AR036812A1 - Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos compuestos para la fabricacion de medicamentos para el tratamiento de enfermedades androgeno-dependientes - Google Patents
Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos compuestos para la fabricacion de medicamentos para el tratamiento de enfermedades androgeno-dependientesInfo
- Publication number
- AR036812A1 AR036812A1 ARP020103851A ARP020103851A AR036812A1 AR 036812 A1 AR036812 A1 AR 036812A1 AR P020103851 A ARP020103851 A AR P020103851A AR P020103851 A ARP020103851 A AR P020103851A AR 036812 A1 AR036812 A1 AR 036812A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- alkyl
- aryl
- heteroaryl
- heteroarylalkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 201000010099 disease Diseases 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 101710088194 Dehydrogenase Proteins 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000001072 heteroaryl group Chemical group 0.000 abstract 8
- 125000003545 alkoxy group Chemical group 0.000 abstract 7
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 7
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 7
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 5
- 125000004104 aryloxy group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- -1 methylenedioxy, difluoromethylenedioxy Chemical group 0.000 abstract 4
- 102000054917 17-beta-hydroxysteroid dehydrogenase type 3 Human genes 0.000 abstract 2
- 108010084625 17-beta-hydroxysteroid dehydrogenase type 3 Proteins 0.000 abstract 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- NFGODEMQGQNUKK-UHFFFAOYSA-M [6-(diethylamino)-9-(2-octadecoxycarbonylphenyl)xanthen-3-ylidene]-diethylazanium;chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCCCCOC(=O)C1=CC=CC=C1C1=C2C=CC(=[N+](CC)CC)C=C2OC2=CC(N(CC)CC)=CC=C21 NFGODEMQGQNUKK-UHFFFAOYSA-M 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 239000003098 androgen Substances 0.000 abstract 1
- 125000003917 carbamoyl group Chemical class [H]N([H])C(*)=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005114 heteroarylalkoxy group Chemical group 0.000 abstract 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 125000004950 trifluoroalkyl group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
- 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
- A61P17/10—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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- A61P5/28—Antiandrogens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3 de la fórmula (1), una de sus prodrogas, o una de las sales o solvatos aceptables para uso farmacéutico del compuesto o de la prodroga, en la cual, R1 se selecciona del grupo conformado por arilo, heteroarilo, arilalquilo, heteroarilalquilo y difenilalquilo, cada uno sustituido en forma opcional con 1 a 6 grupos seleccionados del grupo conformado por: halógeno, -OCF3 u -OCHF2, -CF3, -CN, alquilo o R18-alquilo, heteroalquilo o R18-heteroalquilo, arilo o R18-arilo, heteroarilo o R18-heteroarilo, arilalquilo o R18-arilalquilo, heteroarilalquilo o R18-heteroarilalquilo, hidroxi, alcoxi, ariloxi, -SO2-alquilo, -NR11R12, -N(R11)C(O)R13, metilendioxi, difluorometilendioxi, trifluoroalcoxi, -SCH3 ó -SCF3, y -SO2CF3 ó -NHSO2CF3; R2 y R3 se seleccionan, cada uno en forma independiente, del grupo conformado por: H, -OH, alcoxi, alquilo, cicloalquilo, heterocicloalquilo, cicloalquilalquilo, trifluoroalquilo, heteroalquilo, arilalquilo, heteroarilalquilo, arilalcoxi, heteroarilalcoxi, -(CH2)n-NR11R12 y -(CH2)n-SR11, con la salvedad de que cuando X es N, entonces R2 y R3 no sean, cada uno, -OH, alcoxi, arilalcoxi ó heteroarilalcoxi; R4, R5, R7 y R8 se seleccionan, cada uno en forma independiente, del grupo conformado por: H, -OR14, -NR11R12, -N(R11)C(O)R13, alquilo, arilo, cicloalquilo, arilalquilo, heteroalquilo, heteroarilo, heteroarilalquilo, heterocicloalquilo, fórmulas (2), (3) y (4), con la salvedad de que cuando Z y/o X son N, entonces R4, R5, R7 y R8 no sean, cada uno, -OR14, -NR11R12, ó -N(R11)C(O)R13; R6 se selecciona del grupo conformado por -C(O)R15 y -SO2R15; R9 y R10 se seleccionan, cada uno en forma independiente, del grupo conformado por: H, F, -CF3, -CHF2, alquilo, cicloalquilo, arilalquilo, heteroalquilo, heteroarilalquilo, heterocicloalquilo, hidroxi, alcoxi, ariloxi, -NR11R12 y -N(R11)C(O)R13 con la salvedad de que cuando Z es N, entonces R9 y R10 no sean, cada uno, F, hidroxi, alcoxi, ariloxi, -NR11R12 ó -N(R11)C(O)R13; R11 se selecciona del grupo conformado por H, alquilo, arilo y heteroarilo; R12 se selecciona del grupo conformado por H, alquilo, arilo y heteroarilo; R13 se selecciona del grupo conformado por alquilo, alcoxi y ariloxi; R14 se selecciona del grupo conformado por H, alquilo, arilo y heteroarilo; R15 se selecciona del grupo conformado por: -NR16R17, -OR16, alquilo, cicloalquilo, heterocicloalquilo, arilo, arilalquilo y heteroarilalquilo, cada uno sustituido en forma opcional con R18; R16 y R17 se seleccionan, cada uno en forma independiente, del grupo conformado por: alquilo, arilo, arilalquilo, heteroalquilo, y heteroarilo, cada uno sustituido en forma opcional con R18, y H, con la salvedad de que cuando R15 es -OR16, entonces R16 no sea H; R18 tiene de 1 a 4 sustituyentes cada uno seleccionado en forma independiente del grupo conformado por: alquilo inferior, halo, ciano, nitro, haloalquilo, hidroxi, alcoxi, carboxi, carboxialquilo, carboxamida, mercapto, amino, alquilamino, dialquilamino, sulfonilo, sulfonamido, arilo y heteroarilo; X y Z se seleccionan, cada uno en forma independiente del grupo conformado por C y N; y n es 1-4; que son útiles como inhibidores de 17beta-hidroxiesteroide deshidrogenasa tipo 3: Se describen, además, composiciones farmacéuticas que contienen dichos compuestos y uso para la fabricación de medicamentos para el tratamiento o la prevención de enfermedades andrógeno-dependientes.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33006601P | 2001-10-17 | 2001-10-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036812A1 true AR036812A1 (es) | 2004-10-06 |
Family
ID=23288179
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020103851A AR036812A1 (es) | 2001-10-17 | 2002-10-15 | Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos compuestos para la fabricacion de medicamentos para el tratamiento de enfermedades androgeno-dependientes |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US6969718B2 (es) |
| EP (1) | EP1436281B1 (es) |
| JP (1) | JP4309761B2 (es) |
| CN (1) | CN1571782A (es) |
| AR (1) | AR036812A1 (es) |
| AT (1) | ATE471315T1 (es) |
| CA (1) | CA2463626C (es) |
| DE (1) | DE60236743D1 (es) |
| ES (1) | ES2347643T3 (es) |
| MX (1) | MXPA04003611A (es) |
| PE (1) | PE20030705A1 (es) |
| WO (1) | WO2003033487A1 (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4614770B2 (ja) * | 2002-11-18 | 2011-01-19 | シェーリング コーポレイション | アンドロゲン依存性疾患を処置するための17β−ヒドロキシステロイドデヒドロゲナーゼタイプ3インヒビター |
| AU2003293555A1 (en) | 2002-12-17 | 2004-07-29 | Schering Corporation | 17 beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases |
| GB0314733D0 (en) * | 2003-06-24 | 2003-07-30 | Glaxo Group Ltd | Medicaments |
| US20050153976A1 (en) * | 2003-12-17 | 2005-07-14 | Schering Corporation | Pharmaceutical compositions |
| US7365075B2 (en) * | 2003-12-22 | 2008-04-29 | Amgen Inc. | Aryl sulfonamide compounds and uses related thereto |
| GB0513702D0 (en) | 2005-07-04 | 2005-08-10 | Sterix Ltd | Compound |
| CA2606004A1 (en) * | 2005-08-02 | 2007-02-08 | Neurogen Corporation | Dipiperazinyl ketones and related analogues |
