JP5475235B2 - 医薬化合物 - Google Patents

医薬化合物 Download PDF

Info

Publication number
JP5475235B2
JP5475235B2 JP2007551746A JP2007551746A JP5475235B2 JP 5475235 B2 JP5475235 B2 JP 5475235B2 JP 2007551746 A JP2007551746 A JP 2007551746A JP 2007551746 A JP2007551746 A JP 2007551746A JP 5475235 B2 JP5475235 B2 JP 5475235B2
Authority
JP
Japan
Prior art keywords
group
formula
groups
acid
compounds
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 - Fee Related
Application number
JP2007551746A
Other languages
English (en)
Japanese (ja)
Other versions
JP2008528471A5 (enExample
JP2008528471A (ja
Inventor
ジェーン・エリザベス・カリー
ジョン・フランシス・ライオンズ
マシュー・サイモン・スクワイアーズ
ニール・トーマス・トンプソン
カイラ・メリオム・トンプソン
ポール・グレアム・ワイアット
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.)
Astex Therapeutics Ltd
Original Assignee
Astex Therapeutics Ltd
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 Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of JP2008528471A publication Critical patent/JP2008528471A/ja
Publication of JP2008528471A5 publication Critical patent/JP2008528471A5/ja
Application granted granted Critical
Publication of JP5475235B2 publication Critical patent/JP5475235B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D231/38—Nitrogen 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/255—Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
    • 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Microbiology (AREA)
  • Emergency Medicine (AREA)
  • Mycology (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2007551746A 2005-01-21 2006-01-20 医薬化合物 Expired - Fee Related JP5475235B2 (ja)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US64600305P 2005-01-21 2005-01-21
US64621605P 2005-01-21 2005-01-21
US64600105P 2005-01-21 2005-01-21
US64597405P 2005-01-21 2005-01-21
US64598805P 2005-01-21 2005-01-21
US60/646,003 2005-01-21
US60/645,974 2005-01-21
US60/646,216 2005-01-21
US60/646,001 2005-01-21
US60/645,988 2005-01-21
PCT/GB2006/000210 WO2006077428A1 (en) 2005-01-21 2006-01-20 Pharmaceutical compounds

Publications (3)

Publication Number Publication Date
JP2008528471A JP2008528471A (ja) 2008-07-31
JP2008528471A5 JP2008528471A5 (enExample) 2009-03-12
JP5475235B2 true JP5475235B2 (ja) 2014-04-16

Family

ID=35967000

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2007551746A Expired - Fee Related JP5475235B2 (ja) 2005-01-21 2006-01-20 医薬化合物

Country Status (10)

Country Link
US (1) US20090036435A1 (enExample)
EP (1) EP1845973B1 (enExample)
JP (1) JP5475235B2 (enExample)
KR (1) KR101346886B1 (enExample)
AU (1) AU2006207325B2 (enExample)
BR (1) BRPI0606455A (enExample)
CA (1) CA2594477C (enExample)
ES (1) ES2552338T3 (enExample)
MX (1) MX2007008781A (enExample)
WO (1) WO2006077428A1 (enExample)

