CN102149687B - 作为雄激素受体调节剂的咪唑烷化合物 - Google Patents
作为雄激素受体调节剂的咪唑烷化合物 Download PDFInfo
- Publication number
- CN102149687B CN102149687B CN200980135475.9A CN200980135475A CN102149687B CN 102149687 B CN102149687 B CN 102149687B CN 200980135475 A CN200980135475 A CN 200980135475A CN 102149687 B CN102149687 B CN 102149687B
- Authority
- CN
- China
- Prior art keywords
- dioxo
- methyl
- compounds
- compound
- acceptable salt
- 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.)
- Expired - Fee Related
Links
- 0 CC=C(*)C=CC([C@@](CO)(C(N1c(cc2)cc(C)c2C#N)=O)N(C)C1=O)=CC=C* Chemical compound CC=C(*)C=CC([C@@](CO)(C(N1c(cc2)cc(C)c2C#N)=O)N(C)C1=O)=CC=C* 0.000 description 1
Classifications
-
- 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
- C07D233/56—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 only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D233/60—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 only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
-
- 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
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/26—Androgens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
-
- 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
- C07D233/72—Two oxygen atoms, e.g. hydantoin
- C07D233/74—Two oxygen atoms, e.g. hydantoin with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to other ring members
-
- 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
- C07D233/72—Two oxygen atoms, e.g. hydantoin
- C07D233/76—Two oxygen atoms, e.g. hydantoin with substituted hydrocarbon radicals attached to the third ring carbon atom
- C07D233/78—Radicals substituted by oxygen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Neurology (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19191808P | 2008-09-11 | 2008-09-11 | |
| US61/191,918 | 2008-09-11 | ||
| GB0900333.6A GB2463514C (en) | 2008-09-11 | 2009-01-09 | Imidazolidine compounds and uses therefor |
| GB0900333.6 | 2009-01-09 | ||
| PCT/EP2009/061733 WO2010029119A1 (en) | 2008-09-11 | 2009-09-10 | Novel imidazolidine compounds as androgen receptor modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102149687A CN102149687A (zh) | 2011-08-10 |
| CN102149687B true CN102149687B (zh) | 2014-08-13 |
Family
ID=40379370
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200980135475.9A Expired - Fee Related CN102149687B (zh) | 2008-09-11 | 2009-09-10 | 作为雄激素受体调节剂的咪唑烷化合物 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US7968581B2 (https=) |
| EP (1) | EP2344460B1 (https=) |
| JP (1) | JP5595402B2 (https=) |
| KR (1) | KR101705157B1 (https=) |
| CN (1) | CN102149687B (https=) |
| AR (1) | AR073282A1 (https=) |
| AU (1) | AU2009290849B2 (https=) |
| BR (1) | BRPI0919290A2 (https=) |
| CA (1) | CA2736364C (https=) |
| CO (1) | CO6382130A2 (https=) |
| ES (1) | ES2552684T3 (https=) |
| GB (1) | GB2463514C (https=) |
| IL (1) | IL211277A (https=) |
| MX (1) | MX2011002374A (https=) |
| NZ (1) | NZ591374A (https=) |
| RU (1) | RU2488584C2 (https=) |
| TW (1) | TWI449698B (https=) |
| WO (1) | WO2010029119A1 (https=) |
| ZA (1) | ZA201101707B (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8168667B2 (en) * | 2006-05-31 | 2012-05-01 | Galapagos Nv | Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such |
| DK2683694T3 (en) | 2011-03-10 | 2016-07-18 | Suzhou Kintor Pharmaceuticals Inc | ANDROGEN RECEPTOR ANTAGONISTS AND APPLICATIONS THEREOF |
| GB201311107D0 (en) * | 2013-06-21 | 2013-08-07 | Univ Edinburgh | Bioorthogonal methods and compounds |
| AU2014290368B2 (en) * | 2013-07-18 | 2019-07-11 | Baylor College Of Medicine | Methods and compositions for treatment of muscle wasting, muscle weakness, and/or cachexia |
| CA2928235A1 (en) * | 2013-10-25 | 2015-04-30 | Bush, Ernest D. | Methods for treatment of muscular dystrophies |
| JP6227149B2 (ja) * | 2013-12-31 | 2017-11-08 | イプセン ファルマ ソシエテ パール アクシオン サンプリフィエIpsen Pharma S.A.S. | 新規のイミダゾリジン−2,4−ジオン誘導体 |
| JP7028987B2 (ja) * | 2017-12-06 | 2022-03-02 | アイブライト メディカル テクノロジー (ペキン) カンパニー リミテッド | オルソケラトロジーレンズおよびその製造方法 |
| US11026905B2 (en) | 2018-04-19 | 2021-06-08 | Tvardi Therapeutics, Inc. | STAT3 inhibitors |
| US11826315B2 (en) | 2018-04-19 | 2023-11-28 | Tvardi Therapeutics | STAT3 inhibitors |
| CA3159181A1 (en) | 2020-01-24 | 2021-07-29 | Imran ALIBHAI | Therapeutic compounds, formulations, and uses thereof |
| CN113024513A (zh) * | 2021-03-22 | 2021-06-25 | 中国药科大学 | 新型雄激素受体降解剂、制备方法和医药用途 |
| CN113801064A (zh) * | 2021-09-26 | 2021-12-17 | 甘肃省化工研究院有限责任公司 | 一种[3+2]环加成反应构建苯基乙内酰脲的方法 |
| WO2023244946A1 (en) | 2022-06-15 | 2023-12-21 | Tvardi Therapeutics, Inc. | Prodrugs of stat3 inhibitors |
| CN117327019A (zh) * | 2022-06-23 | 2024-01-02 | 南京思聚生物医药有限公司 | 一种局部作用的雄激素受体拮抗剂的应用 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997019064A1 (fr) * | 1995-11-22 | 1997-05-29 | Hoechst Marion Roussel | Nouvelles phenylimidazolidines fluorees ou hydroxylees ayant une activite anti-androgenique, leur procede de preparation, intermediaires obtenus et compositions pharmaceutiques |
| CN101056862A (zh) * | 2004-09-10 | 2007-10-17 | 詹森药业有限公司 | 作为选择性雄激素受体调节剂(sarms)的新的咪唑烷-2-酮衍生物 |
| WO2007137874A2 (en) * | 2006-05-31 | 2007-12-06 | Galapagos Sas | Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5136332B1 (https=) * | 1970-12-09 | 1976-10-07 | ||
| GB1601310A (en) * | 1978-05-23 | 1981-10-28 | Lilly Industries Ltd | Aryl hydantoins |
| DE2855770A1 (de) | 1978-12-22 | 1980-07-10 | Bayer Ag | Hydantoine |
| US4753957A (en) | 1981-09-28 | 1988-06-28 | Rohm And Haas Company | Substituted 2,4-imidazolidinediones and fungicidal compositions |
| DE3382406D1 (de) | 1982-04-08 | 1991-10-17 | Shell Int Research | Neue hydantoine, ihre herstellung und verwendung. |
| FR2619381B1 (fr) * | 1987-08-13 | 1989-12-08 | Roussel Uclaf | Nouvelles imidazolidines substituees par un radical hydroxymethyle et un radical phenyl substitue, leur procede de preparation, leur application comme medicaments, les compositions pharmaceutiques les renfermant et un intermediaire pour leur preparation |
| JP2566792B2 (ja) | 1987-09-30 | 1996-12-25 | 株式会社資生堂 | 発毛、養毛促進剤 |
| JPH0219363A (ja) | 1988-07-06 | 1990-01-23 | Fujisawa Pharmaceut Co Ltd | イミダゾリジン誘導体 |
| US4992443A (en) | 1990-03-12 | 1991-02-12 | William Chelen | Method of treating motion sickness |
| US5346913A (en) | 1992-05-26 | 1994-09-13 | Rohm And Haas Company | N-iodopropargyl hydantoin compounds, compositions, preparation, and use as antimicrobial agents |
| JP3137430B2 (ja) | 1992-06-10 | 2001-02-19 | 鐘淵化学工業株式会社 | 5,5−二置換ヒダントインの製造法 |
| US6846525B2 (en) | 1993-03-19 | 2005-01-25 | Xerox Corporation | Recording sheets containing purine, pyrimidine, benzimidazole, imidazolidine, urazole, pyrazole, triazole, benzotriazole, tetrazole, and pyrazine compounds |
| FR2715402B1 (fr) * | 1994-01-05 | 1996-10-04 | Roussel Uclaf | Nouvelles phénylimidazolines éventuellement substituées, leur procédé et des intermédiaires de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant. |
| TW521073B (en) * | 1994-01-05 | 2003-02-21 | Hoechst Marion Roussel Inc | New optionally substituted phenylimidazolidines, their preparation process, their use as anti-androgenic agent and the pharmaceutical compositions containing them |
| WO1995029909A1 (en) | 1994-04-29 | 1995-11-09 | Pfizer Inc. | Novel acyclic and cyclic amides as neurotransmitter release enhancers |
| EP0760239A3 (en) | 1995-09-01 | 1999-04-14 | Pfizer Inc. | Therapeutic agents for use in cancer therapy |
| US6355664B1 (en) | 1997-03-03 | 2002-03-12 | Boehringer Ingelheim Pharmaceuticals, Inc. | Phenylpyrrolidines, phenylimidazolidines, 3-phenyl-1,3-oxizolidines and 3-phenyl-1,3-thiazolidines and their use in the treatment of inflammatory disease |
| PL336580A1 (en) * | 1997-03-03 | 2000-07-03 | Boehringer Ingelheim Pharma | Fine-molecular compounds useful in treating inflammatory diseases |
| UA57081C2 (uk) | 1997-06-16 | 2003-06-16 | Пфайзер Продактс Інк. | Фармацевтична композиція для лікування раку або доброякісних проліферативних хвороб у ссавців, спосіб лікування, фармацевтична композиція для інгібування ненормального росту клітин у ссавців та спосіб інгібування |
| US6492553B1 (en) | 1998-01-29 | 2002-12-10 | Aventis Pharamaceuticals Inc. | Methods for preparing N-[(aliphatic or aromatic)carbonyl)]-2-aminoaetamide compounds and for cyclizing such compounds |
| EP0945441A3 (de) | 1998-03-27 | 2002-07-17 | Degussa AG | Verfahren zur Herstellung von cyclischen 4-Oxoamidinen |
| MXPA02011079A (es) | 2000-05-11 | 2004-08-19 | Consejo Superior Investigacion | Inhibidores heterociclicos de quinasa de sintasa de glucogeno gsk3. |
| US6846643B2 (en) | 2000-08-14 | 2005-01-25 | Boehringer Ingelheim Pharmaceuticals, Inc. | Methods and molecules useful for identifying molecules that bind LFA-1 and for determining receptor occupancy |
| KR20080066949A (ko) | 2005-10-11 | 2008-07-17 | 인터뮨, 인크. | 바이러스 복제 억제제 |
-
2009
- 2009-01-09 GB GB0900333.6A patent/GB2463514C/en not_active Expired - Fee Related
- 2009-09-09 AR ARP090103461A patent/AR073282A1/es unknown
- 2009-09-10 AU AU2009290849A patent/AU2009290849B2/en not_active Ceased
- 2009-09-10 EP EP09782854.5A patent/EP2344460B1/en active Active
- 2009-09-10 JP JP2011526487A patent/JP5595402B2/ja not_active Expired - Fee Related
- 2009-09-10 MX MX2011002374A patent/MX2011002374A/es active IP Right Grant
- 2009-09-10 CN CN200980135475.9A patent/CN102149687B/zh not_active Expired - Fee Related
- 2009-09-10 CA CA2736364A patent/CA2736364C/en not_active Expired - Fee Related
- 2009-09-10 RU RU2011113749/04A patent/RU2488584C2/ru not_active IP Right Cessation
- 2009-09-10 WO PCT/EP2009/061733 patent/WO2010029119A1/en not_active Ceased
- 2009-09-10 ES ES09782854.5T patent/ES2552684T3/es active Active
- 2009-09-10 KR KR1020117007686A patent/KR101705157B1/ko not_active Expired - Fee Related
- 2009-09-10 BR BRPI0919290-5A patent/BRPI0919290A2/pt not_active Application Discontinuation
- 2009-09-10 NZ NZ591374A patent/NZ591374A/en not_active IP Right Cessation
- 2009-09-10 US US12/557,368 patent/US7968581B2/en active Active
- 2009-09-11 TW TW098130825A patent/TWI449698B/zh not_active IP Right Cessation
-
2011
- 2011-02-17 IL IL211277A patent/IL211277A/en not_active IP Right Cessation
- 2011-03-04 ZA ZA2011/01707A patent/ZA201101707B/en unknown
- 2011-04-08 CO CO11043783A patent/CO6382130A2/es not_active Application Discontinuation
- 2011-06-23 US US13/167,682 patent/US8383608B2/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997019064A1 (fr) * | 1995-11-22 | 1997-05-29 | Hoechst Marion Roussel | Nouvelles phenylimidazolidines fluorees ou hydroxylees ayant une activite anti-androgenique, leur procede de preparation, intermediaires obtenus et compositions pharmaceutiques |
| CN101056862A (zh) * | 2004-09-10 | 2007-10-17 | 詹森药业有限公司 | 作为选择性雄激素受体调节剂(sarms)的新的咪唑烷-2-酮衍生物 |
| WO2007137874A2 (en) * | 2006-05-31 | 2007-12-06 | Galapagos Sas | Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| ASS | Succession or assignment of patent right |
Owner name: DART THERAPEUTICS, LLC Free format text: FORMER OWNER: GALAPAGOS N. V. Effective date: 20121112 |
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