ECSP12011625A - 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

Info

Publication number
ECSP12011625A
ECSP12011625A EC2012011625A ECSP12011625A ECSP12011625A EC SP12011625 A ECSP12011625 A EC SP12011625A EC 2012011625 A EC2012011625 A EC 2012011625A EC SP12011625 A ECSP12011625 A EC SP12011625A EC SP12011625 A ECSP12011625 A EC SP12011625A
Authority
EC
Ecuador
Prior art keywords
imidazolidin
ona
derivatives
disposed
cyp17 inhibitors
Prior art date
Application number
EC2012011625A
Other languages
English (en)
Inventor
Mark G Bock
Christoph Gaul
Saumitra Sengupta
Venkateshwar Rao Gummadi
Original Assignee
Novartis Ag
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
Family has litigation
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=ECSP12011625(A) "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 ECSP12011625A publication Critical patent/ECSP12011625A/es

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    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/454—Non 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (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)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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, en donde R53, R54, p, q, y n son como se definen en la presente. Se ha encontrado que los compuestos de la presente invención son útiles como inhibidores de 17?-hidroxilasa/liasa-C17,20.
EC2012011625A 2009-06-26 2012-01-26 Derivados de imidazolidin-2-ona 1,3-disustituida como inhibidores de cyp17 ECSP12011625A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1500CH2009 2009-06-26
IN2181DE2009 2009-10-21

Publications (1)

Publication Number Publication Date
ECSP12011625A true ECSP12011625A (es) 2012-02-29

Family

ID=42357251

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2012011625A ECSP12011625A (es) 2009-06-26 2012-01-26 Derivados de imidazolidin-2-ona 1,3-disustituida como inhibidores de cyp17

Country Status (43)