| US8080540B2 (en) | 2006-09-19 | 2011-12-20 | Abbott Products Gmbh | Therapeutically active triazoles and their use |
| US8288367B2 (en) | 2006-11-30 | 2012-10-16 | Solvay Pharmaceuticals Gmbh | Substituted estratriene derivatives as 17BETA HSD inhibitors |
| TW201512215A (zh) | 2013-06-25 | 2015-04-01 | Forendo Pharma Ltd | 治療活性雌三烯噻唑衍生物 |
| AR096727A1 (es) | 2013-06-25 | 2016-01-27 | Forendo Pharma Ltd | Derivados terapéuticamente activos de estratrien-tiazol |
| MX2015017879A (es) | 2013-06-25 | 2017-03-01 | Forendo Pharma Ltd | Derivados de estratrientiazol 17-nitrogeno substitutidos terapeuticamente activos como inhibidores de 17.beta-hidroxiestero ide deshidrogenasa. |
| JP6545266B2 (ja) | 2014-12-23 | 2019-07-17 | フォレンド ファーマ リミテッド | 17β‐HSD1抑制剤のプロドラッグ |
| EP3237431B1 (en) | 2014-12-23 | 2019-03-20 | Forendo Pharma Ltd | Prodrugs of 17.beta.-hsd1 -inhibitors |
| DK3634975T3 (da) | 2017-06-08 | 2024-05-27 | Organon R&D Finland Ltd | 17-oximer af 15.beta.-[3-propanamido]-substituerede estra-1,3,5(10)-trien-17-oner til anvendelse i inhibition af 17.beta.-hydroxysteroid-dehydrogenaser |
| MA51139A (fr) * | 2017-12-15 | 2020-10-21 | Inthera Bioscience AG | Dérivés de 1-(pipéridinocarbonylméthyl)-2-oxopipérazine pour le traitement du cancer |
| EP3891167B1 (en) | 2018-12-05 | 2024-11-13 | Organon R&D Finland Oy | Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1 |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3576810A (en) * | 1968-06-20 | 1971-04-27 | Robins Co Inc A H | 1-substituted-3-(-4)-aroylpiperidines |
| DE2304154A1 (de) * | 1973-01-29 | 1974-08-01 | Ichthyol Ges Cordes Hermanni & | Verfahren zur herstellung von substituierten piperazin- bzw. homopiperazinderivaten |
| DE2304153A1 (de) * | 1973-01-29 | 1974-08-01 | Ichthyol Ges Cordes Hermanni & | Substituierte piperazin- und homopiperazinderivate |
| WO1986001105A1 (en) | 1984-08-02 | 1986-02-27 | Fernand Labrie | Pharmaceutical composition for combination therapy of hormone dependent cancers |
| EP0462189B1 (en) | 1989-03-10 | 1995-09-27 | Endorecherche Inc. | Combination therapy for treatment of estrogen sensitive diseases |
| ATE269066T1 (de) | 1989-07-07 | 2004-07-15 | Endorech Inc | Kombinationstherapie zur prophylaxe und/oder behandlung von gutartiger prostatischer hyperplasie |
| ATE230994T1 (de) | 1989-07-07 | 2003-02-15 | Endorech Inc | Methode zur behandlung androgenbedingter krankheiten |
| IL99320A (en) * | 1990-09-05 | 1995-07-31 | Sanofi Sa | Arylalkylamines, their preparation and pharmaceutical compositions containing them |
| WO1992006971A1 (en) * | 1990-10-10 | 1992-04-30 | Schering Corporation | Pyridine and pyridine n-oxide derivatives of diaryl methyl piperidines or piperazines, and compositions and methods of use thereof |
| US6060503A (en) | 1991-12-02 | 2000-05-09 | Endorecherche, Inc. | Benzopyran-containing compounds and method for their use |
| ATE140224T1 (de) * | 1992-03-27 | 1996-07-15 | Schering Corp | Unverbrückte bis-aryl-carbinol-derivate, zusammensetzungen und ihre verwendung |
| WO1994010165A1 (en) | 1992-10-28 | 1994-05-11 | Merck Sharp & Dohme Limited | 4-arylmethyloxymethyl piperidines as tachykinin antagonists |
| US5661162A (en) | 1992-12-14 | 1997-08-26 | Merck Sharp & Dohme Limited | 4-aminomethyl/thiomethyl/sulfonylmethyl-4-phenylpiperdines as tachykinin receptor antagonists |
| JP2741286B2 (ja) | 1993-05-17 | 1998-04-15 | アンドルシェルシュ・インコーポレイテッド | 改良された抗アンドロゲン |
| JPH08511522A (ja) | 1993-06-07 | 1996-12-03 | メルク エンド カンパニー インコーポレーテッド | ニューロキニンアンタゴニストとしてのスピロ置換アザ環 |
| IL111730A (en) * | 1993-11-29 | 1998-12-06 | Fujisawa Pharmaceutical Co | Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same |
| DE69504300T2 (de) * | 1994-01-13 | 1999-04-29 | Merck Sharp & Dohme Ltd., Hoddesdon, Hertfordshire | Gem-bissubstituierte azazyclische tachykinin-antagonisten |
