BR112015025033A8 - Prodrogas de inibidores da pde-5 do tipo pirimidina bicíclica substituída - Google Patents
Prodrogas de inibidores da pde-5 do tipo pirimidina bicíclica substituídaInfo
- Publication number
- BR112015025033A8 BR112015025033A8 BR112015025033A BR112015025033A BR112015025033A8 BR 112015025033 A8 BR112015025033 A8 BR 112015025033A8 BR 112015025033 A BR112015025033 A BR 112015025033A BR 112015025033 A BR112015025033 A BR 112015025033A BR 112015025033 A8 BR112015025033 A8 BR 112015025033A8
- Authority
- BR
- Brazil
- Prior art keywords
- substituted bicyclic
- bicyclic pyrimidine
- prodrugs
- pde
- type pde
- Prior art date
Links
- 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 title abstract 3
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 title abstract 3
- 239000000651 prodrug Substances 0.000 title abstract 3
- 229940002612 prodrug Drugs 0.000 title abstract 3
- 125000002619 bicyclic group Chemical group 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 abstract 3
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 3
- 201000001880 Sexual dysfunction Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 231100000872 sexual dysfunction Toxicity 0.000 abstract 1
- 230000001568 sexual effect Effects 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
- 230000002485 urinary effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- 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
- A61P13/08—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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- 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
- A61P9/04—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
- A61P9/12—Antihypertensives
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
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)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Hospice & Palliative Care (AREA)
- Gynecology & Obstetrics (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
composto e seu uso como inibidor de pde-5, bem como preparação e composição farmacêuticas compreeendendo o dito composto. são proporcionadas prodrogas de inibidores da pde-5 do tipo pirimidina bicíclica substituída, seus sais ou seus estereoisômeros farmaceuticamente aceitáveis. também são providos os métodos para preparar esses compostos de prodrogas, preparações farmacêuticas e composições farmacêuticas, bem como um uso desses compostos, preparações farmacêuticas e composições farmacêuticas na fabricação de medicamentos para o tratamento e/ou a profilaxia da disfunção sexual e dos sintomas do trato urinário inferior. (i)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201310105971 | 2013-03-29 | ||
CN201310105971.8 | 2013-03-29 | ||
PCT/CN2014/074268 WO2014154168A1 (zh) | 2013-03-29 | 2014-03-28 | 双环取代的嘧啶类pde-5抑制剂的前药 |
Publications (3)
Publication Number | Publication Date |
---|---|
BR112015025033A2 BR112015025033A2 (pt) | 2017-07-18 |
BR112015025033A8 true BR112015025033A8 (pt) | 2021-09-08 |
BR112015025033B1 BR112015025033B1 (pt) | 2022-04-19 |
Family
ID=51622462
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112015025033-5A BR112015025033B1 (pt) | 2013-03-29 | 2014-03-28 | Composto e seu uso como inibidor de pde-5, bem como preparação farmacêutica compreeendendo o dito composto |
Country Status (8)
Country | Link |
---|---|
US (1) | US9527876B2 (pt) |
EP (1) | EP2980087B1 (pt) |
JP (1) | JP6179966B2 (pt) |
KR (1) | KR101749314B1 (pt) |
CN (1) | CN105102447B (pt) |
BR (1) | BR112015025033B1 (pt) |
HK (1) | HK1212338A1 (pt) |
WO (1) | WO2014154168A1 (pt) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2017291826B2 (en) * | 2016-07-07 | 2021-10-21 | Cyclerion Therapeutics, Inc. | Phosphorus prodrugs of sGC stimulators |
CN111433199B (zh) * | 2017-12-11 | 2023-04-04 | 轩竹生物科技股份有限公司 | 磷酸二酯酶-5抑制剂的晶型 |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU767558B2 (en) * | 1999-09-16 | 2003-11-13 | Mitsubishi Tanabe Pharma Corporation | Aromatic nitrogenous six-membered ring compounds |
JP3637961B2 (ja) * | 1999-09-16 | 2005-04-13 | 田辺製薬株式会社 | 芳香族含窒素六員環化合物 |
WO2001027105A1 (fr) * | 1999-10-12 | 2001-04-19 | Takeda Chemical Industries, Ltd. | Composes de pyrimidine-5-carboxamide, procede de preparation et d'utilisation desdits composes |
JP2001233875A (ja) * | 1999-10-12 | 2001-08-28 | Takeda Chem Ind Ltd | ピリミジン−5−カルボキサミド化合物、その製造法およびその用途 |
US20080027037A1 (en) * | 2000-04-28 | 2008-01-31 | Tanabe Seiyaku Co., Ltd. | Cyclic compounds |
US7273868B2 (en) * | 2000-04-28 | 2007-09-25 | Tanabe Seiyaku Co., Ltd. | Pyrazine derivatives |
NZ522217A (en) * | 2000-04-28 | 2004-04-30 | Tanabe Seiyaku Co | Cyclic compounds |
WO2011126250A2 (ko) * | 2010-04-05 | 2011-10-13 | 에스케이케미칼 주식회사 | Pde5 억제제를 함유하는 피부 주름 개선용 조성물 |
CN102372697A (zh) | 2010-08-19 | 2012-03-14 | 山东轩竹医药科技有限公司 | 取代的嘧啶类化合物 |
US8980904B2 (en) * | 2011-07-21 | 2015-03-17 | Xuanzhu Pharma Co., Ltd. | Heterocyclic substituted pyrimidine compound |
EP2886540B1 (en) | 2012-08-14 | 2017-07-26 | Xuanzhu Pharma Co., Ltd. | Bicyclic substituted pyrimidine compounds |
-
2014
- 2014-03-28 JP JP2016504470A patent/JP6179966B2/ja active Active
- 2014-03-28 BR BR112015025033-5A patent/BR112015025033B1/pt active IP Right Grant
- 2014-03-28 WO PCT/CN2014/074268 patent/WO2014154168A1/zh active Application Filing
- 2014-03-28 KR KR1020157031055A patent/KR101749314B1/ko active Search and Examination
- 2014-03-28 EP EP14775142.4A patent/EP2980087B1/en active Active
- 2014-03-28 US US14/780,718 patent/US9527876B2/en active Active
- 2014-03-28 CN CN201480019442.9A patent/CN105102447B/zh active Active
-
2016
- 2016-01-08 HK HK16100204.4A patent/HK1212338A1/xx unknown
Also Published As
Publication number | Publication date |
---|---|
EP2980087A4 (en) | 2016-08-24 |
KR20150135789A (ko) | 2015-12-03 |
KR101749314B1 (ko) | 2017-07-03 |
EP2980087A1 (en) | 2016-02-03 |
US20160046654A1 (en) | 2016-02-18 |
BR112015025033A2 (pt) | 2017-07-18 |
US9527876B2 (en) | 2016-12-27 |
BR112015025033B1 (pt) | 2022-04-19 |
JP6179966B2 (ja) | 2017-08-16 |
CN105102447A (zh) | 2015-11-25 |
WO2014154168A1 (zh) | 2014-10-02 |
CN105102447B (zh) | 2017-08-25 |
EP2980087B1 (en) | 2018-06-06 |
HK1212338A1 (en) | 2016-06-10 |
JP2016516736A (ja) | 2016-06-09 |
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B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
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B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 28/03/2014, OBSERVADAS AS CONDICOES LEGAIS. |