ECSP13012486A - DERIVADOS DE 6,7-DIHIDRO-3H-OXAZOLO[3,4-a]PIRAZIN-5,8-DIONA - Google Patents
DERIVADOS DE 6,7-DIHIDRO-3H-OXAZOLO[3,4-a]PIRAZIN-5,8-DIONAInfo
- Publication number
- ECSP13012486A ECSP13012486A ECSP13012486A ECSP13012486A EC SP13012486 A ECSP13012486 A EC SP13012486A EC SP13012486 A ECSP13012486 A EC SP13012486A EC SP13012486 A ECSP13012486 A EC SP13012486A
- Authority
- EC
- Ecuador
- Prior art keywords
- oxazolo
- pde
- pyrazin
- dihydro
- dione
- Prior art date
Links
- -1 1,3-benzodioxol-5-yl Chemical group 0.000 abstract 2
- 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 abstract 2
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 abstract 2
- MXEOQXYFOPCTIV-JOCHJYFZSA-N (3r)-3-(1,3-benzodioxol-5-yl)-1-(1h-indol-3-yl)-7-methyl-3,6-dihydro-[1,3]oxazolo[3,4-a]pyrazine-5,8-dione Chemical compound C1=C2OCOC2=CC([C@@H]2N3C(=O)CN(C(C3=C(O2)C=2C3=CC=CC=C3NC=2)=O)C)=C1 MXEOQXYFOPCTIV-JOCHJYFZSA-N 0.000 abstract 1
- DRJBVJCTNYPBHF-UHFFFAOYSA-N 3H-[1,3]oxazolo[3,4-a]pyrazine-5,8-dione Chemical compound O=C1C=NC(=O)C2=COCN12 DRJBVJCTNYPBHF-UHFFFAOYSA-N 0.000 abstract 1
- SPNMSIYOCYTIIH-UHFFFAOYSA-N 6,7-dihydro-3h-[1,3]oxazolo[3,4-a]pyrazine-5,8-dione Chemical class O=C1CNC(=O)C2=COCN12 SPNMSIYOCYTIIH-UHFFFAOYSA-N 0.000 abstract 1
- 208000010228 Erectile Dysfunction Diseases 0.000 abstract 1
- 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 abstract 1
- 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 201000001881 impotence Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229940124549 vasodilator Drugs 0.000 abstract 1
- 239000003071 vasodilator agent Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P13/08—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
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- 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
- 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
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D503/00—Heterocyclic compounds containing 4-oxa-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. oxapenicillins, clavulanic acid derivatives; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
- C07D503/02—Preparation
- C07D503/04—Preparation by forming the ring or condensed ring systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invención describe una serie de derivados de 6,7-dihidro-3H-oxazolo[3,4-a]pirazin-5,8-diona, sus mezclas, sus sales farmacéuticamente aceptables, que son inhibidores de PDE-5, que poseen propiedades vasodilatadoras y efectos de relajación. En particular, el derivado (R)-3-(1,3-benzodioxol-5-il)-1-(1H-indol-3-il)-7-metil-6,7-dihidro[1,3]oxazolo[3,4-a]pirazin-5,8-diona, su enantiómero (S)-3-(1,3-benzodioxol-5-il)-1-(1H-indol-3-il)-7-metil-6,7-dihidro[1,3]oxazolo[3,4-a]pirazin-5,8-diona.La presente invención describe, además, procesos para la preparación de dichos compuestos, composiciones farmacéuticas que los contienen, así como usos como inhibidores de la enzima fosfodiesterasa de tipo 5 (PDE-5) en el tratamiento de te disfunción eréctil y trastornos tratables con inhibidor de PDE-5.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37348310P | 2010-08-13 | 2010-08-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP13012486A true ECSP13012486A (es) | 2013-04-30 |
Family
ID=45023415
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP13012486 ECSP13012486A (es) | 2010-08-13 | 2013-03-12 | DERIVADOS DE 6,7-DIHIDRO-3H-OXAZOLO[3,4-a]PIRAZIN-5,8-DIONA |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8338432B2 (es) |
| EP (1) | EP2603512B1 (es) |
| JP (1) | JP5940535B2 (es) |
| KR (1) | KR101871856B1 (es) |
| CN (1) | CN103108878B (es) |
| AR (1) | AR082661A1 (es) |
| BR (1) | BR112013003225B1 (es) |
| CA (1) | CA2807872C (es) |
| CL (1) | CL2013000434A1 (es) |
| CO (1) | CO6680703A2 (es) |
| DK (1) | DK2603512T3 (es) |
| EC (1) | ECSP13012486A (es) |
| ES (1) | ES2565493T3 (es) |
| HK (1) | HK1184786A1 (es) |
| HU (1) | HUE027903T2 (es) |
| IL (1) | IL224683A (es) |
| MX (1) | MX347632B (es) |
| PL (1) | PL2603512T3 (es) |
| RU (1) | RU2581831C2 (es) |
| UY (1) | UY33535A (es) |
| WO (1) | WO2012019254A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY33535A (es) * | 2010-08-13 | 2011-12-01 | Biolab Sanus Farmaceutuca Limitada | Derivados de 6,7-dihidro-3h-oxazolo[3,4]pirazin-5,8-diona |
