AR036674A1 - Inhibidores de fosfodiesterasa v de guanina de policiclicos, composicion farmaceutica, y el uso de dichos compuestos para la preparacion de medicamentos para tratar desordenes fisiologicos - Google Patents
Inhibidores de fosfodiesterasa v de guanina de policiclicos, composicion farmaceutica, y el uso de dichos compuestos para la preparacion de medicamentos para tratar desordenes fisiologicosInfo
- Publication number
- AR036674A1 AR036674A1 ARP020103195A ARP020103195A AR036674A1 AR 036674 A1 AR036674 A1 AR 036674A1 AR P020103195 A ARP020103195 A AR P020103195A AR P020103195 A ARP020103195 A AR P020103195A AR 036674 A1 AR036674 A1 AR 036674A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- cycloalkylalkyl
- heteroaryl
- heterocycloalkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 239000003814 drug Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 102000011016 Type 5 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 title 1
- 108010037581 Type 5 Cyclic Nucleotide Phosphodiesterases Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 18
- 125000000217 alkyl group Chemical group 0.000 abstract 15
- -1 cyano, oximino Chemical group 0.000 abstract 10
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 10
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 7
- RFEBDZANCVHDLP-UHFFFAOYSA-N 3-[(4-cyanophenyl)methylamino]-6-(trifluoromethyl)quinoxaline-2-carboxylic acid Chemical compound OC(=O)C1=NC2=CC=C(C(F)(F)F)C=C2N=C1NCC1=CC=C(C#N)C=C1 RFEBDZANCVHDLP-UHFFFAOYSA-N 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000004414 alkyl thio group Chemical group 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000006682 monohaloalkyl group Chemical group 0.000 abstract 5
- 125000006684 polyhaloalkyl group Chemical group 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000004423 acyloxy group Chemical group 0.000 abstract 3
- 125000006310 cycloalkyl amino group Chemical group 0.000 abstract 3
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000003396 thiol group Chemical class [H]S* 0.000 abstract 3
- 125000005110 aryl thio group Chemical group 0.000 abstract 2
- 125000004104 aryloxy group Chemical group 0.000 abstract 2
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 abstract 2
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 2
- UYTPUPDQBNUYGX-UHFFFAOYSA-N guanine Chemical compound O=C1NC(N)=NC2=C1N=CN2 UYTPUPDQBNUYGX-UHFFFAOYSA-N 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- 125000003627 8 membered carbocyclic group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 201000001880 Sexual dysfunction Diseases 0.000 abstract 1
- 125000004442 acylamino group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000005518 carboxamido group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 abstract 1
- 125000003367 polycyclic group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 231100000872 sexual dysfunction Toxicity 0.000 abstract 1
- 239000012453 solvate Substances 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory 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
-
- 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
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
- A61P13/04—Drugs for disorders of the urinary system for urolithiasis
-
- 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
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Reproductive Health (AREA)
- Ophthalmology & Optometry (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Transplantation (AREA)
- Nutrition Science (AREA)
- Vascular Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Un compuesto inhibidor de fosfodiesterasa V de guanina policíclico que tiene la formula (1) ó (2) o una sal o solvato del mismo farmacéuticamente aceptable, en la cual q = 0 ó 1; R1 es H, cicloalquilo, alquilo, R23-alquilo- ó R26; Ra, Rb y Rc son, independientemente uno del otro, cada uno H, alquilo, cicloalquilo, arilo, R22-arilo- ó R24-alquilo-; ó Ra y Rb, conjuntamente con el carbono al cual están ambos adheridos, forman un anillo de 4 a 7 miembros, y Rc es H ó alquilo; ó Ra y Rc, conjuntamente con los respectivos carbonos a los cuales están adheridos, forman un anillo de 4 a 7 miembros, y Rb es H ó alquilo; (i) X es un enlace; Y es H, R26 es cicloalquilo, alquilo, R25-alquilo- ó -(CH2)tTCOR100, donde t es 1 a 6, T es -O- ó -NH-, y R100 es H, R26, alquilo ó R26-alquilo-; y R2 es monohaloalquilo, polihaloalquilo, con la condición de que no debe ser trifluorometilo, azido, ciano, oximino, cicloalquenilo, heteroarilo, R22-heteroarilo- ó R27-alquilo-; (ii) X es un enlace; Y es Q-V, donde Q es un enlace ó alquilo C1-C8, y V es: (a) arilo sustituido con nitro, aminosulfonilo, ciano, monohaloalquilo, polihaloalquilo, con la condición de que no sea trifluorometilo, tiol, alquiltio, cicloalquilo, cicloalquilalquilo, -OCF3 ó aciloxi, y opcionalmente adicionalmente sustituido con 1 a 3 sustituyentes adicionales independientemente seleccionados del grupo que consiste en R21; (b) R22-heteroarilo-; ó (c) arilo ó heteroarilo, cada uno de los cuales está independientemente sustituido con 2 sustituyentes en átomos adyacentes del grupo V, que están unidos para formar un anillo carbocíclico o heterocíclico de 4 a 8 miembros fusionado no aromático, y opcionalmente adicionalmente sustituido con 1 a 2 sustituyentes adicionales independientemente seleccionados del grupo que consiste en R21; y es R2 es H, halo, -CONHR6, -CONR6R7, -CO2R6, monohaloalquilo, polihaloalquilo, azido, ciano,-C=N-OR6, cicloalquilo, cicloalquilalquilo, R26, aminosulfonilo, alquil ó R23-alquilo-; (iii) X es -O- ó -S-; Y se ha definido en la sección (i) anterior; y R2 es R26, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, cicloalquenilo ó R28-alquilo-; (iv) X es -O- ó -S-; Y se ha definido en la sección (ii) anterior; y R2 es alquilo, R26, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, cicloalquenilo ó R28-alquilo-; (v) X es -SO- ó -SO2-; Y se ha definido en la sección (i) ó (ii) anterior; y R2 es alquilo, R26, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, cicloalquenilo ó R28-alquilo-; (vi) X es -NR8-; Y se ha definido en la sección (i) anterior; y R2 es (R29)p-alquilo-, cicloalquilo, (R30)p-cicloalquilo-, cicloalquenilo, (R30)p-cicloalquenilo-, heterocicloalquilo ó (R30) p-heterocicloalquilo-; (vii) X es -NR8-; Y se ha definido en la sección (ii) anterior; y R2 es alquilo, R26, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, cicloalquenilo ó R31-alquilo-; ó (viii) X es -C:::C-; Y se ha definido en la sección (i) ó (ii) anterior; y R2 es alquilo, R26, cicloalquilo, cicloalquilalquilo ó R23-alquilo-; donde, R6 es H ó R7; R7 es alquilo, cicloalquilo ó cicloalquilalquilo; R8 es heterocicloalquilo ó R6; R21 es 1-6 sustituyentes cada uno independientemente seleccionado del grupo que consiste en halo, hidroxi, alcoxi, fenoxi, fenilo, nitro, aminosulfonilo, ciano, monohaloalquilo, polihaloalquilo, tiol, alquiltio, cicloalquilo, cicloalquilalquilo, amino, alquilamino, acilamino, carboxilo, -C(O)OR34, carboxamido, -OCF3 