Families Citing this family (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0412259B1 (pt) * 2003-07-22 2019-08-20 Astex Therapeutics Limited Compostos de 1H-pirazol 3,4-dissubstituídos como moduladores de quinases dependentes de ciclina (CDK), seus usos, processo para a preparação dos mesmos e composição farmacêutica
TW200533657A (en) 2004-02-17 2005-10-16 Esteve Labor Dr Substituted pyrazoline compounds, their preparation and use as medicaments
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
WO2006077424A1 (en) * 2005-01-21 2006-07-27 Astex Therapeutics Limited Pharmaceutical compounds
US20080139620A1 (en) * 2005-01-21 2008-06-12 Astex Therapeutics Limited Pyrazole Derivatives For The Inhibition Of Cdk's And Gsk's
AR052559A1 (es) * 2005-01-21 2007-03-21 Astex Therapeutics Ltd Derivados de pirazol para inhibir cdk's y gsk's
NZ589276A (en) 2005-02-03 2012-06-29 Topotarget Uk Ltd Combination therapies using hdac inhibitors and erlotinib (tarceva)
KR100973386B1 (ko) * 2005-03-03 2010-07-30 미츠비시 레이온 가부시키가이샤 폴리머 입자, 이를 포함하는 수지 조성물, 성형체
EA023400B1 (ru) 2005-05-13 2016-05-31 Топотаргет Юкей Лимитед Фармацевтические составы, содержащие ингибиторы деацетилазы гистонов
US7897589B2 (en) 2005-07-15 2011-03-01 Laboratorios Del Dr. Esteve, S.A. Substituted pyrazoline compounds, their preparation and use as medicaments
EP1743892A1 (en) 2005-07-15 2007-01-17 Laboratorios del Dr. Esteve S.A. Substituted pyrazoline compounds, their preparation and use as medicaments
EP1743890A1 (en) 2005-07-15 2007-01-17 Laboratorios Del Dr. Esteve, S.A. 4,5-Dihydro-1H-pyrazole derivatives, their preparation and use as medicaments
US8828392B2 (en) * 2005-11-10 2014-09-09 Topotarget Uk Limited Histone deacetylase (HDAC) inhibitors (PXD101) for the treatment of cancer alone or in combination with chemotherapeutic agent
EP2027109A1 (en) * 2006-05-05 2009-02-25 Astex Therapeutics Limited 4- (2, 6-dichloro-benzoylamino) -1h-pyrazole-s-carboxylic acid (1-methanesulph0nyl-piperidin-4-yl) -amide for the treatment of cancer
WO2007129062A1 (en) * 2006-05-08 2007-11-15 Astex Therapeutics Limited Pharmaceutical combinations of diazole derivatives for cancer treatment
WO2008007123A2 (en) * 2006-07-14 2008-01-17 Astex Therapeutics Limited Pharmaceutical compounds
US20090263398A1 (en) * 2006-07-14 2009-10-22 Astex Therapeutics Limited Pharmaceutical combinations
CL2008000119A1 (es) 2007-01-16 2008-05-16 Wyeth Corp Compuestos derivados de pirazol, antagonistas del receptor nicotinico de acetilcolina; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como demencia senil, alzheimer y esquizofrenia.
EP2203421B1 (en) * 2007-09-25 2014-05-07 TopoTarget UK Limited Methods of synthesis of certain n-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide compounds
EP2070925A1 (de) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Neue 2-substituierte Tiazol-4-carbonsäureamid-Derivative deren Herstellung und Verwendung als Arzneimittel
EP2070916A1 (de) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft 2-Aryl-thiazol-4-carbonsäureamid-Derivate, deren Herstellung und Verwendung als Arzneimittel
EP2070924A1 (de) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Neue 2-Hetarylthiazol-4-carbonsäureamid-Derivative, deren Herstellung und Verwendung als Arzneimittel
BRPI0821209A2 (pt) 2007-12-19 2019-09-24 Amgen Inc composto, composição farmacêutica, métodos de tratar câncer, para reduzir o tamanho de tumor, para tratar distúrbios, e para reduzir metástase em um tumor.
EP2250160B1 (en) 2008-01-25 2015-11-11 Millennium Pharmaceuticals, Inc. Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
DK2262493T3 (en) * 2008-03-07 2015-04-27 Onxeo Dk Branch Of Onxeo S A France METHODS OF TREATMENT WITH prolonged continuous infusion of Belinostat
US8389533B2 (en) 2008-04-07 2013-03-05 Amgen Inc. Gem-disubstituted and spirocyclic amino pyridines/pyrimidines as cell cycle inhibitors
US9560967B2 (en) 2008-04-24 2017-02-07 The Invention Science Fund I Llc Systems and apparatus for measuring a bioactive agent effect
US9282927B2 (en) 2008-04-24 2016-03-15 Invention Science Fund I, Llc Methods and systems for modifying bioactive agent use
US9649469B2 (en) 2008-04-24 2017-05-16 The Invention Science Fund I Llc Methods and systems for presenting a combination treatment
US20090270688A1 (en) * 2008-04-24 2009-10-29 Searete Llc, A Limited Liability Corporation Of The State Of Delaware Methods and systems for presenting a combination treatment
US9662391B2 (en) 2008-04-24 2017-05-30 The Invention Science Fund I Llc Side effect ameliorating combination therapeutic products and systems
GB0900555D0 (en) * 2009-01-14 2009-02-11 Topotarget As New methods
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2010090716A1 (en) 2009-01-30 2010-08-12 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as pi3k inhibitors
SMT201700231T1 (it) 2009-10-01 2017-07-18 Janssen Pharmaceutica Nv Inibitori del proteasoma per il trattamento di cancro
WO2012021615A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
UY33554A (es) 2010-08-11 2012-02-29 Millennium Pharm Inc Heteroarilos y usos de los mismos
US9062038B2 (en) 2010-08-11 2015-06-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
BR112013009166A2 (pt) 2010-10-13 2016-07-26 Millennium Pharm Inc heteroarilas e uso das mesmas.
PH12013501940A1 (en) 2011-03-23 2015-12-04 Amgen Inc Fused tricyclic dual inhibitors of cdk 4/6 and flt3
WO2013096642A1 (en) * 2011-12-23 2013-06-27 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
CN103012428A (zh) 2013-01-08 2013-04-03 中国药科大学 4-(五元杂环并嘧啶/吡啶取代)氨基-1H-3-吡唑甲酰胺类CDK/Aurora双重抑制剂及其用途
HK1215250A1 (zh) * 2013-01-30 2016-08-19 Bayer Pharma Aktiengesellschaft 氨基取代的异噻唑
SI2970132T1 (sl) 2013-03-14 2021-02-26 Epizyme, Inc. Inhibitorji argininmetiltransferaze in njihove uporabe
US9765035B2 (en) 2013-03-14 2017-09-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US20160031839A1 (en) 2013-03-14 2016-02-04 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9447079B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. PRMT1 inhibitors and uses thereof
WO2014178954A1 (en) 2013-03-14 2014-11-06 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9045455B2 (en) 2013-03-14 2015-06-02 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970135B1 (en) 2013-03-14 2018-07-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
WO2014153214A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyl transferase inhibtors and uses thereof
JP7054622B2 (ja) 2014-07-21 2022-04-14 ノバルティス アーゲー ヒト化抗ｂｃｍａキメラ抗原受容体を使用した癌の処置
WO2016044576A1 (en) * 2014-09-17 2016-03-24 Epizyme, Inc. Salts, co-crystals, amorphous forms, and crystalline forms of an arginine methyltransferase inhibitor
WO2018004290A1 (ko) * 2016-06-30 2018-01-04 한미약품 주식회사 Alk5 억제제로서의 신규 피라졸 유도체 및 이의 용도
KR102434226B1 (ko) 2016-06-30 2022-08-19 한미약품 주식회사 Alk5 억제제로서의 신규 피라졸 유도체 및 이의 용도
KR102466192B1 (ko) 2016-08-23 2022-11-14 에자이 알앤드디 매니지먼트 가부시키가이샤 간세포성 암종의 치료를 위한 조합 요법
RU2764724C2 (ru) 2017-03-16 2022-01-19 ЭИСАЙ Р энд Д МЕНЕДЖМЕНТ КО., ЛТД. Комбинированная терапия для лечения рака молочной железы
CN112203725A (zh) 2018-06-13 2021-01-08 诺华股份有限公司 Bcma嵌合抗原受体及其用途
GB201903546D0 (en) * 2019-03-15 2019-05-01 Ldn Pharma Ltd Cancer treatment

Family Cites Families (107)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2917432A (en) 1954-10-05 1959-12-15 Burroughs Wellcome Co Leukemia treatment
US2848455A (en) 1955-07-18 1958-08-19 Ciba Pharm Prod Inc Alpha-(p-amino-phenyl)-alpha-lower alkyl glutarimides
US2891079A (en) 1959-01-23 1959-06-16 Searle & Co 6-methyl-4, 6-pregnadiene-3, 20-dione and 17alpha-acyloxy derivatives thereof
US3046301A (en) 1959-10-29 1962-07-24 Burroughs Wellcome Co Method of making chlorambucil
BE637389A (enExample) 1962-09-13
US3732340A (en) 1966-07-11 1973-05-08 Asta Werke Ag Chem Fab N',o-propylene phosphoric acid ester diamides
GB1354939A (en) 1971-10-28 1974-06-05 Ici Ltd Process for the manufacture of 1,1,2-triphenylalk-1-enes
US4005063A (en) 1973-10-11 1977-01-25 Abbott Laboratories [Des-gly]10 -GnRH nonapeptide anide analogs in position 6 having ovulation-inducing activity
US3914412A (en) 1973-10-11 1975-10-21 Abbott Lab {8 Des{13 Gly{9 {0 10 -Gn{13 RH nonapeptide amide analogs in position 6 having ovulation-inducing activity
DE2438350C3 (de) 1974-08-09 1979-06-13 Hoechst Ag, 6000 Frankfurt Peptide mit starker LH-RH/FSH-RH-Wirkung, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Zubereitungen
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
US4282361A (en) * 1978-03-16 1981-08-04 Massachusetts Institute Of Technology Synthesis for 7-alkylamino-3-methylpyrazolo [4,3-d]pyrimidines
DE2845574A1 (de) 1978-10-19 1980-04-24 Deutsches Krebsforsch Durch heterocyclische ringe oder alkylreste substituierte analoga von ccnu und verfahren zu deren herstellung
DE3046719C2 (de) 1980-12-11 1983-02-17 Klinge Pharma GmbH, 8000 München 1,1,2-Triphenyl-but-1-en-Derivate, Verfahren zu ihrer Herstellung und Arzneimittel
US4418068A (en) 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
OA07174A (fr) 1981-08-24 1984-04-30 May & Baker Ltd Nouvelles imidazotétrazionones, leur préparation et les médicaments qui les contiennent.
GB2126576B (en) 1982-06-25 1985-06-19 Farmos Group Limited Alkane and alkene derivatives
EP0100172B1 (en) 1982-07-23 1987-08-12 Imperial Chemical Industries Plc Amide derivatives
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US5003011A (en) 1985-04-09 1991-03-26 The Administrators Of The Tulane Educational Fund Therapeutic decapeptides
US4801531A (en) 1985-04-17 1989-01-31 Biotechnology Research Partners, Ltd. Apo AI/CIII genomic polymorphisms predictive of atherosclerosis
US4978672A (en) 1986-03-07 1990-12-18 Ciba-Geigy Corporation Alpha-heterocyclc substituted tolunitriles
JPS62220196A (ja) 1986-03-20 1987-09-28 Kyowa Hakko Kogyo Co Ltd 新規物質ｕｃｎ―０１
IN164232B (enExample) 1986-04-11 1989-02-04 Hoechst India
NZ224714A (en) 1987-06-01 1990-03-27 Janssen Pharmaceutica Nv Substituted benzotriazole derivatives and pharmaceutical compositions
GB8714013D0 (en) 1987-06-16 1987-07-22 Ici Plc (substituted-aralkyl)heterocyclic compounds
EP0308020A3 (en) 1987-09-18 1990-12-05 Merck & Co. Inc. 5-(aryl and heteroaryl)-6-(aryl and heteroaryl)-1,2-dihydro-2-oxo 3-pyridinecarboxylic acids and derivatives thereof
US5002755A (en) * 1988-02-18 1991-03-26 Vanderbilt University Method of controlling nephrotoxicity of anti-tumor plaintum compounds
US5272057A (en) 1988-10-14 1993-12-21 Georgetown University Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase
US5192659A (en) 1989-08-25 1993-03-09 Genetype Ag Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes
US5514664A (en) * 1990-05-26 1996-05-07 Byk Gulden Lomberg Chemische Fabrik Gmbh 1,4-dihydropyridines for application in combatting resistance to drugs
TW295589B (enExample) 1990-08-30 1997-01-11 Hoechst Ag
GB9112859D0 (en) 1991-06-14 1991-07-31 Ici Plc Peptide process
EP1005870B1 (en) 1992-11-13 2009-01-21 Biogen Idec Inc. Therapeutic application of chimeric antibodies to human B lymphocyte restricted differentiation antigen for treatment of B cell lymphoma
US5595721A (en) 1993-09-16 1997-01-21 Coulter Pharmaceutical, Inc. Radioimmunotherapy of lymphoma using anti-CD20
KR100263817B1 (ko) 1993-11-30 2000-08-16 윌리암스 로저 에이 염증치료용 치환 피라졸일벤젠술폰아미드
US5773001A (en) 1994-06-03 1998-06-30 American Cyanamid Company Conjugates of methyltrithio antitumor agents and intermediates for their synthesis
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US5502068A (en) * 1995-01-31 1996-03-26 Synphar Laboratories, Inc. Cyclopropylpyrroloindole-oligopeptide anticancer agents
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
GB9514380D0 (en) 1995-07-13 1995-09-13 Knoll Ag Therapeutic agents
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
US5675024A (en) 1995-11-22 1997-10-07 Allergan Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and 1,2,3,4,-tetrahydroquinoline carboxylic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity
FR2741881B1 (fr) 1995-12-01 1999-07-30 Centre Nat Rech Scient Nouveaux derives de purine possedant notamment des prorietes anti-proliferatives et leurs applications biologiques
AU703203B2 (en) * 1996-01-30 1999-03-18 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997040017A2 (en) 1996-04-19 1997-10-30 Novo Nordisk A/S Modulators of molecules with phosphotyrosine recognition units
EP0910571B1 (en) * 1996-05-03 2005-07-20 Abbott Laboratories Novel antiangiogenic peptides, polynucleotides encoding same and methods for inhibiting angiogenesis
AU724541B2 (en) 1996-06-21 2000-09-21 Allergan, Inc. Substituted tetrahydronaphthalene and dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
CA2744096C (en) 1996-07-31 2013-07-30 Laboratory Corporation Of America Holdings Biomarkers and targets for diagnosis, prognosis and management of prostate disease
EP0827742A1 (en) 1996-09-04 1998-03-11 Vrije Universiteit Brussel Use of histone deacetylase inhibitors for treating fribosis or cirrhosis
US6020357A (en) * 1996-12-23 2000-02-01 Dupont Pharmaceuticals Company Nitrogen containing heteroaromatics as factor Xa inhibitors
DE69839338T2 (de) 1997-02-05 2008-07-10 Warner-Lambert Company Llc Pyrido (2,3-d) pyrimidine und 4-amino-pyrimidine als inhibitoren der zellulären proliferation
US6306393B1 (en) * 1997-03-24 2001-10-23 Immunomedics, Inc. Immunotherapy of B-cell malignancies using anti-CD22 antibodies
GB9719426D0 (en) 1997-09-13 1997-11-12 Johnson Matthey Plc Novel process
SI20324A (sl) 1997-10-27 2001-02-28 Agouron Pharmaceuticals, Inc. Substituirane 4-amino-tiazol-2-il spojine kot cdk inhibitorji
JP2000186092A (ja) * 1998-12-22 2000-07-04 Kyowa Hakko Kogyo Co Ltd Ｕｃｎ−０１の製造法
CA2320730A1 (en) 1998-12-23 2000-07-06 Renhua Li Thrombin or factor xa inhibitors
ATE241621T1 (de) 1999-04-02 2003-06-15 Bristol Myers Squibb Pharma Co Arylsulfonyle als faktor xa inhibitoren
EP1169038B9 (en) 1999-04-15 2013-07-10 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
FR2795726A1 (fr) 1999-06-30 2001-01-05 Aventis Cropscience Sa Nouveaux pyrazoles fongicides
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
IL148698A0 (en) 1999-09-17 2002-09-12 Cor Therapeutics Inc INHIBITORS OF FACTOR Xa
US6632815B2 (en) * 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
MY125768A (en) 1999-12-15 2006-08-30 Bristol Myers Squibb Co N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
HN2001000008A (es) 2000-01-21 2003-12-11 Inc Agouron Pharmaceuticals Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo
EP1254115A2 (en) 2000-02-11 2002-11-06 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators for treating respiratory and non-respiratory diseases
WO2001064642A2 (en) 2000-02-29 2001-09-07 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
WO2001068585A1 (en) * 2000-03-14 2001-09-20 Fujisawa Pharmaceutical Co., Ltd. Novel amide compounds
AU4262901A (en) 2000-03-29 2001-10-08 Cyclacel Ltd 2-substituted 4-heteroaryl-pyrimidines and their use in the treatmetn of proliferative disorders
JP2004507455A (ja) 2000-04-25 2004-03-11 ブリストル−マイヤーズ　スクイブ　カンパニー サイクリン依存性キナーゼ阻害剤としての、５−チオ−、スルフィニル−およびスルホニルピラゾロ［３，４−ｂ］−ピリジンの用途
US6414013B1 (en) 2000-06-19 2002-07-02 Pharmacia & Upjohn S.P.A. Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
WO2002000651A2 (en) 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Factor xa inhibitors
JP2004524277A (ja) 2000-10-20 2004-08-12 ブリストル−マイヤーズ スクイブ ファーマ カンパニー アシルセミカルバジド及びサイクリン依存性キナーゼ（ｃｄｋ）阻害剤としてのその使用
US6455559B1 (en) 2001-07-19 2002-09-24 Pharmacia Italia S.P.A. Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents
DE60120494T2 (de) 2000-12-22 2006-12-21 Ortho-Mcneil Pharmaceutical, Inc. Substituieten triazoldiamin derivaten und ihre verwendung als kinase inhibitoren
US7105682B2 (en) * 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6995162B2 (en) * 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
US20050119305A1 (en) * 2001-03-21 2005-06-02 Masao Naka Il-6 production inhibitors
US6905669B2 (en) * 2001-04-24 2005-06-14 Supergen, Inc. Compositions and methods for reestablishing gene transcription through inhibition of DNA methylation and histone deacetylase
WO2002092002A2 (en) * 2001-05-11 2002-11-21 The Burnham Institute Screening, diagnostic and therapeutic methods relating to riz
PL367130A1 (en) 2001-05-29 2005-02-21 Schering Aktiengesellschaft Cdk inhibiting pyrimidines, production thereof and their use as medicaments
US20030078232A1 (en) 2001-08-08 2003-04-24 Elfatih Elzein Adenosine receptor A3 agonists
EP1421077A4 (en) 2001-08-31 2004-11-17 Univ Connecticut NEW PYRAZOLANALOGS ON CANNABINOID RECEPTORS
CA2466375A1 (en) 2001-11-08 2003-05-15 Pharmacia & Upjohn Company Azabicyclic-substituted-heteroaryl compounds for the treatment of disease
SE0104462D0 (sv) 2001-12-29 2001-12-29 Carlbiotech Ltd As Peptide purifcation (Peptidrening)
CN101001857B (zh) * 2002-01-22 2011-06-22 沃尼尔·朗伯有限责任公司 2-(吡啶-2-基氨基)-吡啶并[2,3-d]嘧啶-7-酮
EP2266552A3 (en) * 2002-03-04 2011-03-02 Merck HDAC Research, LLC Methods of inducing terminal differentiation
US6995168B2 (en) * 2002-05-31 2006-02-07 Euro-Celtique S.A. Triazaspiro compounds useful for treating or preventing pain
US7015227B2 (en) 2002-06-21 2006-03-21 Cgi Pharmaceuticals, Inc. Certain amino-substituted monocycles as kinase modulators
EP1539756B1 (en) * 2002-09-19 2007-11-14 Schering Corporation Imidazopyridines as cyclin dependent kinase inhibitors
WO2004039795A2 (en) 2002-10-29 2004-05-13 Fujisawa Pharmaceutical Co., Ltd. Amide compounds for the treatment of hyperlipidemia
US20050026877A1 (en) * 2002-12-03 2005-02-03 Novacea, Inc. Pharmaceutical compositions comprising active vitamin D compounds
US7169797B2 (en) * 2003-02-14 2007-01-30 Abbott Laboratories Protein-tyrosine phosphatase inhibitors and uses thereof
US7320989B2 (en) * 2003-02-28 2008-01-22 Encysive Pharmaceuticals, Inc. Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
BRPI0412259B1 (pt) * 2003-07-22 2019-08-20 Astex Therapeutics Limited Compostos de 1H-pirazol 3,4-dissubstituídos como moduladores de quinases dependentes de ciclina (CDK), seus usos, processo para a preparação dos mesmos e composição farmacêutica
RU2377988C2 (ru) * 2004-02-20 2010-01-10 Новартис Вэксинес Энд Дайэгностикс, Инк. Модуляция воспалительных и метастатических процессов
EP1725528B1 (en) * 2004-03-11 2013-05-29 4Sc Ag Sulphonylpyrroles as hdac inhibitors
US20080139620A1 (en) * 2005-01-21 2008-06-12 Astex Therapeutics Limited Pyrazole Derivatives For The Inhibition Of Cdk's And Gsk's
WO2006077424A1 (en) * 2005-01-21 2006-07-27 Astex Therapeutics Limited Pharmaceutical compounds
WO2006077425A1 (en) * 2005-01-21 2006-07-27 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors and further antitumor agents
AR054425A1 (es) * 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
AR052559A1 (es) * 2005-01-21 2007-03-21 Astex Therapeutics Ltd Derivados de pirazol para inhibir cdk's y gsk's

Also Published As

Publication number Publication date
CA2594477C (en) 2016-07-12
AU2006207325B2 (en) 2012-08-16
ES2552338T3 (es) 2015-11-27
MX2007008781A (es) 2007-09-11
KR20070107045A (ko) 2007-11-06
JP2008528471A (ja) 2008-07-31
CA2594477A1 (en) 2006-07-27
BRPI0606455A (pt) 2008-03-11
WO2006077428A1 (en) 2006-07-27
KR101346886B1 (ko) 2014-01-02
US20090036435A1 (en) 2009-02-05
EP1845973B1 (en) 2015-08-12
AU2006207325A1 (en) 2006-07-27
EP1845973A1 (en) 2007-10-24

Similar Documents

Publication Publication Date Title
JP5475235B2 (ja) 医薬化合物
JP5475234B2 (ja) 医薬化合物
JP2008528469A (ja) ピラゾールキナーゼ阻害剤およびさらなる抗癌剤の組合せ剤
JP4681548B2 (ja) ３，４−ジ置換１ｈ−ピラゾール化合物および、そのサイクリン依存性キナーゼ（ｃｄｋ）およびグリコーゲン・シンセターゼ・キナーゼ−３（ｇｓｋ−３）調節剤としての使用
US8404718B2 (en) Combinations of pyrazole kinase inhibitors
JP2009536186A (ja) 癌処置のためのジアゾール誘導体の医薬組合せ
ES2539480T3 (es) Compuestos 1H-pirazol 3,4-disustituidos y su uso como moduladores de las quinasas dependientes de ciclina (CDK) y glucógeno sintasa quinasa-3 (GSK-3)
CN101146531A (zh) 药物化合物
HK1090041B (en) 3,4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20090113

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20090120

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20120327

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20120531

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20120607

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120926

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20121218

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130214

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130221

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130618

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130723

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20131018

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20140128

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20140206

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees