AR057327A1 - Compuestos de benzimidazol-carboxamida como agonistas del receptor 5-ht4. procesos de obtencion y composiciones farmaceuticas - Google Patents

Compuestos de benzimidazol-carboxamida como agonistas del receptor 5-ht4. procesos de obtencion y composiciones farmaceuticas

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Publication number
AR057327A1
AR057327A1 ARP060102166A ARP060102166A AR057327A1 AR 057327 A1 AR057327 A1 AR 057327A1 AR P060102166 A ARP060102166 A AR P060102166A AR P060102166 A ARP060102166 A AR P060102166A AR 057327 A1 AR057327 A1 AR 057327A1
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AR
Argentina
Prior art keywords
alkyl
phenyl
optionally substituted
ochf2
ocf3
Prior art date
Application number
ARP060102166A
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English (en)
Inventor
P Fatheree
D Marquess
S Dalziel
K Phizackerly
R Mckinnell
R Gendron
L Jiang
S Choi
D Long
Original Assignee
Theravance Inc
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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=AR057327(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Theravance Inc filed Critical Theravance Inc
Publication of AR057327A1 publication Critical patent/AR057327A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
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    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008Chemical 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
    • G01N33/5044Chemical 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
    • G01N33/5058Neurological cells

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

Abstract

Composiciones farmacéuticas que comprenden dichos compuestos, métodos para utilizar dichos compuestos para tratar enfermedades asociadas con la actividad del receptor 5HT4, y procesos e intermediarios utiles para preparar dichos compuestos. Formas cristalinas de un compuestos de formula (1). Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1), donde: R1 es alquilo C3-5, opcionalmente sustituido con -OH; y X se selecciona entre: a) -C(O)OR2, donde R2 es alquilo C1-4 o -(CH2)n-fenilo donde n es 0 o 1; b) -C(O)R3, donde R3 se selecciona entre: fenilo opcionalmente sustituido con 1, 2, o 3 sustituyentes seleccionados entre alquilo C1-4, halo, alcoxi C1-4, -CF3, -OCF3, -OCHF2, y -CN; alquilo C1-5; cicloalquilo C4- 5; y -(CH2)m-A, donde m es 0 o 1 y A se selecciona entre amino, furanilo, tiofenilo, morfolinilo, tetrahidrofuranilo, piridinilo, naftalenilo, pirrolilo, tiomorfolinilo, pirrolidinilo, piperidinilo, oxoazetidinilo, tiazolidinilo, 1,1-dioxo isotiazolidinilo, y 2,4-dimetilisoxazolilo; c) -C(O)NR4R5, donde R4 es hidrogeno o alquilo C1-3, y R5 es fenilo opcionalmente sustituido con 1, 2, o 3 sustituyentes seleccionados entre alquilo C1-4, halo, alcoxi C1-4, -CF3, -OCF3, y -OCHF2; d) - C(O)C(R6R7)R8, donde R6 es hidrogeno o alquilo C1-3 y R7 es hidrogeno, -OH, o alquilo C1-3; o R6 y R7 juntos forman oxo o -(CH2)2-; y R8 es fenilo o ciclohexilo, donde fenilo o ciclohexilo están opcionalmente sustituidos con 1, 2, o 3 sustituyentes seleccionados entre alquilo C1-4, halo, alcoxi C1-4, -CF3, -OCF3, -OCHF2, y -CN; e) -C(O)C(HR9)OR10, donde R9 es hidrogeno o alquilo C1-3, y R10 es fenilo opcionalmente sustituido con 1, 2, o 3 sustituyentes seleccionados entre alquilo C1-4, halo, alcoxi C1-4, -CF3, -OCF3, y -OCHF2; y f) -S(O)2R11, donde R11 se selecciona entre alquilo C1-3, -CH2-fenilo, furanilo, tiofenilo, morfolinilo, tetrahidrofuranilo, piridinilo, naftalenilo, pirrolilo, tiomorfolinilo, pirrolidinilo, piperidinilo, oxoazetidinilo, tiazolidinilo, 1,1-dioxo isotiazolidinilo, 2,4-dimetilisoxazolilo, y fenilo opcionalmente sustituido con 1, 2, o 3 sustituyentes seleccionados entre alquilo C1-4, halo, alcoxi C1-4, -CF3, -OCF3, -OCHF2, y -CN; o una sal, un solvato o un estereoisomero aceptable para uso farmacéutico del mismo.
ARP060102166A 2005-05-25 2006-05-24 Compuestos de benzimidazol-carboxamida como agonistas del receptor 5-ht4. procesos de obtencion y composiciones farmaceuticas AR057327A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US68446605P 2005-05-25 2005-05-25
US68447805P 2005-05-25 2005-05-25
US74841505P 2005-12-08 2005-12-08

Publications (1)

Publication Number Publication Date
AR057327A1 true AR057327A1 (es) 2007-11-28

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ID=37452788

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ARP060102166A AR057327A1 (es) 2005-05-25 2006-05-24 Compuestos de benzimidazol-carboxamida como agonistas del receptor 5-ht4. procesos de obtencion y composiciones farmaceuticas

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

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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
CA2755680A1 (en) * 2009-03-23 2010-09-30 Merck Sharp & Dohme Corp. P2x3, receptor antagonists for treatment of pain
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WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
WO2011092290A1 (en) 2010-02-01 2011-08-04 Novartis Ag Pyrazolo[5,1b]oxazole derivatives as crf-1 receptor antagonists
WO2011095450A1 (en) 2010-02-02 2011-08-11 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
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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MY147756A (en) 2005-05-25 2013-01-15 Theravance Inc Benzimidazole-carboxamide compounds as 5-ht4 receptor agonists

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BRPI0611202B8 (pt) 2019-09-24
PT1899324E (pt) 2012-01-24
EA013240B1 (ru) 2010-04-30
US8377964B2 (en) 2013-02-19
BRPI0611202A2 (pt) 2010-08-24
AU2006250009B2 (en) 2012-03-08
TWI388555B (zh) 2013-03-11
HK1110980A1 (en) 2008-07-25
EP1899324B1 (en) 2011-11-30
US7759363B2 (en) 2010-07-20
KR101333280B1 (ko) 2013-11-28
US20130273568A1 (en) 2013-10-17
US20100249186A1 (en) 2010-09-30
WO2006127815A3 (en) 2007-08-02
HRP20120108T1 (en) 2012-02-29
US20190152951A1 (en) 2019-05-23
US20200283408A1 (en) 2020-09-10
NZ563068A (en) 2011-01-28
US20060270652A1 (en) 2006-11-30
CY1112366T1 (el) 2015-12-09
EP1899324A2 (en) 2008-03-19
KR20080021045A (ko) 2008-03-06
TW200716607A (en) 2007-05-01
PE20061446A1 (es) 2007-01-16
WO2006127815A2 (en) 2006-11-30
US9428489B2 (en) 2016-08-30
EA200702612A1 (ru) 2008-06-30
AU2006250009A1 (en) 2006-11-30
US10696656B2 (en) 2020-06-30
US20090209582A1 (en) 2009-08-20
US11254655B2 (en) 2022-02-22
NO20076481L (no) 2007-12-17
US20220274957A1 (en) 2022-09-01
IL186883A0 (en) 2008-02-09
MX2007014762A (es) 2008-02-14
BRPI0611202C1 (pt) 2021-05-25
IL186883A (en) 2013-03-24
US20150183761A1 (en) 2015-07-02
JP2008542281A (ja) 2008-11-27
DK1899324T3 (da) 2012-02-13
HRP20120108T2 (hr) 2012-03-31
CA2607280C (en) 2013-09-17
NO339658B1 (no) 2017-01-16
ES2376115T3 (es) 2012-03-09
JP5072111B2 (ja) 2012-11-14
MA29541B1 (fr) 2008-06-02
MY147756A (en) 2013-01-15
US20170081313A1 (en) 2017-03-23
SI1899324T1 (sl) 2012-03-30
US10233172B2 (en) 2019-03-19
PL1899324T3 (pl) 2012-04-30
US8143279B2 (en) 2012-03-27
US9975877B2 (en) 2018-05-22
ATE535523T1 (de) 2011-12-15
CA2607280A1 (en) 2006-11-30
JP2012197322A (ja) 2012-10-18
US20180237420A1 (en) 2018-08-23
BRPI0611202B1 (pt) 2019-09-24

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