BR112015025033A8 - Prodrogas de inibidores da pde-5 do tipo pirimidina bicíclica substituída - Google Patents

Prodrogas de inibidores da pde-5 do tipo pirimidina bicíclica substituída

Info

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
Application number
BR112015025033A
Other languages
English (en)
Other versions
BR112015025033A2 (pt
BR112015025033B1 (pt
Inventor
Chutian Shu
Yongqian Wu
Original Assignee
Xuanzhu Pharma Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
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

Links

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 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

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)
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
CN201310105971.8 2013-03-29
CN201310105971 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2017291826B2 (en) * 2016-07-07 2021-10-21 Cyclerion Therapeutics, 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
BRPI0014526C1 (pt) * 1999-09-16 2021-05-25 Mitsubishi Tanabe Pharma Corp compostos cíclicos de seis elementos contendo nitrogênio aromático, composição farmacêutica e uso do mesmo
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
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
EP1223170B1 (en) * 1999-10-12 2005-12-28 Takeda Pharmaceutical Company Limited Pyrimidine-5-carboxamide compounds, process for producing the same and use thereof
US7273868B2 (en) * 2000-04-28 2007-09-25 Tanabe Seiyaku Co., Ltd. Pyrazine derivatives
US20080027037A1 (en) * 2000-04-28 2008-01-31 Tanabe Seiyaku Co., Ltd. Cyclic compounds
MXPA02010693A (es) * 2000-04-28 2003-03-10 Tanabe Seiyaku Co Compuestos ciclicos.
CN102970965A (zh) * 2010-04-05 2013-03-13 Sk化学公司 含有pde5抑制剂的减少皮肤皱纹的合成物
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
US9359371B2 (en) 2012-08-14 2016-06-07 Xuanzhu Pharma Co., Ltd. Bicyclic substituted pyrimidine compounds

Also Published As

Publication number Publication date
KR20150135789A (ko) 2015-12-03
WO2014154168A1 (zh) 2014-10-02
JP2016516736A (ja) 2016-06-09
JP6179966B2 (ja) 2017-08-16
US9527876B2 (en) 2016-12-27
BR112015025033A2 (pt) 2017-07-18
US20160046654A1 (en) 2016-02-18
EP2980087A1 (en) 2016-02-03
HK1212338A1 (en) 2016-06-10
EP2980087B1 (en) 2018-06-06
BR112015025033B1 (pt) 2022-04-19
CN105102447A (zh) 2015-11-25
EP2980087A4 (en) 2016-08-24
KR101749314B1 (ko) 2017-07-03
CN105102447B (zh) 2017-08-25

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Legal Events

Date Code Title Description
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.