PE20030708A1 - Derivados de piperazina desestabilizantes del receptor de androgenos - Google Patents
Derivados de piperazina desestabilizantes del receptor de androgenosInfo
- Publication number
- PE20030708A1 PE20030708A1 PE2002001124A PE2002001124A PE20030708A1 PE 20030708 A1 PE20030708 A1 PE 20030708A1 PE 2002001124 A PE2002001124 A PE 2002001124A PE 2002001124 A PE2002001124 A PE 2002001124A PE 20030708 A1 PE20030708 A1 PE 20030708A1
- Authority
- PE
- Peru
- Prior art keywords
- trifluoromethyl
- pentil
- pyrrol
- dihydro
- phenyl
- Prior art date
Links
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical class C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title abstract 2
- 102000001307 androgen receptors Human genes 0.000 title abstract 2
- 108010080146 androgen receptors Proteins 0.000 title abstract 2
- 229940066771 systemic antihistamines piperazine derivative Drugs 0.000 title abstract 2
- 230000000368 destabilizing effect Effects 0.000 title 1
- -1 CYANE Chemical class 0.000 abstract 3
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 3
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 abstract 1
- 208000002874 Acne Vulgaris Diseases 0.000 abstract 1
- 201000004384 Alopecia Diseases 0.000 abstract 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 abstract 1
- UGFAIRIUMAVXCW-UHFFFAOYSA-N Carbon monoxide Chemical class [O+]#[C-] UGFAIRIUMAVXCW-UHFFFAOYSA-N 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 abstract 1
- TUCNEACPLKLKNU-UHFFFAOYSA-N acetyl Chemical class C[C]=O TUCNEACPLKLKNU-UHFFFAOYSA-N 0.000 abstract 1
- 206010000496 acne Diseases 0.000 abstract 1
- 231100000360 alopecia Toxicity 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 239000013067 intermediate product Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 150000003254 radicals Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/44—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
- C07D207/444—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
- C07D207/448—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide
- C07D207/452—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
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- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D403/06—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 only aliphatic carbon atoms
-
- 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
- C07D403/12—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 chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A DERIVADOS DE PIPERAZINA DE FORMULA I DONDE V ES UN RADICAL AROMATICO DE FORMULA II DONDE A ES ACETILO, ACETILAMINO, CIANO, NITRO, TRIFLUOROMETILO, ENTRE OTROS; B ES H, HALOGENO, TRIFLUOROMETILO; A Y B JUNTOS FORMAN UN GRUPO CICLICO; W ES UN HETEROCICLO DE FORMULA III DONDE T ES C, N; i Y j SON 1-2; R Y R' SON O, METILO; Y EQUIVALE A UNA UNION ENTRE EL N Y HETEROCICLICO Y Z A UN GRUPO CARBONILO, SULFONILO, IMINOCARBONILO, IMINOSULFONILO, ENTRE OTROS; Z Y Z' SON ALQUILO C1-C8, CICLOALQUILO C3-C6, FENILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS 4-[5-[1-[4-CIANO-3-(TRIFLUOROMETILO)FENIL]-2,5-DIHIDRO-4-METIL-2,5-DIOXI-1H-PIRROL-3-IL]PENTIL]PIPERAZINI-1-CARBOXILATO DE 1,1-DIMETILETILO, 4-[2,5-DIHIDRO-3-METL-4-[5-[4-[2-(METILSULFANIL)FENIL]-PIPERAZIN-1-IL]PENTIL]-2,5-DIOXI-1H-PIRROL-1-IL]-2-(TRIFLUOROMETIL)BENZONITRILO, 4-[3-[5-[4-(4-CIANOBENZOIL)PIPERAZIN-1-IL]PENTIL]-2,5-DIHIDRO-4-METIL-2,5DIOXO-1H-PIRROL-1-IL]-2-(TRIFLUOROMETIL)BENZONITRILO, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO PARA LA PREPARACION Y PRODUCTOS INTERMEDIOS. LOS COMPUESTOS MENCIONADOS SON DESESTABILIZANTES DEL RECEPTOR DE ANDROGENOS Y SON UTILES PARA EL TRATAMIENTO DE HIPERPLASIA PROSTATICA BENIGNA, ALOPECIA, ACNE
