EP2408762A1 - Hsp90-inhibierende indazolderivate, diese enthaltende zusammensetzungen und anwendung davon - Google Patents

Hsp90-inhibierende indazolderivate, diese enthaltende zusammensetzungen und anwendung davon

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Publication number
EP2408762A1
EP2408762A1 EP10715951A EP10715951A EP2408762A1 EP 2408762 A1 EP2408762 A1 EP 2408762A1 EP 10715951 A EP10715951 A EP 10715951A EP 10715951 A EP10715951 A EP 10715951A EP 2408762 A1 EP2408762 A1 EP 2408762A1
Authority
EP
European Patent Office
Prior art keywords
alkyl
radicals
products
methyl
formula
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP10715951A
Other languages
English (en)
French (fr)
Inventor
Luc Bertin
Jean-Christophe Carry
Patrick Mailliet
Hervé MINOUX
Fabienne Pilorge
Jean-Marie Ruxer
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sanofi SA
Original Assignee
Sanofi SA
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
Priority claimed from FR0901274A external-priority patent/FR2943341B1/fr
Priority claimed from FR1050341A external-priority patent/FR2955323B1/fr
Application filed by Sanofi SA filed Critical Sanofi SA
Publication of EP2408762A1 publication Critical patent/EP2408762A1/de
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • 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
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D407/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems

Definitions

  • Toxoplasmosis Toxoplasma gondii, the parasite responsible for toxoplasmosis, has a chaperone protein Hsp90, for which induction has been shown during tachyzoite conversion. bradyzoite, corresponding to the transition from chronic infection to active toxoplasmosis. In addition, geldanamycin blocks in vitro this tachyzoite-bradyzoite conversion (J. Mol Biol 350: 723, 2005) ix) Treatment-resistant mycoses: It is possible that the Hsp90 protein potentiates the evolution of drug resistance. , allowing new mutations to develop.
  • Hepatitis C The human Hsp90 protein participates in the cleavage step between the NS2 and NS3 proteins by the viral protease.
  • Geldanamycin and radicicol are capable of inhibiting this NS2 / 3 cleavage in vitro (Proc Natl Acad Sci USA 98: 13931, 2001)
  • Herpesvirus Geldanamycin has demonstrated inhibition of HSV-1 replication in vitro, with a good therapeutic index (Antimicrobial Agents and Chemotherapy 48: 867,
  • US2006089495 discloses mixed compounds comprising a quinone ring, such as ansamycin derivatives, and a resorcinol ring such as radicicol analogs, as Hsp90 inhibitors.
  • Patent application WO2007117466 claims Célastrol and Gédunine derivatives as Hsp90 inhibitors.
  • Patent application WO2005000778 claims a family of benzophenone derivatives as Hsp90 inhibitors, useful for the treatment of tumors.
  • Patent Application FR2884252 claims a family of isoindoles as Hsp90 inhibitors
  • Patent application WO2007155809 (Synta Pharma) claims families of phenyltriazoles as Hsp90 inhibitors.
  • Patent applications WO2007139951, WO2007139952, WO2007139960, WO2007139967, WO2007139968, WO2007139955 and WO2007140002 claim families of triazoles as Hsp90 inhibitors and agents for the treatment of non-Hodgkin's lymphomas.
  • Patent application WO2008053319 claims amide derivatives of resorcinol as Hsp90 inhibitors.
  • Patent application WO2008056120 (Chroma Therapeutics) claims amino acid derivatives of adenine as Hsp90 inhibitors.
  • heteroaryl radicals containing at least one heteroatom selected from sulfur, nitrogen and oxygen mention may be made, for example, of benzothienyl, benzofuryl, benzopyrrolyl, benzothiazolyl, benzimidazolyl, imidazopyridyl, purinyl, pyrrolopyrimidinyl, pyrolopyridinyl, benzoxazolyl, benzisoxazolyl and benzisothiazolyl.
  • the subject of the present invention is also, as new industrial products, the synthetic intermediates of formulas (III), (IV), (V) and (VI) as defined above in which the substituents Het, R, R2, R4, W1 and W2 have the meanings indicated above for the products of formula (I) as defined above and Z has the meaning indicated above in scheme (1).
  • the subject of the present invention is also, as new industrial products, the starting products of formula (Ma) as defined above and hereinafter:
  • z represents OCH 2 phenyl and R 4 represents CF 3, CH 2 -CH 3, F, Cl or Br;
  • R4 H, CH3, CF3, CH2-CH3, F, Cl, Br, I as defined above or hereinafter in which z, R4, R2, W1 and W2 have any of the meanings indicated below. above or below.
  • the subject of the present invention is thus also, as new industrial products, the synthesis intermediates (V) of the products of formula (I):
  • the product of general formula (Ma) in which R 4 represents Br can be obtained by bromination of the compound of general formula (Ma) in which R 4 represents H by the use of a bromination reagent known to those skilled in the art such as sodium hypobromite in a basic aqueous medium (analogy to patent WO 2006/50006), bromine in an acetic medium (analogy to patent WO 2007/126841), pyridinium tribromide in an organic solvent such as methanol ( analogy with US patent 2005/277638) or preferably N-bromosuccinimide as an organic solvent such as dimethylformamide (analogy with Bioorg.Med.Chem. 2008, 1 (6), 5962).
  • a bromination reagent known to those skilled in the art such as sodium hypobromite in a basic aqueous medium (analogy to patent WO 2006/50006), bromine in an acetic medium (analogy to patent WO 2007/126841), pyridinium tribromide in
  • the product of general formula (II) in which Z represents the trifluoromethanesulfonyloxy radical and R4 represents Cl can be obtained by chlorination of the compound of general formula (II) in which Z represents the trifluoromethanesulfonyloxy radical and R4 represents H by the use of a chlorination reagent known to those skilled in the art such as for example N-chlorosuccinimide in an organic solvent such as dimethylformamide (analogy with patent WO 1997/12884).
  • a chlorination reagent known to those skilled in the art such as for example N-chlorosuccinimide in an organic solvent such as dimethylformamide (analogy with patent WO 1997/12884).
  • R4 H, CH3, CF3, CH2CH3, F, Cl, Br, I
  • the compounds of general formula (I), in which R is of type D, with W3 a nitrogen atom, can be prepared, advantageously in the context of the invention, by the action of ammonia, on a nitrile of formula (VI), orthosubstituted by a halogen atom, very preferably a fluorine atom, followed by the action of a mixture of ethyl orthoformate and ammonium acetate, operating according to the scheme (37). ), especially under the conditions described in J. Het. Chem. (2006), 43 (4), 913:
  • the present invention thus particularly relates to the processes described above in Schemes 1 to 45 which can thus be used for the synthesis of the products of formula (I) as defined above.
  • X represents an oxygen or sulfur atom, or an NR2, C (O), S (O) or S (O) 2 radical;
  • Step 5 In a 10OmL flask at room temperature under argon to a mixture of 480mg of 2- (4-hydroxy-cyclohexylamino) -4- (3-methyl-4-quinolin-3-yl-indazol-1-one) yl) -benzonitrile obtained according to the preceding step in 5.15 ml of dimethylsulfoxide, 12.4 ml of ethanol and then 2.03 ml of 1 M sodium hydroxide are finally added successively, 1.88 ml of 30% hydrogen peroxide. After stirring at ambient temperature for 0.75 hour, the reaction medium is poured into 100 ml of distilled water.
  • reaction medium is poured onto 50 ml of a saturated aqueous solution of sodium chloride and 50 ml of ethyl acetate.
  • the aqueous phase is re-extracted twice with 25 ml of ethyl acetate.
  • the combined organic phases are washed 4 times with 5 ml of water, dried over sodium sulphate and concentrated under reduced pressure. 335 mg of a mixture containing very predominantly 5- [3-methyl-4-quinolin-3-ylindazol-1-yl] -3- (1, 2,2,6,6-pentamethylpiperidine) are thus obtained.
  • Step 2 To a solution of 0.68 g of 2-bromo-4- (3-methyl-4-quinolin-3-yl-indazol-1-yl) -benzonitrile, obtained according to Step 3 of Example 1 in 4OmL of dioxane under argon, a solution of 392 mg of (7-oxal) bicyclo [2.2.1] hept-2-yl) -methylamine obtained according to the preceding step in 1 ⁇ l of dioxane, 109 mg of 4,5-bis (diphenylphosphino) -9,9-dimethylxanthene, 35 mg of palladium acetate and 1.51g of cesium carbonate. The reaction medium is heated at 90 ° C.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (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)
EP10715951A 2009-03-19 2010-03-18 Hsp90-inhibierende indazolderivate, diese enthaltende zusammensetzungen und anwendung davon Withdrawn EP2408762A1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR0901274A FR2943341B1 (fr) 2009-03-19 2009-03-19 Nouveaux derives d'indazole inhibiteurs d'hsp90,compositions les contenant et utilisation
FR1050341A FR2955323B1 (fr) 2010-01-19 2010-01-19 Nouveaux derives d'indazole inhibiteurs d'hsp90, compositions les contenant et utilisation
PCT/FR2010/050483 WO2010106290A1 (fr) 2009-03-19 2010-03-18 Derives d'indazole inhibiteurs d'hsp90, compositions les contenant et utilisation

Publications (1)

Publication Number Publication Date
EP2408762A1 true EP2408762A1 (de) 2012-01-25

Family

ID=42313103

Family Applications (1)

Application Number Title Priority Date Filing Date
EP10715951A Withdrawn EP2408762A1 (de) 2009-03-19 2010-03-18 Hsp90-inhibierende indazolderivate, diese enthaltende zusammensetzungen und anwendung davon

Country Status (16)

Country Link
US (1) US20120010241A1 (de)
EP (1) EP2408762A1 (de)
JP (1) JP2012520859A (de)
KR (1) KR20110128942A (de)
CN (1) CN102439003A (de)
AR (1) AR075874A1 (de)
AU (1) AU2010224652A1 (de)
BR (1) BRPI1009375A2 (de)
CA (1) CA2755660A1 (de)
IL (1) IL215139A0 (de)
MX (1) MX2011009806A (de)
RU (1) RU2011142151A (de)
SG (1) SG174466A1 (de)
TW (1) TW201038553A (de)
UY (1) UY32505A (de)
WO (1) WO2010106290A1 (de)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101609412B1 (ko) * 2009-07-10 2016-04-05 다이호야쿠힌고교 가부시키가이샤 아자 2 고리형 화합물 또는 그 염
US8912181B2 (en) * 2011-01-07 2014-12-16 Taiho Pharmaceutical Co., Ltd. Bicyclic compound or salt thereof
US9120780B2 (en) * 2011-01-07 2015-09-01 Taiho Pharmaceutical Co., Ltd. Indole or indazole derivative or salt thereof
CA2868258A1 (en) * 2012-03-28 2013-10-03 Synta Pharmaceuticals Corp. Triazole derivatives as hsp90 inhibitors
SG11201407210SA (en) * 2012-05-18 2014-12-30 Sanofi Sa Pyrazole derivatives and their use as lpar5 antagonists
US9096549B2 (en) * 2013-02-01 2015-08-04 Acetylon Pharmaceuticals, Inc. Selective HDAC3 inhibitors
DE102017008073A1 (de) * 2017-08-28 2019-02-28 Henkel Ag & Co. Kgaa Neue anionische Tenside und Wasch- und Reinigungsmittel, welche diese enthalten
CN117003754A (zh) * 2022-04-28 2023-11-07 腾讯科技（深圳）有限公司 吡咯并[2,3-d]嘧啶或吡唑并[3,4-d]嘧啶衍生物及其用途

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US6353007B1 (en) * 2000-07-13 2002-03-05 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted 1-(4-aminophenyl)indoles and their use as anti-inflammatory agents
WO2003027100A1 (en) * 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation Substituted 3-pyridyl pyrimidines as c17,20 lyase inhibitors
US7297709B2 (en) * 2003-05-22 2007-11-20 Abbott Laboratories Indazole, benzisoxazole, and benzisothiazole kinase inhibitors
MX2007010227A (es) * 2005-02-25 2007-11-07 Serenex Inc Derivados de tetrahidroindolona y tetrahidroindazolona.
JP2007145786A (ja) * 2005-11-30 2007-06-14 Toray Ind Inc ピラジン誘導体及びそれを有効成分とする腎炎治療薬
JP2009527562A (ja) * 2006-02-21 2009-07-30 アムゲン インコーポレイティッド ホスホジエステラーゼ１０阻害剤としてのシンノリン誘導体
WO2007114763A1 (en) * 2006-03-31 2007-10-11 Astrazeneca Ab Sulphonamide derivates as modulators of the glucocorticoid receptor
US7678803B2 (en) * 2006-08-24 2010-03-16 Serenex, Inc. Quinazoline derivatives for the treatment of cancer

Non-Patent Citations (1)

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Also Published As

Publication number Publication date
CN102439003A (zh) 2012-05-02
JP2012520859A (ja) 2012-09-10
KR20110128942A (ko) 2011-11-30
US20120010241A1 (en) 2012-01-12
UY32505A (es) 2010-10-29
IL215139A0 (en) 2011-12-29
RU2011142151A (ru) 2013-04-27
TW201038553A (en) 2010-11-01
BRPI1009375A2 (pt) 2016-03-15
WO2010106290A1 (fr) 2010-09-23
CA2755660A1 (fr) 2010-09-23
SG174466A1 (en) 2011-10-28
MX2011009806A (es) 2011-09-29
AU2010224652A1 (en) 2011-10-13
AR075874A1 (es) 2011-05-04

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