y aciloxi; R22 es 1-6 sustituyentes cada uno independientemente seleccionado del grupo que consiste en alquilo y R21; R23 es cicloalcoxi, ariloxi, alquiltio, ariltio, cicloalquilo ó R28; R24 es cicloalquilo ó R26; R25 es hidroxi, alcoxi, amino, monoalquilamino, dialquilamino ó R26; R26 es arilo, R22-arilo-, heteroarilo ó R22-heteroarilo-; R27 es cicloalcoxi, ariloxi, alquiltio, ariltio, heteroarilo, R22-heteroarilo-, cicloalquilo, heterocicloalquilo, cicloalquenilo, cicloalquilamino ó heterocicloalquilamino; R28 es cicloalquilamino, heterocicloalquilamino ó R25; R29 es alcoxi, cicloalquilamino, heterocicloalquilamino ó R26 ; R30 es halo, hidroxi, alcoxi, amino, aminosulfonilo, ciano, monohaloalquilo, polihaloalquilo, tiol, alquiltio, alquilo, cicloalquilo, cicloalquilalquilo ó aciloxi; R31 es cicloalquilo ó R28; R34 es alquilo, arilo, aralquilo y heteroarilo; y p es 1 a 4; composiciones farmacéuticas y el uso de dichos compuestos para la preparación de medicamentos que son útiles para tratar disfunciones sexuales y otros desórdenes fisiológicos. Un ejemplo representativo es el compuesto de fórmula (3).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31539501P | 2001-08-28 | 2001-08-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036674A1 true AR036674A1 (es) | 2004-09-29 |
Family
ID=23224209
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020103195A AR036674A1 (es) | 2001-08-28 | 2002-08-26 | Inhibidores de fosfodiesterasa v de guanina de policiclicos, composicion farmaceutica, y el uso de dichos compuestos para la preparacion de medicamentos para tratar desordenes fisiologicos |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US6969719B2 (es) |
| EP (1) | EP1421084B1 (es) |
| JP (2) | JP4450365B2 (es) |
| CN (2) | CN1315835C (es) |
| AR (1) | AR036674A1 (es) |
| AT (1) | ATE395349T1 (es) |
| CA (1) | CA2457944C (es) |
| DE (1) | DE60226615D1 (es) |
| ES (1) | ES2302835T3 (es) |
| MX (1) | MXPA04001891A (es) |
| PE (1) | PE20030415A1 (es) |
| WO (1) | WO2003020724A1 (es) |
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020091129A1 (en) * | 2000-11-20 | 2002-07-11 | Mitradev Boolell | Treatment of premature ejaculation |
| JP3945985B2 (ja) * | 2000-12-28 | 2007-07-18 | 株式会社リコー | デジタルカメラ装置 |
| US7456184B2 (en) | 2003-05-01 | 2008-11-25 | Palatin Technologies Inc. | Melanocortin receptor-specific compounds |
| US7354923B2 (en) | 2001-08-10 | 2008-04-08 | Palatin Technologies, Inc. | Piperazine melanocortin-specific compounds |
| EP1425029A4 (en) | 2001-08-10 | 2006-06-07 | Palatin Technologies Inc | PEPTIDOMIMETICS OF BIOLOGICALLY ACTIVE METALLOPEPTIDES |
| CN1315835C (zh) * | 2001-08-28 | 2007-05-16 | 先灵公司 | 多环鸟嘌呤磷酸二酯酶v抑制剂 |
| CA2459161A1 (en) | 2001-08-31 | 2003-03-13 | The Rockefeller University | Phosphodiesterase activity and regulation of phosphodiesterase 1b-mediated signaling in brain |
| US6943171B2 (en) * | 2001-11-09 | 2005-09-13 | Schering Corporation | Polycyclic guanine derivative phosphodiesterase V inhibitors |
| EP1719772A1 (en) * | 2002-05-31 | 2006-11-08 | Schering Corporation | Process for preparing xanthine phosphodiesterase v inhibitors and precursors thereof |
| US7074923B2 (en) * | 2002-05-31 | 2006-07-11 | Schering Corporation | Process for preparing xanthine phosphodiesterase V inhibitors and precursors thereof |
| DE10230311A1 (de) * | 2002-07-05 | 2004-01-22 | Degussa Ag | Verfahren zur Katalysator-freien Herstellung von O-Alkyl-N-cyanformimidaten |
| KR20060101762A (ko) * | 2003-11-21 | 2006-09-26 | 쉐링 코포레이션 | 포스포디에스테라제 ｖ 억제제 제형 |
| EP1750862B1 (en) | 2004-06-04 | 2011-01-05 | Teva Pharmaceutical Industries Ltd. | Pharmaceutical composition containing irbesartan |
| CN101146535A (zh) * | 2005-03-25 | 2008-03-19 | 默克公司 | 用睾酮补充剂和5α-还原酶抑制剂治疗男性病人的方法 |
| CN101248050B (zh) | 2005-06-06 | 2013-07-17 | 武田药品工业株式会社 | 有机化合物 |
| CA2613617A1 (en) * | 2005-06-27 | 2007-01-04 | Daniel Drai | Compositions and methods for enhancement of sexual function |
| US20070042957A1 (en) * | 2005-08-19 | 2007-02-22 | Mayo Foundation For Medical Education And Research | Type v phosphodiesterase inhibitors and natriuretic polypeptides |
| EP1919287A4 (en) * | 2005-08-23 | 2010-04-28 | Intra Cellular Therapies Inc | ORGANIC COMPOUNDS FOR TREATING A REDUCED DOPAMINE RECEPTOR SIGNALING ACTIVITY |
| US9012454B2 (en) | 2005-12-09 | 2015-04-21 | Mayo Foundation For Medical Education And Research | Sexual dysfunction |
| JP2007290996A (ja) * | 2006-04-24 | 2007-11-08 | Ube Ind Ltd | ４−アミノテトラヒドロピランの製法 |
| WO2008063505A1 (en) | 2006-11-13 | 2008-05-29 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US9006258B2 (en) * | 2006-12-05 | 2015-04-14 | Intra-Cellular Therapies, Inc. | Method of treating female sexual dysfunction with a PDE1 inhibitor |
| BRPI0812909A2 (pt) * | 2007-06-21 | 2014-12-09 | Schering Corp | Derivados de guanina policíclica e métodos de uso dos mesmos. |
| WO2009075784A1 (en) | 2007-12-06 | 2009-06-18 | Intra-Cellular Therapies, Inc. | Organic compounds |
| AU2008331833A1 (en) | 2007-12-06 | 2009-06-11 | Intra-Cellular Therapies, Inc | Organic compounds |
| KR20110098731A (ko) | 2008-12-06 | 2011-09-01 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| WO2010065147A1 (en) | 2008-12-06 | 2010-06-10 | Intra-Cellular Therapies, Inc. | Organic compounds |
| EP2358204B1 (en) * | 2008-12-06 | 2015-08-05 | Intra-Cellular Therapies, Inc. | 4,5,7,8-tetrahydro-4-oxo-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine compounds as PDE1 inhibitors. |
| CN102223799A (zh) | 2008-12-06 | 2011-10-19 | 细胞内治疗公司 | 有机化合物 |
| CN102232077A (zh) | 2008-12-06 | 2011-11-02 | 细胞内治疗公司 | 有机化合物 |
| EP2367429B1 (en) | 2008-12-06 | 2017-06-07 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CN101747282A (zh) | 2008-12-10 | 2010-06-23 | 上海特化医药科技有限公司 | 一类含有嘧啶酮苯基的化合物、其药物组合物及其制备方法和用途 |
| EP2400970A4 (en) * | 2009-02-25 | 2012-07-18 | Intra Cellular Therapies Inc | PDE-1-HEMMER FOR EYE DRESSING |
| US9468637B2 (en) | 2009-05-13 | 2016-10-18 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2011016861A2 (en) | 2009-08-05 | 2011-02-10 | Intra-Cellular Therapies, Inc. | Novel regulatory proteins and inhibitors |
| EP2523561A4 (en) * | 2009-12-22 | 2013-06-05 | Merck Sharp & Dohme | 7,8-DIHYDRO-1H-IMIDAZO [2,1-B] PURINE-4 (5H) -ONE DERIVATIVES AND METHOD OF USE |
| TW201206937A (en) | 2010-05-31 | 2012-02-16 | Intra Cellular Therapies Inc | Organic compounds |
| WO2011153135A1 (en) | 2010-05-31 | 2011-12-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| JP5911854B2 (ja) | 2010-05-31 | 2016-04-27 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | 有機化合物 |
| JP5879336B2 (ja) | 2010-05-31 | 2016-03-08 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | 有機化合物 |
| US10561656B2 (en) | 2011-06-10 | 2020-02-18 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US9801882B2 (en) | 2013-02-17 | 2017-10-31 | Intra-Cellular Therapies, Inc. | Phosphodiesterase-1 inhibitors and their use in treatment of cardiovascular diseases |
| ES2836129T3 (es) | 2013-03-15 | 2021-06-24 | Intra Cellular Therapies Inc | Compuestos orgánicos |
