CU24039B1 - Derivados de imidazolidin-2-ona 1,3-disustituida como inhibidores de cyp17 - Google Patents

Derivados de imidazolidin-2-ona 1,3-disustituida como inhibidores de cyp17

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Publication number
CU24039B1
CU24039B1 CU2011000235A CU20110235A CU24039B1 CU 24039 B1 CU24039 B1 CU 24039B1 CU 2011000235 A CU2011000235 A CU 2011000235A CU 20110235 A CU20110235 A CU 20110235A CU 24039 B1 CU24039 B1 CU 24039B1
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CU
Cuba
Prior art keywords
imidazolidin
ona
derivatives
disposed
cyp17 inhibitors
Prior art date
Application number
CU2011000235A
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English (en)
Other versions
CU20110235A7 (es
Inventor
Mark G Bock
Christoph Gaul
Venkateshwar Rao Gummadi
Saumitra Sengupta
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Novartis Ag
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42357251&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CU24039(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CU20110235A7 publication Critical patent/CU20110235A7/es
Publication of CU24039B1 publication Critical patent/CU24039B1/es

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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención proporciona los compuestos de la fórmula (I), y (II), o una sal farmacéuticamente aceptables de los mismos: ESPACIO PARA LAS FÓRMULAS en donde R50, R51, R52, R53, R54, p, q, r y n son como se definen en la presente, los cuales son útiles como inhibidores de 17alfa-hidroxilasa/liasa-C17,20.
CU2011000235A 2009-06-26 2011-12-19 Derivados de imidazolidin-2-ona 1,3-disustituida como inhibidores de cyp17 CU24039B1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN1500CH2009 2009-06-26
IN2181DE2009 2009-10-21
PCT/EP2010/059029 WO2010149755A1 (en) 2009-06-26 2010-06-24 1, 3-disubstituted imidazolidin-2-one derivatives as inhibitors of cyp 17

Publications (2)

Publication Number Publication Date
CU20110235A7 CU20110235A7 (es) 2012-06-21
CU24039B1 true CU24039B1 (es) 2014-11-27

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CU2011000235A CU24039B1 (es) 2009-06-26 2011-12-19 Derivados de imidazolidin-2-ona 1,3-disustituida como inhibidores de cyp17

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US (3) US8263635B2 (es)
EP (1) EP2445903B1 (es)
JP (1) JP5456891B2 (es)
KR (1) KR101360725B1 (es)
CN (1) CN102803250B (es)
AR (1) AR078228A1 (es)
AU (1) AU2010264698C1 (es)
BR (1) BRPI1015568B8 (es)
CA (1) CA2765983C (es)
CL (1) CL2011003266A1 (es)
CO (1) CO6480927A2 (es)
CR (1) CR20110684A (es)
CU (1) CU24039B1 (es)
CY (1) CY1115426T1 (es)
DK (1) DK2445903T3 (es)
DO (1) DOP2011000399A (es)
EA (1) EA021011B1 (es)
EC (1) ECSP12011625A (es)
ES (1) ES2475945T3 (es)
GE (1) GEP20156250B (es)
HN (1) HN2011003371A (es)
HR (1) HRP20140593T1 (es)
IL (1) IL216741A (es)
JO (1) JO2892B1 (es)
MA (1) MA33451B1 (es)
ME (1) ME01886B (es)
MX (1) MX2011013771A (es)
MY (1) MY155570A (es)
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NZ (1) NZ596488A (es)
PE (1) PE20121048A1 (es)
PL (1) PL2445903T3 (es)
PT (1) PT2445903E (es)
RS (1) RS53384B (es)
SG (1) SG176105A1 (es)
SI (1) SI2445903T1 (es)
SM (1) SMT201400091B (es)
TN (1) TN2011000611A1 (es)
TW (1) TWI492942B (es)
UA (1) UA105794C2 (es)
UY (1) UY32730A (es)
WO (1) WO2010149755A1 (es)
ZA (1) ZA201108373B (es)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2010266018B2 (en) 2009-06-25 2014-01-09 Alkermes Pharma Ireland Limited Heterocyclic compounds for the treatment of neurological and psychological disorders
KR101926320B1 (ko) 2010-08-04 2018-12-06 펠피큐어 파마슈티걸즈 아이엔씨 전립선 암종의 치료를 위한 병용 요법
EP2627648A1 (en) 2010-09-16 2013-08-21 Novartis AG 17aHYDROXYLASE/C17,20-LYASE INHIBITORS
AU2012205601B2 (en) 2011-01-11 2016-03-24 Novartis Ag Combination
MX359399B (es) * 2011-04-28 2018-09-27 Novartis Ag Inhibidores de 17alfa-hidroxilasa/c17-20-liasa.
KR20140054004A (ko) * 2011-08-26 2014-05-08 메이지 세이카 파루마 가부시키가이샤 유해 생물 방제제의 제조방법
WO2013049263A1 (en) * 2011-09-27 2013-04-04 Bristol-Myers Squibb Company Substituted bicyclic heteroaryl compounds
CN102702223A (zh) * 2012-05-28 2012-10-03 盛世泰科生物医药技术(苏州)有限公司 一种2-溴-4-氯噻吩并[3,2-c]吡啶的制备方法
WO2013184621A1 (en) 2012-06-06 2013-12-12 Novartis Ag Combination of a 17 -alpha -hydroxylase (c17, 20 - lyase) inhibitor and a specific pi-3k inhibitor for treating a tumor disease
WO2014158875A1 (en) 2013-03-14 2014-10-02 Pellficure Pharmaceuticals Inc. Novel therapy for prostate carcinoma
TW201534586A (zh) 2013-06-11 2015-09-16 Orion Corp 新穎cyp17抑制劑/抗雄激素劑
JP2016526538A (ja) 2013-06-20 2016-09-05 バイエル・クロップサイエンス・アクチェンゲゼルシャフト 殺ダニ剤及び殺虫剤としてのアリールスルフィド誘導体及びアリールスルホキシド誘導体
MX2016004267A (es) * 2013-10-01 2016-07-08 Novartis Ag Combinacion.
ES2716685T3 (es) 2014-01-24 2019-06-14 Dana Farber Cancer Inst Inc Moléculas de anticuerpo para PD-1 y usos de las mismas
DK3099717T3 (da) 2014-01-31 2019-07-01 Novartis Ag Antistofmolekyler med tim-3 og anvendelser deraf
TWI777174B (zh) 2014-03-14 2022-09-11 瑞士商諾華公司 針對lag-3之抗體分子及其用途
CA2960750A1 (en) 2014-09-12 2016-03-17 Pellficure Pharmaceuticals, Inc. Compositions and methods for treatment of prostate carcinoma
US9783527B2 (en) * 2014-09-16 2017-10-10 Abbvie Inc. Indazole ureas and method of use
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
UY36351A (es) 2014-10-14 2016-06-01 Novartis Ag Moléculas de anticuerpo que se unen a pd-l1 y usos de las mismas
EP3233918A1 (en) 2014-12-19 2017-10-25 Novartis AG Combination therapies
CA2979215A1 (en) 2015-03-10 2016-09-15 Aduro Biotech, Inc. Compositions and methods for activating "stimulator of interferon gene"-dependent signalling
CA2992698A1 (en) 2015-07-17 2017-01-26 Toyama Chemical Co., Ltd. Nitrogen-containing heterocyclic compound
CN108025051B (zh) 2015-07-29 2021-12-24 诺华股份有限公司 包含抗pd-1抗体分子的联合疗法
EP3316902A1 (en) 2015-07-29 2018-05-09 Novartis AG Combination therapies comprising antibody molecules to tim-3
LT3317301T (lt) 2015-07-29 2021-07-26 Novartis Ag Kombinuotos terapijos, apimančios antikūno molekules prieš lag-3
SMT202200118T1 (it) 2015-11-03 2022-05-12 Janssen Biotech Inc Anticorpi che legano specificamente pd-1 e loro usi
ES2986067T3 (es) 2015-12-17 2024-11-08 Novartis Ag Moléculas de anticuerpos frente a PD-1 y usos de las mismas
US11345724B2 (en) 2016-06-06 2022-05-31 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Proteasome inhibitors
WO2017211818A1 (en) * 2016-06-06 2017-12-14 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Proteasome inhibitors
WO2018009466A1 (en) 2016-07-05 2018-01-11 Aduro Biotech, Inc. Locked nucleic acid cyclic dinucleotide compounds and uses thereof
WO2018080933A1 (en) 2016-10-24 2018-05-03 Pellficure Pharmaceuticals Inc. Pharmaceutical compositions of 5-hydroxy-2-methylnaphthalene-1, 4-dione
EP3563851B1 (en) 2016-12-27 2021-04-21 FUJIFILM Corporation Antitumor agent and bromodomain inhibitor
CN108264509B (zh) * 2016-12-30 2021-05-04 复旦大学 取代的苯并噻吩并[2,3-c]四氢吡啶衍生物及其制备方法和用途
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
WO2018237173A1 (en) 2017-06-22 2018-12-27 Novartis Ag Antibody molecules to cd73 and uses thereof
CN111278816B (zh) * 2017-09-04 2024-03-15 C4医药公司 二氢喹啉酮
US11358948B2 (en) * 2017-09-22 2022-06-14 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
WO2019173230A1 (en) 2018-03-05 2019-09-12 Alkermes Pharma Ireland Limited Aripiprazole dosing strategy
BR112020019111A2 (pt) * 2018-03-22 2021-01-12 Aurigene Discovery Technologies Limited Derivados de imidazolidin-2-ona substituída como inibidores de prmt5
TWI869346B (zh) 2018-05-30 2025-01-11 瑞士商諾華公司 Entpd2抗體、組合療法、及使用該等抗體和組合療法之方法
US20210038578A1 (en) 2019-08-08 2021-02-11 Laekna Limited Method of treating cancer
WO2021053559A1 (en) 2019-09-18 2021-03-25 Novartis Ag Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies
TW202321210A (zh) * 2021-07-22 2023-06-01 瑞士商諾華公司 用於治療冠狀病毒相關疾病之化合物及組成物
KR20240136392A (ko) * 2022-01-18 2024-09-13 오리진 온콜로지 리미티드 Malt-1 억제제로서의 치환된 바이사이클릭 헤테로사이클
CN115304591B (zh) * 2022-07-08 2024-10-01 广州中医药大学(广州中医药研究院) 一种桥环甾体合成酶抑制剂及其制备方法和应用
WO2025190395A2 (en) * 2024-03-14 2025-09-18 Pharmaengine, Inc. Mta-cooperative prmt5 inhibitor

Family Cites Families (92)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL39283A (en) 1971-05-03 1976-01-30 Ciba Geigy Ag Substituted 2-oxo or thioxo-3-(5-nitro-imidazol-2-yl)-tetrahydroimidazoles and their manufacture
CH590267A5 (es) * 1972-10-04 1977-07-29 Ciba Geigy Ag
DE2701794A1 (de) * 1976-01-21 1977-07-28 Ciba Geigy Ag Oxigenierte n-aryl-diazacyclen
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
ATE28864T1 (de) 1982-07-23 1987-08-15 Ici Plc Amide-derivate.
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
ZA882717B (en) 1987-04-22 1988-10-17 Merrell Dow Pharmaceuticals Inc. 17beta-(cyclopropylamino)-androst-5-eb-3beta-ol and related compounds useful as c17-20 lyase inhibitors
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
US4966898A (en) 1989-08-15 1990-10-30 Merrell Dow Pharmaceuticals Inc. 4-substituted 17β-(cyclopropylamino)androst-5-en-3β-ol and related compounds useful as C17-20 lyase inhibitors
US5395855A (en) 1990-05-07 1995-03-07 Ciba-Geigy Corporation Hydrazones
WO1992015404A1 (en) 1991-03-01 1992-09-17 S.L. Electrostatic Technology, Inc. Powder coating method for producing circuit board laminae and the like
US5145845A (en) 1991-05-14 1992-09-08 Warner-Lambert Co. Substituted 2-carboxylindoles having pharmaceutical activity
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
US5457102A (en) 1994-07-07 1995-10-10 Janssen Pharmaceutica, N.V. Pyrroloimidazolyl and imidazopyridinyl substituted 1H-benzimidazole derivatives
CZ287434B6 (en) 1992-03-31 2000-11-15 British Tech Group Use of steroids, substituted in position 17, steroids functioning as carcinostatics and pharmaceutical preparation containing thereof
TW225528B (es) 1992-04-03 1994-06-21 Ciba Geigy Ag
EP0666868B2 (en) 1992-10-28 2006-06-14 Genentech, Inc. Use of anti-VEGF antibodies for the treatment of cancer
US5270329A (en) * 1992-12-10 1993-12-14 Eli Lilly And Company Antitumor compositions and methods of treatment
DE4332168A1 (de) * 1993-02-22 1995-03-23 Thomae Gmbh Dr K Cyclische Derivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
GB9310635D0 (en) 1993-05-21 1993-07-07 Glaxo Group Ltd Chemical compounds
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
JP3916092B2 (ja) 1993-09-17 2007-05-16 杏林製薬株式会社 イミダゾリジノン誘導体とその酸付加塩及び老年性痴呆症の治療薬
EP0721943A4 (en) 1993-09-30 1996-09-04 Yamanouchi Pharma Co Ltd AZOLE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
DK0721461T3 (da) 1993-09-30 1999-09-20 Btg Int Ltd Syntese af 17-(3-pyridyl)-steroider
WO1996014090A1 (en) 1994-11-07 1996-05-17 Janssen Pharmaceutica N.V. Compositions comprising carbazoles and cyclodextrins
JPH08176111A (ja) * 1994-12-20 1996-07-09 Kyorin Pharmaceut Co Ltd N,n′−ジ置換エチレンジアミン誘導体及びそれらを用いたn,n′−ジ置換イミダゾリジノン誘導体の製造方法
DE69522717T2 (de) 1995-03-30 2002-02-14 Pfizer Inc., New York Chinazolinderivate
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
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
WO1997000257A1 (en) 1995-06-14 1997-01-03 Yamanouchi Pharmaceutical Co., Ltd. Fused imidazole derivatives and medicinal composition thereof
ATE212993T1 (de) 1995-07-06 2002-02-15 Novartis Erfind Verwalt Gmbh Pyrolopyrimidine und verfahren zu ihrer herstellung
AU1592697A (en) 1995-08-22 1997-03-19 Du Pont Merck Pharmaceutical Company, The Substituted cyclic ureas and derivatives thereof useful as retroviral protease inhibitors
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
HU228446B1 (en) 1996-04-12 2013-03-28 Warner Lambert Co Kinazoline derivatives as irreversible inhibitors of protein-kinase, pharmaceutical compositions containing these compounds and use thereof
CA2254769A1 (en) * 1996-05-20 1997-11-27 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
DE69734513T2 (de) 1996-06-24 2006-07-27 Pfizer Inc. Phenylamino-substituierte tricyclische derivate zur behandlung hyperproliferativer krankheiten
EP0923583A1 (de) 1996-08-30 1999-06-23 Novartis AG Verfahren zur herstellung von epothilonen und zwischenprodukte innerhalb des verfahrens
EP0938597B1 (en) 1996-09-06 2003-08-20 Obducat Aktiebolag Method for anisotropic etching of structures in conducting materials
DE19638745C2 (de) 1996-09-11 2001-05-10 Schering Ag Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR)
WO1998010767A2 (en) 1996-09-13 1998-03-19 Sugen, Inc. 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
ES2312695T3 (es) 1996-11-18 2009-03-01 Gesellschaft Fur Biotechnologische Forschung Mbh (Gbf) Epotilones e y f.
