BRPI0611202B8 - compostos de benzimidazola-carboxamida como agonistas do receptor 5-ht4 - Google Patents

compostos de benzimidazola-carboxamida como agonistas do receptor 5-ht4 Download PDF

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Publication number
BRPI0611202B8
BRPI0611202B8 BRPI0611202A BRPI0611202A BRPI0611202B8 BR PI0611202 B8 BRPI0611202 B8 BR PI0611202B8 BR PI0611202 A BRPI0611202 A BR PI0611202A BR PI0611202 A BRPI0611202 A BR PI0611202A BR PI0611202 B8 BRPI0611202 B8 BR PI0611202B8
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BR
Brazil
Prior art keywords
compounds
receptor agonists
carboxamide compounds
benzimidazole carboxamide
relates
Prior art date
Application number
BRPI0611202A
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English (en)
Inventor
D Long Daniel
Marquess Daniel
M Phizackerley Kirsten
Jiang Lan
Ross Fatheree Paul
Murray Mckinnell Robert
Gendron Roland
M Dalziel Sean
Choi Seok-Ki
Original Assignee
Theravance Biopharma R&D Ip Llc
Theravance Inc
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37452788&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0611202(B8) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Theravance Biopharma R&D Ip Llc, Theravance Inc filed Critical Theravance Biopharma R&D Ip Llc
Publication of BRPI0611202A2 publication Critical patent/BRPI0611202A2/pt
Publication of BRPI0611202B8 publication Critical patent/BRPI0611202B8/pt
Publication of BRPI0611202B1 publication Critical patent/BRPI0611202B1/pt
Publication of BRPI0611202C1 publication Critical patent/BRPI0611202C1/pt

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    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/08—Antiallergic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5044—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics involving specific cell types
    • G01N33/5058—Neurological cells

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

a invenção se refere a compostos agonistas do receptor 5-ht~4~ de benzimidazola-carboxamida de fórmula (1): em que r^1^ e x são conforme definido na especificação ou um sal ou solvato ou estereoisômero farmaceuticamente aceitável dos mesmos. a invenção também se refere à composições farmacêuticas compreendendo tais compostos, métodos de uso de tais compostos para tratar doenças associadas à atividade do receptor 5-ht~4~ e processos e intermediários úteis para preparo de tais compostos. a invenção ainda se refere à formas cristalinas de um composto de fórmula (i).
BRPI0611202A 2005-05-25 2006-05-24 compostos de benzimidazola-carboxamida como agonistas do receptor 5-ht4 BRPI0611202C1 (pt)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US68446605P 2005-05-25 2005-05-25
US68447805P 2005-05-25 2005-05-25
US60/684.466 2005-05-25
US60/684.478 2005-05-25
US74841505P 2005-12-08 2005-12-08
US60/748.415 2005-12-08
PCT/US2006/020085 WO2006127815A2 (en) 2005-05-25 2006-05-24 Benzimidazole-carboxamide compounds as 5-ht4 receptor agonists

Publications (4)

Publication Number Publication Date
BRPI0611202A2 BRPI0611202A2 (pt) 2010-08-24
BRPI0611202B8 true BRPI0611202B8 (pt) 2019-09-24
BRPI0611202B1 BRPI0611202B1 (pt) 2019-09-24
BRPI0611202C1 BRPI0611202C1 (pt) 2021-05-25

Family

ID=37452788

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Application Number Title Priority Date Filing Date
BRPI0611202A BRPI0611202C1 (pt) 2005-05-25 2006-05-24 compostos de benzimidazola-carboxamida como agonistas do receptor 5-ht4

Country Status (27)

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US (10) US7759363B2 (pt)
EP (1) EP1899324B1 (pt)
JP (2) JP5072111B2 (pt)
KR (1) KR101333280B1 (pt)
AR (1) AR057327A1 (pt)
AT (1) ATE535523T1 (pt)
AU (1) AU2006250009B2 (pt)
BR (1) BRPI0611202C1 (pt)
CA (1) CA2607280C (pt)
CY (1) CY1112366T1 (pt)
DK (1) DK1899324T3 (pt)
EA (1) EA013240B1 (pt)
ES (1) ES2376115T3 (pt)
HK (1) HK1110980A1 (pt)
HR (1) HRP20120108T2 (pt)
IL (1) IL186883A (pt)
MA (1) MA29541B1 (pt)
MX (1) MX2007014762A (pt)
MY (1) MY147756A (pt)
NO (1) NO339658B1 (pt)
NZ (1) NZ563068A (pt)
PE (1) PE20061446A1 (pt)
PL (1) PL1899324T3 (pt)
PT (1) PT1899324E (pt)
SI (1) SI1899324T1 (pt)
TW (1) TWI388555B (pt)
WO (1) WO2006127815A2 (pt)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0414105B8 (pt) * 2003-09-03 2021-05-25 Askat Inc compostos de benzimidazolona com atividade agonista do receptor 5-ht4
US8309575B2 (en) 2004-04-07 2012-11-13 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
US7256294B2 (en) * 2005-05-25 2007-08-14 Theravance, Inc. Crystalline form of a benzimidazole-carboxamide medicinal compound
MY147756A (en) * 2005-05-25 2013-01-15 Theravance Inc Benzimidazole-carboxamide compounds as 5-ht4 receptor agonists
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
US9238647B2 (en) 2009-03-23 2016-01-19 Merck Sharp & Dohme Corp. P2X3 receptor antagonists for treatment of pain
KR20120017421A (ko) * 2009-04-13 2012-02-28 세라밴스 인코포레이티드 인지 장애의 치료를 위한 ５-ｈｔ₄ 수용체 아고니스트 화합물
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
EP2531510B1 (en) 2010-02-01 2014-07-23 Novartis AG Pyrazolo[5,1b]oxazole derivatives as crf-1 receptor antagonists
ES2527849T3 (es) 2010-02-02 2015-01-30 Novartis Ag Derivados de ciclohexilamida como antagonistas del receptor de CRF
CN105473557A (zh) * 2013-08-09 2016-04-06 参天制药株式会社 3,3－二甲基－3,4－二氢－1h－喹喔啉－2－酮衍生物的制造方法及该制造方法的中间体

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BRPI0414105B8 (pt) 2003-09-03 2021-05-25 Askat Inc compostos de benzimidazolona com atividade agonista do receptor 5-ht4
MY147756A (en) * 2005-05-25 2013-01-15 Theravance Inc Benzimidazole-carboxamide compounds as 5-ht4 receptor agonists
US7256294B2 (en) * 2005-05-25 2007-08-14 Theravance, Inc. Crystalline form of a benzimidazole-carboxamide medicinal compound

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ES2376115T3 (es) 2012-03-09
JP5072111B2 (ja) 2012-11-14
US20100249186A1 (en) 2010-09-30
US20060270652A1 (en) 2006-11-30
US8377964B2 (en) 2013-02-19
NZ563068A (en) 2011-01-28
NO339658B1 (no) 2017-01-16
HRP20120108T2 (hr) 2012-03-31
EA013240B1 (ru) 2010-04-30
BRPI0611202C1 (pt) 2021-05-25
US20190152951A1 (en) 2019-05-23
CA2607280C (en) 2013-09-17
EP1899324B1 (en) 2011-11-30
PT1899324E (pt) 2012-01-24
US20200283408A1 (en) 2020-09-10
US9975877B2 (en) 2018-05-22
EA200702612A1 (ru) 2008-06-30
US20130273568A1 (en) 2013-10-17
US7759363B2 (en) 2010-07-20
MX2007014762A (es) 2008-02-14
IL186883A0 (en) 2008-02-09
HRP20120108T1 (en) 2012-02-29
US20220274957A1 (en) 2022-09-01
MA29541B1 (fr) 2008-06-02
DK1899324T3 (da) 2012-02-13
MY147756A (en) 2013-01-15
US20170081313A1 (en) 2017-03-23
US8143279B2 (en) 2012-03-27
CA2607280A1 (en) 2006-11-30
US10233172B2 (en) 2019-03-19
WO2006127815A3 (en) 2007-08-02
US20150183761A1 (en) 2015-07-02
JP2012197322A (ja) 2012-10-18
KR20080021045A (ko) 2008-03-06
SI1899324T1 (sl) 2012-03-30
JP2008542281A (ja) 2008-11-27
WO2006127815A2 (en) 2006-11-30
TW200716607A (en) 2007-05-01
KR101333280B1 (ko) 2013-11-28
NO20076481L (no) 2007-12-17
PL1899324T3 (pl) 2012-04-30
PE20061446A1 (es) 2007-01-16
HK1110980A1 (en) 2008-07-25
AU2006250009B2 (en) 2012-03-08
AU2006250009A1 (en) 2006-11-30
AR057327A1 (es) 2007-11-28
TWI388555B (zh) 2013-03-11
US10696656B2 (en) 2020-06-30
EP1899324A2 (en) 2008-03-19
BRPI0611202B1 (pt) 2019-09-24
BRPI0611202A2 (pt) 2010-08-24
US11254655B2 (en) 2022-02-22
CY1112366T1 (el) 2015-12-09
US20180237420A1 (en) 2018-08-23
US20090209582A1 (en) 2009-08-20
ATE535523T1 (de) 2011-12-15
IL186883A (en) 2013-03-24
US9428489B2 (en) 2016-08-30

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