EA200601002A1 - 6-алкенил и 6-фенилалкил замещённые 2-хинолиноны и 2-хиноксалиноны в качестве ингибиторов поли(адф-рибоза) полимеразы - Google Patents

6-алкенил и 6-фенилалкил замещённые 2-хинолиноны и 2-хиноксалиноны в качестве ингибиторов поли(адф-рибоза) полимеразы

Info

Publication number
EA200601002A1
EA200601002A1 EA200601002A EA200601002A EA200601002A1 EA 200601002 A1 EA200601002 A1 EA 200601002A1 EA 200601002 A EA200601002 A EA 200601002A EA 200601002 A EA200601002 A EA 200601002A EA 200601002 A1 EA200601002 A1 EA 200601002A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
quinoxalinones
quinolinones
adp
ribose
Prior art date
Application number
EA200601002A
Other languages
English (en)
Other versions
EA009875B1 (ru
Inventor
Доминик Жан-Пьер Мабир
Жером Эмиль Жорж Гийемон
Якобус Альфонсус Йозефус Ван Дюн
Мария Викторина Франциска Сомерс
Вальтер Баудевейн Леопольд Ваутерс
Original Assignee
Янссен Фармацевтика Н. В.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Янссен Фармацевтика Н. В. filed Critical Янссен Фармацевтика Н. В.
Publication of EA200601002A1 publication Critical patent/EA200601002A1/ru
Publication of EA009875B1 publication Critical patent/EA009875B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4704—2-Quinolinones, e.g. carbostyril
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/10—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 two hetero rings linked by a carbon chain containing aromatic 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
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

Настоящее изобретение предлагает соединения формулы (I) и соединения формулы (VII-a), а также фармацевтические композиции, содержащие указанные соединения, и их применение в качестве ингибиторов PARP,где n, R, R, R, R, R, R, R, R, Rи Х имеют определенные значения.
EA200601002A 2003-11-20 2004-11-18 6-алкенил и 6-фенилалкил замещенные 2-хинолиноны и 2-хиноксалиноны в качестве ингибиторов поли(адф-рибоза) полимеразы EA009875B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP0313028 2003-11-20
EP03078860 2003-12-05
PCT/EP2004/013163 WO2005054201A1 (en) 2003-11-20 2004-11-18 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp-ribose) polymerase inhibitors

Publications (2)

Publication Number Publication Date
EA200601002A1 true EA200601002A1 (ru) 2006-10-27
EA009875B1 EA009875B1 (ru) 2008-04-28

Family

ID=37101690

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200601002A EA009875B1 (ru) 2003-11-20 2004-11-18 6-алкенил и 6-фенилалкил замещенные 2-хинолиноны и 2-хиноксалиноны в качестве ингибиторов поли(адф-рибоза) полимеразы

Country Status (11)

Country Link
US (4) US7855207B2 (ru)
EP (1) EP1687277B1 (ru)
KR (1) KR101118582B1 (ru)
AU (1) AU2004295058B9 (ru)
BR (1) BRPI0416206A (ru)
CA (1) CA2546300C (ru)
EA (1) EA009875B1 (ru)
MX (1) MXPA06005687A (ru)
NO (1) NO338869B1 (ru)
SG (1) SG150533A1 (ru)
WO (1) WO2005054201A1 (ru)

Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101118582B1 (ko) 2003-11-20 2012-02-27 얀센 파마슈티카 엔.브이. 폴리(ａｄｐ-리보스)폴리머라제 저해제로서의 6-알케닐 및6-페닐알킬 치환된 2-퀴놀리논 및 2-퀴녹살리논
SG150534A1 (en) 2003-11-20 2009-03-30 Janssen Pharmaceutica Nv 7-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp- ribose) polymerase inhibitors
ES2551299T3 (es) * 2003-12-05 2015-11-17 Janssen Pharmaceutica Nv 2-Quinolinonas y 2-quinoxalinonas 6-sustituidas como inhibidores de poli(ADP-ribosa) polimerasa
CA2553269C (en) * 2004-01-23 2012-07-10 Janssen Pharmaceutica N.V. Quinoline derivatives and use thereof as mycobacterial inhibitors
ES2563954T3 (es) 2004-06-30 2016-03-16 Janssen Pharmaceutica Nv Derivados de ftalazina como inhibidores de PARP
CA2569827C (en) 2004-06-30 2013-04-09 Janssen Pharmaceutica N.V. Quinazolinedione derivatives as parp inhibitors
CA2569826C (en) 2004-06-30 2013-07-16 Janssen Pharmaceutica N.V. Substituted 2-alkyl quinazolinone derivatives as parp inhibitors
ZA200800907B (en) 2005-07-18 2010-04-28 Bipar Sciences Inc Treatment of cancer
WO2007087518A2 (en) 2006-01-24 2007-08-02 Janssen Pharmaceutica N.V. 2-substituted benzimidazoles as selective androgen receptor modulators (sarms)
DK2061765T3 (en) * 2006-09-01 2015-01-26 Senhwa Biosciences Inc Serine-threonine protein kinase AND PARP-MODULATOR
WO2008030891A2 (en) 2006-09-05 2008-03-13 Bipar Sciences, Inc. Inhibition of fatty acid synthesis by parp inhibitors and methods of treatment thereof
US8143447B2 (en) 2006-09-05 2012-03-27 Bipar Sciences, Inc. Treatment of cancer
ES2381446T3 (es) * 2007-03-08 2012-05-28 Janssen Pharmaceutica, N.V. Derivado de quinolinona como inhibidores de PARP y TANK
EP2215075B1 (en) 2007-10-26 2013-12-11 Janssen Pharmaceutica, N.V. Quinolinone derivatives as parp inhibitors
EP2217227B1 (en) 2007-11-12 2013-08-21 BiPar Sciences, Inc. Treatment of breast cancer with 4-iodo-3-nitrobenzamide in combination with anti-tumor agents
WO2009118384A1 (en) 2008-03-27 2009-10-01 Janssen Pharmaceutica Nv Quinazolinone derivatives as tubulin polymerization inhibitors
CA2716726C (en) 2008-03-27 2017-01-24 Janssen Pharmaceutica Nv Tetrahydrophenanthridinones and tetrahydrocyclopentaquinolinones as parp and tubulin polymerization inhibitors
WO2011058367A2 (en) 2009-11-13 2011-05-19 Astrazeneca Ab Diagnostic test for predicting responsiveness to treatment with poly(adp-ribose) polymerase (parp) inhibitor
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) * 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
EP2909193B1 (en) 2012-10-16 2017-04-19 Janssen Pharmaceutica NV Phenyl linked quinolinyl modulators of ror-gamma-t
BR112015008515A2 (pt) 2012-10-16 2017-07-04 Janssen Pharmaceutica Nv moduladores de ror t de quinolinila ligada à heteroarila
WO2014062658A1 (en) 2012-10-16 2014-04-24 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of ror-gamma-t
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
KR20160070133A (ko) 2013-10-15 2016-06-17 얀센 파마슈티카 엔.브이. RORyt의 알킬 결합 퀴놀리닐 조절제
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
KR20160068956A (ko) 2013-10-15 2016-06-15 얀센 파마슈티카 엔.브이. RORyT의 퀴놀리닐 조절제
US9403816B2 (en) 2013-10-15 2016-08-02 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of RORγt
US10555941B2 (en) 2013-10-15 2020-02-11 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORγt
US9328095B2 (en) 2013-10-15 2016-05-03 Janssen Pharmaceutica Nv Heteroaryl linked quinolinyl modulators of RORgammat
AU2013403336A1 (en) * 2013-10-15 2016-04-21 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORyt
US9284308B2 (en) 2013-10-15 2016-03-15 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of RORγt
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
SI3122358T1 (sl) 2014-03-26 2021-04-30 Astex Therapeutics Ltd. Kombinacije FGFR- in CMET-inhibitorjev za zdravljenje raka
BR112016022062B1 (pt) 2014-03-26 2023-04-11 Astex Therapeutics Limited Combinação, composição farmacêutica, uso de uma combinação ou de uma composição farmacêutica, e, produto farmacêutico
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
PT3325623T (pt) 2015-07-23 2019-09-04 Inst Curie Utilização de uma combinação de molécula dbait e de inibidores de parp para o tratamento do cancro
ES2811845T3 (es) 2015-09-23 2021-03-15 Janssen Pharmaceutica Nv Heterociclos tricíclicos para el tratamiento del cáncer
HUE057090T2 (hu) 2015-09-23 2022-04-28 Janssen Pharmaceutica Nv BI-heteroaril-szubsztituált 1,4-benzodiazepinek és alkalmazásuk rák kezelésében
GB201519573D0 (en) 2015-11-05 2015-12-23 King S College London Combination
WO2018022851A1 (en) 2016-07-28 2018-02-01 Mitobridge, Inc. Methods of treating acute kidney injury
AU2017355402A1 (en) 2016-11-02 2019-05-30 Health Research, Inc. Combination treatment with antibody-drug conjugates and PARP inhibitors
WO2018162439A1 (en) 2017-03-08 2018-09-13 Onxeo New predictive biomarker for the sensitivity to a treatment of cancer with a dbait molecule
US20200129476A1 (en) 2017-04-28 2020-04-30 Akribes Biomedical Gmbh PARP Inhibitor in Combination with a Glucocorticoid and/or Ascorbic Acid and/or a Protein Growth Factor for the Treatment of Impaired Wound Healing
WO2019012001A1 (en) 2017-07-12 2019-01-17 Syngenta Participations Ag MICROBIOCIDE OXADIAZOLE DERIVATIVES
JP2021515580A (ja) 2018-03-13 2021-06-24 オンクセオＯｎｘｅｏ がんの治療における獲得耐性に対抗するｄｂａｉｔ分子
WO2020007658A1 (en) 2018-07-02 2020-01-09 Syngenta Crop Protection Ag 3-(2-thienyl)-5-(trifluoromethyl)-1,2,4-oxadiazole derivatives as agrochemical fungicides
CR20220070A (es) 2019-07-19 2022-03-21 Astrazeneca Ab Inhibidores de parp1
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use

Family Cites Families (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB732581A (en) 1952-01-18 1955-06-29 Ciba Ltd Manufacture of hydrazine compounds
DE1006423B (de) 1952-01-18 1957-04-18 Ciba Geigy Verfahren zur Herstellung von Hydrazinophthalazinen
US3274194A (en) 1963-03-29 1966-09-20 Miles Lab Quinazolinedione derivatives
GB1062357A (en) 1965-03-23 1967-03-22 Pfizer & Co C Quinazolone derivatives
GB1293565A (en) 1969-05-03 1972-10-18 Aspro Nicholas Ltd Aminophthalazines and pharmaceutical compositions thereof
US3919425A (en) 1971-04-09 1975-11-11 Miles Lab Method of producing vasodilation using certain 3-substituted-quinazoline derivatives
BE792206A (ru) 1971-12-02 1973-06-01 Byk Gulden Lomberg Chem Fab
US3879393A (en) 1973-06-18 1975-04-22 Miles Lab Derivatives of 1,3-disubstituted 2,4(1h,3h)-quinazolinediones
FR2436781A1 (fr) 1978-09-19 1980-04-18 Berri Balzac Derives d'amino-3 (1h,3h) quinazolinedione-2,4, leur procede de preparation et leurs applications en therapeutique
US4335127A (en) 1979-01-08 1982-06-15 Janssen Pharmaceutica, N.V. Piperidinylalkyl quinazoline compounds, composition and method of use
JPS5976082A (ja) 1982-10-23 1984-04-28 Kyowa Hakko Kogyo Co Ltd 新規なピペリジン誘導体
JPS60120872A (ja) 1983-12-01 1985-06-28 Kyowa Hakko Kogyo Co Ltd 新規なヘテロ環状化合物及び強心剤
US5001125A (en) 1984-03-26 1991-03-19 Janssen Pharmaceutica N.V. Anti-virally active pyridazinamines
ZM1785A1 (en) 1984-03-26 1986-03-27 Janssen Pharmaceutica Nv Anti-virally active phyridazinamines
DK623586A (da) 1985-12-27 1987-06-28 Eisai Co Ltd Piperidinderivater eller salte deraf og farmaceutiske kompositioner indeholdende forbindelserne
US5231184A (en) 1987-11-23 1993-07-27 Janssen Pharmaceutica N.V. Pridazinamine derivatives
US5177075A (en) 1988-08-19 1993-01-05 Warner-Lambert Company Substituted dihydroisoquinolinones and related compounds as potentiators of the lethal effects of radiation and certain chemotherapeutic agents; selected compounds, analogs and process
CA2002864C (en) 1988-11-29 1999-11-16 Eddy J. E. Freyne (1h-azol-1-ylmethyl) substituted quinoline, quinazoline or quinoxaline derivatives
KR0149162B1 (ko) * 1988-11-29 1998-10-15 구스타프 반 리이트 (1h-아졸-1-일메틸) 치환된 퀴놀린, 퀴나졸린 또는 퀴녹살린 유도체
GB8827822D0 (en) * 1988-11-29 1988-12-29 Janssen Pharmaceutica Nv (1h-azol-1-ylmethyl)substituted quinoline derivatives
US5374637A (en) 1989-03-22 1994-12-20 Janssen Pharmaceutica N.V. N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives
EP0391462A1 (en) 1989-04-05 1990-10-10 Janssen Pharmaceutica N.V. Synergistic compositions containing ketanserin
US5160727A (en) 1990-02-13 1992-11-03 Warner-Lambert Company Tumor cell sensitization method using quinazolinedione derivatives
IE913473A1 (en) 1990-10-15 1992-04-22 Fujisawa Pharmaceutical Co Quinazoline derivatives and their preparation
CA2134077C (en) 1992-04-23 2002-05-21 Thaddeus R. Nieduzak 4-imidomethyl-1-[2'phenyl-2'oxoethyl-]piperidines as serotonin 5ht2-antagonists, their preparation and use in therapy
TW294595B (ru) 1992-11-20 1997-01-01 Janssen Pharmaceutica Nv
EP0638567A4 (en) 1993-02-18 1995-05-10 Kyowa Hakko Kogyo Kk ADENOSINE INHIBITORS.
GB9404485D0 (en) 1994-03-09 1994-04-20 Cancer Res Campaign Tech Benzamide analogues
TW445263B (en) 1996-02-29 2001-07-11 Janssen Pharmaceutica Nv Novel esters of 1,4-disubstituted piperidine derivatives
JPH107572A (ja) 1996-06-17 1998-01-13 Sumitomo Pharmaceut Co Ltd 腫瘍壊死因子産生阻害剤
EA004037B1 (ru) 1996-09-10 2003-12-25 Др. Карл Томэ ГмбХ Модифицированные аминокислоты и лекарственное средство на их основе
WO1998054135A1 (fr) 1997-05-30 1998-12-03 Meiji Seika Kaisha, Ltd. Composes heterocycliques azotes et medicament contre l'hyperlipemie en contenant
JPH10330377A (ja) 1997-06-02 1998-12-15 Kyowa Hakko Kogyo Co Ltd ピペリジン誘導体
US6635642B1 (en) 1997-09-03 2003-10-21 Guilford Pharmaceuticals Inc. PARP inhibitors, pharmaceutical compositions comprising same, and methods of using same
US20020022636A1 (en) 1997-09-03 2002-02-21 Jia-He Li Oxo-substituted compounds, process of making, and compositions and methods for inhibiting parp activity
US20030069231A1 (en) 1999-10-12 2003-04-10 Klaus Rudolf Modified aminoacids, pharmaceuticals containing these compounds and method for their production
WO1999014203A1 (fr) 1997-09-16 1999-03-25 Takeda Chemical Industries, Ltd. Composes azotes a cycles condenses, procede de preparation de ces composes et medicaments
US6133277A (en) 1997-12-05 2000-10-17 Janssen Pharmaceutica N.V. (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties
DK1094839T3 (da) * 1998-07-06 2003-08-18 Janssen Pharmaceutica Nv Farnesylproteintransferaseinhibitorer med in vivo radiosensibiliserende egenskaber
JP2000191659A (ja) 1999-01-04 2000-07-11 Sumitomo Pharmaceut Co Ltd 腫瘍壊死因子産生阻害剤
BR0007664A (pt) 1999-01-29 2002-05-07 Abbott Lab Derivados diazabicìclicos como ligantes receptores de acetilcolina nicotìnicos
US7265115B2 (en) 1999-01-29 2007-09-04 Abbott Laboratories Diazabicyclic CNS active agents
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
UA76726C2 (ru) 2000-10-02 2006-09-15 Янссен Фармацевтика Н.В. Метаботропические антагонисты рецептора глутамата, способ их получения (варианты), фармацевтическая композиция и способ ее получения
ITMI20002358A1 (it) 2000-10-31 2002-05-01 Flavio Moroni Derivati di tieno ,2, 3-c|isochinolin-3-one come inibitori della poli(a dp-ribosio)polimerasi
AUPR201600A0 (en) 2000-12-11 2001-01-11 Fujisawa Pharmaceutical Co., Ltd. Quinazolinone derivative
JP2002284699A (ja) 2001-03-28 2002-10-03 Sumitomo Pharmaceut Co Ltd 視細胞変性疾患治療剤
EP1396488A1 (en) 2001-05-23 2004-03-10 Mitsubishi Pharma Corporation Fused heterocyclic compound and medicinal use thereof
WO2003015785A1 (en) 2001-08-15 2003-02-27 Icos Corporation 2h-phthalazin-1-ones and methods for use thereof
US7060705B2 (en) 2001-11-07 2006-06-13 Merck & Co., Inc. Mitotic kinesin inhibitors
US6822097B1 (en) 2002-02-07 2004-11-23 Amgen, Inc. Compounds and methods of uses
MXPA04009435A (es) 2002-03-29 2005-01-25 Janssen Pharmaceutica Nv Derivados de quinolina y quinolinona radiomarcados y su uso como ligandos de receptor de glutamato metabotropico.
US7119111B2 (en) 2002-05-29 2006-10-10 Amgen, Inc. 2-oxo-1,3,4-trihydroquinazolinyl derivatives and methods of use
AR043059A1 (es) * 2002-11-12 2005-07-13 Bayer Pharmaceuticals Corp Derivados de indolil pirazinona utiles para el tratamiento de trastornos hiper-proliferativos
EP1566380B1 (en) 2002-11-22 2012-01-11 Mitsubishi Tanabe Pharma Corporation Isoquinoline compounds and medicinal use thereof
US20050075364A1 (en) 2003-07-01 2005-04-07 Kap-Sun Yeung Indole, azaindole and related heterocyclic N-substituted piperazine derivatives
KR101118582B1 (ko) 2003-11-20 2012-02-27 얀센 파마슈티카 엔.브이. 폴리(ａｄｐ-리보스)폴리머라제 저해제로서의 6-알케닐 및6-페닐알킬 치환된 2-퀴놀리논 및 2-퀴녹살리논
SG150534A1 (en) 2003-11-20 2009-03-30 Janssen Pharmaceutica Nv 7-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp- ribose) polymerase inhibitors
AU2004294354B2 (en) 2003-12-03 2009-02-19 Ym Biosciences Australia Pty Ltd Tubulin inhibitors
ES2551299T3 (es) 2003-12-05 2015-11-17 Janssen Pharmaceutica Nv 2-Quinolinonas y 2-quinoxalinonas 6-sustituidas como inhibidores de poli(ADP-ribosa) polimerasa
UA91007C2 (ru) 2003-12-10 2010-06-25 Янссен Фармацевтика Н.В. Замещенные 6-циклогексилалкилом замещенные 2-хинолиноны и 2-хиноксалиноны как ингибиторы поли-(адф-рибоза)полимеразы
PE20060285A1 (es) 2004-03-30 2006-05-08 Aventis Pharma Inc Piridonas sustituidas como inhibidores de pol(adp-ribosa)-polimerasa (parp)
DE102004023332A1 (de) 2004-05-12 2006-01-19 Bayer Cropscience Gmbh Chinoxalin-2-on-derivate, diese enthaltende nutzpflanzenschützende Mittel und Verfahren zu ihrer Herstellung und deren Verwendung
CN1988907B (zh) 2004-06-01 2010-12-22 弗吉尼亚大学专利基金会 癌瘤及血管生成的双重小分子抑制剂
CA2569826C (en) 2004-06-30 2013-07-16 Janssen Pharmaceutica N.V. Substituted 2-alkyl quinazolinone derivatives as parp inhibitors
CA2569827C (en) 2004-06-30 2013-04-09 Janssen Pharmaceutica N.V. Quinazolinedione derivatives as parp inhibitors
ES2563954T3 (es) 2004-06-30 2016-03-16 Janssen Pharmaceutica Nv Derivados de ftalazina como inhibidores de PARP
JP5123671B2 (ja) 2005-02-17 2013-01-23 シンタ ファーマシューティカルズ コーポレーション 増殖性疾患の治療のための化合物
JP5075624B2 (ja) 2005-04-28 2012-11-21 田辺三菱製薬株式会社 シアノピリジン誘導体及びその医薬としての用途
EP1937268A4 (en) 2005-08-24 2009-07-22 Inotek Pharmaceuticals Corp INDENOISOQUINOLINONE ANALOGUES AND METHODS OF USE
EP1984333B1 (en) 2006-02-03 2012-04-25 Bionomics Limited Substituted benzofurans, benzothiophenes, benzoselenophenes and indoles and their use as tubulin polymerisation inhibitors
CN101421268B (zh) 2006-02-15 2016-01-06 Abbvie公司 作为有效parp抑制剂的吡唑并喹诺酮
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
US8466150B2 (en) 2006-12-28 2013-06-18 Abbott Laboratories Inhibitors of poly(ADP-ribose)polymerase
ES2381446T3 (es) 2007-03-08 2012-05-28 Janssen Pharmaceutica, N.V. Derivado de quinolinona como inhibidores de PARP y TANK
US8153633B2 (en) 2007-06-25 2012-04-10 Amgen Inc. Phthalazine compounds, compositions and methods of use

Also Published As

Publication number Publication date
NO20062894L (no) 2006-08-09
AU2004295058B2 (en) 2011-05-19
US8071612B2 (en) 2011-12-06
US9115084B2 (en) 2015-08-25
NO338869B1 (no) 2016-10-31
US20070072842A1 (en) 2007-03-29
AU2004295058B9 (en) 2011-06-30
CA2546300C (en) 2012-10-02
US8450486B2 (en) 2013-05-28
US20130237528A1 (en) 2013-09-12
EP1687277A1 (en) 2006-08-09
EP1687277B1 (en) 2018-04-04
EA009875B1 (ru) 2008-04-28
US20120046274A1 (en) 2012-02-23
US7855207B2 (en) 2010-12-21
US20110124673A1 (en) 2011-05-26
BRPI0416206A (pt) 2006-12-26
WO2005054201A1 (en) 2005-06-16
KR101118582B1 (ko) 2012-02-27
MXPA06005687A (es) 2006-08-17
SG150533A1 (en) 2009-03-30
CA2546300A1 (en) 2005-06-16
KR20060115393A (ko) 2006-11-08
AU2004295058A1 (en) 2005-06-16

Similar Documents

Publication Publication Date Title
EA200601002A1 (ru) 6-алкенил и 6-фенилалкил замещённые 2-хинолиноны и 2-хиноксалиноны в качестве ингибиторов поли(адф-рибоза) полимеразы
EA200601007A1 (ru) 7-фенилалкилзамещённые 2-хинолиноны и 2-хиноксалиноны в качестве ингибиторов поли(адф-рибоза)полимеразы
EA200601100A1 (ru) 6-замещённые 2-хинолиноны и 2-хиноксалиноны как ингибиторы поли(адф-рибоза)полимеразы
EA200700188A1 (ru) Производные замещенного 2-алкилхиназолинона как ингибиторы parp
EA200700185A1 (ru) Производные хиназолиндиона в качестве ингибиторов parp
EA200601125A1 (ru) 6-замещённые циклогексилалкил 2-замещённые хинолиноны и 2-хиноксалиноны в качестве ингибиторов поли(adp-рибоза)полимеразы
EA200801291A1 (ru) Карбониламинопирролопиразолы в качестве эффективных ингибиторов киназ
EA201000494A1 (ru) Новые гидрокси-8-гетероарилфенантридины и их применение в качестве ингибиторов pde4
ATE433447T1 (de) Pyrimiidinverbindungen
EA200401202A1 (ru) Сульфонилпроизводные в качестве новых ингибиторов гистон-деацетилазы
SE0301373D0 (sv) Novel compounds
DE60314623D1 (de) Substituierte pyrazolopyrimidine
SG154433A1 (en) Phthalazine derivatives as parp inhibitors
EA200701257A1 (ru) Пирролопиразолы в качестве сильнодействующих ингибиторов киназы
DK1501507T3 (da) Tetrahydropyranyl-cyclopentyl-tertrahydropyridopyrindin-modulatorer af kemokin-receptor-aktivitet
EA200601587A1 (ru) Новые амидозамещённые гидрокси-6-фенилфенантридины
CY1111197T1 (el) Tριαζολες χρησιμες ως αναστολεις πρετεϊνικων κινασων
SE0302139D0 (sv) Novel compounds
EA200500528A1 (ru) Пиперазинил- и диазапанилбензамиды и бензтиоамиды
CO5680420A2 (es) Compuestos de 6-amino-1h-indazol y 4-aminobenzenofurano como inhibidores de la fosfodiesterasa 4
EA200501341A1 (ru) Противобактериальные индолоноксазолидиноны, промежуточные соединения для их получения и содержащие их фармацевтические композиции
EA200600100A1 (ru) Производные никотинамида, полезные в качестве ингибиторов pde4
DE602004005881D1 (de) Substituierte pyrazinonverbindungen zur behandlung von entzündungen
EA200400690A1 (ru) Нуклеозиды, их препараты и их применение в качестве ингибиторов вирусных рнк-полимераз
DK1377574T3 (da) 6-phenylbenzonaphtyridiner

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU