PE20121470A1 - Compuestos de diarilhidantoina como antagonistas del receptor de androgeno - Google Patents
Compuestos de diarilhidantoina como antagonistas del receptor de androgenoInfo
- Publication number
- PE20121470A1 PE20121470A1 PE2012000638A PE2012000638A PE20121470A1 PE 20121470 A1 PE20121470 A1 PE 20121470A1 PE 2012000638 A PE2012000638 A PE 2012000638A PE 2012000638 A PE2012000638 A PE 2012000638A PE 20121470 A1 PE20121470 A1 PE 20121470A1
- Authority
- PE
- Peru
- Prior art keywords
- thioxo
- oxo
- trifluoromethyl
- phenyl
- androgen receptor
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 229940123407 Androgen receptor antagonist Drugs 0.000 title abstract 2
- 239000003936 androgen receptor antagonist Substances 0.000 title abstract 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical compound BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 2
- 229910052794 bromium Inorganic materials 0.000 abstract 2
- 229910052801 chlorine Inorganic materials 0.000 abstract 2
- 239000000460 chlorine Substances 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- -1 4- (3-CYANOPROPYL) PHENYL Chemical class 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical compound ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 206010062904 Hormone-refractory prostate cancer Diseases 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- CFHIDWOYWUOIHU-UHFFFAOYSA-N oxomethyl Chemical compound O=[CH] CFHIDWOYWUOIHU-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- 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
- C07D403/10—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 aromatic rings
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- 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
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
- C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
SE REFIERE A UN COMPUESTO DERIVADO DE DIARILHIDANTOINA DE FORMULA (I) DONDE: R1 Y R2 JUNTOS COMPRENDEN DE 2-8 ATOMOS DE CARBONO Y SON INDEPENDIENTEMENTE UN GRUPO ALQUILO C1-8 O UN GRUPO ALQUILO C1-8 SUSTITUIDO CON UN SUSTIUYENTE SELECCIONADO DE HIDROXI, BROMO, FLUORO, CLORO, ENTRE OTROS; R3 ES H Y FORMILO; R4 ES H, F, Cl, Br Y I.; R11 Y R12 SON INDEPENDIENTEMENTE H Y METILO. SON COMPUESTOS PREFERIDOS: 4-(3-(4-(3-CIANOPROPIL)FENIL)-4,4-DIMETIL-5-OXO-2-TIOXO-IMIDAZOLIN-1-IL)-2-(TRIFLUOROMETIL)BENZONITRILO; 4-(8-OXO-5-(4-(4-OXOBUTIL)FENIL)-6-TIOXO-5,7-DIAZASPIRO[3.4]OCTAN-7-IL)-2-(TRIFLUOROMETIL)BENZONITRILO; 4-(4-(7-(4-CIANO-3-(TRIFLUOROMETIL)FENIL)-8-OXO-6-TIOXO-5,7-DIAZASPIRO[3.4]OCT-AN-5-IL)-2-FLUOROFENIL)-2,2-DIMETIL-N-METIBUTANAMIDA; ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN ANTAGONISTA DEL RECEPTOR DE ANDROGENO SIENDO UTIL EN EL TRATAMIENTO DE CANCER DE PROSTATA REFRACTARIO A LA HORMONA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US99607607P | 2007-10-26 | 2007-10-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20121470A1 true PE20121470A1 (es) | 2012-11-18 |
Family
ID=40278902
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017000081A PE20170428A1 (es) | 2007-10-26 | 2008-10-24 | Compuestos de diarilhidantoina |
| PE2008001821A PE20091262A1 (es) | 2007-10-26 | 2008-10-24 | Compuestos de diarilhidantoina como antagonistas del receptor de androgeno |
| PE2012000638A PE20121470A1 (es) | 2007-10-26 | 2008-10-24 | Compuestos de diarilhidantoina como antagonistas del receptor de androgeno |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017000081A PE20170428A1 (es) | 2007-10-26 | 2008-10-24 | Compuestos de diarilhidantoina |
| PE2008001821A PE20091262A1 (es) | 2007-10-26 | 2008-10-24 | Compuestos de diarilhidantoina como antagonistas del receptor de androgeno |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US8680291B2 (es) |
| EP (3) | EP2620432A3 (es) |
| JP (4) | JP5535925B2 (es) |
| AR (1) | AR069039A1 (es) |
| CA (2) | CA2703635C (es) |
| CL (1) | CL2008003158A1 (es) |
| PE (3) | PE20170428A1 (es) |
| TW (3) | TWI469971B (es) |
| UY (1) | UY31432A1 (es) |
| WO (1) | WO2009055053A2 (es) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7709517B2 (en) * | 2005-05-13 | 2010-05-04 | The Regents Of The University Of California | Diarylhydantoin compounds |
| AU2007245022A1 (en) * | 2006-03-29 | 2007-11-08 | The Regents Of The University Of California | Diarylthiohydantoin compounds |
| WO2009055053A2 (en) | 2007-10-26 | 2009-04-30 | The Regents Of The University Of California | Diarylhydantoin compounds as androgen receptor modulators |
| BRPI1007990A2 (pt) | 2009-02-24 | 2015-09-01 | Medivation Prostate Therapeutics Inc | Compostos específicos de diaril-hidantoína e diariltioidantoína. |
| WO2010118354A1 (en) * | 2009-04-09 | 2010-10-14 | Medivation Prostate Therapeutics, Inc. | Substituted di-arylhydantoin and di-arylthiohydantoin compounds and methods for use thereof |
| WO2011029392A1 (en) * | 2009-09-10 | 2011-03-17 | Youzhi Tong | Androgen receptor antagonists and uses thereof |
| TW201111378A (en) | 2009-09-11 | 2011-04-01 | Bayer Schering Pharma Ag | Substituted (heteroarylmethyl) thiohydantoins |
| EP2485804A4 (en) * | 2009-10-07 | 2015-07-29 | Medivation Technologies Inc | SUBSTITUTED PHENYLCARBAMOYL ALKYLAMINOAREN COMPOUNDS AND N, N'-BIS-ARYL UREA COMPOUNDS |
| AR078793A1 (es) | 2009-10-27 | 2011-12-07 | Orion Corp | Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros |
| EP3124481B1 (en) * | 2010-02-16 | 2018-03-28 | Aragon Pharmaceuticals, Inc. | Androgen receptor modulators and uses thereof |
| CA2790924C (en) | 2010-02-24 | 2016-08-02 | Medivation Prostate Therapeutics, Inc. | Processes for the synthesis of diarylthiohydantoin and diarylhydantoin compounds |
| AU2011258009B2 (en) * | 2010-05-28 | 2016-04-21 | The Board Of Regents Of The University Of Texas System | Oligo-benzamide compounds and their use |
| AU2011326034B2 (en) * | 2010-11-12 | 2016-02-04 | Roche Innovation Center Copenhagen A/S | Compositions and methods for treating androgen receptor dependent disorders including cancers |
| CA2829322C (en) | 2011-03-10 | 2017-01-10 | Suzhou Kintor Pharmaceuticals, Inc. | Substituted thioimidazolidinone androgen receptor antagonists and uses thereof |
| CA2831338C (en) | 2011-04-21 | 2018-07-17 | Orion Corporation | Androgen receptor modulating carboxamides |
| EP3430907A1 (en) | 2011-07-29 | 2019-01-23 | Medivation Prostate Therapeutics LLC | Treatment of breast cancer |
| UY34646A (es) | 2012-03-02 | 2013-10-31 | Novartis Ag | Compuestos de espirohidantoína y su uso como moduladores selectivos del receptor de andrógenos |
| MX2014016054A (es) * | 2012-06-26 | 2015-04-10 | Bayer Pharma AG | N-[4-(quinolin-4-iloxi)ciclohexil(metil)](hetero)arilcarboxamidas como antagonistas del receptor de androgenos, su produccion y usos como productos medicinales. |
| SG10201912719TA (en) | 2012-09-26 | 2020-02-27 | Aragon Pharmaceuticals Inc | Anti-androgens for the treatment of non-metastatic castrate-resistant prostate cancer |
| JOP20200097A1 (ar) | 2013-01-15 | 2017-06-16 | Aragon Pharmaceuticals Inc | معدل مستقبل أندروجين واستخداماته |
| US9682960B2 (en) | 2013-12-19 | 2017-06-20 | Endorecherche, Inc. | Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety |
| US10196693B2 (en) | 2014-12-12 | 2019-02-05 | Medivation Prostate Therapeutics Llc | Method for predicting response to breast cancer therapeutic agents and method of treatment of breast cancer |
| CN106146403B (zh) * | 2015-04-02 | 2018-11-20 | 正大天晴药业集团股份有限公司 | 一种恩杂鲁胺的纯化方法 |
| TWI726969B (zh) | 2016-01-11 | 2021-05-11 | 比利時商健生藥品公司 | 用作雄性激素受體拮抗劑之經取代之硫尿囊素衍生物 |
| JP7201694B2 (ja) | 2017-10-16 | 2023-01-10 | アラゴン ファーマシューティカルズ,インコーポレイテッド | 非転移性去勢抵抗性前立腺癌の治療のための抗アンドロゲン剤 |
| JP2022509917A (ja) | 2018-11-05 | 2022-01-25 | ファイザー・インク | がんを処置するための組合せ |
| KR20230159510A (ko) | 2021-03-24 | 2023-11-21 | 화이자 인코포레이티드 | Ddr 유전자 돌연변이된 전이성 거세-감수성 전립선암의 치료를 위한 탈라조파립과 항안드로겐의 조합 |
| CN115181043B (zh) * | 2022-07-27 | 2024-05-07 | 爱斯特(成都)生物制药股份有限公司 | 一种连续流制备4-异硫氰基-2-(三氟甲基)苯甲腈的方法 |
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-
2008
- 2008-10-24 WO PCT/US2008/012149 patent/WO2009055053A2/en not_active Ceased
- 2008-10-24 TW TW97140820A patent/TWI469971B/zh active
- 2008-10-24 JP JP2010531057A patent/JP5535925B2/ja active Active
- 2008-10-24 CL CL2008003158A patent/CL2008003158A1/es unknown
- 2008-10-24 TW TW105126199A patent/TW201716385A/zh unknown
- 2008-10-24 EP EP13157028.5A patent/EP2620432A3/en not_active Withdrawn
- 2008-10-24 EP EP11178889.9A patent/EP2397469B1/en active Active
- 2008-10-24 AR ARP080104661A patent/AR069039A1/es unknown
- 2008-10-24 PE PE2017000081A patent/PE20170428A1/es not_active Application Discontinuation
- 2008-10-24 TW TW103138505A patent/TWI557111B/zh active
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- 2008-10-24 PE PE2008001821A patent/PE20091262A1/es not_active Application Discontinuation
- 2008-10-24 UY UY31432A patent/UY31432A1/es not_active Application Discontinuation
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- 2008-10-24 EP EP08841272A patent/EP2220050A2/en not_active Withdrawn
- 2008-10-24 PE PE2012000638A patent/PE20121470A1/es not_active Application Discontinuation
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2014
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2015
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|---|---|
| CA2703635A1 (en) | 2009-04-30 |
| TWI557111B (zh) | 2016-11-11 |
| JP5914538B2 (ja) | 2016-05-11 |
| EP2620432A2 (en) | 2013-07-31 |
| JP2014074070A (ja) | 2014-04-24 |
| JP2017052796A (ja) | 2017-03-16 |
| PE20091262A1 (es) | 2009-09-09 |
| HK1165198A1 (en) | 2012-09-28 |
| CA2703635C (en) | 2017-06-27 |
| CL2008003158A1 (es) | 2009-05-29 |
| WO2009055053A2 (en) | 2009-04-30 |
| CA2966280A1 (en) | 2009-04-30 |
| TW200934762A (en) | 2009-08-16 |
| WO2009055053A3 (en) | 2009-06-11 |
| JP2015180672A (ja) | 2015-10-15 |
| US20090111864A1 (en) | 2009-04-30 |
| US9896437B2 (en) | 2018-02-20 |
| UY31432A1 (es) | 2009-05-29 |
| TWI469971B (zh) | 2015-01-21 |
| TW201522315A (zh) | 2015-06-16 |
| AR069039A1 (es) | 2009-12-23 |
| JP5535925B2 (ja) | 2014-07-02 |
| TW201716385A (zh) | 2017-05-16 |
| EP2620432A3 (en) | 2013-12-18 |
| JP2011500813A (ja) | 2011-01-06 |
| PE20170428A1 (es) | 2017-05-14 |
| EP2397469A1 (en) | 2011-12-21 |
| EP2397469B1 (en) | 2014-12-31 |
| US20150065546A1 (en) | 2015-03-05 |
| US8680291B2 (en) | 2014-03-25 |
| EP2220050A2 (en) | 2010-08-25 |
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