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AR044821A1 - 4-(aminometil)-piperidin benzamidas como antagonistas de 5ht4 - Google Patents

4-(aminometil)-piperidin benzamidas como antagonistas de 5ht4

Info

Publication number
AR044821A1
AR044821A1 ARP040102131A ARP040102131A AR044821A1 AR 044821 A1 AR044821 A1 AR 044821A1 AR P040102131 A ARP040102131 A AR P040102131A AR P040102131 A ARP040102131 A AR P040102131A AR 044821 A1 AR044821 A1 AR 044821A1
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
hydroxy
halo
independently selected
Prior art date
Application number
ARP040102131A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR044821A1 publication Critical patent/AR044821A1/es

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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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/06Anti-spasmodics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs 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
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Compuestos antagonistas de 5HT4, métodos para prepararlos, composiciones farmacéuticas que los contienen, uso de dichos compuestos como medicamentos. Reivindicación 1: Un compuesto de fórmula (1) una forma estereoquímicamente isomérica del mismo, una forma N-óxido del mismo, o una sal de adición de ácido o base farmacéuticamente aceptable del mismo, en donde -R1-R2- es un radical bivalente de fórmula -O-CH2-O- (a-1), -O-CH2-CH2- (a-2), -O-CH2-CH2-O- (a-3), -O-CH2-CH2-CH2- (a-4), -O-CH2-CH2-CH2-O- (a-5), -O-CH2-CH2-CH2-CH2- (a-6), -O-CH2-CH2-CH2-CH2-O- (a-7), -O-CH2-CH2-CH2-CH2-CH2- (a-8), donde en dichos radicales bivalentes opcionalmente uno o dos átomos de H en el mismo átomo de C o en un átomo de C diferente se puede reemplazar por alquilo C1-6 o hidroxi; R3 es H, halo, alquilo C1-4; R4 es alquilo C1-6, alquilo C1-6 sustituido con ciano, o alquiloxi C1-6; alquiloxi C1-6; ciano; amino o mono o di(alquil C1-6)amino; R5 es H o alquilo C1-6, y el radical -OR5 está situado en la posición 3 o 4 del grupo piperidina; L es H, o L es un radical de fórmula -Alq-R6 (b-1), -Alq-X-R7 (b-2), -Alq-Y-C(=O)-R9 (b-3), o Alq-Z-C(=O)-NR11R12 (b-4), donde cada Alq es alcandiilo C1-12; y R6 es H, hidroxi, ciano, cicloalquilo C3-6; alquilsulfonilamino C1-6, arilo o Het; R7 es alquilo C1-6, alquilo C1-6 sustituido con hidroxi, cicloalquilo C346; arilo o Het; X es O, S, SO2 o NR8, siendo dicho R8 H o alquilo C1-6; R9 es H, alquilo c1-6, cicloalquilo C3-6, hidroxi o arilo; Y es un enlace directo, o NR10 donde R10 es H o alquilo C1-6; Z es un enlace directo, O, S, o NR10 donde R10 es H o alquilo C1-6; R11 y R12 son independientemente entre sí H, alquilo C1-6, cicloalquilo C3-6, o R11 y R12 combinados con el átomo de N que porta R11 y R12 pueden formar un anillo pirrolidinilo, piperidinilo, piperazinilo o 4-morfolinilo, estando ambos opcionalmente sustituidos con alquilo C1-; arilo representa fenilo no sustituido o fenilo sustituido con 1, 2, o 3 sustituyentes seleccionados independientemente entre sí de halo, hidroxi, alquilo C1-6, alquiloxi C1-6, alquilcarbonilo C1-6, nitro, trifluorometilo, amino, aminocarbonilo y aminosulfonilo; y Het es furanilo; furanilo sustituido con alquilo C1-6 o halo; tetrahidrofuranilo; tetrahidrofuranilo sustituido con alquilo C1-6; dioxolanilo; dioxolanilo sustituido con alquilo C1-6, dioxanilo; dioxanilo sustituido con alquilo C1-6; tetrahidropiranilo; tetrahidropiranilo sustituido con alquilo C1-6; 2,3-dihidro-2-oxo-1H-imidazolilo; 2,3-dihidro-2-oxo-1H-imidazolilo sustituido con uno o dos sustituyentes seleccionados independientemente entre sí de halo o alquilo C1-6; pirrolidinilo; pirrolidinilo sustituido con uno o dos sustituyentes seleccionados independientemente entre sí de halo, hidroxi o alquilo C1-6; piridinilo; piridinilo sustituido con uno o dos sustituyentes seleccionados independientemente entre sí de halo, hidroxi o alquilo C1-6; pirimidinilo; pirimidinilo sustituido con uno o dos sustituyentes seleccionados independientemente entre sí e halo, hidroxi o alquilo C1-6; piridazinilo; piridazinilo sustituido con uno o dos sustituyentes seleccionados independientemente entre sí de hidroxi, alquiloxi C1-6, alquilo C1-6 o halo; pirazinilo; pirazinilo sustituido con uno o dos sustituyentes seleccionados independientemente entre sí de hidroxi, alquiloxi C1-6, alquilo C1-6 o halo.
ARP040102131A 2003-06-19 2004-06-18 4-(aminometil)-piperidin benzamidas como antagonistas de 5ht4 AR044821A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP0350236 2003-06-19

Publications (1)

Publication Number Publication Date
AR044821A1 true AR044821A1 (es) 2005-10-05

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ID=33547568

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ARP040102131A AR044821A1 (es) 2003-06-19 2004-06-18 4-(aminometil)-piperidin benzamidas como antagonistas de 5ht4

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US (1) US7638535B2 (es)
EP (1) EP1641784B1 (es)
JP (1) JP4688800B2 (es)
KR (1) KR101151645B1 (es)
CN (1) CN100537565C (es)
AR (1) AR044821A1 (es)
AT (1) ATE364602T1 (es)
AU (1) AU2004251825B2 (es)
BR (1) BRPI0411603B1 (es)
CA (1) CA2528590C (es)
CY (1) CY1106857T1 (es)
DE (1) DE602004006997T2 (es)
DK (1) DK1641784T3 (es)
EA (1) EA008504B1 (es)
ES (1) ES2288258T3 (es)
HR (1) HRP20070393T3 (es)
IL (1) IL172604A (es)
JO (1) JO2478B1 (es)
MX (1) MXPA05013772A (es)
MY (1) MY139454A (es)
NZ (1) NZ544592A (es)
PA (1) PA8605101A1 (es)
PL (1) PL1641784T3 (es)
PT (1) PT1641784E (es)
SI (1) SI1641784T1 (es)
TW (1) TWI346107B (es)
UA (1) UA88607C2 (es)
WO (1) WO2005000838A1 (es)

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TW200533348A (en) 2004-02-18 2005-10-16 Theravance Inc Indazole-carboxamide compounds as 5-ht4 receptor agonists
US8309575B2 (en) 2004-04-07 2012-11-13 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
US7728006B2 (en) 2004-04-07 2010-06-01 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
TWI351282B (en) 2004-04-07 2011-11-01 Theravance Inc Quinolinone-carboxamide compounds as 5-ht4 recepto
ATE441646T1 (de) 2004-11-05 2009-09-15 Theravance Inc 5-ht4-rezeptoragonistenverbindungen
ATE431824T1 (de) 2004-11-05 2009-06-15 Theravance Inc Chinolinon-carboxamid-verbindungen
MX2007007818A (es) 2004-12-22 2007-09-11 Theravance Inc Compuestos de indazol-carboxamida.
NZ560828A (en) 2005-03-02 2011-01-28 Theravance Inc Quinolinone compounds as 5-HT4 receptor agonists
US9101160B2 (en) 2005-11-23 2015-08-11 The Coca-Cola Company Condiments with high-potency sweetener
US8017168B2 (en) 2006-11-02 2011-09-13 The Coca-Cola Company High-potency sweetener composition with rubisco protein, rubiscolin, rubiscolin derivatives, ace inhibitory peptides, and combinations thereof, and compositions sweetened therewith
US20100081981A1 (en) * 2008-10-01 2010-04-01 Cheng Shien-Che Wrist support
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CA2854266A1 (en) 2011-11-30 2013-06-06 Actelion Pharmaceuticals Ltd 3,7-disubstituted octahydro-2h-pyrido[4,3-e][1,3]oxazin-2-one antibiotics
GB201403093D0 (en) 2014-02-21 2014-04-09 Cancer Rec Tech Ltd Therapeutic compounds and their use
WO2017122722A1 (ja) 2016-01-15 2017-07-20 大日本住友製薬株式会社 2環性複素環化合物
GB201715194D0 (en) 2017-09-20 2017-11-01 Carrick Therapeutics Ltd Compounds and their therapeutic use
GB201918541D0 (en) 2019-12-16 2020-01-29 Carrick Therapeutics Ltd Therapeutic compounds and their use
CN115974856B (zh) * 2022-12-28 2023-08-11 北京康立生医药技术开发有限公司 一种治疗成人t细胞白血病淋巴瘤药物伐美妥司他的制备方法

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Publication number Publication date
US7638535B2 (en) 2009-12-29
HRP20070393T3 (en) 2007-10-31
AU2004251825B2 (en) 2009-11-26
WO2005000838A1 (en) 2005-01-06
PA8605101A1 (es) 2005-02-04
CA2528590A1 (en) 2005-01-06
DE602004006997T2 (de) 2008-05-15
AU2004251825A1 (en) 2005-01-06
JP4688800B2 (ja) 2011-05-25
IL172604A (en) 2010-12-30
CA2528590C (en) 2012-04-03
ATE364602T1 (de) 2007-07-15
CN100537565C (zh) 2009-09-09
TW200517376A (en) 2005-06-01
CN1809558A (zh) 2006-07-26
EA200600061A1 (ru) 2006-06-30
IL172604A0 (en) 2006-04-10
PL1641784T3 (pl) 2007-11-30
DK1641784T3 (da) 2007-09-24
BRPI0411603B1 (pt) 2017-10-31
PT1641784E (pt) 2007-08-28
KR101151645B1 (ko) 2012-06-08
BRPI0411603A (pt) 2006-08-08
KR20060018263A (ko) 2006-02-28
JO2478B1 (en) 2009-01-20
SI1641784T1 (sl) 2007-10-31
MXPA05013772A (es) 2006-03-08
MY139454A (en) 2009-10-30
US20060281753A1 (en) 2006-12-14
DE602004006997D1 (de) 2007-07-26
EP1641784B1 (en) 2007-06-13
ES2288258T3 (es) 2008-01-01
UA88607C2 (en) 2009-11-10
CY1106857T1 (el) 2012-05-23
EP1641784A1 (en) 2006-04-05
JP2006527716A (ja) 2006-12-07
HK1095327A1 (zh) 2007-05-04
EA008504B1 (ru) 2007-06-29
TWI346107B (en) 2011-08-01
NZ544592A (en) 2008-05-30

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