PE20091262A1 - Compuestos de diarilhidantoina como antagonistas del receptor de androgeno - Google Patents
Compuestos de diarilhidantoina como antagonistas del receptor de androgenoInfo
- Publication number
- PE20091262A1 PE20091262A1 PE2008001821A PE2008001821A PE20091262A1 PE 20091262 A1 PE20091262 A1 PE 20091262A1 PE 2008001821 A PE2008001821 A PE 2008001821A PE 2008001821 A PE2008001821 A PE 2008001821A PE 20091262 A1 PE20091262 A1 PE 20091262A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- androgen receptor
- thioxo
- oxo
- phenyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 229940123407 Androgen receptor antagonist Drugs 0.000 title 1
- 239000003936 androgen receptor antagonist Substances 0.000 title 1
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 abstract 3
- -1 4- (3-CYANOPROPYL) PHENYL Chemical class 0.000 abstract 2
- 102000001307 androgen receptors Human genes 0.000 abstract 2
- 108010080146 androgen receptors Proteins 0.000 abstract 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 abstract 2
- 206010062904 Hormone-refractory prostate cancer Diseases 0.000 abstract 1
- RAXXELZNTBOGNW-UHFFFAOYSA-O Imidazolium Chemical compound C1=C[NH+]=CN1 RAXXELZNTBOGNW-UHFFFAOYSA-O 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
- 239000005557 antagonist Substances 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)
- Medicinal Preparation (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
REFERIDA A UN DERIVADO DE DIARILHIDANTOINA DE FORMULA (I), DONDE R1 Y R2 SON ALQUILO C1-C8, CICLOALQUILO C3-C20, ENTRE OTROS; R3 ES H, CN, FORMILO, IMIDAZOL, ENTRE OTROS; R4 ES H, F, Cl, Br, I; R11 Y R12 SON H O METILO. SON COMPUESTOS PREFERIDOS: 4-(3-(4-(3-CIANOPROPIL)FENIL)-4,4-DIMETIL-5-OXO-2-TIOXO-IMIDAZOLIDIN-1-IL)-2-(TRIFLUOROMETIL)BENZONITRILO, 4-(1-(4-(3-CIANOPROPIL)FENIL)-4-OXO-2-TIOXO-1,3-DIAZASPIRO[4,4]NON-3-IL)-2-TRIFLUOROMETILBENZONITRILO, 4-(8-OXO-5-(4-(4-OXOBUTIL)FENIL)-6-TIOXO-5,7-DIAZASPIRO[3.4]OCTAN-7-IL)-2-(TRIFLUOROMETIL)BENZONITRILO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD ANTAGONISTA SOBRE EL RECEPTOR DE ANDROGENO (AR) Y SON UTILES EN EL TRATAMIENTO DEL 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 |
|---|---|
| PE20091262A1 true PE20091262A1 (es) | 2009-09-09 |
Family
ID=40278902
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
| PE2017000081A PE20170428A1 (es) | 2007-10-26 | 2008-10-24 | Compuestos de diarilhidantoina |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2012000638A PE20121470A1 (es) | 2007-10-26 | 2008-10-24 | Compuestos de diarilhidantoina como antagonistas del receptor de androgeno |
| PE2017000081A PE20170428A1 (es) | 2007-10-26 | 2008-10-24 | Compuestos de diarilhidantoina |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US8680291B2 (es) |
| EP (3) | EP2620432A3 (es) |
| JP (4) | JP5535925B2 (es) |
| AR (1) | AR069039A1 (es) |
| CA (2) | CA2966280A1 (es) |
| CL (1) | CL2008003158A1 (es) |
| PE (3) | PE20091262A1 (es) |
| TW (3) | TWI557111B (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 |
| US8110594B2 (en) | 2006-03-29 | 2012-02-07 | The Regents Of The University Of California | Diarylthiohydantoin compounds |
| PE20091262A1 (es) * | 2007-10-26 | 2009-09-09 | Univ California | Compuestos de diarilhidantoina como antagonistas del receptor de androgeno |
| KR20110130439A (ko) | 2009-02-24 | 2011-12-05 | 메디베이션 프로스테이트 테라퓨틱스 인코퍼레이티드 | 특정 디아릴히단토인 및 디아릴티오히단토인 화합물 |
| US8710086B2 (en) * | 2009-04-09 | 2014-04-29 | Medivation Technologies, Inc. | Substituted di-arylhydantoin and di-arylthiohydantoin compounds and methods of 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 |
| WO2011044327A1 (en) | 2009-10-07 | 2011-04-14 | Medivation Prostate Therapeutics, Inc. | Substituted phenylcarbamoyl alkylamino arene compounds and n,n'-bis-arylurea 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 |
| PH12012501652A1 (en) | 2010-02-16 | 2012-10-22 | Aragon Pharmaceuticals Inc | Androgen receptor modulators and uses thereof |
| MX2012009782A (es) | 2010-02-24 | 2012-11-29 | Medivation Prostate Therapeutics Inc | Procesos para la sintesis de diariltiohidantoina y compuestos de diarilhidantoina. |
| CN102958364A (zh) * | 2010-05-28 | 2013-03-06 | 德克萨斯大学系统董事会 | 低聚苯甲酰胺化合物及其用途 |
| EP2646553A4 (en) * | 2010-11-12 | 2015-01-07 | Santaris Pharma As | COMPOSITIONS AND METHODS OF TREATING ANDROGEN RECEPTOR DEPENDENT DISORDERS INCLUDING CANCER |
| CN103608333B (zh) * | 2011-03-10 | 2016-01-06 | 苏州开拓药业有限公司 | 雄激素受体拮抗剂及其用途 |
| US8921378B2 (en) | 2011-04-21 | 2014-12-30 | Orion Corporation | Androgen receptor modulating carboxamides |
| ES2696074T3 (es) | 2011-07-29 | 2019-01-14 | Medivation Prostate Therapeutics Llc | Tratamiento del cáncer de mama |
| UY34646A (es) | 2012-03-02 | 2013-10-31 | Novartis Ag | Compuestos de espirohidantoína y su uso como moduladores selectivos del receptor de andrógenos |
| PL2864291T3 (pl) | 2012-06-26 | 2017-07-31 | Bayer Pharma Aktiengesellschaft | N-[4-(chinolin-4-yloksy)cykloheksylo(metylo)](hetero)arylokarboksyamidy jako antagoniści receptora androgenowego, ich wytwarzanie i zastosowanie jako produktów medycznych |
| ES2836424T3 (es) | 2012-09-26 | 2021-06-25 | Aragon Pharmaceuticals Inc | Antiandrógenos para tratar el cáncer de próstata no metastásico y resistente a la castración |
| 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 |
| AU2015360767A1 (en) | 2014-12-12 | 2017-06-08 | 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 |
| US10702508B2 (en) | 2017-10-16 | 2020-07-07 | Aragon Pharmaceuticals, Inc. | Anti-androgens for the treatment of non-metastatic castration-resistant prostate cancer |
| EP3876929A1 (en) | 2018-11-05 | 2021-09-15 | Pfizer Inc. | Combination for treating cancer |
| 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 PE PE2008001821A patent/PE20091262A1/es not_active Application Discontinuation
- 2008-10-24 PE PE2012000638A patent/PE20121470A1/es not_active Application Discontinuation
- 2008-10-24 CA CA2966280A patent/CA2966280A1/en not_active Abandoned
- 2008-10-24 JP JP2010531057A patent/JP5535925B2/ja active Active
- 2008-10-24 AR ARP080104661A patent/AR069039A1/es unknown
- 2008-10-24 EP EP13157028.5A patent/EP2620432A3/en not_active Withdrawn
- 2008-10-24 UY UY31432A patent/UY31432A1/es not_active Application Discontinuation
- 2008-10-24 CL CL2008003158A patent/CL2008003158A1/es unknown
- 2008-10-24 US US12/257,743 patent/US8680291B2/en active Active
- 2008-10-24 TW TW103138505A patent/TWI557111B/zh active
- 2008-10-24 EP EP11178889.9A patent/EP2397469B1/en active Active
- 2008-10-24 PE PE2017000081A patent/PE20170428A1/es not_active Application Discontinuation
- 2008-10-24 WO PCT/US2008/012149 patent/WO2009055053A2/en not_active Ceased
- 2008-10-24 EP EP08841272A patent/EP2220050A2/en not_active Withdrawn
- 2008-10-24 CA CA2703635A patent/CA2703635C/en active Active
- 2008-10-24 TW TW105126199A patent/TW201716385A/zh unknown
- 2008-10-24 TW TW97140820A patent/TWI469971B/zh active
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2014
- 2014-01-27 JP JP2014012363A patent/JP5914538B2/ja active Active
- 2014-03-24 US US14/224,005 patent/US9896437B2/en active Active
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2015
- 2015-06-03 JP JP2015112863A patent/JP2015180672A/ja active Pending
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|---|---|
| WO2009055053A2 (en) | 2009-04-30 |
| EP2220050A2 (en) | 2010-08-25 |
| US9896437B2 (en) | 2018-02-20 |
| JP2015180672A (ja) | 2015-10-15 |
| TWI557111B (zh) | 2016-11-11 |
| UY31432A1 (es) | 2009-05-29 |
| US20150065546A1 (en) | 2015-03-05 |
| TW200934762A (en) | 2009-08-16 |
| PE20121470A1 (es) | 2012-11-18 |
| JP2011500813A (ja) | 2011-01-06 |
| US20090111864A1 (en) | 2009-04-30 |
| TW201716385A (zh) | 2017-05-16 |
| TW201522315A (zh) | 2015-06-16 |
| EP2397469B1 (en) | 2014-12-31 |
| JP5535925B2 (ja) | 2014-07-02 |
| JP2017052796A (ja) | 2017-03-16 |
| US8680291B2 (en) | 2014-03-25 |
| EP2620432A2 (en) | 2013-07-31 |
| TWI469971B (zh) | 2015-01-21 |
| CA2703635C (en) | 2017-06-27 |
| JP5914538B2 (ja) | 2016-05-11 |
| CA2703635A1 (en) | 2009-04-30 |
| AR069039A1 (es) | 2009-12-23 |
| EP2620432A3 (en) | 2013-12-18 |
| CA2966280A1 (en) | 2009-04-30 |
| CL2008003158A1 (es) | 2009-05-29 |
| HK1165198A1 (en) | 2012-09-28 |
| EP2397469A1 (en) | 2011-12-21 |
| WO2009055053A3 (en) | 2009-06-11 |
| JP2014074070A (ja) | 2014-04-24 |
| PE20170428A1 (es) | 2017-05-14 |
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