| AR099523A1 (es) * | 2014-02-24 | 2016-07-27 | Biolab Sanus Farmacêutica Ltda | Compuestos derivados de 6,7-dihidro-3h-oxazolo[3,4-a]pirazina-5,8-diona |
| PT3191099T (pt) * | 2014-09-12 | 2018-12-18 | Biolab Sanus Farmaceutica Ltda | Derivados de piridopirimidinas |
| CN114158266A (zh) * | 2019-07-15 | 2022-03-08 | 生物实验萨纽斯药物有限公司 | 化合物3-(苯并[d][1,3]二氧杂环戊烯-5-基)-7-(1-羟基丙-2-基)-1-(1H-吲哚-3-基)-6,7-二氢-3H-噁唑并[3,4-a]吡嗪-5,8-二酮的立体异构体及其作为抗肿瘤剂和磷酸二酯酶抑制剂的用途 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996026940A1 (fr) | 1995-03-01 | 1996-09-06 | Kyowa Hakko Kogyo Co., Ltd. | Derives d'imidazoquinazoline |
| GB9514464D0 (en) * | 1995-07-14 | 1995-09-13 | Glaxo Lab Sa | Medicaments |
| MXPA03011082A (es) | 2001-06-05 | 2004-07-08 | Lilly Icos Llc | Derivados de pirazino-1',2': 1,6-prirido-3,4-b-indol-1,4-diona. |
| ES2269679T3 (es) | 2001-06-21 | 2007-04-01 | Lilly Icos Llc | Derivados de carbolina como inhibidores de pdev. |
| AR045950A1 (es) | 2003-10-09 | 2005-11-16 | Speedel Experimenta Ag | Compuestos derivados de piperazina, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos. |
| ATE417849T1 (de) | 2004-04-07 | 2009-01-15 | Pfizer | Pyrazoloä4,3-düpyrimidine |
| RU2418590C2 (ru) * | 2006-04-04 | 2011-05-20 | Донг-А Фарматех Ко. Лтд. | Средство для предупреждения и лечения гиперплазии предстательной железы, содержащее производное пиразолопиримидинона |
| BRPI0903803B1 (pt) * | 2009-09-30 | 2019-07-09 | Biolab Sanus Farmacêutica Ltda. | Composto, processo de preparação, composição farmacêutica e uso dos compostos |
| UY33535A (es) * | 2010-08-13 | 2011-12-01 | Biolab Sanus Farmaceutuca Limitada | Derivados de 6,7-dihidro-3h-oxazolo[3,4]pirazin-5,8-diona |
-
2011
- 2011-07-27 UY UY0001033535A patent/UY33535A/es active IP Right Grant
- 2011-08-02 KR KR1020137006343A patent/KR101871856B1/ko active IP Right Grant
- 2011-08-02 HU HUE11815927A patent/HUE027903T2/hu unknown
- 2011-08-02 JP JP2013523443A patent/JP5940535B2/ja active Active
- 2011-08-02 MX MX2013001692A patent/MX347632B/es active IP Right Grant
- 2011-08-02 DK DK11815927.6T patent/DK2603512T3/en active
- 2011-08-02 ES ES11815927.6T patent/ES2565493T3/es active Active
- 2011-08-02 WO PCT/BR2011/000255 patent/WO2012019254A1/en active Application Filing
- 2011-08-02 PL PL11815927.6T patent/PL2603512T3/pl unknown
- 2011-08-02 BR BR112013003225-1A patent/BR112013003225B1/pt active IP Right Grant
- 2011-08-02 EP EP11815927.6A patent/EP2603512B1/en active Active
- 2011-08-02 CN CN201180039626.8A patent/CN103108878B/zh active Active
- 2011-08-02 CA CA2807872A patent/CA2807872C/en active Active
- 2011-08-02 RU RU2013110795/04A patent/RU2581831C2/ru active
- 2011-08-02 US US13/196,363 patent/US8338432B2/en active Active
- 2011-08-09 AR ARP110102892A patent/AR082661A1/es active IP Right Grant
-
2013
- 2013-02-12 IL IL224683A patent/IL224683A/en active IP Right Grant
- 2013-02-12 CL CL2013000434A patent/CL2013000434A1/es unknown
- 2013-03-08 CO CO13046988A patent/CO6680703A2/es active IP Right Grant
- 2013-03-12 EC ECSP13012486 patent/ECSP13012486A/es unknown
- 2013-10-30 HK HK13112233.7A patent/HK1184786A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2013533290A (ja) | 2013-08-22 |
| MX2013001692A (es) | 2013-03-18 |
| US20120040988A1 (en) | 2012-02-16 |
| RU2581831C2 (ru) | 2016-04-20 |
| MX347632B (es) | 2017-05-04 |
| DK2603512T3 (en) | 2016-04-04 |
| HK1184786A1 (zh) | 2014-01-30 |
| BR112013003225B1 (pt) | 2021-03-30 |
| CN103108878B (zh) | 2016-01-27 |
| CL2013000434A1 (es) | 2013-06-07 |
| PL2603512T3 (pl) | 2016-09-30 |
| KR20130109110A (ko) | 2013-10-07 |
| EP2603512A4 (en) | 2014-07-16 |
| CA2807872A1 (en) | 2012-02-16 |
| CO6680703A2 (es) | 2013-05-31 |
| CN103108878A (zh) | 2013-05-15 |
| HUE027903T2 (hu) | 2016-11-28 |
| IL224683A (en) | 2016-03-31 |
| WO2012019254A1 (en) | 2012-02-16 |
| UY33535A (es) | 2011-12-01 |
| ES2565493T3 (es) | 2016-04-05 |
| EP2603512A1 (en) | 2013-06-19 |
| BR112013003225A2 (pt) | 2016-06-07 |
| RU2013110795A (ru) | 2014-09-20 |
| US8338432B2 (en) | 2012-12-25 |
| EP2603512B1 (en) | 2015-12-30 |
| CA2807872C (en) | 2018-07-24 |
| AR082661A1 (es) | 2012-12-26 |
| KR101871856B1 (ko) | 2018-06-28 |
| JP5940535B2 (ja) | 2016-06-29 |
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