AR054378A1 - Inhibidores de adenilatociclasa soluble, composiciones farmaceuticas que los contienen, y usos para controlar la fertilidad masculina - Google Patents
Inhibidores de adenilatociclasa soluble, composiciones farmaceuticas que los contienen, y usos para controlar la fertilidad masculinaInfo
- Publication number
- AR054378A1 AR054378A1 ARP060102365A ARP060102365A AR054378A1 AR 054378 A1 AR054378 A1 AR 054378A1 AR P060102365 A ARP060102365 A AR P060102365A AR P060102365 A ARP060102365 A AR P060102365A AR 054378 A1 AR054378 A1 AR 054378A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- acyl
- aryl
- alkoxy
- cyano
- Prior art date
Links
- 230000035558 fertility Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 37
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 13
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 9
- 229910052736 halogen Inorganic materials 0.000 abstract 8
- 150000002367 halogens Chemical class 0.000 abstract 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 5
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229940124530 sulfonamide Drugs 0.000 abstract 2
- 150000003456 sulfonamides Chemical class 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
- C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D333/70—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- 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
- A61P15/16—Masculine contraceptives
-
- 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
- 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
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Saccharide Compounds (AREA)
- Furan Compounds (AREA)
Abstract
Reivindicacion 1: compuestos de la formula general (1) caracterizado porque R1 representa un H, halogeno, CF3, C3-6-cicloalquilo, que es opcionalmente polisaturado y opcionalmente polisustituido, o representa el grupo C1-6-alquilo, C1-6-arilo, C1-6- acilo, halo-C1-6-alquilo, C1-6-alquilo-C1-6-alquilo, C1-6-alquilo-C1-6-acilo, C1-6-acilo-C1-6-acilo, C1-6-alquilo-C1-6-arilo, C1-6-arilo-C1-6-alquilo o CF3; donde C1-6-alquilo, C1-6-arilo, C1-6-acilo, halo-C1-6-alquilo, C1-6-alquilo-C1-6-alquilo, C1- 6-alquilo-C1-6-acilo, C1-6-acilo-C1-6-acilo, C1-6-alquilo-C1-6-arilo o C1-6-arilo-C1-6-alquilo puede estar opcionalmente interrumpido de manera igual o diferentes con uno más O, S o N, o representa el grupo sulfonil-C1-6-alquilo, sulfonamida o ciano; R2 representa un halogeno, CF3, un C3-6-cicloalquilo, que es opcionalmente polisaturado y opcionalmente polisustituido, o representa el grupo C1-6-alquilo, C1-6-arilo, C1-6-acilo, halo-C1-6-alquilo, C1-6-alquilo-C1-6-alquilo, C1-6-alquilo-C1- 6-acilo, C1-6-acilo-C1-6-acilo, C1-6-alquilo-C1-6-arilo, C1-6-arilo-C1-6-alquilo o CF3; donde C1-6-alquilo, C1-6-arilo, C1-6-acilo, halo-C1-6-alquilo, C1-6-alquilo-C1-6-alquilo, C1-6-alquilo-C1-6-acilo, C1-6-acilo-C1-6-acilo, C1-6-alquilo-C1-6-arilo o C1-6-arilo-C1-6-alquilo puede estar opcionalmente interrumpido de manera igual o diferentes con uno más O, S o N, o representa el grupo sulfonil-C1-6-alquilo, sulfonamida o ciano; R3 representa C6-12-arilo, el que está sustituido opcionalmente con uno o más C1-6-alquilo o C1-6-acilo de manera igual o diferente, que puede estar mono- o polisustituido, o puede estar sustituido con C1-6-alcoxilo hidroxilo, ciano, CO2-(C1-6-alquilo), N-(C1-6-alquilo)2, CO-NR4R5 o con CF3, representa un C5-12- heteroarilo, que está sustituido de manera igual o diferente con uno o más halogeno, con C1-6-alquilo, C1-6-acilo, C1-6-alcoxilo hidroxilo, ciano, CO2-(C1-6-alquilo), N-(C1-6-alquilo)2, CO-NR4R5 o con CF3 o representa un C3-6-cicloalquilo, que está sustituido con uno o más halogeno, CF3, hidroxilo, ciano, CO2-(C1-6-alquilo), C1-6-alquilo, C1-6-acilo, N-(C1-6-alquilo)2, CO-NR4R5 o C1-6-alcoxilo, de manera igual o diferente R4 representa un H, un C3-6-cicloalquilo, que está opcionalmente sustituido con uno o más C1-6-alquilo, C1-6-acilo, C1-6-alcoxilo o CF3 de manera igual o diferente, representa un C6-12-arilo, que está opcionalmente sustituido con uno o más, halogeno, C1-6-alquilo, C1-6-acilo, C1-6-alcoxilo N-C1-6-alquilo-C1-6- alquilo, CF3 o ciano de manera igual o diferente, o representa un C5-12-heteroarilo, que está opcionalmente sustituido con uno o más, halogeno, C1-6-alquilo, C1-6-acilo, C1-6-alcoxilo N-C1-6-alquilo-C1-6-alquilo, CF3 o ciano, de manera igual o diferente, o es un C1-6-alquilo, que puede estar sustituido aleatoriamente, R5 es un H, un C3-6-cicloalquilo, que está opcionalmente sustituido con uno más, C1-6-alquilo, C1-6-acilo, 1-6-alcoxilo o CF3 de manera igual o diferente, o es un C6-12- arilo, que está opcionalmente sustituido de manera igual o diferente con uno o más halogeno o con un C1-6-alquilo, C1-6-acilo, C1-6-alcoxilo N-C1-6-alquilo-C1-6-alquilo, CF3 o ciano, o es un C5-12-heteroarilo, que está opcionalmente sustituido con uno o más, halogeno, C1-6-alquilo, C1-6-acilo, C1-6-alcoxilo N-C1-6-alquilo-C1-6-alquilo, CF3 o ciano, de manera igual o diferente, o es un C1-6-alquilo, que puede estar sustituido aleatoriamente, R4 y R5 juntos pueden formar un anillo de 5-8 miembros que puede contener otros heteroátomos, y X es el grupo sulfonilo, (CH2)n o carbonilo; Y es un grupo -(CH2)2- o carbonilo; Z es un N; A es un O o S y n significa 0-4; así como sus isomeros, diastereomeros, enantiomeros y sales.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102005027274A DE102005027274A1 (de) | 2005-06-08 | 2005-06-08 | Inhibitoren der löslichen Adenylatzyklase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR054378A1 true AR054378A1 (es) | 2007-06-20 |
Family
ID=37398540
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060102365A AR054378A1 (es) | 2005-06-08 | 2006-06-07 | Inhibidores de adenilatociclasa soluble, composiciones farmaceuticas que los contienen, y usos para controlar la fertilidad masculina |
Country Status (23)
| Country | Link |
|---|---|
| EP (1) | EP1888058B1 (es) |
| JP (1) | JP2008542422A (es) |
| KR (1) | KR20080016617A (es) |
| CN (1) | CN101193631A (es) |
| AR (1) | AR054378A1 (es) |
| AT (1) | ATE431736T1 (es) |
| AU (1) | AU2006256857A1 (es) |
| BR (1) | BRPI0610934A2 (es) |
| CA (1) | CA2606692A1 (es) |
| CR (1) | CR9578A (es) |
| DE (2) | DE102005027274A1 (es) |
| DO (1) | DOP2006000130A (es) |
| EA (1) | EA200702590A1 (es) |
| EC (1) | ECSP078024A (es) |
| GT (1) | GT200600244A (es) |
| IL (1) | IL186914A0 (es) |
| MX (1) | MX2007015493A (es) |
| NO (1) | NO20080104L (es) |
| PE (1) | PE20061488A1 (es) |
| TW (1) | TW200716090A (es) |
| UY (1) | UY29583A1 (es) |
| WO (1) | WO2006131398A2 (es) |
| ZA (1) | ZA200800153B (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102006014319B4 (de) * | 2006-03-23 | 2009-01-08 | Bayer Schering Pharma Aktiengesellschaft | Inhibitoren der löslichen Adenylatzyklase |
| EP2036906A1 (de) * | 2007-09-05 | 2009-03-18 | Bayer Schering Pharma Aktiengesellschaft | Azaindole als Inhibitoren der löslichen Adenylatzyklase |
| WO2023100061A1 (en) | 2021-12-01 | 2023-06-08 | Pfizer Inc. | 3-phenyl-1-benzothiophene-2-carboxylic acid derivatives as branched-chain alpha keto acid dehydrogenase kinase inhibitors for the treatment of diabetes, kidney diseases, nash and heart failure |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2635776B1 (fr) * | 1988-09-01 | 1993-06-11 | Rhone Poulenc Agrochimie | Derives amides, procede pour leur fabrication et compositions fongicides les contenant |
| AU2001287060A1 (en) * | 2000-09-05 | 2002-03-22 | University Of Virginia Patent Foundation | Human soluble testicular adenylyl cyclase |