Country Link
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)
NI (1) NI201100223A (es)
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
PT2445502T (pt) 2009-06-25 2017-09-22 Alkermes Pharma Ireland Ltd Compostos heterocíclicos para o tratamento de distúrbios neurológicos e psicológicos
KR101594660B1 (ko) 2010-08-04 2016-02-16 펠피큐어 파마슈티걸즈 아이엔씨 전립선 암종의 치료를 위한 병용 요법
EP2627648A1 (en) 2010-09-16 2013-08-21 Novartis AG 17aHYDROXYLASE/C17,20-LYASE INHIBITORS
BR112013017722A2 (pt) 2011-01-11 2016-07-12 Glaxosmithkline Llc combinação
MX359399B (es) * 2011-04-28 2018-09-27 Novartis Ag Inhibidores de 17alfa-hidroxilasa/c17-20-liasa.
HUE056549T2 (hu) * 2011-08-26 2022-02-28 Meiji Seika Pharma Co Ltd Eljárás kártevõirtószer elõállítására
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
CA2872541A1 (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
AU2014241816B9 (en) 2013-03-14 2019-02-14 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
BR112015031155A2 (pt) 2013-06-20 2017-07-25 Bayer Cropscience Ag derivados de sulfureto de arila e derivados de aril sulfóxido como acaricidas e inseticidas
MX2016004267A (es) * 2013-10-01 2016-07-08 Novartis Ag Combinacion.
UA122479C2 (uk) 2014-01-24 2020-11-25 Дана-Фарбер Кенсер Інстітьют, Інк. Виділена молекула антитіла, яка зв’язується з людським білком програмованої смерті-1 (pd-1)
PL3099717T3 (pl) 2014-01-31 2019-10-31 Novartis Ag Cząsteczki przeciwciała dla TIM-3 i ich zastosowanie
EA201691765A1 (ru) 2014-03-14 2016-12-30 Новартис Аг Молекулы антител против lag-3 и их применения
WO2016040896A1 (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
SG11201702401RA (en) 2014-10-14 2017-04-27 Novartis Ag Antibody molecules to pd-l1 and uses thereof
EP3233918A1 (en) 2014-12-19 2017-10-25 Novartis AG Combination therapies
TWI706958B (zh) 2015-03-10 2020-10-11 美商艾杜諾生物科技公司 活化「干擾素基因刺激因子」依賴性訊息傳導之組合物及方法
HK1249105A1 (zh) 2015-07-17 2018-10-26 富士胶片富山化学株式会社 含氮杂环化合物
US20180207273A1 (en) 2015-07-29 2018-07-26 Novartis Ag Combination therapies comprising antibody molecules to tim-3
EP3328418A1 (en) 2015-07-29 2018-06-06 Novartis AG Combination therapies comprising antibody molecules to pd-1
US20180340025A1 (en) 2015-07-29 2018-11-29 Novartis Ag Combination therapies comprising antibody molecules to lag-3
PT3370768T (pt) 2015-11-03 2022-04-21 Janssen Biotech Inc Anticorpos que se ligam especificamente ao pd-1 e seus usos
CN108495651A (zh) 2015-12-17 2018-09-04 诺华股份有限公司 抗pd-1的抗体分子及其用途
CA3026564A1 (en) * 2016-06-06 2017-12-14 Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften E.V. Proteasome inhibitors
CN109563126B (zh) * 2016-06-06 2023-06-16 马克斯-普朗克科学促进学会 蛋白酶体抑制剂
EP3507367A4 (en) 2016-07-05 2020-03-25 Aduro BioTech, Inc. CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS 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
US20200172628A1 (en) 2017-06-22 2020-06-04 Novartis Ag Antibody molecules to cd73 and uses thereof
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
WO2019060693A1 (en) * 2017-09-22 2019-03-28 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
AU2019230014B2 (en) 2018-03-05 2024-11-28 Alkermes Pharma Ireland Limited Aripiprazole dosing strategy
KR102767362B1 (ko) * 2018-03-22 2025-02-13 오리진 온콜로지 리미티드 Prmt5 억제제로서 치환된 이미다졸리딘-2-온 유도체
UY38247A (es) 2018-05-30 2019-12-31 Novartis Ag Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación
KR20220047589A (ko) * 2019-08-08 2022-04-18 래크나 리미티드 암 치료 방법
JP2022548881A (ja) 2019-09-18 2022-11-22 ノバルティス アーゲー Ｅｎｔｐｄ２抗体、組合せ療法並びに抗体及び組合せ療法を使用する方法
UY39863A (es) * 2021-07-22 2023-02-28 Novartis Ag Compuestos y composiciones para el tratamiento de enfermedades relacionadas con el coronavirus
JP2025503727A (ja) * 2022-01-18 2025-02-04 オーリジーン オンコロジー リミテッド Ｍａｌｔ－１阻害剤としての置換二環式複素環関連出願の相互参照 この出願は、２０２２年１月１８日に提出されたインド仮特許出願第２０２２４１００２８５９号に対する優先権を主張する。この仮出願の全内容は、参照により本明細書に組み込まれる。
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
CH590266A5 (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
DE3372965D1 (en) 1982-07-23 1987-09-17 Ici Plc Amide derivatives
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
EP0573534B1 (en) 1991-03-01 1998-12-23 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
ES2138618T3 (es) 1992-03-31 2000-01-16 Btg Int Ltd Esteroides 17-sustituidos utiles en el tratamiento del cancer.
TW225528B (es) 1992-04-03 1994-06-21 Ciba Geigy Ag
KR100335584B1 (ko) 1992-10-28 2002-11-29 제넨테크, 인코포레이티드 혈관내피세포성장인자에대한길항제
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 AZOL DERIVATIVES AND PHARMACEUTICAL PREPARATIONS
ES2127413T3 (es) 1993-09-30 1999-04-16 Btg Int Ltd Sintesis de esteroides 17-(3-piridilo).
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
ATE446955T1 (de) 1995-03-30 2009-11-15 Pfizer Prod Inc Chinazolinone derivate
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
AU6015796A (en) 1995-06-14 1997-01-15 Yamanouchi Pharmaceutical Co., Ltd. Fused imidazole derivatives and medicinal composition thereof
PL188959B1 (pl) 1995-07-06 2005-05-31 Novartis Ag Pirolopirymidyny i sposoby ich wytwarzania
WO1997008150A1 (en) 1995-08-22 1997-03-06 The Du Pont Merck Pharmaceutical Company 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
CN100503580C (zh) 1996-04-12 2009-06-24 沃尼尔·朗伯公司 酪氨酸激酶的不可逆抑制剂
CA2254769A1 (en) * 1996-05-20 1997-11-27 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
BR9709959A (pt) 1996-06-24 2000-05-09 Pfizer Derivados tricìclicos de fenilamino substituìdo para o tratamento de doenças hiperproliferativas
AU716610B2 (en) 1996-08-30 2000-03-02 Novartis Ag Method for producing epothilones, and intermediate products obtained during the production process
DE938597T1 (de) 1996-09-06 2000-03-09 Obducat Ab Verfahren für das anisotrope ätzen von strukturen in leitende materialien
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
ATE267197T1 (de) 1996-11-18 2004-06-15 Biotechnolog Forschung Gmbh Epothilon d, dessen herstellung und dessen verwendung als cytostatisches mittel bzw. als pflanzenschutzmittel
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
DK1028110T3 (da) 1997-10-02 2004-07-19 Daiichi Seiyaku Co Hidtil ukendte dihydronaphthalenforbindelser og fremgangsmåde til fremstilling deraf
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
US6194181B1 (en) 1998-02-19 2001-02-27 Novartis Ag Fermentative preparation process for and crystal forms of cytostatics
CA2322157C (en) 1998-02-25 2012-05-29 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US6573289B1 (en) 1998-04-23 2003-06-03 Takeda Chemical Industries, Ltd. Naphthalene derivatives, their production and use
ES2342240T3 (es) 1998-08-11 2010-07-02 Novartis Ag Derivados de isoquinolina con actividad que inhibe la angiogenia.
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
CN100381566C (zh) 1998-11-20 2008-04-16 科森生物科学公司 产生环氧噻酮及其衍生物的重组方法和材料
EP1579871A1 (en) 1998-12-22 2005-09-28 Genentech, Inc. Vascular endothelial cell growth factor antagonists and uses thereof
ATE329596T1 (de) 1999-03-30 2006-07-15 Novartis Pharma Gmbh Phthalazinderivate zur behandlung von entzündlicher erkrankungen
WO2001054694A1 (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
AU2001288605A1 (en) 2000-09-06 2002-03-22 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
EP1542667B1 (en) * 2002-07-24 2012-03-07 PTC Therapeutics, Inc. Ureido substituted benzoic acid compounds and their use for nonsense suppression and the treatment of disease
CN1681805A (zh) 2002-09-18 2005-10-12 辉瑞产品公司 作为转化生长因子(tgf)抑制剂的新的咪唑类化合物
GB0418900D0 (en) 2004-08-24 2004-09-29 Btg Int Ltd Novel salt forms
US20080070867A1 (en) * 2005-01-19 2008-03-20 Metabasis Therapeutics, Inc. 2-Imidazolone and 2-Imidazolidinone Heterocyclic Inhibitors of Tyrosine Phosphatases
JP5130453B2 (ja) 2005-03-02 2013-01-30 ユニバーシティ オブ メリーランド，ボルティモア 新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性
EP1864971A4 (en) * 2005-03-31 2010-02-10 Takeda Pharmaceutical PROPHYLACTIC / THERAPEUTIC AGENT AGAINST DIABETES
WO2007109330A2 (en) 2006-03-21 2007-09-27 Epix Delaware, Inc. S1p receptor modulating compounds
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
US20110039893A1 (en) * 2006-10-11 2011-02-17 Takeda Pharmaceutical Company Limited Gsk-3beta inhibitor
WO2008094556A2 (en) 2007-01-30 2008-08-07 Biogen Idec Ma Inc. Imidazolone compounds as tgf-beta family type i receptors, alk5 and/or alk4 antagonists
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
EP2250176B1 (en) * 2008-01-30 2012-08-01 Cephalon, Inc. Substituted spirocyclic piperidine derivatives as histamine-3 (h3) receptor ligands
JP5504259B2 (ja) * 2008-05-19 2014-05-28 メルク・シャープ・アンド・ドーム・コーポレーション 第ｉｘａ因子阻害剤としての複素環式化合物
CN102131801B (zh) 2008-06-25 2015-04-08 福拉姆医药股份有限公司 1,2-二取代的杂环化合物
WO2009156484A2 (en) 2008-06-27 2009-12-30 Novartis Ag Organic compounds
EP2350067A2 (en) 2008-10-16 2011-08-03 Schering Corporation Pyrrolidine, piperidine and piperazine derivatives and methods of use thereof
US8431699B2 (en) * 2009-02-27 2013-04-30 Vertichem Corporation Method for manufacture of 2-oxoimidazolidines
EP2461814A4 (en) 2009-08-07 2012-12-05 Tokai Pharmaceuticals Inc PROSTATE CANCER TREATMENT
AU2010319697B2 (en) 2009-11-13 2016-05-19 Tokai Pharmaceuticals, Inc. Mammalian metabolites of steroids
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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