IN2012DN01693A - - Google Patents

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Publication number
IN2012DN01693A
IN2012DN01693A IN1693DEN2012A IN2012DN01693A IN 2012DN01693 A IN2012DN01693 A IN 2012DN01693A IN 1693DEN2012 A IN1693DEN2012 A IN 1693DEN2012A IN 2012DN01693 A IN2012DN01693 A IN 2012DN01693A
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IN
India
Prior art keywords
compounds
independently
heteroarylic
mdm4
mdm2
Prior art date
Application number
Inventor
Guido Bold
Pascal Furet
Francois Gessier
Joerg Kallen
Lisztwann Joanna Hergovich
Keiichi Masuya
Andrea Vaupel
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Novartis Ag
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Publication of IN2012DN01693A publication Critical patent/IN2012DN01693A/en

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/84—Sulfur atoms
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    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/88—Nitrogen atoms, e.g. allantoin
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    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
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    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
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    • C07F9/6503—Five-membered rings
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Molecular Biology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The invention relates to tetra-substituted heteroarylic compounds of the formula (I) wherein X1, X3 and X4 are independently C or N, Y is C-H, N-H or N, wherein the total number of nitrogen atoms represented by X1, X3, X4 and Y is 1 or 2; rings A and B are independently selected from phenyl or pyridyl; R1, R4, R', R", n and m are as defined herein. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
IN1693DEN2012 2009-08-26 2010-08-24 IN2012DN01693A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23710709P 2009-08-26 2009-08-26
PCT/EP2010/062300 WO2011023677A1 (en) 2009-08-26 2010-08-24 Tetra-substituted heteroaryl compounds and their use as mdm2 and/or mdm4 modulators

Publications (1)

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IN2012DN01693A true IN2012DN01693A (en) 2015-06-05

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Country Status (12)

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US (1) US20120149661A1 (en)
EP (1) EP2470502A1 (en)
JP (1) JP2013503129A (en)
KR (1) KR20120050492A (en)
CN (1) CN102574785A (en)
AU (1) AU2010288534A1 (en)
BR (1) BR112012008075A2 (en)
CA (1) CA2771936A1 (en)
EA (1) EA201200321A1 (en)
IN (1) IN2012DN01693A (en)
MX (1) MX2012002420A (en)
WO (1) WO2011023677A1 (en)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2118123B1 (en) 2007-01-31 2015-10-14 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
WO2008121767A2 (en) 2007-03-28 2008-10-09 President And Fellows Of Harvard College Stitched polypeptides
BR112012008849A2 (en) 2009-10-14 2015-09-22 Schering Corp compound, pharmaceutical composition, and use of a compound
JO2998B1 (en) 2010-06-04 2016-09-05 Amgen Inc Piperidinone derivatives as mdm2 inhibitors for the treatment of cancer
