AR081650A1 - Derivados 1,4-diazepanos de pirazolo[4,3-d]pirimidina, procedimiento de preparacion, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de la disfuncion erectil - Google Patents
Derivados 1,4-diazepanos de pirazolo[4,3-d]pirimidina, procedimiento de preparacion, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de la disfuncion erectilInfo
- Publication number
- AR081650A1 AR081650A1 ARP110101965A ARP110101965A AR081650A1 AR 081650 A1 AR081650 A1 AR 081650A1 AR P110101965 A ARP110101965 A AR P110101965A AR P110101965 A ARP110101965 A AR P110101965A AR 081650 A1 AR081650 A1 AR 081650A1
- Authority
- AR
- Argentina
- Prior art keywords
- proton
- straight
- branched chain
- chain alkyl
- cycloalkyl
- Prior art date
Links
- 208000010228 Erectile Dysfunction Diseases 0.000 title 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 201000001881 impotence Diseases 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 150000001732 carboxylic acid derivatives Chemical class 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004122 cyclic group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- -1 methylfluorenyl Chemical group 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
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 101100440695 Dictyostelium discoideum corB gene Proteins 0.000 abstract 1
- 101100134925 Gallus gallus COR6 gene Proteins 0.000 abstract 1
- NMNLTKAZEGKZNL-UHFFFAOYSA-N [N].C1CNCCNC1 Chemical compound [N].C1CNCCNC1 NMNLTKAZEGKZNL-UHFFFAOYSA-N 0.000 abstract 1
- 125000006242 amine protecting group Chemical group 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
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000524 functional group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Reproductive Health (AREA)
- Emergency Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Reivindicación 1: Un compuesto de la fórmula general (1) en donde A presenta un átomo de carbono o nitrógeno; R1 representa un protón, alquilo C1-6 de cadena lineal o ramificada, cicloalquilo C3-6, un grupo COR6, un derivado de ácido carboxílico C1-8, un sistema heterocíclico monoanular o de anillos fusionados de tres hasta seis miembros cada anillo, de uno hasta cinco heteroátomos; R2 representa un protón, alquilo C1-6 de cadena lineal o ramificada, un cicloalquilo C3-6 o un alcoxilo C1-3; R3 representa un protón, un alquilo C1-6 de cadena lineal o ramificada, un hidroxilo, alcoxilo C1-3 opcionalmente sustituido, un halógeno, un sistema heterocíclico monoanular o de anillos fusionados de tres hasta seis miembros cada uno, de uno hasta cinco heteroátomos; R4 representa un protón, alquilo C1-8 de cadena lineal o ramificada donde puede o no tener un grupo hidroxilo al final de la cadena, cicloalquilo C3-6 donde puede o no tener un grupo hidroxilo en el ciclo, un grupo derivado de COR7, un grupo derivado de CO2R8, un derivado de ácido carboxílico C1-8 que puede estar unido directamente al nitrógeno del 1,4-diazepano o le preceden una, dos o tres unidades de metileno, o un grupo protector de aminas; R5 representa un protón, alquilo C1-6 de cadena lineal o ramificada, o un grupo funcional como hidroxilo, metoxilo, o ácido carboxílico; R6 representa un protón o un alquilo C1-6 de cadena lineal o ramificada; R7 representa un protón, alquilo C1-6 de cadena lineal o ramificada, cicloalquilo C3-6 donde puede ser un ciclo saturado o aromático, también puede contener un heterociclo el cual puede ser parcial o totalmente saturado o insaturado; R8 representa un protón, alquilo C1-6 de cadena lineal o ramificada, cicloalquilo C3-6 donde el anillo puede ser saturado o aromático, también puede contener grupos como bencilo o metilfluorenilo; y sus sales, compuestos N-óxidos, enantiómeros, diastereoisómeros, isótopos y formas tautoméricas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| MX2010006227A MX2010006227A (es) | 2010-06-07 | 2010-06-07 | Nuevos derivados 1,4-diazepanos, inhibidores de pde-5. |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR081650A1 true AR081650A1 (es) | 2012-10-10 |
Family
ID=45097594
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110101965A AR081650A1 (es) | 2010-06-07 | 2011-06-07 | Derivados 1,4-diazepanos de pirazolo[4,3-d]pirimidina, procedimiento de preparacion, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de la disfuncion erectil |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP2578588A4 (es) |
| AR (1) | AR081650A1 (es) |
| BR (1) | BR112012031289A2 (es) |
| CO (1) | CO6660496A2 (es) |
| EC (1) | ECSP13012372A (es) |
| MX (1) | MX2010006227A (es) |
| WO (1) | WO2011154798A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102134242B (zh) * | 2011-01-21 | 2013-08-28 | 浙江大德药业集团有限公司 | 一种用于治疗阳痿的快速长效的化合物 |
| BR112021009958A2 (pt) * | 2018-11-28 | 2021-08-17 | Topadur Pharma Ag | modo duplo de ação de ativadores de guanilato ciclase solúveis e inibidores de fosfodiesterase e seus usos |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5250534A (en) | 1990-06-20 | 1993-10-05 | Pfizer Inc. | Pyrazolopyrimidinone antianginal agents |
| GB9013750D0 (en) | 1990-06-20 | 1990-08-08 | Pfizer Ltd | Therapeutic agents |
| GB9612514D0 (en) | 1996-06-14 | 1996-08-14 | Pfizer Ltd | Novel process |
| AU748352B2 (en) | 1998-04-20 | 2002-06-06 | Pfizer Inc. | Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction |
| CA2235642C (en) | 1998-05-15 | 2007-11-13 | Torcan Chemical Ltd. | Processes for preparing sildenafil |
| WO2000024745A1 (en) * | 1998-10-23 | 2000-05-04 | Pfizer Limited | PYRAZOLOPYRIMIDINONE cGMP PDE5 INHIBITORS FOR THE TREATMENT OF SEXUAL DYSFUNCTION |
| GB9823101D0 (en) * | 1998-10-23 | 1998-12-16 | Pfizer Ltd | Pharmaceutically active compounds |
| EP1002798A1 (en) | 1998-11-20 | 2000-05-24 | Orchid Chemicals & Pharmaceuticals Ltd. | An improved process for preparing a therapeutically active pyrazolopyrimidinone derivative |
| AU5925500A (en) | 1999-07-09 | 2001-01-30 | Picower Institute For Medical Research, The | Pyrazolopyrimidinone derivatives conjugated to thiophene moieties or benzo [fused] 5-membered heterocycles for erectile dysfunction |
| EP1077214A1 (en) | 1999-08-16 | 2001-02-21 | Orchid Chemicals & Pharmaceuticals Ltd. | An improved process for preparing a pyrazolopyrimidinone derivative |
| AU1888800A (en) | 1999-09-13 | 2001-04-17 | Cipla Limited | A novel process for the synthesis of sildenafil citrate |
| MXPA99010322A (es) | 1999-11-10 | 2003-07-15 | Europharm S A De C V | Proceso para la preparacion de sildenafil. |
| ES2223863T3 (es) | 2000-06-22 | 2005-03-01 | Pfizer Inc. | Procedimiento para la preparacion de pirazolopirimidinonas. |
| ES2310144B1 (es) | 2007-06-15 | 2010-01-12 | Galenicum Health, S.L. | Intermedios para la preparacion de un inhibidor de la fosfodiesterasa tipo 5. |
| EA201070056A1 (ru) | 2007-06-26 | 2010-06-30 | Солвей Фармасьютикалс Б.В. | N-оксид силденафила в качестве пролекарства |
-
2010
- 2010-06-07 MX MX2010006227A patent/MX2010006227A/es not_active Application Discontinuation
-
2011
- 2011-06-03 BR BR112012031289A patent/BR112012031289A2/pt not_active IP Right Cessation
- 2011-06-03 WO PCT/IB2011/001228 patent/WO2011154798A1/es active Application Filing
- 2011-06-03 EP EP11792009.0A patent/EP2578588A4/en not_active Withdrawn
- 2011-06-07 AR ARP110101965A patent/AR081650A1/es unknown
-
2012
- 2012-12-28 CO CO12235720A patent/CO6660496A2/es not_active Application Discontinuation
-
2013
- 2013-01-07 EC ECSP13012372 patent/ECSP13012372A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ECSP13012372A (es) | 2013-02-28 |
| BR112012031289A2 (pt) | 2016-11-01 |
| MX2010006227A (es) | 2011-12-14 |
| CO6660496A2 (es) | 2013-04-30 |
| WO2011154798A1 (es) | 2011-12-15 |
| EP2578588A1 (en) | 2013-04-10 |
| EP2578588A4 (en) | 2013-12-04 |
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| FB | Suspension of granting procedure |