| ATE242231T1 (de) * | 1995-04-07 | 2003-06-15 | Schering Corp | Carbonyl-piperaznyl und piperidinyl derivate zur hemmung farnesyl protein transferase |
| US5688960A (en) * | 1995-05-02 | 1997-11-18 | Schering Corporation | Substituted oximes, hydrazones and olefins useful as neurokinin antagonists |
| US5696267A (en) * | 1995-05-02 | 1997-12-09 | Schering Corporation | Substituted oximes, hydrazones and olefins as neurokinin antagonists |
| US5719156A (en) * | 1995-05-02 | 1998-02-17 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| US5795894A (en) * | 1995-05-02 | 1998-08-18 | Schering Corporation | Piperazino derivatives as neurokinn antagonists |
| US5654316A (en) * | 1995-06-06 | 1997-08-05 | Schering Corporation | Piperidine derivatives as neurokinin antagonists |
| US5892039A (en) * | 1995-08-31 | 1999-04-06 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| US6124115A (en) | 1995-09-22 | 2000-09-26 | Endorecherche Inc. | Production and use of isolated type 5 17β-hydroxysteroid dehydrogenase |
| DE19614204A1 (de) * | 1996-04-10 | 1997-10-16 | Thomae Gmbh Dr K | Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| US5691362A (en) * | 1996-06-05 | 1997-11-25 | Schering-Plough Corporation | Substituted benzene-fused hetero- and carbocyclics as nuerokinin antagonists |
| US5789422A (en) * | 1996-10-28 | 1998-08-04 | Schering Corporation | Substituted arylalkylamines as neurokinin antagonists |
| US5968929A (en) * | 1996-10-30 | 1999-10-19 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| US5945428A (en) * | 1996-11-01 | 1999-08-31 | Schering Corporation | Substituted oximes, hydrazones and olefins as neurokinin antagonists |
| US5783579A (en) * | 1996-12-20 | 1998-07-21 | Schering Corporation | Spiro-substituted azacyclic-substituted piperazino derivatives as neurokinin antagonists |
| US6063926A (en) * | 1998-11-18 | 2000-05-16 | Schering Corporation | Substituted oximes as neurokinin antagonists |
| ATE299140T1 (de) * | 1998-12-23 | 2005-07-15 | Schering Corp | Farnesyl-protein transferase inhibitoren |
| US6204265B1 (en) * | 1998-12-23 | 2001-03-20 | Schering Corporation | Substituted oximes and hydrazones as neurokinin antagonists |
| EP1146873B1 (en) | 1999-01-25 | 2005-03-16 | Smithkline Beecham Corporation | Anti-androgens and methods for treating disease |
| AU1413301A (en) * | 1999-11-17 | 2001-05-30 | Sumitomo Pharmaceuticals Company, Limited | Diabetic remedy containing dipiperazine derivative |
| AR036492A1 (es) * | 2001-09-06 | 2004-09-15 | Schering Corp | Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos inhibidores para la elaboracion de un medicamento para el tratamiento de enfermedades androgeno dependientes |
-
2002
- 2002-10-15 ES ES02773770T patent/ES2347643T3/es not_active Expired - Lifetime
- 2002-10-15 WO PCT/US2002/032979 patent/WO2003033487A1/en not_active Ceased
- 2002-10-15 CN CNA02820557XA patent/CN1571782A/zh active Pending
- 2002-10-15 US US10/271,358 patent/US6969718B2/en not_active Expired - Fee Related
- 2002-10-15 DE DE60236743T patent/DE60236743D1/de not_active Expired - Lifetime
- 2002-10-15 PE PE2002001016A patent/PE20030705A1/es not_active Application Discontinuation
- 2002-10-15 CA CA2463626A patent/CA2463626C/en not_active Expired - Fee Related
- 2002-10-15 MX MXPA04003611A patent/MXPA04003611A/es active IP Right Grant
- 2002-10-15 JP JP2003536227A patent/JP4309761B2/ja not_active Expired - Fee Related
- 2002-10-15 AT AT02773770T patent/ATE471315T1/de not_active IP Right Cessation
- 2002-10-15 AR ARP020103851A patent/AR036812A1/es unknown
- 2002-10-15 EP EP02773770A patent/EP1436281B1/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| ATE471315T1 (de) | 2010-07-15 |
| CA2463626A1 (en) | 2003-04-24 |
| JP2005506356A (ja) | 2005-03-03 |
| DE60236743D1 (de) | 2010-07-29 |
| MXPA04003611A (es) | 2004-07-30 |