WO2012021876A2 (en) 2010-08-13 2012-02-16 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
MX352672B (en) 2011-09-27 2017-12-04 Amgen Inc Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer.
AU2012326026B2 (en) 2011-10-18 2017-04-13 Aileron Therapeutics, Inc. Peptidomimetic macrocyles
CN102503930B (en) * 2011-10-28 2014-07-02 浙江大学 3, 4, 5-tri-substituted aminothiopene chemical compound and preparation and application thereof
US8987274B2 (en) 2011-10-28 2015-03-24 Merck Sharp & Dohme Corp Macrocycles that increase p53 activity and the uses thereof
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
US9062071B2 (en) 2011-12-21 2015-06-23 Merck Sharp & Dohme Corp. Substituted piperidines as HDM2 inhibitors
US8987414B2 (en) 2012-02-15 2015-03-24 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
KR102112373B1 (en) 2012-02-15 2020-05-18 에일러론 테라퓨틱스 인코포레이티드 Peptidomimetic macrocycles
WO2013123349A1 (en) 2012-02-16 2013-08-22 Dow Agrosciences Llc Methods of producing sulfilimine compounds
JP6171003B2 (en) * 2012-05-24 2017-07-26 ノバルティス アーゲー Pyrrolopyrrolidinone compounds
SG11201503052RA (en) 2012-11-01 2015-05-28 Aileron Therapeutics Inc Disubstituted amino acids and methods of preparation and use thereof
WO2014100065A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
US11407721B2 (en) 2013-02-19 2022-08-09 Amgen Inc. CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer
MX368703B (en) 2013-02-28 2019-10-11 Amgen Inc A benzoic acid derivative mdm2 inhibitor for the treatment of cancer.
CA2906538C (en) 2013-03-14 2021-02-02 Ana Gonzalez Buenrostro Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer
AU2014267360B2 (en) 2013-05-14 2018-07-05 Active Biotech Ab N-(heteroaryl)-sulfonamide derivatives useful as S100-inhibitors
JOP20200296A1 (en) 2013-06-10 2017-06-16 Amgen Inc Processes of Making and Crystalline Forms of a MDM2 Inhibitor
WO2016049359A1 (en) 2014-09-24 2016-03-31 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
CN107106642B (en) 2014-09-24 2021-02-26 艾瑞朗医疗公司 Peptidomimetic macrocycles and formulations thereof
EP3206683A4 (en) 2014-10-16 2018-06-13 The Board of Trustees of the Leland Stanford Junior University Novel methods, compounds, and compositions for anesthesia
AU2016235424A1 (en) 2015-03-20 2017-10-05 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
CN108368161A (en) 2015-09-10 2018-08-03 艾瑞朗医疗公司 Peptidomimetic macrocyclic compound as MCL-1 conditioning agents
WO2017201449A1 (en) 2016-05-20 2017-11-23 Genentech, Inc. Protac antibody conjugates and methods of use
PL3904350T3 (en) 2018-04-12 2024-02-19 Bayer Aktiengesellschaft N-(cyclopropylmethyl)-5-(methylsulfonyl)-n-{1-[1-(pyrimidin-2-yl)-1h-1,2,4-triazol-5-yl]ethyl}benzamide derivatives and the corresponding pyridine-carboxamide derivatives as pesticides
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same
MX2024006752A (en) * 2021-12-08 2024-07-29 Ishihara Sangyo Kaisha Ltd Hydrate crystal of 5-chloro-4-(3-chloro-4-methylphenyl)-1h-imidaz ole-2-carbonitrile.
US11932607B1 (en) 2023-10-27 2024-03-19 King Faisal University 4-(2,4,5-tris(4-chlorophenyl)-1H-imidazol-1-yl)benzoic acid as an antimicrobial compound

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
ATE28864T1 (en) 1982-07-23 1987-08-15 Ici Plc AMIDE DERIVATIVES.
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
US5010099A (en) 1989-08-11 1991-04-23 Harbor Branch Oceanographic Institution, Inc. Discodermolide compounds, compositions containing same and method of preparation and use
US5395855A (en) 1990-05-07 1995-03-07 Ciba-Geigy Corporation Hydrazones
SG54187A1 (en) * 1990-12-26 1998-11-16 American Cyanamid Co Process for the preparation of 2-aryl-1- substituted-5-(trifluromethyl) pyrrole compounds useful as insecticidal acaricidal and nematocidal agents and as intermediates for the mac of saic ag
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
TW225528B (en) 1992-04-03 1994-06-21 Ciba Geigy Ag
DE69233803D1 (en) 1992-10-28 2011-03-31 Genentech Inc Use of vascular endothelial growth factor antagonists
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
EP3103799B1 (en) 1995-03-30 2018-06-06 OSI Pharmaceuticals, LLC Quinazoline derivatives
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
CA2224435C (en) 1995-07-06 2008-08-05 Novartis Ag Pyrrolopyrimidines and processes for the preparation thereof
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
IL126351A0 (en) 1996-04-12 1999-05-09 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
JP2000512990A (en) 1996-06-24 2000-10-03 ファイザー・インク Phenylamino-substituted tricyclic derivatives for treating hyperproliferative diseases
CA2259149A1 (en) 1996-07-05 1998-01-15 Novartis Ag Inhibitors of the interaction between p53 and mdm2
NZ334821A (en) 1996-08-30 2000-12-22 Novartis Ag Method for producing epothilones
DE69724269T2 (en) 1996-09-06 2004-06-09 Obducat Ab METHOD FOR ANISOTROPE ETCHING STRUCTURES IN CONDUCTIVE MATERIALS
DE19638745C2 (en) 1996-09-11 2001-05-10 Schering Ag Monoclonal antibodies against the extracellular domain of the human VEGF receptor protein (KDR)
CA2265630A1 (en) 1996-09-13 1998-03-19 Gerald Mcmahon Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
DK1367057T3 (en) 1996-11-18 2009-01-19 Biotechnolog Forschung Gmbh Epothilones E and F
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
CO4950519A1 (en) 1997-02-13 2000-09-01 Novartis Ag PHTHALAZINES, PHARMACEUTICAL PREPARATIONS THAT UNDERSTAND THEM AND THE PROCESS FOR THEIR PREPARATION
GEP20033053B (en) * 1997-05-22 2003-08-25 Searle & Co Substituted Pyrazoles as P38 Kinase Inhibitors, Methods for their Production, Pharmaceutical Compositions Containing Them and Methods for Treatment
CO4940418A1 (en) 1997-07-18 2000-07-24 Novartis Ag MODIFICATION OF A CRYSTAL OF A DERIVATIVE OF N-PHENYL-2-PIRIMIDINAMINE, PROCESSES FOR ITS MANUFACTURE AND USE
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
US6194181B1 (en) 1998-02-19 2001-02-27 Novartis Ag Fermentative preparation process for and crystal forms of cytostatics
CA2322157C (en) 1998-02-25 2012-05-29 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
BR9912938B1 (en) 1998-08-11 2011-06-28 isoquinoline derivatives, composition comprising them, process for preparation and use thereof.
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
UA71587C2 (en) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Anthranilic acid amides and use thereof as medicaments
EP1135470A2 (en) 1998-11-20 2001-09-26 Kosan Biosciences, Inc. Recombinant methods and materials for producing epothilone and epothilone derivatives
EP2016953A3 (en) 1998-12-22 2009-04-15 Genentech, Inc. Vascular endothelial cell growth factor antagonists and uses thereof
PT1165085E (en) 1999-03-30 2006-10-31 Novartis Ag DERIVATIVES OF FTALAZINE TO TREAT INFLAMMATORY DISEASES
PE20020354A1 (en) 2000-09-01 2002-06-12 Novartis Ag HYDROXAMATE COMPOUNDS AS HISTONE-DESACETILASE (HDA) INHIBITORS
AR035885A1 (en) 2001-05-14 2004-07-21 Novartis Ag DERIVATIVES OF 4-AMINO-5-FENIL-7-CYCLLOBUTILPIRROLO (2,3-D) PYRIMIDINE, A PROCESS FOR ITS PREPARATION, A PHARMACEUTICAL COMPOSITION AND THE USE OF SUCH DERIVATIVES FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
WO2003051359A1 (en) * 2001-12-18 2003-06-26 F.Hoffmann-La Roche Ag Cis-2,4,5- triphenyl-imidazolines and their use in the treatment of tumors
JP2007524596A (en) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド Co-crystal pharmaceutical composition
JP4643570B2 (en) * 2003-06-17 2011-03-02 エフ．ホフマン−ラ ロシュ アーゲー Cis-imidazolines as MDM2 inhibitors
US20050026983A1 (en) 2003-07-30 2005-02-03 Pfizer Inc Imidazole compounds and uses thereof
BRPI0508532A (en) 2004-03-08 2007-08-07 Wyeth Corp Ion channel modulators
JP2007527920A (en) 2004-03-08 2007-10-04 ワイス Ion channel modulator
US20060160869A1 (en) * 2005-01-05 2006-07-20 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
RU2411238C2 (en) * 2005-03-16 2011-02-10 Ф.Хоффманн-Ля Рош Аг Cis-2,4,5-triarylimidazolines and use thereof as anticancer medicinal agents
BRPI0619236A2 (en) * 2005-12-01 2011-09-20 Hoffmann La Roche 2,4,5-triphenyl imidazoline derivatives, pharmaceutical composition comprising them, use and process for their synthesis
KR101015073B1 (en) * 2006-01-18 2011-02-16 에프. 호프만-라 로슈 아게 Cis-4,5-biaryl-2-heterocyclic-imidazolines as mdm2 inhibitors
EP2053046A1 (en) * 2007-10-26 2009-04-29 Syngeta Participations AG Novel imidazole derivatives
PE20091953A1 (en) * 2008-05-08 2010-01-09 Du Pont SUBSTITUTED AZOLS AS FUNGICIDES

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