BR112015025033A2 - prodrogas de inibidores da pde-5 do tipo pirimidina bicíclico substituídas - Google Patents

prodrogas de inibidores da pde-5 do tipo pirimidina bicíclico substituídas Download PDF

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Publication number
BR112015025033A2
BR112015025033A2 BR112015025033A BR112015025033A BR112015025033A2 BR 112015025033 A2 BR112015025033 A2 BR 112015025033A2 BR 112015025033 A BR112015025033 A BR 112015025033A BR 112015025033 A BR112015025033 A BR 112015025033A BR 112015025033 A2 BR112015025033 A2 BR 112015025033A2
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BR
Brazil
Prior art keywords
substituted bicyclic
inhibitors
bicyclic pyrimidine
type pde
prodrugs
Prior art date
Application number
BR112015025033A
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English (en)
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BR112015025033A8 (pt
BR112015025033B1 (pt
Inventor
Shu Chutian
Wu Yongqian
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Xuanzhu Pharma Co Ltd
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Publication date
Application filed by Xuanzhu Pharma Co Ltd filed Critical Xuanzhu Pharma Co Ltd
Publication of BR112015025033A2 publication Critical patent/BR112015025033A2/pt
Publication of BR112015025033A8 publication Critical patent/BR112015025033A8/pt
Publication of BR112015025033B1 publication Critical patent/BR112015025033B1/pt

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    • 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 System
    • 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

Abstract

resumo “prodrogas de inibidores da pde-5 do tipo pirimidina bicíclico substituídas” são proporcionadas prodrogas de inibidores da pde-5 do tipo pirimidina bicíclico substituídas, seus sais ou estereoisômeros farmaceuticamente aceitáveis. também são providos os métodos de preparação dessas prodrogas de compostos, 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)
BR112015025033-5A 2013-03-29 2014-03-28 Composto e seu uso como inibidor de pde-5, bem como preparação farmacêutica compreeendendo o dito composto BR112015025033B1 (pt)

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 true BR112015025033A2 (pt) 2017-07-18
BR112015025033A8 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3029374A1 (en) * 2016-07-07 2018-01-11 Ironwood Pharmaceuticals, Inc. Phosphorus prodrugs of sgc stimulators
CN111406053B (zh) * 2017-12-11 2023-03-31 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1219609E (pt) * 1999-09-16 2007-06-19 Tanabe Seiyaku Co ''compostos cíclicos aromático azotados de seis membros''
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
AU7683500A (en) * 1999-10-12 2001-04-23 Takeda Chemical Industries Ltd. Pyrimidine-5-carboxamide compounds, process for producing the same and use thereof
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
WO2001083460A1 (fr) * 2000-04-28 2001-11-08 Tanabe Seiyaku Co., Ltd. Composes cycliques
US7273868B2 (en) * 2000-04-28 2007-09-25 Tanabe Seiyaku Co., Ltd. Pyrazine derivatives
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
EP2735567B1 (en) * 2011-07-21 2016-10-26 Xuanzhu Pharma Co., Ltd. Heterocyclic substituted pyrimidine compound
EP2886540B1 (en) 2012-08-14 2017-07-26 Xuanzhu Pharma Co., Ltd. Bicyclic substituted pyrimidine compounds

Also Published As

Publication number Publication date
US20160046654A1 (en) 2016-02-18
KR20150135789A (ko) 2015-12-03
EP2980087A1 (en) 2016-02-03
JP6179966B2 (ja) 2017-08-16
US9527876B2 (en) 2016-12-27
BR112015025033A8 (pt) 2021-09-08
KR101749314B1 (ko) 2017-07-03
CN105102447A (zh) 2015-11-25
JP2016516736A (ja) 2016-06-09
EP2980087A4 (en) 2016-08-24
CN105102447B (zh) 2017-08-25
HK1212338A1 (en) 2016-06-10
WO2014154168A1 (zh) 2014-10-02
EP2980087B1 (en) 2018-06-06
BR112015025033B1 (pt) 2022-04-19

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

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.