| CN1571782A (zh) | 2005-01-26 |
| EP1436281B1 (en) | 2010-06-16 |
| ES2347643T3 (es) | 2010-11-03 |
| JP4309761B2 (ja) | 2009-08-05 |
| US20030232837A1 (en) | 2003-12-18 |
| EP1436281A1 (en) | 2004-07-14 |
| PE20030705A1 (es) | 2003-08-21 |
| CA2463626C (en) | 2011-05-24 |
| WO2003033487A1 (en) | 2003-04-24 |
| US6969718B2 (en) | 2005-11-29 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR036492A1 (es) | Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos inhibidores para la elaboracion de un medicamento para el tratamiento de enfermedades androgeno dependientes | |
| AR036812A1 (es) | Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos compuestos para la fabricacion de medicamentos para el tratamiento de enfermedades androgeno-dependientes | |
| AR038703A1 (es) | Derivados de 5-feniltiazol y uso como inhibidor de quinasa p i 3 | |
| PE20070078A1 (es) | Compuestos heterociclicos macrociclicos como inhibidores de aspartil proteasa | |
| CO4960641A1 (es) | Derivados de piperidina 1,4-disustituida conteniendo fluor | |
| AR049263A1 (es) | Heterociclos biciclicos inhibidores de quinasa utiles como agentes anticancer | |
| AR054024A1 (es) | Derivados de piridina -3- carboxamida como agonistas inversos de cb1 | |
| AR044909A1 (es) | Derivados de tiazolilpiperidina, procesos para su preparacion, composiciones farmaceuticas que los comprenden y aplicaciones de dichos derivados en el tratamiento de hipertrigliceridemia , hipercolesterolemia y dislipidemia | |
| AR041260A1 (es) | Piperazinas sustituidas por heterociclos para el tratamiento de la esquizofrenia | |
| CO5271658A1 (es) | Antagonistas del factor liberador de corticotropina | |
| AR035497A1 (es) | Compuestos no-imidazol, composicion farmaceutica que los comprenden y el uso de los mismos para la preparacion de medicamentos | |
| AR044629A1 (es) | Derivados de bencimidazol, composiciones que los contienen, preparacion y usos de los mismos. | |
| AR083367A1 (es) | Compuestos de tipo quinazolinona como antagonistas de crth | |
| PE20030762A1 (es) | Compuestos heterociclicos como antagonistas nk1 | |
| CO5580747A2 (es) | Derivados e intermediarios de n-adamantilmetilo como composiciones farmaceuticas y procesos para su preparacion | |
| AR077267A1 (es) | Derivados nitrogenados heterociclicos inhibidores selectivos de pi3k, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades inflamatorias y/o autoinmunes. | |
| AR006720A1 (es) | Un compuesto derivado de azahexano heterociclico, su uso para la preparacion de una composicion farmaceutica, procedimiento para prepararlo y una composicion farmaceutica que lo comprende | |
| AR023152A1 (es) | Compuesto tienopirimidina, procedimiento para producirlo, composicion farmaceutica que lo comprende y uso de dicho compuesto para preparar dichacomposicion | |
| AR042936A1 (es) | Derivados de urea ciclica, su preparacion y su utilizacion farmaceutica como inhibidores de quinasas | |
| CO5640041A2 (es) | Un inhibidor de pde4 y un agente anticolinergico en combinacion para tratar enfermedades obstructivas de vias respiratorias | |
| AR064729A1 (es) | Derivados de 2,4-dianilinopirimidinas, su preparacion, composiciones farmaceuticas y usos como inhibidores de ikk | |
| AR062499A1 (es) | Derivados de n-fenil pirazol y piridil pirazoles, composiciones farmaceuticas que los contienen y usos como agentes antiagregantes plaquetarios y antitromboticos. | |
| PE20080136A1 (es) | Arilsulfonamidas sustituidas como agentes antivirales | |
| ECSP077215A (es) | Derivados de n-(1h-indolil)-1h-indol-2-carboxamidas, su preparación y su aplicación en terapéutica | |
| AR040247A1 (es) | Derivados de piperazinilacilpiperidina substituidos, su preparacion, composicion farmaceutica y medicamento que lo comprenden |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |