BR112018012579A2 - derivados de 4-amino-2-(1h-pirazolo[3,4-b]piridin-3-il)-6-oxo-6,7-di-hidro-5h-pirrolo[2,3-d]pirimidina e os respectivos derivados de (1h-indazol-3-il) como moduladores de cgmp para o tratamento de doenças cardiovasculares - Google Patents

derivados de 4-amino-2-(1h-pirazolo[3,4-b]piridin-3-il)-6-oxo-6,7-di-hidro-5h-pirrolo[2,3-d]pirimidina e os respectivos derivados de (1h-indazol-3-il) como moduladores de cgmp para o tratamento de doenças cardiovasculares

Info

Publication number
BR112018012579A2
BR112018012579A2 BR112018012579-2A BR112018012579A BR112018012579A2 BR 112018012579 A2 BR112018012579 A2 BR 112018012579A2 BR 112018012579 A BR112018012579 A BR 112018012579A BR 112018012579 A2 BR112018012579 A2 BR 112018012579A2
Authority
BR
Brazil
Prior art keywords
pharmaceutically acceptable
acceptable salts
compounds
pulmonary
derivatives
Prior art date
Application number
BR112018012579-2A
Other languages
English (en)
Other versions
BR112018012579B8 (pt
BR112018012579B1 (pt
Inventor
BERGER Raphelle
Chen Yi-Heng
Li Guoqing
Garfunkle Joie
Li Hong
Miao Shouwu
Raghavan Subharekha
J. Smith Cameron
Stelmach John
Whitehead Alan
Zhang Rui
Zhang Yong
Fu Jianmin
Ji Gang
Jiang Falong
Original Assignee
Merck Sharp & Dohme Corp.
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 Merck Sharp & Dohme Corp. filed Critical Merck Sharp & Dohme Corp.
Publication of BR112018012579A2 publication Critical patent/BR112018012579A2/pt
Publication of BR112018012579B1 publication Critical patent/BR112018012579B1/pt
Publication of BR112018012579B8 publication Critical patent/BR112018012579B8/pt

Links

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
    • C07D487/02—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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61P9/10—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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

a presente invenção fornece compostos da fórmula (i) ou sais farmaceuticamente aceitáveis dos mesmos, em que x, y, z, r1, r2, r4, ra, e os índices m, p, e q são como descrito aqui. os compostos ou seus sais farmaceuticamente aceitáveis podem modular a produção corporal de monofosfato cíclico de guanosina ("cgmp") e são geralmente adequados para a terapia e profilaxia de doenças que são associadas com um equilíbrio de cgmp perturbado como doença cardiovascular, disfunção endotelial, disfunção diastólica, aterosclerose, hipertensão, falência cardíaca, hipertensão pulmonar (who grupos i, ii, iii, iv), angina pectoris, trombose, restenose, infarto do miocárdio, acidente vascular cerebral, insuficiência cardíaca, fibrose, hipertonia pulmonar, disfunção erétil, asma, síndrome do desconforto respiratório agudo (ards), doença renal crônica, fibrose cística, anemia falciforme, esclerodermia, síndrome de raynaud, diabetes, retinopatia diabética, cirrose do fígado, doença pulmonar obstrutiva crônica (copd), lesão pulmonar aguda, fibrose pulmonar ou doença pulmonar intersticial. a invenção também fornece composições farmacêuticas que compreendem compostos da fórmula (i) ou sais farmaceuticamente aceitáveis dos mesmos. a invenção também se refere a compostos ou seus sais farmaceuticamente aceitáveis para o uso em terapia e profilaxia das doenças mencionadas acima e para preparações farmacêuticas com este propósito.
BR112018012579A 2015-12-22 2016-12-20 Composto modulador de cgmp, sua composição farmacêutica e seu uso BR112018012579B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2015/098251 2015-12-22
PCT/CN2015/098251 WO2017107052A1 (en) 2015-12-22 2015-12-22 Soluble guanylate cyclase stimulators
PCT/US2016/067654 WO2017112617A1 (en) 2015-12-22 2016-12-20 4-amino-2-(1h-pyrazolo[3,4-b]pyridin-3-yl)-6-oxo-6,7-dihydro-5h-pyrrolo[2,3-d]pyrimidine derivatives and the respective (1h-indazol-3-yl) derivatives as cgmp modulators for treating cardiovascular diseases

Publications (3)

Publication Number Publication Date
BR112018012579A2 true BR112018012579A2 (pt) 2018-12-04
BR112018012579B1 BR112018012579B1 (pt) 2023-10-24
BR112018012579B8 BR112018012579B8 (pt) 2023-11-21

Family

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BR112018012579A BR112018012579B8 (pt) 2015-12-22 2016-12-20 Composto modulador de cgmp, sua composição farmacêutica e seu uso

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EP (1) EP3394067B1 (pt)
JP (1) JP6454448B2 (pt)
KR (1) KR102191312B1 (pt)
CN (1) CN108738320B (pt)
AR (1) AR107154A1 (pt)
AU (1) AU2016377364B2 (pt)
BR (1) BR112018012579B8 (pt)
CA (1) CA3009193C (pt)
CL (1) CL2018001671A1 (pt)
CO (1) CO2018006300A2 (pt)
CR (1) CR20180330A (pt)
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DO (1) DOP2018000153A (pt)
EA (1) EA036445B1 (pt)
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ES (1) ES2794654T3 (pt)
HK (1) HK1255028A1 (pt)
HR (1) HRP20200857T1 (pt)
HU (1) HUE049941T2 (pt)
IL (1) IL260020B (pt)
LT (1) LT3394067T (pt)
ME (1) ME03748B (pt)
MX (2) MX2018007728A (pt)
MY (1) MY194021A (pt)
NI (1) NI201800069A (pt)
PE (1) PE20181802A1 (pt)
PH (1) PH12018501342A1 (pt)
PL (1) PL3394067T3 (pt)
PT (1) PT3394067T (pt)
RS (1) RS60344B1 (pt)
SG (1) SG11201805272XA (pt)
SI (1) SI3394067T1 (pt)
SV (1) SV2018005715A (pt)
TN (1) TN2018000219A1 (pt)
TW (1) TWI724079B (pt)
UA (1) UA122264C2 (pt)
WO (2) WO2017107052A1 (pt)

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TW201734017A (zh) 2017-10-01
PL3394067T3 (pl) 2020-08-24
AU2016377364B2 (en) 2019-02-14
ECSP18054606A (es) 2018-12-31
MY194021A (en) 2022-11-08
ES2794654T3 (es) 2020-11-18
SV2018005715A (es) 2018-10-19
SG11201805272XA (en) 2018-07-30
TN2018000219A1 (en) 2019-10-04
JP6454448B2 (ja) 2019-01-16
EA201891303A1 (ru) 2018-11-30
US10428076B2 (en) 2019-10-01
BR112018012579B8 (pt) 2023-11-21
US20180305366A1 (en) 2018-10-25
AR107154A1 (es) 2018-03-28
DK3394067T3 (da) 2020-06-15
EP3394067B1 (en) 2020-04-01
HRP20200857T1 (hr) 2020-11-13
EP3394067A1 (en) 2018-10-31
EA036445B1 (ru) 2020-11-11
CO2018006300A2 (es) 2018-07-10
HUE049941T2 (hu) 2020-11-30
SI3394067T1 (sl) 2020-07-31
CY1123173T1 (el) 2021-10-29
WO2017112617A1 (en) 2017-06-29
KR102191312B1 (ko) 2020-12-15
PT3394067T (pt) 2020-06-02
NI201800069A (es) 2018-10-05
AU2016377364A1 (en) 2018-06-14
US20170174693A1 (en) 2017-06-22
BR112018012579B1 (pt) 2023-10-24
LT3394067T (lt) 2020-06-10
KR20180095904A (ko) 2018-08-28
PE20181802A1 (es) 2018-11-19
IL260020B (en) 2021-05-31
MX2018007728A (es) 2018-08-15
TWI724079B (zh) 2021-04-11
UA122264C2 (uk) 2020-10-12
CN108738320A (zh) 2018-11-02
DOP2018000153A (es) 2018-11-30
CA3009193A1 (en) 2017-06-29
US10030027B2 (en) 2018-07-24
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PH12018501342A1 (en) 2019-02-18
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CR20180330A (es) 2018-08-21
RS60344B1 (sr) 2020-07-31
ME03748B (me) 2021-04-20
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WO2017107052A1 (en) 2017-06-29
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CL2018001671A1 (es) 2018-08-03

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