JP5528807B2 - 複合薬剤 - Google Patents

複合薬剤 Download PDF

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Publication number
JP5528807B2
JP5528807B2 JP2009531918A JP2009531918A JP5528807B2 JP 5528807 B2 JP5528807 B2 JP 5528807B2 JP 2009531918 A JP2009531918 A JP 2009531918A JP 2009531918 A JP2009531918 A JP 2009531918A JP 5528807 B2 JP5528807 B2 JP 5528807B2
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Prior art keywords
group
phenyl
dihydro
dihydroxy
isopropyl
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Expired - Fee Related
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JP2009531918A
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Japanese (ja)
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JP2010505932A (ja
JP2010505932A5 (https=
Inventor
ニール、ジェームス、ギャラガー
ジョン、フランシス、ライアンズ
ニール、トーマス、トンプソン
スティーブン、マレー、ユール
クリストファー、ウィリアム、マレー
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Astex Therapeutics Ltd
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Astex Therapeutics Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
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    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P31/14Antivirals for RNA viruses
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    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • AHUMAN NECESSITIES
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    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
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    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
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    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
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    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • C07D215/04Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/08Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
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    • C07D401/04Heterocyclic 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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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/08Bridged systems
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    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Biotechnology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
JP2009531918A 2006-10-12 2007-10-12 複合薬剤 Expired - Fee Related JP5528807B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US82922106P 2006-10-12 2006-10-12
US60/829,221 2006-10-12
PCT/GB2007/003891 WO2008044045A1 (en) 2006-10-12 2007-10-12 Pharmaceutical combinations

Publications (3)

Publication Number Publication Date
JP2010505932A JP2010505932A (ja) 2010-02-25
JP2010505932A5 JP2010505932A5 (https=) 2011-12-15
JP5528807B2 true JP5528807B2 (ja) 2014-06-25

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Family Applications (1)

Application Number Title Priority Date Filing Date
JP2009531918A Expired - Fee Related JP5528807B2 (ja) 2006-10-12 2007-10-12 複合薬剤

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Country Link
US (1) US8883790B2 (https=)
EP (1) EP2073807A1 (https=)
JP (1) JP5528807B2 (https=)
WO (1) WO2008044045A1 (https=)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
MX2007008008A (es) 2004-12-30 2007-11-12 Astex Therapeutics Ltd Compuestos de pirazol que modulan la actividad de las cinasas cdk, gsk y aurora.
JP5154406B2 (ja) 2005-04-13 2013-02-27 アステックス、セラピューティックス、リミテッド 医薬化合物
US8399442B2 (en) * 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
US7754725B2 (en) 2006-03-01 2010-07-13 Astex Therapeutics Ltd. Dihydroxyphenyl isoindolymethanones
JP5523829B2 (ja) * 2006-06-29 2014-06-18 アステックス、セラピューティックス、リミテッド 複合薬剤
EP2043635A2 (en) * 2006-06-29 2009-04-08 Astex Therapeutics Limited Pharmaceutical combinations
EP2073807A1 (en) 2006-10-12 2009-07-01 Astex Therapeutics Limited Pharmaceutical combinations
JP5518478B2 (ja) * 2006-10-12 2014-06-11 アステックス、セラピューティックス、リミテッド 医薬化合物
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
JP5410285B2 (ja) * 2006-10-12 2014-02-05 アステックス、セラピューティックス、リミテッド 医薬化合物
GB0620259D0 (en) 2006-10-12 2006-11-22 Astex Therapeutics Ltd Pharmaceutical compounds