| EP2968338B1 (en) | 2013-03-15 | 2019-01-09 | Intra-Cellular Therapies, Inc. | Pde1 inhibitors for use in the treatment and/or prevention of cns injuries, and pns diseases, disorders or injuries |
| JP6696904B2 (ja) | 2014-01-08 | 2020-05-20 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | 製剤および医薬組成物 |
| US9884872B2 (en) | 2014-06-20 | 2018-02-06 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US9546175B2 (en) | 2014-08-07 | 2017-01-17 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US10285992B2 (en) | 2014-08-07 | 2019-05-14 | Intra-Cellular Therapies, Inc. | Combinations of PDE1 inhibitors and NEP inhibitors and associated methods |
| ES2745819T3 (es) | 2014-08-07 | 2020-03-03 | Intra Cellular Therapies Inc | Derivados de imidazo[1,2-a]-pirazolo[4,3-e]-pirimidin-4-ona con actividad inhibidora de la PDE1 |
| EP3193878B1 (en) | 2014-09-17 | 2021-01-06 | Intra-Cellular Therapies, Inc. | 7,8-dihydro-[2h]-imidazo-[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5h)-one derivatives as phosphodiesterase 1 (pde1) inhibitors for treating diseases, disorders or injuries of the central nervous system (cns) |
| HK1243936A1 (zh) | 2014-12-06 | 2018-07-27 | Intra-Cellular Therapies, Inc. | 有机化合物 |
| HK1243935A1 (zh) | 2014-12-06 | 2018-07-27 | Intra-Cellular Therapies, Inc. | 有机化合物 |
| JP2019510039A (ja) | 2016-03-28 | 2019-04-11 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | 新規組成物および方法 |
| JP7134168B6 (ja) | 2016-09-12 | 2024-02-02 | イントラ－セルラー・セラピーズ・インコーポレイテッド | 新規使用 |
| EP3746081A4 (en) | 2018-01-31 | 2021-10-27 | Intra-Cellular Therapies, Inc. | Novel uses |
| EP4413980A3 (en) | 2019-09-03 | 2024-10-30 | Intra-Cellular Therapies, Inc. | Novel compounds |
| US12364695B2 (en) | 2020-06-02 | 2025-07-22 | Intra-Cellular Therapies, Inc. | Methods of treating inflammatory disease |
| CN119039287A (zh) * | 2023-05-29 | 2024-11-29 | 中国药科大学 | 一类四氢吡啶并嘧啶酮衍生物及其制备方法与应用 |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1938016A1 (de) | 1969-07-23 | 1971-01-28 | Fischer Ohg Arzneimittelwerk | Verfahren zur Herstellung von 8-(N-Methyl-N-aethanolamin)-coffein als Arzneimittel gegen Erkaeltungskrankheiten |
| FR2116302A1 (en) | 1970-12-07 | 1972-07-13 | Brun Lab Sa Le | 8-aminotheophyllines - with coronary - vasodilator bronchodilator diuretic, spasmolytic, antiinflammatory and analgesic activity |
| DE3779374D1 (en) | 1986-08-28 | 1992-07-02 | Sandoz Ag | Xanthinderivate. |
| US5321029A (en) * | 1988-11-14 | 1994-06-14 | Beecham-Wuelfing Gmbh & Co.K.G. | Xanthines |
| GB8906792D0 (en) | 1989-03-23 | 1989-05-10 | Beecham Wuelfing Gmbh & Co Kg | Treatment and compounds |
| FR2654935B1 (fr) * | 1989-11-28 | 1994-07-01 | Lvmh Rech | Utilisation de xanthines, eventuellement incorporees dans des liposomes, pour favoriser la pigmentation de la peau ou des cheveux. |
| GB9013750D0 (en) | 1990-06-20 | 1990-08-08 | Pfizer Ltd | Therapeutic agents |
| NZ238609A (en) * | 1990-06-21 | 1993-12-23 | Schering Corp | Polycyclic guanine derivatives; preparation, pharmaceutical compositions, |
| GB9020959D0 (en) | 1990-09-26 | 1990-11-07 | Beecham Group Plc | Novel compounds |
| GB9020921D0 (en) | 1990-09-26 | 1990-11-07 | Beecham Group Plc | Novel compounds |
| WO1992011260A1 (en) * | 1990-12-21 | 1992-07-09 | Beecham Group Plc | Xanthine derivatives |
| GB9210839D0 (en) | 1992-05-21 | 1992-07-08 | Smithkline Beecham Plc | Novel compounds |
| GB9226532D0 (en) * | 1992-12-21 | 1993-02-17 | Smithkline Beecham Plc | Compounds |
| CA2156918A1 (en) | 1993-02-26 | 1994-09-01 | Deen Tulshian | 2-benzyl-polycyclic guanine derivatives and process for preparing them |
| GB9311920D0 (en) * | 1993-06-09 | 1993-07-28 | Pfizer Ltd | Therapeutic agents |
| GB9423911D0 (en) * | 1994-11-26 | 1995-01-11 | Pfizer Ltd | Therapeutic agents |
| US5731339A (en) * | 1995-04-28 | 1998-03-24 | Zonagen, Inc. | Methods and formulations for modulating the human sexual response |
| GB9514464D0 (en) * | 1995-07-14 | 1995-09-13 | Glaxo Lab Sa | Medicaments |
| US5824683A (en) * | 1995-11-28 | 1998-10-20 | Schering Corporation | 2'- 4'-halo- 1,1'-biphenyl!-4-yl!methyl!-5'-methyl-spiro cyclopentane-1,7' (8'H)- 3H! imidazo 2,1-b!purin!-4' (5'H)-ones |
| GB9612514D0 (en) * | 1996-06-14 | 1996-08-14 | Pfizer Ltd | Novel process |
| US6403597B1 (en) * | 1997-10-28 | 2002-06-11 | Vivus, Inc. | Administration of phosphodiesterase inhibitors for the treatment of premature ejaculation |
| US6037346A (en) * | 1997-10-28 | 2000-03-14 | Vivus, Inc. | Local administration of phosphodiesterase inhibitors for the treatment of erectile dysfunction |
| DK1174431T3 (da) | 1997-11-12 | 2012-08-20 | Bayer Pharma AG | 2-phenyl-substitueret imidazo triazinon som phoshodiesterase-inhibitorer |
| DE19816857A1 (de) | 1998-04-16 | 1999-10-21 | Boehringer Ingelheim Pharma | Neue unsymmetrisch substituierte Xanthin-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| WO1999062905A1 (en) | 1998-06-03 | 1999-12-09 | Almirall Prodesfarma, S.A. | 8-phenylxanthine derivatives and their use as phosphodiesterase inhibitors |
| US6087362A (en) * | 1999-03-16 | 2000-07-11 | Pentech Pharmaceuticals, Inc. | Apomorphine and sildenafil composition |
| US6023640A (en) * | 1999-03-29 | 2000-02-08 | Ross; Jesse | Method contributing to obviating male impotency |
| US20020091129A1 (en) * | 2000-11-20 | 2002-07-11 | Mitradev Boolell | Treatment of premature ejaculation |
| CN1315835C (zh) * | 2001-08-28 | 2007-05-16 | 先灵公司 | 多环鸟嘌呤磷酸二酯酶v抑制剂 |
-
2002
- 2002-08-26 CN CNB028167066A patent/CN1315835C/zh not_active Expired - Fee Related
- 2002-08-26 JP JP2003524994A patent/JP4450365B2/ja not_active Expired - Fee Related
- 2002-08-26 AR ARP020103195A patent/AR036674A1/es unknown
- 2002-08-26 MX MXPA04001891A patent/MXPA04001891A/es active IP Right Grant
- 2002-08-26 AT AT02761506T patent/ATE395349T1/de not_active IP Right Cessation
- 2002-08-26 ES ES02761506T patent/ES2302835T3/es not_active Expired - Lifetime
- 2002-08-26 WO PCT/US2002/027181 patent/WO2003020724A1/en not_active Ceased
- 2002-08-26 CN CNA2005101248185A patent/CN1781920A/zh active Pending
- 2002-08-26 DE DE60226615T patent/DE60226615D1/de not_active Expired - Lifetime
- 2002-08-26 US US10/227,778 patent/US6969719B2/en not_active Expired - Fee Related
- 2002-08-26 EP EP02761506A patent/EP1421084B1/en not_active Expired - Lifetime
- 2002-08-26 CA CA002457944A patent/CA2457944C/en not_active Expired - Fee Related
- 2002-08-27 PE PE2002000821A patent/PE20030415A1/es not_active Application Discontinuation
-
2005
- 2005-08-08 JP JP2005230176A patent/JP2005325138A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CN1315835C (zh) | 2007-05-16 |
| CA2457944C (en) | 2009-09-29 |
| ATE395349T1 (de) | 2008-05-15 |
| PE20030415A1 (es) | 2003-05-22 |
| JP4450365B2 (ja) | 2010-04-14 |
| DE60226615D1 (es) | 2008-06-26 |
| JP2005325138A (ja) | 2005-11-24 |
| JP2005502684A (ja) | 2005-01-27 |
| EP1421084B1 (en) | 2008-05-14 |
| HK1064668A1 (en) | 2005-02-04 |
| US20030153587A1 (en) | 2003-08-14 |
| ES2302835T3 (es) | 2008-08-01 |
