AR038377A1 - Derivados de n-bifenil-aminocicloalcancarboxamida (con sustitucion con metilo) - Google Patents

Derivados de n-bifenil-aminocicloalcancarboxamida (con sustitucion con metilo)

Info

Publication number
AR038377A1
AR038377A1 ARP030100276A ARP030100276A AR038377A1 AR 038377 A1 AR038377 A1 AR 038377A1 AR P030100276 A ARP030100276 A AR P030100276A AR P030100276 A ARP030100276 A AR P030100276A AR 038377 A1 AR038377 A1 AR 038377A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
halogen
independently selected
nrbrc
ring
Prior art date
Application number
ARP030100276A
Other languages
English (en)
Original Assignee
Merck & Co 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
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR038377A1 publication Critical patent/AR038377A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • 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
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/06—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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A61P25/04—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
    • A61P25/28—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members 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
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Los derivados N-bifenilo (con sustitución con metilo) de la aminocicloalcancarboxamida son antagonistas o agonistas inversos de la bradicinina B1, útiles en el tratamiento o la prevención de síntomas, tales como dolor e inflamación, asociados con el pasaje de la bradicinina B1. Reivindicación 1: Un compuesto de fórmula (1) y sus sales farmacéuticamente aceptables; donde R1 y R2 se seleccionan independientemente a partir de hidrógeno y alquilo C1-4; R3a se selecciona a partir de hidrógeno y alquilo C1-4 optativamente sustituido con 1 a 5 átomos de halógeno; R3b es alquilo C1-4 optativamente sustituido con 1 a 5 átomos de halógeno; R4a y R4b se seleccionan independientemente a partir de hidrógeno; halógeno y alquilo C1-4 optativamente sustituido con 1 a 4 grupos seleccionados a partir de halógeno, ORa, OC(O)Ra, S(O)kRd, OS(O)2Rd y NR1R2, o R4a y R4b conjuntamente con el átomo de carbono al que se encuentran ligados, forman un metileno exocíclico optativamente sustituido con 1 a 2 grupos seleccionados a partir de alquilo C1-4 optativamente sustituido con 1 a 5 halógenos y alquiloxi C1-4; R5 se selecciona a partir de alquilo C1-6 optativamente sustituido con 1 a 5 grupos independientemente seleccionados a partir de halógeno, nitro, ciano, ORa, SRa, CORa, SO2Rd, CO2Ra, OC(O)Ra, NRbRc, NRbC(O)Ra, NRbC(O)2Ra, C(O)NRbRc, cicloalquilo C3-8; cicloalquilo C3-8 optativamente sustituido con 1 a 5 grupos independientemente seleccionados a partir de halógeno, nitro, ciano y fenilo; alquinilo C3-6; alquenilo C2-6 optativamente sustituido con hidroxietilo; (CH2)k-arilo optativamente sustituido con 1 a 3 grupos independientemente seleccionados a partir de halógeno, nitro, ciano, ORa, SRa, C(O)2Ra, alquilo C1-4 y haloalquilo C1-3, donde arilo se selecciona a partir de fenilo, 3,4-metilendioxifenilo y naftilo; (CH2)k-heterociclo optativamente sustituido con 1 a 3 grupos independientemente seleccionados a partir de halógeno, nitro, ciano, ORa, SRa, alquilo C1-4 y haloalquilo C1-3 donde dicho heterociclo es seleccionado a partir de (a) un anillo heteroaromático de 5 miembros que consta de un heteroátomo del anillo, seleccionado a partir de N, O y S y teniendo, optativamente, hasta 3 átomos de nitrógeno del anillo adicionales, donde dicho anillo está optativamente benzofundido; (b) un anillo hetearomático de 6 miembros que contiene 1 a 3 átomos de nitrógeno del anillo y sus N-óxidos, donde dicho anillo está, optativamente, benzofundido; y (c) un anillo heterocíclico no aromático de 5 o 6 miembros, seleccionados a partir de tetrahidrofuranilo, 5-oxotetrahidrofuranilo, 2-oxo-2H-piranilo, 6-oxo-1,6-dihidropiridacinilo; C(O)2Ra y C(O)NRbRc; R6a se selecciona a partir de alquilo C1-8 optativamente sustituido con 1 a 5 grupos independientemente seleccionados a partir de halógeno, nitro, ciano, CORa, CO2Ra, C(O)NRbRc, ORa, OC(O)Ra, SRa, SO2Rd, S(O)Rd, NRbRc, NRbC(O)Ra, NRbSO2Rd, NRbCO2Ra; cicloalquilo C3-8; alquenilo C2-8 optativamente sustituido con CO2Ra; halógeno; ciano; nitro; NRbRc; NRbC(O)Ra; NRbCO2Ra; NRbC(O)NRbRc; NRbC(O)NRbCO2Ra; NRbSO2Rd; CO2Ra; CORa; C(O)NRbRc; C(O)NHORa; C(=NORa)Ra; C(=NORa)NRbRc; ORa; OC(O)Ra, S(O)kRd; SO2NRbRc; y heterociclo optativamente sustituido, donde el heterociclo es un anillo heteroaromático de 5 miembros que consta de un heteroátomo del anillo, seleccionado a partir de N, O y S y teniendo, optativamente hasta 3 átomos adicionales de anillo de nitrógeno, 4,5-dihidro-oxazolilo y 4,5-dihidro-1,2,4-oxadiazolilo, y donde dicho sustituyente comprende 1 a 3 grupos independientemente seleccionados a partir de alquilo C1-4 optativamente sustituido con 1 a 5 átomos de halógeno, ORa u OC(O)Ra; R6b y R6c son independientemente seleccionados a partir de hidrógeno, y un grupo de R6a; con la condición de que no más de uno de R6a, R6b y R6c sea un heterociclo; R7a y R7b son independientemente seleccionados a partir de hidrógeno; halógeno; ciano; nitro; ORa; CO2Ra; C(O)NRbRc; alquilo C1-4 optativamente sustituido con 1 a 5 átomos de halógeno; NRbRc; y S(O)kRd; R6a se selecciona a partir de hidrógeno; alquilo C1-4 optativamente sustituido con 1 a 5 átomos de halógeno; fenilo optativamente sustituido con 1 a 3 grupos independientemente seleccionados a partir de halógeno, ciano, nitro, OH, alquiloxi C1-4, cicloalquilo C3-6 y alquilo C1-4 optativamente sustituido con 1 a 5 átomos de halógeno; cicloalquilo C3-6; y piridilo optativamente sustituido con 1 a 3 grupos independientemente seleccionados a partir de halógeno y alquilo C1-4; Rb y Rc son independientemente seleccionados a partir de hidrógeno; alquilo C1-4 optativamente sustituido con 1 a 5 grupos independientemente seleccionados a partir de halógeno, amino, mono-alquilaminoC1-4, di-alquilaminoC1-4 y SO2Rd; (CH2)k-fenilo optativamente sustituido con 1 a 3 grupos seleccionados a partir de halógeno, ciano, nitro, OH, alquiloxi C1-4, cicloalquilo C3-6 y alquilo C1-4 optativamente sustituido con 1 a 5 átomos de halógenos; y cicloalquilo C3-6; o Rb y Rc, conjuntamente con el átomo de nitrógeno al cual se encuentran ligados, forman un anillo de 4, 5 o 6 miembros que contiene, optativamente un heteroátomo adicional seleccionado a partir de N, O y S; o Rb y Rc conjuntamente con el átomo de nitrógeno al cual se encuentran ligados, forman una imida cíclica; Rd se selecciona a partir de alquilo C1-4 optativamente sustituido con 1 a 5 átomos de halógeno; alquiloxi C1-4 y fenilo optativamente sustituido con 1 a 3 grupos seleccionados a partir de halógeno, ciano, nitro, OH, alquiloxi C1-4, cicloalquilo C3-6 y alquilo C1-4 optativamente sustituido con 1 a 5 átomos de halógeno; k es 0, 1 o 2; y m es 0 o 1.
ARP030100276A 2002-02-08 2003-01-30 Derivados de n-bifenil-aminocicloalcancarboxamida (con sustitucion con metilo) AR038377A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US35506202P 2002-02-08 2002-02-08
US41017202P 2002-09-12 2002-09-12

Publications (1)

Publication Number Publication Date
AR038377A1 true AR038377A1 (es) 2005-01-12

Family

ID=27737481

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030100276A AR038377A1 (es) 2002-02-08 2003-01-30 Derivados de n-bifenil-aminocicloalcancarboxamida (con sustitucion con metilo)

Country Status (27)

Country Link
US (2) US6919343B2 (es)
EP (1) EP1501787B1 (es)
JP (1) JP4098249B2 (es)
KR (1) KR20040083440A (es)
CN (1) CN1328247C (es)
AR (1) AR038377A1 (es)
AT (1) ATE309202T1 (es)
AU (1) AU2003216169B2 (es)
BR (1) BR0307508A (es)
CA (1) CA2474373C (es)
DE (1) DE60302240T2 (es)
DK (1) DK1501787T3 (es)
EA (1) EA007297B1 (es)
EC (1) ECSP045217A (es)
ES (1) ES2250899T3 (es)
HR (1) HRP20040677A2 (es)
IS (1) IS7372A (es)
JO (1) JO2356B1 (es)
MA (1) MA27108A1 (es)
MX (1) MXPA04007660A (es)
NO (1) NO20043739L (es)
NZ (1) NZ534062A (es)
PE (1) PE20030986A1 (es)
PL (1) PL371664A1 (es)
RS (1) RS65404A (es)
TW (1) TWI259079B (es)
WO (1) WO2003066577A1 (es)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003057671A1 (fr) * 2001-12-28 2003-07-17 Takeda Chemical Industries, Ltd. Compose biaryle et son utilisation
ATE316954T1 (de) * 2002-02-08 2006-02-15 Merck & Co Inc N-biphenylmethylaminocycloalkancarboxamid- derivative
US7163951B2 (en) * 2002-08-29 2007-01-16 Merck & Co., Inc. N-biarylmethyl aminocycloalkanecarboxamide derivatives
US20070093485A1 (en) * 2002-12-19 2007-04-26 Elan Pharmaceuticals, Inc. Substituted n-phenyl sulfonamide bradykinin antagonists
CA2534188A1 (en) * 2003-08-07 2005-02-24 Merck & Co., Inc. Sulfonyl substituted n-(biarylmethyl) aminocyclopropanecarboxamides
CA2550372C (en) 2003-12-22 2009-09-29 Merck & Co., Inc. Alpha-hydroxy amides as bradykinin antagonists or inverse agonists
JP2007526311A (ja) * 2004-03-02 2007-09-13 メルク　エンド　カムパニー　インコーポレーテッド ブラジキニンアンタゴニストとしてのアミノシクロプロパンカルボキサミド誘導体
US20050245543A1 (en) * 2004-04-30 2005-11-03 Pfizer Inc Histamine-3 receptor antagonists
CA2575706A1 (en) * 2004-08-02 2006-02-23 Bebaas, Inc. Vitamin b12 compositions
DE102004060542A1 (de) * 2004-12-16 2006-07-06 Sanofi-Aventis Deutschland Gmbh Hydroxybiphenyl-Carbonsäuren und Derivate, Verfahren zu deren Herstellung und deren Verwendung
JP4966202B2 (ja) * 2004-12-24 2012-07-04 スピニフェクス ファーマシューティカルズ ピーティーワイ リミテッド 治療または予防のための方法
US20070178141A1 (en) * 2005-09-07 2007-08-02 Bebaas, Inc. Vitamin B12 compositions
US20130131007A1 (en) 2005-09-07 2013-05-23 Bebaas, Inc. Vitamin b12 compositions
CN102885818B (zh) 2006-03-20 2016-05-04 诺华股份有限公司 治疗或预防炎性痛的方法
US8945505B2 (en) * 2007-02-02 2015-02-03 Panaphix, Inc. Use of arsenic compounds for treatment of pain and inflammation
ES2569660T3 (es) 2007-06-08 2016-05-12 Mannkind Corporation Inhibidores de la IRE-1alfa
EP2188254B1 (de) 2007-08-29 2012-03-21 Boehringer Ingelheim International GmbH Neue bradykinin b1-antagonisten
US20090270394A1 (en) * 2008-04-28 2009-10-29 Galemmo Jr Robert Cyclylamine derivatives as calcium channel blockers
WO2010097373A1 (de) * 2009-02-26 2010-09-02 Boehringer Ingelheim International Gmbh Verbindungen als bradykinin b1 antagonisten
WO2010097374A1 (de) * 2009-02-26 2010-09-02 Boehringer Ingelheim International Gmbh Verbindungen als bradykinin-b1-antagonisten
BRPI1008779A2 (pt) * 2009-02-26 2020-12-22 Boehringer Ingelheim International Gmbh. Compostos como antagonistas de bradiquinina-b1
US10457810B2 (en) 2009-08-24 2019-10-29 Board Of Trustees Of Michigan State University Densified biomass products containing pretreated biomass fibers
KR101843341B1 (ko) * 2010-02-23 2018-03-30 베링거 인겔하임 인터내셔날 게엠베하 브라디키닌 ｂ１ 길항제로서의 화합물
BR112012026710B8 (pt) 2010-04-19 2020-06-23 Univ Michigan State método para produzir um produto extraído a partir de biomassa lignocelulósica e método para produzir um produto digerido a partir de biomassa lignocelulósica
US8937073B2 (en) * 2010-08-20 2015-01-20 Boehringer Ingelheim International Gmbh Disubstituted tetrahydrofuranyl compounds and their use as B1-receptor antagonists
HUP1000598A2 (en) * 2010-11-05 2012-09-28 Richter Gedeon Nyrt Indole derivatives
US8912221B2 (en) * 2010-12-27 2014-12-16 Hoffmann-La Roche Inc. Biaryl amide derivatives
US8592426B2 (en) * 2011-01-24 2013-11-26 Hoffmann—La Roche Inc. Aryl-benzocycloalkyl amide derivatives
US11939320B2 (en) 2017-11-02 2024-03-26 Abbvie Inc. Modulators of the integrated stress pathway
TWI771621B (zh) 2018-10-11 2022-07-21 美商嘉來克生命科學有限責任公司 整合應激路徑之前藥調節劑

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5270317A (en) 1990-03-20 1993-12-14 Elf Sanofi N-substituted heterocyclic derivatives, their preparation and the pharmaceutical compositions in which they are present
IL99372A0 (en) 1990-09-10 1992-08-18 Ciba Geigy Ag Azacyclic compounds
US5208236A (en) 1992-09-23 1993-05-04 Schering Corporation N-(acylaminomethyl)glutaryl amino acids and use
EP0655461B1 (en) 1993-11-16 2000-06-07 Novartis AG Cyclic amino acid derivatives having ACE and NEP inhibiting activity
AU7211696A (en) 1995-09-27 1997-04-17 Ciba-Geigy Ag Treatment of chronic progressive renal failure
US6433185B1 (en) 1996-01-11 2002-08-13 Sanofi-Synthelabo N-(arylsulphonyl) amino acid derivatives, process for their preparation and pharmaceutical compositions containing them
FR2743562B1 (fr) 1996-01-11 1998-04-03 Sanofi Sa Derives de n-(arylsulfonyl) aminoacides, leur preparation, les compositions pharmaceutiques en contenant
PL343594A1 (en) 1998-04-23 2001-08-27 Novartis Ag Certain thiol inhibitors of endothelin-converting enzyme
DE69923676T2 (de) 1998-04-23 2006-01-12 Novartis Ag Bestimmte heteroaryl substituierte thiol inhibitoren von endothelin wechselnden enzymen
US20020052370A1 (en) 2000-07-06 2002-05-02 Barber Christopher Gordon Cyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
DE10036121A1 (de) 2000-07-25 2002-02-07 Merck Patent Gmbh N-Substituierte-1-amino-1,1-dialkyl-carbonsäurederivate
ATE316954T1 (de) 2002-02-08 2006-02-15 Merck & Co Inc N-biphenylmethylaminocycloalkancarboxamid- derivative

Also Published As

Publication number Publication date
US20050084463A1 (en) 2005-04-21
TWI259079B (en) 2006-08-01
DK1501787T3 (da) 2006-03-20
CN1328247C (zh) 2007-07-25
NZ534062A (en) 2006-06-30
TW200302718A (en) 2003-08-16
EA200401054A1 (ru) 2005-02-24
WO2003066577A1 (en) 2003-08-14
AU2003216169A1 (en) 2003-09-02
HRP20040677A2 (en) 2005-06-30
IS7372A (is) 2004-07-26
MXPA04007660A (es) 2004-11-10
ECSP045217A (es) 2004-09-28
BR0307508A (pt) 2004-12-07
CA2474373C (en) 2009-05-26
JP2005517006A (ja) 2005-06-09
DE60302240T2 (de) 2006-07-13
PE20030986A1 (es) 2003-11-19
US20030220375A1 (en) 2003-11-27
NO20043739L (no) 2004-10-29
ATE309202T1 (de) 2005-11-15
EP1501787B1 (en) 2005-11-09
US6919343B2 (en) 2005-07-19
CN1630633A (zh) 2005-06-22
DE60302240D1 (de) 2005-12-15
ES2250899T3 (es) 2006-04-16
JO2356B1 (en) 2006-12-12
AU2003216169B2 (en) 2008-12-04
RS65404A (en) 2007-02-05
EP1501787A1 (en) 2005-02-02
CA2474373A1 (en) 2003-08-14
EA007297B1 (ru) 2006-08-25
PL371664A1 (en) 2005-06-27
JP4098249B2 (ja) 2008-06-11
KR20040083440A (ko) 2004-10-01
MA27108A1 (fr) 2004-12-20

Similar Documents

Publication Publication Date Title
AR038377A1 (es) Derivados de n-bifenil-aminocicloalcancarboxamida (con sustitucion con metilo)
AR074002A1 (es) Pirazolo e imidazopiridinilpirimidinaminas como inhibidores de la tirosina kinasa (igr-ir)
RU2008112691A (ru) Азотсодержащее гетероциклическое соединение и его фармацевтическое применение
RU2386622C2 (ru) Гетероароматические производные мочевины и их применение в качестве активаторов глюкокиназы
AR062510A1 (es) Derivados de piridona con actividad antagonista de mch y medicamentos que comprenden estos compuestos
AR077434A1 (es) Compuestos para la reduccion de produccion de beta - amiloide
AR045414A1 (es) Derivados de 2 - piridincarboxamida y composiciones farmaceuticas que las contienen.
AR062125A1 (es) Compuestos que modulan el receptor cb2 y su utilizacion como medicamentos
AR048641A1 (es) Compuestos de aril- o heteroarilamida ortosustituidos utiles como antago-nistas del receptor de prostaglandinas e2; composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicame
AR073688A1 (es) Agonistas de receptores cb2, derivados de oxazoles y/o triazoles, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del dolor, enfermedades autoinmunes y alergicas, entre otras.
AR054365A1 (es) Derivados de heteroaril benzamidas, composiciones farmaceuticas que los contienen, usos en enfermedades mediadas por glucoquinasasy metodo de preparacion de los mismos.
AR052559A1 (es) Derivados de pirazol para inhibir cdk's y gsk's
AR081387A1 (es) Derivados de ciclohexilamina que tienen actividad como agonistas adrenergicos beta 2 y como antagonistas muscarinicos m3, composiciones farmaceuticas y uso de los mismos.
PE20130306A1 (es) Morfolinopirimidinas y su uso en terapia
AR069412A1 (es) Derivados de pirimidina, proceso para prepararlos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades virales, bacterianas y alergicas, entre otras.
RU2009133472A (ru) Пиримидин-замещенные макроциклические ингибиторы hcv
AR046244A1 (es) Activadores de glucoquinasa heteroaromaticos de seis miembros 5- sustituidos
AR078152A1 (es) Compuestos heterociclicos, utiles para el tratamiento de hcv y composiciones farmaceuticas que los comprenden
CO6251264A2 (es) Derivados de 1-ciano ciclopropilo como inhibidores de la captesina k
EA200600925A1 (ru) Производные триазола в качестве антагонистов вазопрессина
RU2003102389A (ru) Замещенные производные хиназолина и их применение в качестве ингибиторов
PE20080706A1 (es) Arilmidazolonas y ariltriazolonas sustituidas como inhibidores de receptores de vasopresina
AR067327A1 (es) Derivados de piperidina / piperazina
AR059138A1 (es) Derivados de 1,2,4-triazol antagonistas de edg-1
PE20141674A1 (es) Derivados de heterociclos biciclicos para el tratamiento de la hipertension arterial pulmonar

Legal Events

Date Code Title Description
FA Abandonment or withdrawal