AR021757A1 - Metodo para inhibir la conversion de 4-androstan-3,17-diona en testosterona o de 3alfa-androstan-3,17-diona en dihidrotestosterona, inhibir la actividadde la 3alfa-hidroxiesteroide deshidrogenasa de tipo 3 humana, para determinar la eficacia de un inhibidor putativo de la conversion de 4-androsten-3 - Google Patents
Metodo para inhibir la conversion de 4-androstan-3,17-diona en testosterona o de 3alfa-androstan-3,17-diona en dihidrotestosterona, inhibir la actividadde la 3alfa-hidroxiesteroide deshidrogenasa de tipo 3 humana, para determinar la eficacia de un inhibidor putativo de la conversion de 4-androsten-3Info
- Publication number
- AR021757A1 AR021757A1 ARP990103961A ARP990103961A AR021757A1 AR 021757 A1 AR021757 A1 AR 021757A1 AR P990103961 A ARP990103961 A AR P990103961A AR P990103961 A ARP990103961 A AR P990103961A AR 021757 A1 AR021757 A1 AR 021757A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- type
- hydrogen
- androstan
- alkyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 5
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 title abstract 4
- 238000006243 chemical reaction Methods 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- NVKAWKQGWWIWPM-ABEVXSGRSA-N 17-β-hydroxy-5-α-Androstan-3-one Chemical compound C1C(=O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CC[C@H]21 NVKAWKQGWWIWPM-ABEVXSGRSA-N 0.000 title abstract 2
- 229960003473 androstanolone Drugs 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title abstract 2
- 229960003604 testosterone Drugs 0.000 title abstract 2
- 101710088194 Dehydrogenase Proteins 0.000 title 1
- 230000000694 effects Effects 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 150000002431 hydrogen Chemical class 0.000 abstract 5
- 101710172561 3alpha-hydroxysteroid dehydrogenase Proteins 0.000 abstract 3
- 102100036504 Dehydrogenase/reductase SDR family member 9 Human genes 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 150000001408 amides Chemical class 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 150000002576 ketones Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 1
- 102000012394 17beta-dehydrogenases Human genes 0.000 abstract 1
- 108050002933 17beta-dehydrogenases Proteins 0.000 abstract 1
- 201000004384 Alopecia Diseases 0.000 abstract 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 abstract 1
- 229940124186 Dehydrogenase inhibitor Drugs 0.000 abstract 1
- 206010020112 Hirsutism Diseases 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 229940124139 Hydroxysteroid dehydrogenase inhibitor Drugs 0.000 abstract 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 abstract 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 1
- 206010039792 Seborrhoea Diseases 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 201000002996 androgenic alopecia Diseases 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000001246 bromo group Chemical group Br* 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- KXGVEGMKQFWNSR-LLQZFEROSA-N deoxycholic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 KXGVEGMKQFWNSR-LLQZFEROSA-N 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- -1 nitro, hydroxyl Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 201000007094 prostatitis Diseases 0.000 abstract 1
- 208000008742 seborrheic dermatitis Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/566—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol having an oxo group in position 17, e.g. estrone
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
- A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9562398P | 1998-08-07 | 1998-08-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR021757A1 true AR021757A1 (es) | 2002-08-07 |
Family
ID=22252842
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990103961A AR021757A1 (es) | 1998-08-07 | 1999-08-06 | Metodo para inhibir la conversion de 4-androstan-3,17-diona en testosterona o de 3alfa-androstan-3,17-diona en dihidrotestosterona, inhibir la actividadde la 3alfa-hidroxiesteroide deshidrogenasa de tipo 3 humana, para determinar la eficacia de un inhibidor putativo de la conversion de 4-androsten-3 |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP1102582A2 (fr) |
| JP (1) | JP2002522380A (fr) |
| CN (1) | CN1322130A (fr) |
| AR (1) | AR021757A1 (fr) |
| AU (1) | AU5144999A (fr) |
| CA (1) | CA2339368A1 (fr) |
| ID (1) | ID28791A (fr) |
| NO (1) | NO20010651L (fr) |
| WO (1) | WO2000007576A2 (fr) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5504074A (en) | 1993-08-06 | 1996-04-02 | Children's Medical Center Corporation | Estrogenic compounds as anti-angiogenic agents |
| US6908910B2 (en) | 1993-08-06 | 2005-06-21 | The Children's Medical Center Corporation | Estrogenic compounds as anti-mitotic agents |
| EP1321146A3 (fr) * | 1998-03-11 | 2004-06-02 | Endorecherche Inc. | Inhibiteurs de la 17beta-hydroxysteroide deshydrogénase du type 5 et du type 3 ainsi que leurs méthodes d'utilisation |
| US7087592B1 (en) | 1999-08-23 | 2006-08-08 | Entre Med, Inc. | Compositions comprising purified 2-methoxyestradiol and methods of producing same |
| US6891953B1 (en) | 2000-06-27 | 2005-05-10 | Microsoft Corporation | Method and system for binding enhanced software features to a persona |
| US7135581B2 (en) | 2000-08-18 | 2006-11-14 | Entremed, Inc. | Antiangiogenic agents |
| US6995278B2 (en) * | 2000-08-18 | 2006-02-07 | Entre Med, Inc. | Antiangiogenic agents |
| AU2001288386B2 (en) * | 2000-11-27 | 2006-11-02 | Entremed, Inc. | 2-substituted estrogens as antiangiogenic agents |
| US6710037B2 (en) * | 2001-05-01 | 2004-03-23 | Schering Corporation | Method of treating androgen-dependent disorders |
| DE60239207D1 (de) * | 2001-08-10 | 2011-03-31 | Takeda Pharmaceutical | Gnrh-agonistische kombinationsmittel |
| US7524866B2 (en) | 2001-11-29 | 2009-04-28 | Gtx, Inc. | Prevention and treatment of androgen—deprivation induced osteoporosis |
| MXPA04005112A (es) * | 2001-11-29 | 2005-04-29 | Gtx Inc | Prevencion y tratamiento de osteoporosis inducida por privacion de androgeno. |
| JP2006526025A (ja) | 2003-05-28 | 2006-11-16 | エントレメッド インコーポレイテッド | 抗血管新生剤 |
| US7498322B2 (en) | 2004-03-12 | 2009-03-03 | Entremed, Inc. | Antiangiogenic agents |
| US7419972B2 (en) | 2004-07-02 | 2008-09-02 | Schering Ag | 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17β-hydroxy steroid dehydrogenase type 1 |
| DE102004032674A1 (de) * | 2004-07-02 | 2006-01-26 | Schering Ag | Neue 2-substituierte Estra-1,3,5(10)-trien-17-one als Inhibitoren der 17β-Hydroxysteroiddehydrogenase Typ 1 |
| WO2007109312A2 (fr) | 2006-03-20 | 2007-09-27 | Entremed, Inc. | 2-méthoxyestradiol présentant une activité anti-arthritique pouvant modifier l'évolution de la maladie |
| US9284345B2 (en) * | 2007-04-12 | 2016-03-15 | Endorecherche, Inc. | 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators |
| US8513422B2 (en) * | 2007-08-31 | 2013-08-20 | Astellas Pharma Inc. | Piperidine derivative |
| CN101698834B (zh) * | 2009-09-08 | 2012-05-23 | 北京利德曼生化股份有限公司 | 3α-羟基类固醇脱氢酶及其核苷酸序列、重组载体、重组宿主细胞和试剂盒 |
| US9512169B2 (en) * | 2012-07-10 | 2016-12-06 | Bayer Pharma Aktiengesellschaft | 3-substituted estra-1,3,5(10),16-tetraene derivatives, methods for the production thereof, pharmaceutical preparations containing same, and use thereof for the production of medicaments |
| EA201500851A1 (ru) * | 2013-02-21 | 2016-02-29 | Байер Фарма Акциенгезельшафт | ЭСТРА-1,3,5(10),16-ТЕТРАЕН-3-КАРБОКСАМИДЫ ДЛЯ ИНГИБИРОВАНИЯ 17β-ГИДРОКСИСТЕРОИД-ДЕГИДРОГЕНАЗЫ (AKR1C3) |
| CN104873520A (zh) * | 2014-02-27 | 2015-09-02 | 天津药物研究院 | 一种11β-羟基类固醇脱氢酶抑制剂、药用组合物及其用途 |
| CN104873525A (zh) * | 2014-02-27 | 2015-09-02 | 天津药物研究院 | 一种11β-羟基类固醇脱氢酶抑制剂及其药用组合物和用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3562260A (en) * | 1965-08-23 | 1971-02-09 | Ormonoterapia Richter Spa | 2-carbonyl-estratrienes and method of their preparation |
| US4340602A (en) * | 1978-10-18 | 1982-07-20 | Wayne State University | Compositions inhibiting estrogen sulfotransferase activity |
| GB2135189B (en) * | 1983-02-22 | 1986-07-09 | Joachim Georg Liehr | Estrogen deficiency conditioned with 2-fluoroestradiols |
| US4568673A (en) * | 1984-03-20 | 1986-02-04 | Wayne State University | Compositions inhibiting murine MXT ductal carcinoma |
| US5504074A (en) * | 1993-08-06 | 1996-04-02 | Children's Medical Center Corporation | Estrogenic compounds as anti-angiogenic agents |
| TR200002784T2 (tr) * | 1998-03-11 | 2000-12-21 | Endorecherche, Inc | Tip 5 ve tip 3 17beta-Hidroksisteroid dehidrojenaz inhibitörleri ve bunların kullanımı için metodlar |
-
1999
- 1999-08-06 AR ARP990103961A patent/AR021757A1/es unknown
- 1999-08-06 EP EP99936218A patent/EP1102582A2/fr not_active Withdrawn
- 1999-08-06 WO PCT/CA1999/000724 patent/WO2000007576A2/fr not_active Ceased
- 1999-08-06 ID IDW20010531A patent/ID28791A/id unknown
- 1999-08-06 CA CA002339368A patent/CA2339368A1/fr not_active Abandoned
- 1999-08-06 JP JP2000563261A patent/JP2002522380A/ja active Pending
- 1999-08-06 AU AU51449/99A patent/AU5144999A/en not_active Abandoned
- 1999-08-06 CN CN99811739A patent/CN1322130A/zh active Pending
-
2001
- 2001-02-07 NO NO20010651A patent/NO20010651L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CA2339368A1 (fr) | 2000-02-17 |
| EP1102582A2 (fr) | 2001-05-30 |
| WO2000007576A2 (fr) | 2000-02-17 |
| NO20010651L (no) | 2001-04-05 |
| JP2002522380A (ja) | 2002-07-23 |
| CN1322130A (zh) | 2001-11-14 |
| AU5144999A (en) | 2000-02-28 |
| ID28791A (id) | 2001-07-05 |
| WO2000007576A3 (fr) | 2000-03-30 |
| NO20010651D0 (no) | 2001-02-07 |
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