2008-11-13 2014-08-12 Radu O. Minea Method of expressing proteins with disulfide bridges with enhanced yields and activity
CN102101863B (zh) 2009-12-17 2014-10-15 唐莉 新型环氧噻酮化合物及其制备方法和用途
WO2011153221A1 (en) 2010-06-01 2011-12-08 Plus Chemicals Sa Solid state forms of ixabepilone
US8618146B2 (en) 2011-01-03 2013-12-31 Dr. Reddy's Laboratories Limited Epothilone compound formulations
AU2012207142B2 (en) 2011-01-20 2017-04-27 Board Of Regents, The University Of Texas System MRI markers, delivery and extraction systems, and methods of manufacture and use thereof
JP5926374B2 (ja) 2011-06-10 2016-05-25 メルサナ セラピューティクス，インコーポレイティド タンパク質−高分子−薬剤コンジュゲート
CN102863474A (zh) 2011-07-09 2013-01-09 陈小平 一类治疗细胞增殖性疾病的铂化合物、其制备方法和应用
WO2013008091A1 (en) * 2011-07-13 2013-01-17 Xellia Pharmaceuticals Aps Manufacturing of epothilone derivatives and the use thereof
CN102993239A (zh) 2011-09-19 2013-03-27 陈小平 离去基团含氨基或烷胺基的丁二酸衍生物的铂类化合物
WO2013164102A1 (en) 2012-04-30 2013-11-07 Xellia Pharmaceuticals Aps Process for preparation of ixabepilone and intermediates useful in said process.
CN104768962B (zh) 2012-11-17 2017-04-05 北京市丰硕维康技术开发有限责任公司 离去基团是含氨基或烷氨基的丙二酸衍生物的铂类化合物
JP6334553B2 (ja) 2012-12-10 2018-05-30 メルサナ セラピューティクス，インコーポレイティド タンパク質−高分子−薬剤コンジュゲート
EP2931316B1 (en) 2012-12-12 2019-02-20 Mersana Therapeutics, Inc. Hydroxyl-polymer-drug-protein conjugates
US9309259B2 (en) 2013-03-08 2016-04-12 Scinopharm Taiwan, Ltd. Process for ixabepilone, and intermediates thereof
EP3007692A1 (en) 2013-06-11 2016-04-20 Bayer Pharma Aktiengesellschaft Combinations for the treatment of cancer comprising a mps-1 kinase inhibitor and a mitotic inhibitor
EP3054991B1 (en) 2013-10-11 2019-04-03 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
US10316080B2 (en) 2013-10-11 2019-06-11 Asana Biosciences, Llc Protein-polymer-drug conjugates
WO2015087351A2 (en) * 2013-12-11 2015-06-18 Msn Laboratories Private Limited Process for the preparation of (1s,3s,7s,10r,11s,12s,16r)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-[(1e)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl]-17-oxa-4-azabicyclo[14.1.0]heptadecane-5,9-dione and intermediates thereof
WO2016186744A1 (en) * 2015-05-20 2016-11-24 Pharmaren, Llc Process for the manufacture of ixabepilone
WO2018004338A1 (en) 2016-06-27 2018-01-04 Tagworks Pharmaceuticals B.V. Cleavable tetrazine used in bio-orthogonal drug activation
US11135307B2 (en) 2016-11-23 2021-10-05 Mersana Therapeutics, Inc. Peptide-containing linkers for antibody-drug conjugates
US10772971B2 (en) 2017-06-22 2020-09-15 Mersana Therpeutics, Inc. Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
CA3099419A1 (en) 2018-05-04 2019-11-07 Tagworks Pharmaceuticals B.V. Tetrazines for high click conjugation yield in vivo and high click release yield
EP3788032B1 (en) 2018-05-04 2024-01-24 Tagworks Pharmaceuticals B.V. Compounds comprising a linker for increasing transcyclooctene stability
JP2022513400A (ja) 2018-10-29 2022-02-07 メルサナ セラピューティクス インコーポレイテッド ペプチド含有リンカーを有するシステイン操作抗体－薬物コンジュゲート
JP2022537543A (ja) 2019-06-17 2022-08-26 タグワークス ファーマシューティカルス ビー．ブイ． 高速で且つ効率的なクリック放出の為の化合物
IL289094A (en) 2019-06-17 2022-02-01 Tagworks Pharmaceuticals B V Tetrazines for increasing the speed and yield of the "click release" reaction
EP4399283A2 (en) 2021-09-06 2024-07-17 Veraxa Biotech GmbH Novel aminoacyl-trna synthetase variants for genetic code expansion in eukaryotes
WO2023094525A1 (en) 2021-11-25 2023-06-01 Veraxa Biotech Gmbh Improved antibody-payload conjugates (apcs) prepared by site-specific conjugation utilizing genetic code expansion
EP4186529A1 (en) 2021-11-25 2023-05-31 Veraxa Biotech GmbH Improved antibody-payload conjugates (apcs) prepared by site-specific conjugation utilizing genetic code expansion
WO2023104941A1 (en) 2021-12-08 2023-06-15 European Molecular Biology Laboratory Hydrophilic tetrazine-functionalized payloads for preparation of targeting conjugates
EP4314031B1 (en) 2022-02-15 2024-03-13 Tagworks Pharmaceuticals B.V. Masked il12 protein
WO2024013724A1 (en) 2022-07-15 2024-01-18 Pheon Therapeutics Ltd Antibody-drug conjugates
WO2024080872A1 (en) 2022-10-12 2024-04-18 Tagworks Pharmaceuticals B.V. Strained bicyclononenes
WO2024153789A1 (en) 2023-01-20 2024-07-25 Basf Se Stabilized biopolymer composition, their manufacture and use
WO2024191293A1 (en) 2023-03-10 2024-09-19 Tagworks Pharmaceuticals B.V. Trans-cyclooctene with improved t-linker

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4138042C2 (de) 1991-11-19 1993-10-14 Biotechnolog Forschung Gmbh Epothilone, deren Herstellungsverfahren sowie diese Verbindungen enthaltende Mittel
EP1440973A3 (de) 1995-11-17 2004-10-20 Gesellschaft für biotechnologische Forschung mbH (GBF) Epothilonderivate, Herstellung und Mittel
DE19542986A1 (de) 1995-11-17 1997-05-22 Biotechnolog Forschung Gmbh Epothilon-Derivate und deren Verwendung
DE19639456A1 (de) 1996-09-25 1998-03-26 Biotechnolog Forschung Gmbh Epothilon-Derivate, Herstellung und Mittel
DE19645361A1 (de) 1996-08-30 1998-04-30 Ciba Geigy Ag Zwischenprodukte innerhalb der Totalsynthese von Epothilon A und B, Teil II
DE19645362A1 (de) 1996-10-28 1998-04-30 Ciba Geigy Ag Verfahren zur Herstellung von Epothilon A und B und Derivaten
JP2001500851A (ja) 1996-08-30 2001-01-23 ノバルティス アクチエンゲゼルシャフト エポシロンの製造法および製造過程中に得られる中間生産物
HU229833B1 (en) 1996-11-18 2014-09-29 Biotechnolog Forschung Gmbh Epothilone d production process, and its use as cytostatic as well as phytosanitary agents
US6515016B2 (en) 1996-12-02 2003-02-04 Angiotech Pharmaceuticals, Inc. Composition and methods of paclitaxel for treating psoriasis
DE69734362T2 (de) 1996-12-03 2006-07-20 Sloan-Kettering Institute For Cancer Research Synthese von epothilonen, zwischenprodukte dazu, analoga und verwendungen davon
US6204388B1 (en) 1996-12-03 2001-03-20 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US6380394B1 (en) 1996-12-13 2002-04-30 The Scripps Research Institute Epothilone analogs
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
DE19701758A1 (de) 1997-01-20 1998-07-23 Wessjohann Ludgar A Dr Epothilone-Synthesebausteine
CA2281105A1 (en) 1997-02-25 1998-09-03 Gesellschaft Fur Biotechnologische Forschung Mbh (Gbf) Epothilones with a modified side chain
DE19713970B4 (de) 1997-04-04 2006-08-31 R&D-Biopharmaceuticals Gmbh Epothilone-Synthesebausteine II - Prenylderivate
US6348551B1 (en) 1997-04-18 2002-02-19 Studiengesellschaft Kohle Mbh Selective olefin metathesis of bifunctional or polyfunctional substrates in compressed carbon dioxide as reaction medium
DE19821954A1 (de) 1997-05-15 1998-11-19 Biotechnolog Forschung Gmbh Verfahren zur Herstellung eines Epothilon-Derivats
DE19720312A1 (de) 1997-05-15 1998-11-19 Hoechst Ag Zubereitung mit erhöhter in vivo Verträglichkeit
DE19726627A1 (de) 1997-06-17 1998-12-24 Schering Ag Zwischenprodukte, Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung von Epothilon
US6605599B1 (en) * 1997-07-08 2003-08-12 Bristol-Myers Squibb Company Epothilone derivatives
JP2001510189A (ja) 1997-07-16 2001-07-31 シエーリング アクチエンゲゼルシヤフト チアゾール誘導体、その製造法および使用
DE59814067D1 (de) 1997-08-09 2007-09-06 Bayer Schering Pharma Ag Neue epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung
BR9907647B1 (pt) 1998-02-05 2014-04-01 Novartis Ag Novartis S A Novartis Inc Formulação farmacêutica na forma de um concentrado para infusão, o qual deve ser diluído antes da administração, e solução para infusão
US6194181B1 (en) 1998-02-19 2001-02-27 Novartis Ag Fermentative preparation process for and crystal forms of cytostatics
FR2775187B1 (fr) 1998-02-25 2003-02-21 Novartis Ag Utilisation de l'epothilone b pour la fabrication d'une preparation pharmaceutique antiproliferative et d'une composition comprenant l'epothilone b comme agent antiproliferatif in vivo
NZ506742A (en) 1998-02-25 2003-09-26 Sloan Kettering Inst Cancer Synthesis of desoxyepothilones and hydroxy acid derivative intermediates
WO2000000485A1 (de) 1998-06-30 2000-01-06 Schering Aktiengesellschaft Epothilon-derivate, verfahren zu deren herstellung, zwischenprodukte und ihre pharmazeutische verwendung
NZ511722A (en) 1998-11-20 2004-05-28 Kosan Biosciences Inc Recombinant methods and materials for producing epothilone and epothilone derivatives
AU2795000A (en) 1998-12-22 2000-07-12 Novartis Ag Epothilone derivatives and their use as antitumor agents
PL349863A1 (en) 1999-02-18 2002-09-23 Schering Ag 16-halogen-epothilone derivatives, method for producing them and their pharmaceutical use
US6211412B1 (en) 1999-03-29 2001-04-03 The University Of Kansas Synthesis of epothilones
PE20010116A1 (es) 1999-04-30 2001-02-15 Schering Ag Derivados de 6-alquenil-, 6-alquinil- y 6-epoxi-epotilona, procedimientos para su preparacion

