BRPI0611202C1 - compostos de benzimidazola-carboxamida como agonistas do receptor 5-ht4 - Google Patents

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

Info

Publication number
BRPI0611202C1
BRPI0611202C1 BRPI0611202A BRPI0611202A BRPI0611202C1 BR PI0611202 C1 BRPI0611202 C1 BR PI0611202C1 BR PI0611202 A BRPI0611202 A BR PI0611202A BR PI0611202 A BRPI0611202 A BR PI0611202A BR PI0611202 C1 BRPI0611202 C1 BR PI0611202C1
Authority
BR
Brazil
Prior art keywords
compounds
benzimidazole
receptor agonists
carboxamide
carboxamide compounds
Prior art date
Application number
BRPI0611202A
Other languages
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
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
Family has litigation
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(C1) "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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Cell Biology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biotechnology (AREA)
  • Pathology (AREA)
  • Microbiology (AREA)
  • General Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Food Science & Technology (AREA)
  • Toxicology (AREA)
  • Pulmonology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

compostos de benzimidazola-carboxamida como agonistas do receptor 5-ht4. a invenção se refere a compostos agonistas do receptor 5-ht4 de benzimidazola-carboxamida de fõrmula (i): (i) em que r1 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-ht4 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
US68447805P 2005-05-25 2005-05-25
US68446605P 2005-05-25 2005-05-25
US60/684.478 2005-05-25
US60/684.466 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 BRPI0611202B8 (pt) 2019-09-24
BRPI0611202B1 BRPI0611202B1 (pt) 2019-09-24
BRPI0611202C1 true BRPI0611202C1 (pt) 2021-05-25

Family

ID=37452788

Family Applications (1)

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)

Country Link
US (10) US8143279B2 (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)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE539077T1 (de) * 2003-09-03 2012-01-15 Pfizer Benzimidazolonverbindungen mit agonistischer wirkung am 5-ht4 rezeptor
US8309575B2 (en) 2004-04-07 2012-11-13 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
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
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
AU2010229142A1 (en) 2009-03-23 2011-10-13 Merck Sharp & Dohme Corp. P2X3, receptor antagonists for treatment of pain
US8404711B2 (en) * 2009-04-13 2013-03-26 Theravance, Inc. 5-HT4 receptor agonist compounds for treatment of cognitive disorders
AR080055A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de pirazolo-[5,1-b]-oxazol como antagonistas de los receptores de crf -1
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
ES2527849T3 (es) 2010-02-02 2015-01-30 Novartis Ag Derivados de ciclohexilamida como antagonistas del receptor de CRF
TW201536760A (zh) * 2013-08-09 2015-10-01 參天製藥股份有限公司 ３，３－二甲基－３，４－二氫－１ｈ－喹啉－２－酮衍生物的製造方法及該製造方法的中間體

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JPH111472A (ja) 1996-04-30 1999-01-06 Dainippon Pharmaceut Co Ltd ベンズアミド誘導体及びそれを含有する医薬組成物
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PT1546134E (pt) 2002-08-05 2007-08-10 Lilly Co Eli ''arilbenzodiazepinas substituídas com piperazina''
BR0314584A (pt) 2002-09-20 2005-08-09 Pfizer Compostos piperidinil-imidazopiridina n-substituìda como moduladores e receptores 5-ht4
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ATE539077T1 (de) * 2003-09-03 2012-01-15 Pfizer Benzimidazolonverbindungen mit agonistischer wirkung am 5-ht4 rezeptor
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

Also Published As

Publication number Publication date
NZ563068A (en) 2011-01-28
IL186883A0 (en) 2008-02-09
HK1110980A1 (en) 2008-07-25
NO339658B1 (no) 2017-01-16
US20180237420A1 (en) 2018-08-23
US20100249186A1 (en) 2010-09-30
IL186883A (en) 2013-03-24
US11254655B2 (en) 2022-02-22
US9428489B2 (en) 2016-08-30
US20060270652A1 (en) 2006-11-30
MX2007014762A (es) 2008-02-14
US20190152951A1 (en) 2019-05-23
AU2006250009A1 (en) 2006-11-30
US20200283408A1 (en) 2020-09-10
BRPI0611202B8 (pt) 2019-09-24
US20130273568A1 (en) 2013-10-17
US20150183761A1 (en) 2015-07-02
AU2006250009B2 (en) 2012-03-08
BRPI0611202B1 (pt) 2019-09-24
KR20080021045A (ko) 2008-03-06
MY147756A (en) 2013-01-15
US20170081313A1 (en) 2017-03-23
US9975877B2 (en) 2018-05-22
US7759363B2 (en) 2010-07-20
US20090209582A1 (en) 2009-08-20
US10696656B2 (en) 2020-06-30
KR101333280B1 (ko) 2013-11-28
US10233172B2 (en) 2019-03-19
HRP20120108T1 (en) 2012-02-29
SI1899324T1 (sl) 2012-03-30
MA29541B1 (fr) 2008-06-02
WO2006127815A3 (en) 2007-08-02
TWI388555B (zh) 2013-03-11
WO2006127815A2 (en) 2006-11-30
CA2607280A1 (en) 2006-11-30
PT1899324E (pt) 2012-01-24
US8143279B2 (en) 2012-03-27
EA200702612A1 (ru) 2008-06-30
US8377964B2 (en) 2013-02-19
PE20061446A1 (es) 2007-01-16
US20220274957A1 (en) 2022-09-01
EP1899324B1 (en) 2011-11-30
JP2008542281A (ja) 2008-11-27
BRPI0611202A2 (pt) 2010-08-24
JP2012197322A (ja) 2012-10-18
ES2376115T3 (es) 2012-03-09
NO20076481L (no) 2007-12-17
JP5072111B2 (ja) 2012-11-14
PL1899324T3 (pl) 2012-04-30
ATE535523T1 (de) 2011-12-15
HRP20120108T2 (hr) 2012-03-31
EA013240B1 (ru) 2010-04-30
CY1112366T1 (el) 2015-12-09
DK1899324T3 (da) 2012-02-13
AR057327A1 (es) 2007-11-28
CA2607280C (en) 2013-09-17
EP1899324A2 (en) 2008-03-19
TW200716607A (en) 2007-05-01

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