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
EP1028110B1 (en) 1997-10-02 2004-04-14 Daiichi Pharmaceutical Co., Ltd. Novel dihydronaphthalene compounds and process for producing the same
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
IL138113A0 (en) 1998-02-25 2001-10-31 Sloan Kettering Inst Cancer Synthesis of epothilones, intermediates thereto and analogues thereof
CA2328973A1 (en) 1998-04-23 1999-10-28 Akio Ojida Naphthalene derivatives, their production and use
WO2000009495A1 (en) 1998-08-11 2000-02-24 Novartis Ag Isoquinoline derivatives with angiogenesis inhibiting activity
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
US6303342B1 (en) 1998-11-20 2001-10-16 Kason Biosciences, Inc. Recombinant methods and materials for producing epothilones C and D
DK1140173T4 (da) 1998-12-22 2013-06-10 Genentech Inc Vaskulære endothelcellevækstfaktorantagonister og anvendelser deraf
PT1165085E (pt) 1999-03-30 2006-10-31 Novartis Ag Derivados de ftalazina para tratar doencas inflamatorias
CA2396596A1 (en) 2000-01-28 2001-08-02 Bristol-Myers Squibb Company Tetrahydropyrimidone inhibitors of fatty acid binding protein and method
JP2002302488A (ja) * 2000-03-30 2002-10-18 Takeda Chem Ind Ltd 置換1,3−チアゾール化合物、その製造法および用途
NO312876B1 (no) * 2000-07-21 2002-07-15 Balans Man As Regulerbar stol
WO2002020493A2 (en) 2000-09-06 2002-03-14 Chugai Seiyaku Kabushiki Kaisha A traceless solid-phase synthesis of 2-imidazolones
TWI238824B (en) 2001-05-14 2005-09-01 Novartis Ag 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
US20040198773A1 (en) 2001-09-26 2004-10-07 Barry Hart Substituted 3-pyridyl oxazoles as c17,20 lyase inhibitors
GB0200283D0 (en) * 2002-01-08 2002-02-20 Smithkline Beecham Plc Compounds
CA2493458A1 (en) * 2002-07-24 2004-01-29 Ptc Therapeutics, Inc. Ureido substituted benzoic acid compounds, their use for nonsense suppression and the treatment of diseases caused by such mutations
HRP20050252A2 (en) 2002-09-18 2005-10-31 Pfizer Products Inc. Novel imidazole compounds as transforming growth factor (tfg) inhibitors
GB0418900D0 (en) 2004-08-24 2004-09-29 Btg Int Ltd Novel salt forms
WO2006078698A1 (en) 2005-01-19 2006-07-27 Cengent Therapeutics, Inc. 2-imidazolone and 2-imidazolidinone heterocyclic inhibitors of tyrosine phosphatases
EA019560B1 (ru) 2005-03-02 2014-04-30 Юнивесити Оф Мэриленд, Балтимор Способ лечения простаты (варианты)
JPWO2006104280A1 (ja) 2005-03-31 2008-09-11 武田薬品工業株式会社 糖尿病の予防・治療剤
TW200806633A (en) 2006-03-21 2008-02-01 Epix Pharm Inc S1P receptor modulating compounds and use thereof
CA2838089A1 (en) 2006-08-25 2008-02-28 Cougar Biotechnology, Inc. Methods for treating cancer comprising the administration of a vitamin d compound and an additional therapeutic agent, and compositions containing the same
WO2008044700A1 (en) * 2006-10-11 2008-04-17 Takeda Pharmaceutical Company Limited GSK-3β INHIBITOR
US20100035918A1 (en) 2007-01-30 2010-02-11 Biogen Idec Ma Inc Imidazolone Compounds and Methods of Making and Using the Same
WO2008154382A1 (en) 2007-06-06 2008-12-18 University Of Maryland, Baltimore Hdac inhibitors and hormone targeted drugs for the treatment of cancer
CN101084881B (zh) 2007-06-23 2012-08-29 淮北辉克药业有限公司 靶向速释泡腾制剂及其制备方法
WO2009078992A1 (en) * 2007-12-17 2009-06-25 Amgen Inc. Linear tricyclic compounds as p38 kinase inhibitors
CA2712897A1 (en) * 2008-01-30 2009-08-06 Pharmacopeia, Inc. Substituted spirocyclic piperidine derivatives as histamine-3 (h3) receptor ligands
CA2724430A1 (en) * 2008-05-19 2009-11-26 Schering Corporation Heterocyclic compounds as factor ixa inhibitors
MX2011000175A (es) 2008-06-25 2011-06-27 Envivo Pharmaceuticals Inc Compuestos heterociclicos 1,2-di-substituidos.
MX2010014572A (es) 2008-06-27 2011-03-24 Novartis Ag Compuestos organicos.
US20110224187A1 (en) 2008-10-16 2011-09-15 Anandan Palani Pyrrolidine, piperidine and piperazine derivatives and methods of use thereof
WO2010099518A2 (en) 2009-02-27 2010-09-02 Thesis Chemistry, Llc Method for manufacture of 2-oxoimidazolidines
AU2010279398A1 (en) 2009-08-07 2012-03-08 Tokai Pharmaceuticals, Inc. Treatment of prostate cancer
EP2499151A4 (en) 2009-11-13 2013-03-20 Tokai Pharmaceuticals Inc MAMMALIAN STEROID METABOLITES
WO2011088160A2 (en) 2010-01-15 2011-07-21 Biomarin Pharmaceutical Inc. Novel cyp17 inhibitors
GB201002563D0 (en) 2010-02-15 2010-03-31 Cambridge Entpr Ltd Compounds

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