Also Published As

Publication number Publication date
WO1999027890A2 (en) 1999-06-10
CA2312098C (en) 2008-12-30
ZA9810993B (en) 2000-06-01
AU739380B2 (en) 2001-10-11
AR017808A1 (es) 2001-10-24
JP2003522722A (ja) 2003-07-29
CA2312098A1 (en) 1999-06-10
EP1035824A1 (en) 2000-09-20
AU1613499A (en) 1999-06-16
US6365749B1 (en) 2002-04-02
UY25279A1 (es) 1999-07-19
EP1035824A4 (en) 2001-10-24

Similar Documents

Publication Publication Date Title
PE134099A1 (es) Un proceso para la preparacion de intermediarios de epotilona de anillo abierto utiles para la preparacion de analogos de epotilona
PE20011104A1 (es) Un proceso para la preparacion de analogos de epotilona
PE20020721A1 (es) Derivados de quinuclidina como agentes antimuscarinicos m3
GR3015850T3 (en) Substituted dihydroisoquinolinones and related compounds as potentiators of the lethal effects of radiation and certain chemotherapeutic agents; selected compounds, analogs and process.
FI883050A (fi) Menetelmä terapeuttisesti aktiivisten pyranoindolitsinokinoliinijohdannaisten valmistamiseksi
PE20010211A1 (es) Compuestos de tiazol y composiciones farmaceuticas para inhibir las quinasas de proteina
NO168304C (no) Analogifremgangsmaate til fremstilling av terapeutisk aktive 2-(heterocyklyltio)karbapenemderivater
IE811217L (en) Para-substituted 3-phenoxy-1-alkylaminopropan-2-ols having¹beta receptor blocking properties
GB1467138A (en) Acetylene derivatives of amino acids
SE7611047L (sv) Forfarande for framstellning av antibakteriella emnen
FR2619818B1 (fr) Imidazo (1,2-b) pyridazines, procede pour leur preparation et compositions pharmaceutiques les contenant
ATE26273T1 (de) 3-indolcarboxamid-verbindungen.
MX2022015866A (es) Metil 2-(fluorometil)-5-oxo-4-fenil-4,5,6,7-tetrahidro-1h- ciclopenta[b]piridin-3-carboxilatos y metil 2-(fluorometil)-5-oxo- 4-fenil- 1,4,5,7-tetrahidrofuro[3,4-b]piridin-3-carboxilatos como activadores de cav1.2.
KR850008490A (ko) β-락탐 항생물질의 제조방법
DE3274860D1 (en) Triazoloquinazolones and their salts, process and intermediates for preparing them, their use as medicines and compositions containing them
ZA826453B (en) Tricyclic thiazolyloxamic acids and their derivatives,their preparation,and therapeutic agents containing these compounds
GB1306883A (en) Fused ring indole derivatives process for their preparation and therapeutic composition containing same
PE20000244A1 (es) Derivados de 5`-desoxicitidina
DE3362260D1 (en) (-)-15-deoxyspergualin, a process for the preparation of the same, and a pharmaceutical composition containing the same
DE3375784D1 (en) 1,3,4,6,7,11b-hexahydro-7-aryl-2h-pyrazino (2,1-alpha) isoquinolines useful as intermediates and pharmaceutical compounds and methods of preparation
NO163056C (no) Analogifremgangsmaate for fremstilling av terapeutisk aktive pyrazolo (3,4-d) - pyridin-3-on-derivater.
HUT47020A (en) Process for production of stabilly injectable medical compounds containing as active substance 1,4-dihidroxi-5,8-bis/2/2-hidroxi-ethil-amin/-ethil-amin-antraquinon-dihydrochlorid
AR029331A1 (es) Uso de derivados anticonvulsivos para la manufactura de un medicamento en el tratamiento de la bulimia nerviosa
OA09379A (fr) Polyméthylène-imines disubstituées, leur procédé de préparation et les compositions pharmaceutiques les contenant.
EP0229963A3 (en) 4-thienyl-dihydropyridines, process for their preparation and their use as pharmaceutical preparations

Legal Events

Date Code Title Description
FA Abandonment or withdrawal