| UA75660C2 (en) * | 2001-06-28 | 2006-05-15 | Pfizer Prod Inc | Triamide-substituted indoles, benzofuranes and benzothiophenes as inhibitors of microsomal triglyceride transfer protein (mtp) and/or apolipoprotein b (apo b) secretion |
| AU2002327627B2 (en) * | 2001-09-14 | 2006-09-14 | Methylgene Inc. | Inhibitors of histone deacetylase |
| UA79504C2 (en) * | 2002-11-07 | 2007-06-25 | Organon Nv | Indols for treating diseases associated with androgen receptors |
| JP4741491B2 (ja) * | 2003-08-07 | 2011-08-03 | ライジェル ファーマシューティカルズ， インコーポレイテッド | 抗増殖剤としての２，４−ピリミジンジアミン化合物および使用 |
| US7935724B2 (en) * | 2003-10-09 | 2011-05-03 | Merck Hdac Research, Llc | Thiophene and benzothiophene hydroxamic acid derivatives |
| CA2553848A1 (en) * | 2004-01-21 | 2005-08-04 | Cornell Research Foundation, Inc. | Chemical inhibitors of soluble adenylyl cyclase (sac) |
| WO2005092899A1 (en) * | 2004-03-26 | 2005-10-06 | Methylgene Inc. | Inhibitors of histone deacetylase |
| DE102004047272A1 (de) * | 2004-09-24 | 2006-04-06 | Schering Ag | Inhibitoren der löslichen Adenylatzyklase |
-
2005
- 2005-06-08 DE DE102005027274A patent/DE102005027274A1/de not_active Withdrawn
-
2006
- 2006-06-07 AR ARP060102365A patent/AR054378A1/es unknown
- 2006-06-07 KR KR1020077028637A patent/KR20080016617A/ko not_active Withdrawn
- 2006-06-07 DE DE602006006908T patent/DE602006006908D1/de not_active Expired - Fee Related
- 2006-06-07 CA CA002606692A patent/CA2606692A1/en not_active Abandoned
- 2006-06-07 AT AT06762012T patent/ATE431736T1/de not_active IP Right Cessation
- 2006-06-07 MX MX2007015493A patent/MX2007015493A/es not_active Application Discontinuation
- 2006-06-07 PE PE2006000622A patent/PE20061488A1/es not_active Application Discontinuation
- 2006-06-07 EA EA200702590A patent/EA200702590A1/ru unknown
- 2006-06-07 CN CNA2006800201485A patent/CN101193631A/zh active Pending
- 2006-06-07 AU AU2006256857A patent/AU2006256857A1/en not_active Abandoned
- 2006-06-07 BR BRPI0610934-9A patent/BRPI0610934A2/pt not_active IP Right Cessation
- 2006-06-07 EP EP06762012A patent/EP1888058B1/en not_active Not-in-force
- 2006-06-07 UY UY29583A patent/UY29583A1/es not_active Application Discontinuation
- 2006-06-07 WO PCT/EP2006/005608 patent/WO2006131398A2/en not_active Ceased
- 2006-06-07 JP JP2008515154A patent/JP2008542422A/ja active Pending
- 2006-06-07 GT GT200600244A patent/GT200600244A/es unknown
- 2006-06-08 TW TW095120397A patent/TW200716090A/zh unknown
- 2006-06-08 DO DO2006000130A patent/DOP2006000130A/es unknown
-
2007
- 2007-10-25 IL IL186914A patent/IL186914A0/en unknown
- 2007-12-07 CR CR9578A patent/CR9578A/es not_active Application Discontinuation
- 2007-12-17 EC EC2007008024A patent/ECSP078024A/es unknown
-
2008
- 2008-01-07 ZA ZA200800153A patent/ZA200800153B/xx unknown
- 2008-01-07 NO NO20080104A patent/NO20080104L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| KR20080016617A (ko) | 2008-02-21 |
| EA200702590A1 (ru) | 2008-06-30 |
| ECSP078024A (es) | 2008-01-23 |
| AU2006256857A1 (en) | 2006-12-14 |
| ATE431736T1 (de) | 2009-06-15 |
| UY29583A1 (es) | 2007-01-31 |
| NO20080104L (no) | 2008-03-03 |
| EP1888058B1 (en) | 2009-05-20 |
| PE20061488A1 (es) | 2007-02-03 |
| DE602006006908D1 (de) | 2009-07-02 |
| IL186914A0 (en) | 2008-02-09 |
| EP1888058A2 (en) | 2008-02-20 |
| GT200600244A (es) | 2007-01-23 |
| CN101193631A (zh) | 2008-06-04 |
| DOP2006000130A (es) | 2006-11-30 |
| WO2006131398A2 (en) | 2006-12-14 |
| BRPI0610934A2 (pt) | 2010-08-03 |
| JP2008542422A (ja) | 2008-11-27 |
| CR9578A (es) | 2008-03-06 |
| WO2006131398A3 (en) | 2007-04-19 |
| DE102005027274A1 (de) | 2006-12-14 |
| TW200716090A (en) | 2007-05-01 |
| MX2007015493A (es) | 2008-02-22 |
| CA2606692A1 (en) | 2006-12-14 |
| ZA200800153B (en) | 2009-03-25 |
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