GB0806527D0 (en) 2008-04-11 2008-05-14 Astex Therapeutics Ltd Pharmaceutical compounds
CA2759083A1 (en) 2009-04-30 2010-11-04 Novartis Ag Imidazole derivatives and their use as modulators of cyclin dependent kinases
US10774278B2 (en) * 2013-02-27 2020-09-15 Mitsubishi Heavy Industries Engineering, Ltd. CO shift catalyst, CO shift reaction apparatus, and method for purifying gasified gas
AU2015210833B2 (en) 2014-02-03 2019-01-03 Vitae Pharmaceuticals, Llc Dihydropyrrolopyridine inhibitors of ROR-gamma
JP6564029B2 (ja) 2014-10-14 2019-08-21 ヴァイティー ファーマシューティカルズ,エルエルシー Ror−ガンマのジヒドロピロロピリジン阻害剤
US9845308B2 (en) 2014-11-05 2017-12-19 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ROR-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
DK3331876T3 (da) 2015-08-05 2021-01-11 Vitae Pharmaceuticals Llc Modulators of ror-gamma
MA53943A (fr) 2015-11-20 2021-08-25 Vitae Pharmaceuticals Llc Modulateurs de ror-gamma
TWI757266B (zh) 2016-01-29 2022-03-11 美商維它藥物有限責任公司 ROR-γ調節劑
US9481674B1 (en) 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
EP3568128B1 (en) * 2017-01-12 2022-07-06 The University of Kansas Hsp90b n-terminal isoform-selective inhibitors
CN115650976A (zh) 2017-07-24 2023-01-31 生命医药有限责任公司 RORγ的抑制剂
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA

Family Cites Families (240)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1973A (en) 1841-02-10 Method oe cowstettctiitg clocks
US2802005A (en) 1957-08-06 S-eluorourace
US2512572A (en) 1950-06-20 Substituted pteridines and method
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
US3116282A (en) 1960-04-27 1963-12-31 Upjohn Co Pyrimidine nucleosides and process
BE637389A (https=) 1962-09-13
US3432549A (en) 1965-04-22 1969-03-11 Egyt Gyogyszervegyeszeti Gyar Pharmacologically active new substituted benzamides
US3732340A (en) 1966-07-11 1973-05-08 Asta Werke Ag Chem Fab N',o-propylene phosphoric acid ester diamides
US3803124A (en) 1968-04-12 1974-04-09 Farmaceutici It Soc Process for the preparation of adriamycin and adriamycinone and adriamycin derivatives
CH527207A (de) 1968-05-08 1972-08-31 Ceskoslovenska Akademie Ved Verfahren zur Herstellung von 1-Glycosyl-5-azacytosinen
GB1235022A (en) 1969-06-04 1971-06-09 Laeaeke Ag A new method for the production of cyclophosphamide
CH526500A (de) 1969-12-31 1972-08-15 Hoffmann La Roche Verfahren zur Herstellung von Polyenverbindungen
DE2124023C3 (de) 1970-05-27 1980-07-10 Richter Gedeon Vegyeszeti Gyar R.T., Budapest Verfahren zur selektiven Gewinnung von Vinblastin, Vinleurosin und Vincristin oder von deren Sulfaten
GB1354939A (en) 1971-10-28 1974-06-05 Ici Ltd Process for the manufacture of 1,1,2-triphenylalk-1-enes
JPS4910506A (https=) 1972-05-31 1974-01-30
CH605550A5 (https=) 1972-06-08 1978-09-29 Research Corp
AR204004A1 (es) 1973-04-02 1975-11-12 Lilly Co Eli Procedimientos para preparar derivados de vinblastina leurosidina y leurocristina
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
US4005063A (en) 1973-10-11 1977-01-25 Abbott Laboratories [Des-gly]10 -GnRH nonapeptide anide analogs in position 6 having ovulation-inducing activity
GB1457632A (en) 1974-03-22 1976-12-08 Farmaceutici Italia Adriamycins
US4020270A (en) 1974-05-02 1977-04-26 Societa' Farmaceutici Italia S.P.A. L-lyxohex-1-enopyranose derivative
GB1467383A (en) 1974-06-12 1977-03-16 Farmaceutici Italia Daunomycin analogues
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
JPS6041077B2 (ja) 1976-09-06 1985-09-13 喜徳 喜谷 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体
US4197249A (en) 1977-08-15 1980-04-08 American Cyanamid Company 1,4-Bis(substituted-amino)-5,8-dihydroxyanthraquinones and leuco bases thereof
US4307100A (en) 1978-08-24 1981-12-22 Agence Nationale De Valorisation De La Recherche (Anvar) Nor bis-indole compounds usable as medicaments
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
US4357324A (en) 1981-02-24 1982-11-02 The United States Of America As Represented By The Department Of Health And Human Services Prodrug derivatives of 9β-D-arabinofuranosyl-2-fluoroadenine
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
ATE28864T1 (de) 1982-07-23 1987-08-15 Ici Plc Amide-derivate.
EP0111058B1 (en) 1982-11-26 1987-11-04 Nippon Kayaku Kabushiki Kaisha Process for producing 4'-demethyl-epipodophyllotoxin-beta-d-ethylidene-glucoside and acyl-derivative thereof
US4526988A (en) 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
JPS6019790A (ja) 1983-07-14 1985-01-31 Yakult Honsha Co Ltd 新規なカンプトテシン誘導体
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
US4582909A (en) * 1984-02-02 1986-04-15 Warner-Lambert Company Benzobicyclic lactam acids and derivatives as cognition activators
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4760064A (en) * 1984-12-18 1988-07-26 Otsuka Pharmaceutical Co., Ltd. Carbostyril compounds, compositions containing same and processes for preparing same
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
US4691918A (en) 1985-10-08 1987-09-08 Diversified Products Corporation Multiple exercise device
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 (https=) 1986-04-11 1989-02-04 Hoechst India
FR2601675B1 (fr) 1986-07-17 1988-09-23 Rhone Poulenc Sante Derives du taxol, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2601676B1 (fr) 1986-07-17 1988-09-23 Rhone Poulenc Sante Procede de preparation du taxol et du desacetyl-10 taxol
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
US5004758A (en) 1987-12-01 1991-04-02 Smithkline Beecham Corporation Water soluble camptothecin analogs useful for inhibiting the growth of animal tumor cells
KR0143565B1 (ko) 1988-06-13 1998-07-15 사노 가즈오 피발산의 p-치환된 페닐 에스테르 유도체, 그의 제조 방법 및 이를 포함하는 조성물.
US4990511A (en) 1988-08-03 1991-02-05 Takeda Chemical Industries, Ltd. Amide compounds, their production and use
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
GB8926560D0 (en) 1989-11-24 1990-01-17 Zambeletti Spa L Pharmaceuticals
IL96531A (en) 1989-12-11 1995-08-31 Univ Princeton History of Acid N- (Diomeric-H1-Pyrolo] D-2,3 [Pyrimidine-3-Ilacyl (-glutamic, preparation and pharmaceutical preparations containing them)
US5124350A (en) * 1990-06-28 1992-06-23 G. D. Searle & Co. Leukotriene b4 antagonists
US5177064A (en) 1990-07-13 1993-01-05 University Of Florida Targeted drug delivery via phosphonate derivatives
ZA916555B (en) 1990-08-27 1993-04-28 Lilly Co Eli Method of treating inflammatory bowel disease
TW295589B (https=) 1990-08-30 1997-01-11 Hoechst Ag
FR2669029B1 (fr) 1990-11-14 1994-09-02 Adir Nouveaux derives de la n-benzoyl proline, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
MX9102128A (es) 1990-11-23 1992-07-08 Rhone Poulenc Rorer Sa Derivados de taxano,procedimiento para su preparacion y composicion farmaceutica que los contiene
US5280046A (en) 1991-02-22 1994-01-18 The University Of Colorado Foundation, Inc. Method of treating type I diabetes
WO1992017467A1 (en) 1991-04-06 1992-10-15 Dr Lo. Zambeletti S.P.A. Substituted azacyclic compounds, process for their preparation and their use as analgesics
GB9112859D0 (en) 1991-06-14 1991-07-31 Ici Plc Peptide process
EP1400536A1 (en) 1991-06-14 2004-03-24 Genentech Inc. Method for making humanized antibodies
IT1250692B (it) 1991-07-23 1995-04-21 Procedimento per la preparazione di demetilepipodofillotossina- beta-d-glucosidi.
TW225528B (https=) 1992-04-03 1994-06-21 Ciba Geigy Ag
ATE195716T1 (de) 1992-04-22 2000-09-15 Ligand Pharm Inc Retinoid-x rezeptor selektive verbindungen
DE4222910A1 (de) 1992-07-11 1994-01-13 Asta Medica Ag Neue Phospholipidderivate
AU687727B2 (en) 1992-10-28 1998-03-05 Genentech Inc. Vascular endothelial cell growth factor antagonists
DK0752248T3 (da) 1992-11-13 2000-11-13 Idec Pharma Corp Terapeutisk anvendelse af kimæriske og radioaktivt mærkede antistoffer mod humant B-lymfocytbegrænset differentieringsantig
US5466861A (en) 1992-11-25 1995-11-14 Sri International Bridged bicyclic aromatic compounds and their use in modulating gene expression of retinoid receptors
US5595721A (en) 1993-09-16 1997-01-21 Coulter Pharmaceutical, Inc. Radioimmunotherapy of lymphoma using anti-CD20
DE69422306T4 (de) 1993-11-30 2000-09-07 G.D. Searle & Co., Chicago Substituierte pyrazolyl-benzolsulfonamide zur behandlung von entzündungen
US5773001A (en) 1994-06-03 1998-06-30 American Cyanamid Company Conjugates of methyltrithio antitumor agents and intermediates for their synthesis
US5476932A (en) 1994-08-26 1995-12-19 Hoffmann-La Roche Inc. Process for producing N4-acyl-5'-deoxy-5-fluorocytidine derivatives
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US5633283A (en) 1995-01-23 1997-05-27 Eli Lilly And Company Method for treating multiple sclerosis
DE69536015D1 (de) 1995-03-30 2009-12-10 Pfizer Prod Inc Chinazolinone Derivate
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
JPH11507535A (ja) 1995-06-07 1999-07-06 イムクローン システムズ インコーポレイテッド 腫瘍の成長を抑制する抗体および抗体フラグメント類
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
EP0951541B1 (en) 1995-07-31 2005-11-30 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate disease
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
US5663357A (en) 1995-11-22 1997-09-02 Allergan Substituted heteroarylamides 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
JP3855026B2 (ja) 1996-01-16 2006-12-06 富士レビオ株式会社 アミド誘導体の製造方法
AU709113B2 (en) 1996-01-29 1999-08-19 Regents Of The University Of California, The Method for treating sexual dysfunctions
GB9606187D0 (en) 1996-03-23 1996-05-29 Inst Of Food Research Production of vanillin
WO1997036876A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU714477B2 (en) 1996-04-19 2000-01-06 Regents Of The University Of California, The Treatment of mood/affective disorders by glutamatergic upmodulators
IL118657A0 (en) 1996-06-14 1996-10-16 Arad Dorit Inhibitors for picornavirus proteases
JP2000511558A (ja) 1996-06-21 2000-09-05 アラーガン・セイルズ・インコーポレイテッド レチノイドおよび/またはレチノイド拮抗剤様生物学的活性を有する置換テトラヒドロナフタレンおよびジヒドロナフタレン誘導体
US5723632A (en) 1996-08-08 1998-03-03 Mgi Pharma, Inc. Total synthesis of antitumor acylfulvenes
EP0827742A1 (en) 1996-09-04 1998-03-11 Vrije Universiteit Brussel Use of histone deacetylase inhibitors for treating fribosis or cirrhosis
WO1998033798A2 (en) 1997-02-05 1998-08-06 Warner Lambert Company Pyrido[2,3-d]pyrimidines and 4-amino-pyrimidines as inhibitors of cell proliferation
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
EP0973778A1 (en) 1997-03-07 2000-01-26 Novo Nordisk A/S 4,5,6,7-TETRAHYDRO-THIENO 3,2-c]PYRIDINE DERIVATIVES, THEIR PREPARATION AND USE
UY24949A1 (es) 1997-04-08 2001-04-30 Smithkline Beecham Corp Compuestos calcilíticos
EP0975614A1 (en) 1997-04-18 2000-02-02 Smithkline Beecham Plc A bicyclic aryl or a bicyclic heterocyclic ring containing compounds having a combined 5ht1a, 5ht1b and 5ht1d receptor antagonistic activity
US6235883B1 (en) 1997-05-05 2001-05-22 Abgenix, Inc. Human monoclonal antibodies to epidermal growth factor receptor
US6329368B1 (en) 1997-05-09 2001-12-11 The Regents Of The University Of California Endocrine modulation with positive modulators of AMPA type glutamate receptors
GB9719426D0 (en) 1997-09-13 1997-11-12 Johnson Matthey Plc Novel process
DK1026950T3 (da) 1997-10-27 2006-06-26 Univ California Behandling af skizofreni med ampakiner og neuroleptika
AU1804299A (en) 1997-12-08 1999-06-28 Glycomed Incorporated Sialyl lewis x and sialyl lewis a glycomimetics
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
EP1140840B1 (en) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
EP1165492A1 (en) 1999-03-30 2002-01-02 Pharmacor Inc. Hydroxyphenyl derivatives with hiv integrase inhibitory properties
EP1169038B9 (en) 1999-04-15 2013-07-10 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
US6166244A (en) 1999-05-07 2000-12-26 Allergan Sales, Inc. Oxygen, sulfur and nitrogen substituted cyclohexene and cyclohexane derivatives having retinoid-like biological activity
US6127382A (en) 1999-08-16 2000-10-03 Allergan Sales, Inc. Amines substituted with a tetrahydroquinolinyl group an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
CZ20021428A3 (cs) 1999-10-27 2002-11-13 Cytokinetics, Inc. Způsoby a kompozice vyuľívající chinazoliny
US6545004B1 (en) 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
KR100881105B1 (ko) 1999-11-05 2009-02-02 아스트라제네카 아베 Vegf 억제제로서의 퀴나졸린 유도체
DE19955283A1 (de) 1999-11-17 2001-05-23 Aventis Res & Tech Gmbh & Co Verfahren zur enantioselektiven Gewinnung von Aminosäuren und Aminosäurederivaten unter Verwendung von Racemisierungskatalysatoren
US6677473B1 (en) 1999-11-19 2004-01-13 Corvas International Inc Plasminogen activator inhibitor antagonists
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
AU2001243158A1 (en) 2000-02-18 2001-08-27 Merck And Co., Inc. Inhibitors of prenyl-protein transferase
WO2001064194A2 (en) 2000-02-29 2001-09-07 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations with camptothecin compounds
US6613917B1 (en) 2000-03-23 2003-09-02 Allergan, Inc. Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity
ATE310728T1 (de) * 2000-05-11 2005-12-15 Bristol Myers Squibb Co Tetrahydroisochinolin-analoga als wachstumshormon-sekretagoga
US7229986B2 (en) * 2000-05-16 2007-06-12 Takeda Pharmaceutical Company Ltd. Melanin-concentrating hormone antagonist
DE10024939A1 (de) 2000-05-19 2001-11-29 Bayer Ag Neue Diphenylmethanderivate für Arzneimittel
CA2308994A1 (en) * 2000-05-19 2001-11-19 Aegera Therapeutics Inc. Neuroprotective compounds
IL136458A0 (en) 2000-05-30 2001-06-14 Peptor Ltd Protein kinase inhibitors
IL153246A0 (en) 2000-06-28 2003-07-06 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors
AU2001273071B2 (en) 2000-06-30 2005-09-08 Glaxo Group Limited Quinazoline ditosylate salt compounds
FR2812876B1 (fr) * 2000-08-08 2002-09-27 Galderma Res & Dev Nouveaux composes bi-aromatiques activateurs des recepteurs de type ppar-gamma et leur utilisation dans des compositions cosmetiques ou pharmaceutiques
DK1320531T3 (da) 2000-08-10 2011-01-03 Pfizer Italia Srl Bicyclo-pyrazoler, der er aktive som kinase inhibitorer, fremgangsmåde til fremstilling deraf og farmaceutiske sammensætninger, der indeholder disse
SK2072003A3 (en) 2000-08-25 2004-01-08 Warner Lambert Co Process for making N-aryl-anthranilic acids and their derivatives
DE60115069T2 (de) 2000-09-11 2006-08-03 Chiron Corp., Emeryville Chinolinonderivate als tyrosin-kinase inhibitoren
AU2002217866A1 (en) 2000-11-06 2002-05-15 The Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services Geldanamycin derivatives useful for the treatment of cancer
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
JP4224566B2 (ja) 2000-12-18 2009-02-18 株式会社医薬分子設計研究所 炎症性サイトカイン産生遊離抑制剤
US6989385B2 (en) 2000-12-21 2006-01-24 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
MXPA03005777A (es) 2000-12-22 2005-02-14 Johnson & Johnson Derivados de triazol diaminas sustituidos como inhibidores de cinasa.
CA2440809A1 (en) 2001-03-01 2002-09-12 Conforma Therapeutics Corp. Methods for treating genetically-defined proliferative disorders with hsp90 inhibitors
BR0209774A (pt) 2001-05-29 2004-06-01 Schering Ag Pirimidinas inibidoras de cdk, sua preparação e aplicação como medicamento
AU2002330998A1 (en) 2001-08-06 2003-02-24 Kosan Biosciences, Inc. Benzoquinone ansamycins
CA2460498A1 (en) 2001-09-24 2003-04-03 Conforma Therapeutics Corporation Process for preparing 17-allyl amino geldanamycin (17-aag) and other ansamycins
WO2003051877A1 (en) 2001-12-18 2003-06-26 Bayer Corporation 2-substituted pyrrolo[2.1-a]isoquinolines against cancer
CN1620294A (zh) 2001-12-20 2005-05-25 Osi药物公司 嘧啶a2b选择性拮抗剂化合物,它们的合成及用途
ATE374753T1 (de) 2001-12-21 2007-10-15 Vernalis Cambridge Ltd 3-(2,4)dihydroxyphenyl-4-phenylpyrazole und deren medizinische verwendung
SE0104462D0 (sv) 2001-12-29 2001-12-29 Carlbiotech Ltd As Peptide purifcation (Peptidrening)
WO2003061385A1 (en) 2002-01-17 2003-07-31 Ribapharm Inc. Tricyclic nucleoside library compounds, synthesis, and use as antiviral agents
AU2002316231A1 (en) 2002-02-19 2003-09-29 Xenoport, Inc. Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
AU2003223491A1 (en) 2002-04-05 2003-10-27 Nitromed, Inc. Nitric oxide donors, compositions and methods of use
WO2003091255A1 (en) 2002-04-26 2003-11-06 Warner-Lambert Company Llc Inhibitors of checkpoint kinases (wee1 and chk1)
CN101103977A (zh) 2002-06-05 2008-01-16 株式会社医药分子设计研究所 糖尿病治疗药
CN1658854A (zh) 2002-06-05 2005-08-24 株式会社医药分子设计研究所 免疫关联蛋白激酶抑制剂
EP1512396A4 (en) 2002-06-05 2008-12-31 Inst Med Molecular Design Inc HEMMER AGAINST ACTIVATION OF AP-1 AND NFAT
EA009701B1 (ru) 2002-06-06 2008-02-28 Инститьют Оф Медисинал Молекьюлар Дизайн. Инк. Противоаллергические средства
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
SE0202133D0 (sv) 2002-07-08 2002-07-08 Astrazeneca Ab Novel compounds
CA2393720C (en) 2002-07-12 2010-09-14 Eli Lilly And Company Crystalline 2,5-dione-3-(1-methyl-1h-indol-3-yl)-4-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1h-indol-3-yl]-1h-pyrrole mono-hydrochloride
WO2004007501A1 (en) 2002-07-16 2004-01-22 Amura Therapeutics Limited Biologically active compounds
US6800655B2 (en) 2002-08-20 2004-10-05 Sri International Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents
WO2004035571A1 (en) * 2002-10-15 2004-04-29 Rigel Pharmaceuticals, Inc. Substituted indoles and their use as hcv inhibitors
AU2003302589A1 (en) 2002-12-02 2004-06-23 Kyukyu Pharmaceutical Co., Ltd. Method for producing orally administrable edible agent of laminate film form and pressure bonding apparatus of the agent.
TWI228885B (en) * 2003-01-23 2005-03-01 Mediatek Inc Method for controlling a mobile communication device to enter a power-saving mode and to recover timing after the mobile communication device leaves the power-saving mode
SI1611112T1 (sl) 2003-02-11 2012-12-31 Vernalis (R&D) Limited Izoksazolne spojine kot inhibitorji vroäśinskih ĺ ok proteinov
CA2514500A1 (en) * 2003-02-20 2004-09-10 University Of Connecticut Health Center Methods for using compositions comprising heat shock proteins or alpha-2-macroglobulin in the treatment of cancer and infectious disease
MXPA05008878A (es) 2003-02-21 2005-10-05 Pfizer Derivados de aminotiazol sustituidos con cicloalquilo que contiene n y composiciones farmaceuticas para inhibir la proliferacion celular, y metodos para su uso.
JP3876265B2 (ja) 2003-02-26 2007-01-31 ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト ジヒドロプテリジノン、その製造方法及び薬物形態での使用
US7038038B2 (en) 2003-03-17 2006-05-02 Pharmion Corporation Synthesis of 5-azacytidine
US6943249B2 (en) 2003-03-17 2005-09-13 Ash Stevens, Inc. Methods for isolating crystalline Form I of 5-azacytidine
US6887855B2 (en) 2003-03-17 2005-05-03 Pharmion Corporation Forms of 5-azacytidine
AU2004226586B2 (en) 2003-04-03 2008-12-11 Pfizer Inc. Dosage forms comprising AG013736
MXPA05011597A (es) 2003-04-30 2005-12-15 Novartis Ag Derivados de aminopropanol como moduladores del receptor 1-fosfato de esfingosina.
GB0315111D0 (en) 2003-06-27 2003-07-30 Cancer Rec Tech Ltd Substituted 5-membered ring compounds and their use
AU2004251949B2 (en) 2003-06-27 2009-05-07 Kyowa Hakko Kirin Co., Ltd. Hsp90 family protein inhibitors
TWI312345B (en) * 2003-06-30 2009-07-21 Mitsubishi Tanabe Pharma Corp Process of preparating 3-acylaminobenzofuran-2-carboxylic acid derivatives
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
JPWO2005007151A1 (ja) * 2003-07-16 2006-08-31 株式会社医薬分子設計研究所 皮膚色素沈着の治療剤
CA2532965C (en) 2003-07-22 2013-05-14 Astex Therapeutics Limited 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
DE602004027504D1 (de) 2003-07-24 2010-07-15 Leo Pharma As Aminobenzophenonverbindungen
ATE403654T1 (de) 2003-07-28 2008-08-15 Janssen Pharmaceutica Nv Benzimidazol-, benzothiazol- und benzoxazolderivate und deren verwendung als lta4h-modulatoren
DE10335584B4 (de) 2003-07-31 2006-06-29 Philipps-Universität Marburg Verfahren zur Herstellung zyklischer Moleküle
DE10335726A1 (de) * 2003-08-05 2005-03-03 Bayer Cropscience Gmbh Verwendung von Hydroxyaromaten als Safener
WO2005016889A1 (en) 2003-08-08 2005-02-24 Virginia Commonwealth University Compounds having antiestrogenic and tissue selective estrogenic properties
WO2005023818A2 (en) 2003-09-10 2005-03-17 Gpc Biotech Ag Heterobicyclic compounds as pharmaceutically active agents
JP4845736B2 (ja) 2003-10-14 2011-12-28 アリゾナ ボード オブ リージェンツ オン ビハーフ ザ ユニバーシティー オブ アリゾナ プロテインキナーゼ阻害剤
WO2005037214A2 (en) 2003-10-14 2005-04-28 Intermune, Inc. Macrocyclic carboxylic acids and acylsulfonamides as inhibitors of hcv replication
US20050209247A1 (en) 2003-11-07 2005-09-22 Chiron Corporation Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties
KR20060123292A (ko) 2003-11-10 2006-12-01 쉐링 악티엔게젤샤프트 Ccr-5 길항제로서 유용한 벤질에테르 아민 화합물
CN101693031A (zh) 2003-11-18 2010-04-14 诺瓦提斯公司 Kit突变形式的抑制剂
AU2004309395C1 (en) 2003-12-23 2012-10-04 Infinity Discovery, Inc. Analogs of benzoquinone-containing ansamycins for the treatment of cancer
JPWO2005063222A1 (ja) 2003-12-26 2007-07-19 協和醗酵工業株式会社 Hsp90ファミリー蛋白質阻害剤
US7652146B2 (en) 2004-02-06 2010-01-26 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-carboxamides useful as kinase inhibitors
TWI338004B (en) 2004-02-06 2011-03-01 Bristol Myers Squibb Co Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
US20050256097A1 (en) 2004-05-11 2005-11-17 Kosan Biosciences, Inc. Pharmaceutical solution formulations containing 17-AAG
AU2005243175B2 (en) 2004-05-14 2011-12-01 Millennium Pharmaceuticals, Inc. Compounds and methods for inhibiting mitotic progression by inhibition of Aurora kinase
US7351709B2 (en) * 2004-06-09 2008-04-01 Wyeth Estrogen receptor ligands
US20060014949A1 (en) 2004-07-13 2006-01-19 Supergen Inc. Compositions and formulations of decitabine polymorphs and methods of use thereof
WO2006015123A1 (en) 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US20060035903A1 (en) 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
US7728134B2 (en) 2004-08-14 2010-06-01 Boehringer Ingelheim International Gmbh Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament
US7759485B2 (en) 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
AU2005277223C1 (en) 2004-08-20 2009-05-21 The Regents Of The University Of Michigan Small molecule inhibitors of anti-apoptotic Bcl-2 family members and the uses thereof
US20060069060A1 (en) 2004-09-27 2006-03-30 Sanjeev Redkar Salts of decitabine
US20060067953A1 (en) 2004-09-29 2006-03-30 Conforma Therapeutics Corporation Oral pharmaceutical formulations and methods for producing and using same
DE102004049078A1 (de) 2004-10-08 2006-04-13 Merck Patent Gmbh Phenylpyrazole
US7208630B2 (en) 2004-10-27 2007-04-24 University Of Kansas Heat shock protein 90 inhibitors
WO2006050333A2 (en) 2004-11-02 2006-05-11 The Regents Of The University Of California Methods and compositions for modulating apoptosis
WO2006048746A2 (en) 2004-11-02 2006-05-11 Pfizer Inc. Methods for the removal of heavy metals
KR20070058689A (ko) 2004-11-02 2007-06-08 화이자 인코포레이티드 인다졸 화합물의 제조 방법
WO2006051808A1 (ja) 2004-11-09 2006-05-18 Kyowa Hakko Kogyo Co., Ltd. Hsp90ファミリー蛋白質阻害剤
EP1817295B1 (en) 2004-11-18 2012-11-07 Synta Pharmaceuticals Corp. Triazole compounds that modulate hsp90 activity
MX2007008008A (es) * 2004-12-30 2007-11-12 Astex Therapeutics Ltd Compuestos de pirazol que modulan la actividad de las cinasas cdk, gsk y aurora.
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.
DE602006010665D1 (en) * 2005-02-07 2010-01-07 Hoffmann La Roche Heterocyclsche substituierte phenylmethanone als inhibitoren des glycintransporters 1
US20060183902A1 (en) * 2005-02-15 2006-08-17 Baxter Ellen W Dihydroindolyl methanones as alpha 1a/1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms
US20090042883A1 (en) 2005-02-21 2009-02-12 Kyowa Hakkokogyo Co. Antitumor agent
JP5154406B2 (ja) * 2005-04-13 2013-02-27 アステックス、セラピューティックス、リミテッド 医薬化合物
JP2008540395A (ja) * 2005-05-03 2008-11-20 ファイザー・インク アミドレソルシノール化合物
DK2444079T3 (en) 2005-05-17 2017-01-30 Sarcode Bioscience Inc Compositions and Methods for the Treatment of Eye Diseases
WO2007050124A1 (en) 2005-05-19 2007-05-03 Xenon Pharmaceuticals Inc. Fused piperidine derivatives and their uses as therapeutic agents
US7425633B2 (en) * 2005-08-26 2008-09-16 National Health Research Institutes Pyrrolidine compounds
US8399442B2 (en) 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
US7785275B2 (en) * 2006-01-31 2010-08-31 Cook Incorporated Wire guide having distal coupling tip
US7754725B2 (en) * 2006-03-01 2010-07-13 Astex Therapeutics Ltd. Dihydroxyphenyl isoindolymethanones
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
EP2073807A1 (en) 2006-10-12 2009-07-01 Astex Therapeutics Limited Pharmaceutical combinations
JP5410285B2 (ja) 2006-10-12 2014-02-05 アステックス、セラピューティックス、リミテッド 医薬化合物
EP2073802A1 (en) 2006-10-12 2009-07-01 Astex Therapeutics Limited Pharmaceutical combinations
JP5518478B2 (ja) * 2006-10-12 2014-06-11 アステックス、セラピューティックス、リミテッド 医薬化合物
GB0620259D0 (en) * 2006-10-12 2006-11-22 Astex Therapeutics Ltd Pharmaceutical compounds
WO2008053319A1 (en) 2006-10-30 2008-05-08 Pfizer Products Inc. Amide resorcinol compounds
DK2233011T3 (da) * 2008-06-11 2013-05-27 Morinaga Milk Industry Co Ltd Fremgangsmåde til fremstilling af fermenteret mælk

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