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE2001159035 DE10159035A1 (de) | 2001-11-23 | 2001-11-23 | Androgenrezeptor destabilisierende Piperazinderivate |
| DE2002138742 DE10238742A1 (de) | 2002-08-19 | 2002-08-19 | Androgenrezeptor destabilisierende Piperazinderivate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20030708A1 true PE20030708A1 (es) | 2003-08-28 |
Family
ID=26010698
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2002001124A PE20030708A1 (es) | 2001-11-23 | 2002-11-22 | Derivados de piperazina desestabilizantes del receptor de androgenos |
Country Status (5)
| Country | Link |
|---|---|
| AU (1) | AU2002360932A1 (es) |
| PE (1) | PE20030708A1 (es) |
| TW (1) | TW200301117A (es) |
| UY (1) | UY27544A1 (es) |
| WO (1) | WO2003043983A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030195192A1 (en) * | 2002-04-05 | 2003-10-16 | Fortuna Haviv | Nicotinamides having antiangiogenic activity |
| JP2006519755A (ja) * | 2002-11-20 | 2006-08-31 | ロレアル | ピラゾール−カルボキシアミドを含有する毛髪の手入れ用又は睫毛用の組成物、毛髪及び睫毛の成長を刺激し、及び/又は抜毛を防止するためのそれらの使用 |
| FR2847160A1 (fr) * | 2002-11-20 | 2004-05-21 | Oreal | Composition capillaire contenant un compose pyrasol-carboxamide, son utilisation pour stimuler la pousse des cheveux et/ou freiner leur chute |
| US7592466B2 (en) | 2003-10-09 | 2009-09-22 | Abbott Laboratories | Ureas having antiangiogenic activity |
| AU2005216200A1 (en) * | 2004-02-22 | 2005-09-09 | Government Of The United States Of America, As Represented By The Secretary Department Of Health And Human Services | Maleiimide anti-tumor phosphatase inhibitors |
| CN101039927A (zh) * | 2004-09-09 | 2007-09-19 | 财团法人乙卯研究所 | 5-羟色胺5-ht3受体激动剂 |
| CN102464631B (zh) * | 2010-11-08 | 2016-08-10 | 中国科学院上海药物研究所 | 哌嗪取代的1,3-二取代脲类化合物及哌嗪取代的酰胺类化合物及其制备方法和用途 |
| BR102012000187A2 (pt) * | 2012-01-05 | 2018-04-10 | Univ Rio De Janeiro | Derivados n-fenilpiperazínicos antagonistas de adrenoceptores a1a, a1d e de receptores 5-ht1a no tratamento da hiperplasia prostática benigna, composições farmacêuticas contendo os mesmos |
| US12152035B2 (en) | 2020-12-30 | 2024-11-26 | Industrial Technology Research Institute | Androgen receptor binding molecule and use thereof |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2693461B1 (fr) * | 1992-07-08 | 1994-09-02 | Roussel Uclaf | Nouvelles phénylimidazolidines substituées, leur procédé de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant. |
| US5859014A (en) * | 1995-06-09 | 1999-01-12 | Syntex (U.S.A.) Inc. | Pyrimidinedione, pyrimidinetrione, triazinedione and tetrahydroquinazolinedione derivatives as α1 -adrenergic receptor antagonists |
| US5656651A (en) * | 1995-06-16 | 1997-08-12 | Biophysica Inc. | Androgenic directed compositions |
| US6673799B1 (en) * | 1998-09-22 | 2004-01-06 | Yamanouchi Pharmaceutical Co. Ltd. | Cyanophenyl derivative |
-
2002
- 2002-10-31 AU AU2002360932A patent/AU2002360932A1/en not_active Abandoned
- 2002-10-31 WO PCT/EP2002/012182 patent/WO2003043983A1/de not_active Ceased
- 2002-11-21 UY UY27544A patent/UY27544A1/es not_active Application Discontinuation
- 2002-11-22 TW TW091134064A patent/TW200301117A/zh unknown
- 2002-11-22 PE PE2002001124A patent/PE20030708A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AU2002360932A1 (en) | 2003-06-10 |
| UY27544A1 (es) | 2003-06-30 |
| WO2003043983A1 (de) | 2003-05-30 |
| TW200301117A (en) | 2003-07-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |