AR082498A1 - Derivados ciclicos de carboxamida y urea sustituidos como ligandos del receptor de vainiloide - Google Patents

Derivados ciclicos de carboxamida y urea sustituidos como ligandos del receptor de vainiloide

Info

Publication number
AR082498A1
AR082498A1 ARP110103024A ARP110103024A AR082498A1 AR 082498 A1 AR082498 A1 AR 082498A1 AR P110103024 A ARP110103024 A AR P110103024A AR P110103024 A ARP110103024 A AR P110103024A AR 082498 A1 AR082498 A1 AR 082498A1
Authority
AR
Argentina
Prior art keywords
unsubstituted
substituted
unsaturated
several times
case
Prior art date
Application number
ARP110103024A
Other languages
English (en)
Inventor
Frank Robert Dr
Bahrenberg Gregor Dr
Christoph Thomas Dr
De Vry Jean Dr
Schiene Klaus Dr
Original Assignee
Gruenenthal Gmbh
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 Gruenenthal Gmbh filed Critical Gruenenthal Gmbh
Publication of AR082498A1 publication Critical patent/AR082498A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P9/10—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
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Métodos para su producción, a medicamentos que contienen estos compuestos y al uso de estos compuestos para producir medicamentos útiles para el tratamiento del dolor, enfermedades del sistema nervioso central, trastornos de sangre o fluido extracelular, trastornos del aparato respiratorio.Reivindicación 1: Compuestos sustituidos de la fórmula general (1) en la que X significa CR3 o N siendo que R3 significa H; o alquilo C1-10, saturado o insaturado, ramificado o no ramificado, insustituido o sustituido una o varias veces; A significa N, C o CH; T significa N, C o CR7b; el circulo punteado significa que el anillo no aromático ta opcionalmente puede tener al menos un enlace insaturado con la condición de que si A es N, A no es parte de un enlace insaturado, y con la condición de que si T es N, T no es parte de un enlace insaturado; p significa 1, 2 ó 3; n significa 1, 2, 3 ó 4; R0 significa alquilo C1-10, saturado o insaturado, ramificado o no ramificado, insustituido o sustituido una o varias veces; cicloalquilo C3-10 o heterociclilo, en cada caso saturado o insaturado, insustituido o sustituido una o varias veces; arilo o heteroarilo, en cada caso insustituido o sustituido una o varias veces; cicloalquilo C3-10 o heterociclilo puenteado por vía de alquilo C1-8, en cada caso saturado o insaturado, insustituido o sustituido una o varias veces, siendo que la cadena de alquilo en cada caso puede estar ramificada o no ramificada, saturada o insaturada, insustituida, sustituida una o varias veces; o arilo o heteroarilo puenteado por vía de alquilo C1-8, en cada caso insustituido o sustituido una o varias veces, siendo que la cadena de alquilo en cada caso puede estar ramificada o no ramificada, saturada o insaturada, insustituida, sustituida una o varias veces; R1 significa H; alquilo C1-10, saturado o insaturado, ramificado o no ramificado, insustituido o sustituido una o varias veces; cicloalquilo1 C3-10 o heterociclilo1, en cada caso saturado o insaturado, insustituido o sustituido una o varias veces; arilo o heteroarilo, en cada caso insustituido o sustituido una o varias veces; cicloalquilo1 C3-10 o heterociclilo1 puenteado por vía de alquilo C1-8, en cada caso saturado o insaturado, insustituido o sustituido una o varias veces, siendo que la cadena de alquilo en cada caso puede estar ramificada o no ramificada, saturada o insaturada, insustituida, sustituida una o varias veces; o arilo o heteroarilo puenteado por vía de alquilo C1-8, en cada caso insustituido o sustituido una o varias veces, siendo que la cadena de alquilo en cada caso puede estar ramificada o no ramificada, saturada o insaturada, insustituida, sustituida una o varias veces; C(=O)R0; C(=O)-OH; C(=O)-OR0; C(=O)-NHR0; C(=O)-N(R0)2; OH; O-R0; SH; S-R0; S(=O)2-R0; S(=O)2-OR0; S(=O)2-NHR0; S(=O)2-N(R0)2; NH2; NHR0; N(R0)2; NH-S(=O)2-R0; N(R0)(S(=O)2-R0; o SCl3; R2 significa H; R0; NO2; CN; OH; SH; F; Cl; Br; I; CF3; CF2H; CFH2, CF2Cl, CFCl2, CH2CF3, OCF3, OCF2H, OCFH2, OCF2Cl; OCFCl2; SCF3; SCF2H; SCFH2; SCF2Cl; SCFCl2; S(=O)2-CF3; S(=O)2-CF2H; S(=O)2-CFH2 o SF5; preferiblemente es ¹ H; R4 significa H; R5, R6 y R8 significan, en cada caso independientemente uno de otro H; F; Cl; Br; I; OH; OR0; o R0; R7a significa R0; C(=O)-R0; C(=O)OH; C(=O)-OR0; C(=O)-NHR0; C(=O)-N(R0)2 OH; O-R7c; SH; S-R0; S(=O)2-R0; S(=O)2-OR0; S(=O)2-NHR0; S(=O)2-N(R0)2; NH2; NHR0; N(R0)2; NH-S(=O)2-R0; N(R0) (S(=O)2-R0); R7b significa H; F; Cl; Br; I; u OH; con la condición de que R7a no puede ser OH si T es CR7b y R7b significa OH; con la condición de que R7a no puede significar NH2; NHR0; N(R0)2; NH-S(=O)2-R0; N(R0)(S(=O)2-R0) si T significa N; R7c alquilo C1-10, saturado o insaturado, ramificado o no ramificado, insustituido o sustituido una o varias veces; arilo o heteroarilo; en donde “sustituido con alquilo”, “sustituido con heterociclilo” y “sustituido con cicloalquilo” en los radicales correspondientes significa la sustitución de uno o varios átomos de hidrógeno en cada caso independientemente uno de otro por F; Cl; Br; I; NO2 CN; =O; =NH; =C(NH2)2; CF3; CF2H; CFH2; CF2Cl; CFCl2; R0; C(=O)H; C(=O)R0; CO2H; C(=O)OR0; CONH2 C(=O)NHR0; C(=O)N(R0)2; OH; OCF3; OCF2H; OCFH2; OCF2Cl; OCFCl2; OR0; O-C(=O)-R0; O-C(=O)-O-R0; O-(C=O)-NH-R0; O-C(=O)-N(R0)2; O-S(=O)2-R0; O-S(=O)2OH; O-S(=O)2OR0; O-S(=O)2NH2; O-S(=O)2NHR0; O-S(=O)2N(R0)2; NH2; NH-R0; N(R0)2; NH-C(=O)-R0; NH-C(=O)-O-R0; NH-C(=O)-NH2; NH-C(=O)-NH-R0; NH-C(=O)-N(R0)2; NR0-C(=O)-R0; NR0-C(=O)-O-R0; NR0-C(=O)-NH2; NR0-C(=O)-NH-R0; NR0-C(=O)-N(R0)2; NH-S(=O)2OH; NH-S(=O)2R0; NH-S(=O)2OR0; NH-S(=O)2NH2; NH-S(=O)2NHR0; NH-S(=O)2N(R0)2; NR0-S(=O)2OH; NR0-S(=O)2R0; NR0-S(=O)2OR0; NR0-S(=O)2NH2; NR0-S(=O)2NHR0; NR0-S(=O)2N(R0)2; SH; SCF3; SCF2H; SCFH2; SCF2Cl; SCFCl2; SR0; S(=O)R0; S(=O)2R0; S(=O)2OH; S(=O)2OR0; S(=O)2NH2; S(=O)2NHR0; o S(=O)2N(R0)2; en donde “sustituido con cicloalquilo1” y “sustituido con heterociclilo1” en los radicales correspondientes equivale a la sustitución de uno o varios átomos de hidrógeno en cada caso independientemente uno de otro por F; Cl; Br; I; NO2; CN; =O; =C(NH2)2; CF3; CF2H; CFH2; CF2Cl; CFCl2; R0; C(=O)H; C(=O)R0; CO2H; C(=O)OR0; CONH2, C(=O)NHR0; C(=O)N(R0)2; OH; OCF3; OCF2H; OCFH2, OCF2Cl; OCFCl2; OR0; O-C(=O)-R0; O-C(=O)-O-R0; O-(C=O)-NH-R0; O-C(=O)-N(R0)2; O-S(=O)2-R0; O-S(=O)2OH; O-S(=O)2OR0; O-S(=O)2NH2; O-S(=O)2NHR0; O-S(=O)2N(R0)2; SH; SCF3; SCF2H; SCFH2; SCF2Cl; SCFCl2; SR0; S(=O)R0; S(=O)2R0; S(=O)2OH; S(=O)2OR0; S(=O)2NH2; S(=O)2NHR0; o S(=O)2N(R0)2; en donde “sustituido con arilo” y “sustituido con heteroarilo” en los radicales correspondientes equivale a la sustitución de uno o varios átomos de hidrógeno en cada caso independientemente uno de otro por F; Cl; Br; I; NO2; CN; CF3; CF2H; CFH2; CF2Cl; CFCl2; R0; C(=O)H; C(=O)R0; CO2H; C(=O)OR0; CONH2, C(=O)NHR0; C(=O)N(R0)2; OH; OCF3; OCF2H; OCFH2, OCF2Cl; OCFCl2; OR0; O-C(=O)-R0; O-C(=O)-O-R0; O-(C=O)-NH-R0; O-C(=O)-N(R0)2; O-S(=O)2-R0; O-S(=O)2OH; O-S(=O)2OR0; O-S(=O)2NH2; O-S(=O)2NHR0; O-S(=O)2N(R0)2; NH2; NH-R0; N(R0)2; NH-C(=O)-R0; NH-C(=O)-O-R0; NH-C(=O)-NH2; NH-C(=O)-NH-R0; NH-C(=O)-N(R0)2; NR0-C(=O)-R0; NR0-C(=O)-O-R0; NR0-C(=O)-NH2; NR0-C(=O)-NH-R0; NR0-C(=O)-N(R0)2; NH-S(=O)2OH; NH-S(=O)2R0; NH-S(=O)2OR0; NH-S(=O)2NH2; NH-S(=O)2NHR0; NH-S(=O)2N(R0)2; NR0-S(=O)2OH; NR0-S(=O)2R0; NR0-S(=O)2OR0; NR0-S(=O)2NH2; NR0-S(=O)2NHR0; NR0-S(=O)2N(R0)2; SH; SCF3; SCF2H; SCFH2; SCF2Cl; SCFCl2; SR0; S(=O)R0; S(=O)2R0; S(=O)2OH; S(=O)2OR0; S(=O)2NH2; S(=O)2NHR0; o S(=O)2N(R0)2; en la forma de los compuestos libres; de los tautómeros; de los óxidos de N; del racemato; de los enantiómeros, diastereómeros, mezclas de los enantiómeros y diastereómeros o de un enantiómero o diastereómero individual; o en la forma de las sales de los ácidos o bases fisiológicamente tolerables.
ARP110103024A 2010-08-20 2011-08-19 Derivados ciclicos de carboxamida y urea sustituidos como ligandos del receptor de vainiloide AR082498A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10008723 2010-08-20

Publications (1)

Publication Number Publication Date
AR082498A1 true AR082498A1 (es) 2012-12-12

Family

ID=42985573

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110103024A AR082498A1 (es) 2010-08-20 2011-08-19 Derivados ciclicos de carboxamida y urea sustituidos como ligandos del receptor de vainiloide

Country Status (10)

Country Link
US (1) US20120046301A1 (es)
EP (1) EP2606033A1 (es)
JP (1) JP2013534229A (es)
AR (1) AR082498A1 (es)
AU (1) AU2011291034A1 (es)
BR (1) BR112013003815A2 (es)
CA (1) CA2806634A1 (es)
MX (1) MX2013002011A (es)
TW (1) TW201211029A (es)
WO (1) WO2012022487A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2871222A1 (en) 2012-05-02 2013-11-07 Lupin Limited Substituted pyrazole compounds as crac modulators
JP2016501264A (ja) 2012-12-14 2016-01-18 ビーエーエスエフ ソシエタス・ヨーロピアＢａｓｆ Ｓｅ 動物有害生物を防除するためのマロノニトリル化合物
HUE060660T2 (hu) 2014-03-07 2023-04-28 Biocryst Pharm Inc Szubsztituált pirazolok mint humán plazma kallikrein-gátlók
WO2015161224A1 (en) 2014-04-17 2015-10-22 Merial, Inc. Use of malononitrile compounds for protecting animals from parasites
CA2986083A1 (en) 2015-06-11 2016-12-15 Basilea Pharmaceutica International AG Efflux-pump inhibitors and therapeutic uses thereof
AU2017275657B2 (en) 2016-06-02 2021-08-19 Novartis Ag Potassium channel modulators
LT3571193T (lt) 2017-01-23 2022-02-10 Cadent Therapeutics, Inc. Kalio kanalo moduliatoriai
CN109232422B (zh) * 2018-09-17 2020-07-07 烟台万润药业有限公司 一种塞来昔布的制备方法
US11459340B2 (en) 2018-09-18 2022-10-04 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives as Src homology-2 phosphatase inhibitors
CN112480004B (zh) * 2020-11-04 2022-08-12 华南理工大学 一种5-三氟甲基取代吡唑衍生物及其合成方法与应用

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6387900B1 (en) * 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
US6723730B2 (en) * 2000-07-20 2004-04-20 Neurogen Corporation Capsaicin receptor ligands
US20050209297A1 (en) * 2000-08-31 2005-09-22 Pfizer Inc Pyrazole derivatives
EP2080757A1 (en) * 2003-07-24 2009-07-22 Euro-Celtique S.A. Heteroaryl-tetrahydropiperidyl compounds useful for treating or preventing pain
US7453002B2 (en) * 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
TW200633990A (en) * 2004-11-18 2006-10-01 Takeda Pharmaceuticals Co Amide compound
US20060116368A1 (en) * 2004-11-29 2006-06-01 Calvo Raul R 4-Piperidinecarboxamide modulators of vanilloid VR1 receptor
JP5197014B2 (ja) * 2004-12-10 2013-05-15 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・エルレ・エルレ ヒストンデアセチラーゼ（ｈｄａｃ）阻害剤としての複素環誘導体
WO2008010061A2 (en) * 2006-07-17 2008-01-24 Glenmark Pharmaceuticals S.A. 3-azabicyclo [3.1.0] hexane vanilloid receptor ligands, pharmaceutical compositions containing them, and processes for their preparation
JP4785881B2 (ja) * 2007-02-27 2011-10-05 大塚製薬株式会社 医薬
CA2688343A1 (en) * 2007-05-25 2008-12-18 Janssen Pharmaceutica N.V. Heteroaryl-substituted urea modulators of fatty acid amide hydrolase
TW200916447A (en) * 2007-08-29 2009-04-16 Methylgene Inc Sirtuin inhibitors
JP2011500820A (ja) * 2007-10-25 2011-01-06 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃｂ２受容体を制御するジアゼパン化合物

Also Published As

Publication number Publication date
JP2013534229A (ja) 2013-09-02
CA2806634A1 (en) 2012-02-23
WO2012022487A1 (de) 2012-02-23
TW201211029A (en) 2012-03-16
US20120046301A1 (en) 2012-02-23
BR112013003815A2 (pt) 2019-09-24
AU2011291034A1 (en) 2013-03-14
MX2013002011A (es) 2013-03-25
EP2606033A1 (de) 2013-06-26

Similar Documents

Publication Publication Date Title
AR082498A1 (es) Derivados ciclicos de carboxamida y urea sustituidos como ligandos del receptor de vainiloide
AR054035A1 (es) Derivados benzodioxano y benzodioxolano y uso de los mismos
AR063331A1 (es) Derivados de biaril eter urea y composiciones farmaceuticas
AR083817A1 (es) Derivados de carboxamida y urea heteroaromaticos sustituidos como ligandos del receptor vanilloide
AR127309A2 (es) Derivados de piridazinona
EA200970510A1 (ru) Гетеромоноциклическое соединение и его применение
AR040773A1 (es) Pirazoles utiles como inhibidores de gsk-3
AR058885A1 (es) Compuestos de piperidina 3,5-sustituidos
AR045595A1 (es) Composiciones utiles como inhibidores de proteinas quinasas
ES2530943T3 (es) Derivados de la cromenona con actividad antitumoral
PE20142456A1 (es) COMPUESTOS DE OXAZOLIDIN-2-ONA Y USOS DE LOS MISMOS COMO INHIBIDORES DE LA PI3Ks
AR082633A1 (es) Analogos de tetraciclina
AR072906A1 (es) Nucleosidos modificados utiles como antivirales
AR056892A1 (es) Derivados de cinolin-3-carboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion del receptor gabaa
AR036604A1 (es) Derivados de 4-pirimidona 3-sustituida
EA201100942A1 (ru) Циклические пиримидин-4-карбоксамиды в качестве антагонистов рецептора ccr2, предназначенные для лечения воспаления, астмы и хозл
AR070578A1 (es) Imidazolidinas fenil- sustituidas, medicamentos que comprenden dichos compuestos y su uso para producir medicamentos
PE20091100A1 (es) Nuevos compuestos 010
EA200870358A1 (ru) 2-(циклический амино) пиримидоновые производные в качестве ингибиторов tpk1
AR077328A1 (es) Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
AR086538A1 (es) COMPUESTOS PARA REDUCIR LA PRODUCCION DE b-AMILOIDE
AR063988A1 (es) Derivados heterociclicos, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen
AR087301A1 (es) Derivados de carboxamida y urea que contienen pirazol heteroaromatico sustituido como ligandos del receptor de vanilloide
AR083167A1 (es) Derivados heterociclicos de benzamidas sustituidas, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del dolor, diabetes, obesidad y otras enfermedades neurologicas
BR112014023384A2 (pt) inibidores de bace de di-hidro-tiazina e di-hidro-oxazina espirocíclicos, e composições e usos dos mesmos

Legal Events

Date Code Title Description
FA Abandonment or withdrawal