| CN1547583A (zh) | 2004-11-17 |
| CN1781920A (zh) | 2006-06-07 |
| EP1421084A1 (en) | 2004-05-26 |
| WO2003020724A1 (en) | 2003-03-13 |
| US6969719B2 (en) | 2005-11-29 |
| CA2457944A1 (en) | 2003-03-13 |
| MXPA04001891A (es) | 2004-06-15 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR036674A1 (es) | Inhibidores de fosfodiesterasa v de guanina de policiclicos, composicion farmaceutica, y el uso de dichos compuestos para la preparacion de medicamentos para tratar desordenes fisiologicos | |
| ES2150577T3 (es) | Aminoeteres aromaticos como agentes para aliviar el dolor. | |
| AR045595A1 (es) | Composiciones utiles como inhibidores de proteinas quinasas | |
| AR050261A2 (es) | Aminoacidos con afinidad por la proteina alfa-2-delta y composiciones farmaceuticas que los contienen y su uso para preparar un medicamento | |
| PE20010211A1 (es) | Compuestos de tiazol y composiciones farmaceuticas para inhibir las quinasas de proteina | |
| AR035783A1 (es) | Compuesto, composicion farmaceutica que lo comprende y su uso en la fabricacion de medicamentos para modular efectos de los receptores de histamina 3 | |
| AR004219A1 (es) | Nuevos derivados de quinazolina, procedimientos para su preparacion, composiciones que los contienen y su uso en la preparacion de medicamentos,particularmente en el tratamiento de trastornos inflamatorios | |
| AR029151A1 (es) | Una sal cuaternaria de piperidina, su uso, un proceso para su preparacion, y una composicion farmaceutica que la contiene | |
| AR000039A2 (es) | Compuestos de piridinosulfonamida sustituidos, composiciones herbicidas que los contienen, metodo para preparar estos compuestos y compuestosintermediarios. | |
| PE20050130A1 (es) | Compuestos organicos | |
| 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 | |
| AR046297A1 (es) | Inhibidores de la dpp - iv metodos para prepararlos y composiciones farmaceuticas que los contienen como agente activo | |
| PE20040164A1 (es) | Mimeticos de glucocorticoides, procedimientos para su preparacion y composiciones farmaceuticas | |
| PE20070218A1 (es) | COMPUESTOS DE CICLOALQUILO AMINO-HIDANTOINA Y USO DE ESTOS PARA LA MODULACION DE ß-SECRETASA | |
| ES2093367T3 (es) | Derivados de quinazolina. | |
| MX9202943A (es) | Compuestos triciclo, proceso para prepararlos y composicion farmaceutica que los contiene. | |
| CO5251381A1 (es) | Derivados de adamantano, un proceso para su preparacion y composiciones farmaceuticas que los contienen | |
| EA200301216A1 (ru) | Замещенные хинуклидинами мультициклические гетероарилы для лечения заболевания | |
| CO5271658A1 (es) | Antagonistas del factor liberador de corticotropina | |
| AR012489A1 (es) | Tiofenopiridinas antagonistas del factor de liberacion de corticotropina. procedimiento para su preparacion, el uso de las mismas en la preparacionde un medicamento, composicion farmaceutica que las comprende, procedimiento para la preparacion de dicha composicion, un compuesto intermediario y | |
| ES2037753T3 (es) | Compuestos heterociclicos y su preparacion y uso. | |
| ATE103812T1 (de) | Zusammensetzung zur behandlung von ischaemischen stoerungen in organen. | |
| AR045040A1 (es) | Derivados de compuestos espiroazabiciclicos, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos | |
| AR045793A1 (es) | Compuestos derivados de 3-heterociclil-indol | |
| PT96030A (pt) | Processo para a preparacao de aminocarbonilcarbamatos relacionados com fisoestigmina e de composicoes farmaceuticas que os contem |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |