AR079938A1 - Compuestos de 4-- fenoxi -nicotinamida o 4- fenoxi -pirimidina - 5- carboxamida - Google Patents

Compuestos de 4-- fenoxi -nicotinamida o 4- fenoxi -pirimidina - 5- carboxamida

Info

Publication number
AR079938A1
AR079938A1 ARP110100173A ARP110100173A AR079938A1 AR 079938 A1 AR079938 A1 AR 079938A1 AR P110100173 A ARP110100173 A AR P110100173A AR P110100173 A ARP110100173 A AR P110100173A AR 079938 A1 AR079938 A1 AR 079938A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
halogen
alkoxycarbonyl
unsubstituted
Prior art date
Application number
ARP110100173A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR079938A1 publication Critical patent/AR079938A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • 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
    • 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
    • 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
    • A61P17/06—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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • 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
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic 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
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Nutrition Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)

Abstract

Así como las sales farmacéuticamente aceptables de los mismos. Estos compuestos son agonistas del GPBAR1 y pueden utilizarse como medicamentos para el tratamiento de enfermedades, por ejemplo de la diabetes de tipo 2. Reivindicacion 1: Compuestos de la formula (1) en la que A1 es CR13 o N; A2 es CR14 o N; R1 y R2 se eligen con independencia entre sí entre el grupo formado por hidrogeno, alquilo C1-7, halogeno, halogeno- alquilo C1-7, ciano y alcoxi C1-7; R13 y R14 se eligen con independencia entre sí entre el grupo formado por hidrogeno, alquilo C1-7, halogeno, halogeno-alquilo C1-7, ciano, alcoxi C1-7, amino y alquil C1-7-sulfanilo; R3 se elige entre el grupo formado por hidrogeno, alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, ciano, cicloalquilo C3-7, N-heterociclilo, heteroarilo de cinco eslabones, fenilo y -NR15R16, en el que R15 y R16 se eligen con independencia entre sí entre hidrogeno, alquilo C1-7 y cicloalquilo C3-7; R4 se elige entre el grupo formado por hidrogeno, alquilo C1-7, halogeno-alquilo C1-7 y cicloalquilo C3-7; o R3 y R4 o R3 y R14 juntos son -X-(CR17R18)n- y forman parte de un anillo; en el que X se elige entre el grupo formado por -CR19R20-, O, S, C=O y NR21; R17 y R18 se eligen con independencia entre sí entre hidrogeno o alquilo C1-7; R19 y R20 se eligen con independencia entre sí entre el grupo formado por hidrogeno, alquilo C1-7, alcoxi C1-7-carbonilo, heterociclilo sin sustituir y heterociclilo sustituido por uno o dos grupos elegidos entre alquilo C1-7 y halogeno, o R19 y R20 junto con el átomo de C al que están unidos forman un anillo ciclopropilo u oxetanilo o juntos forman un grupo =CH2 o =CF2; R21 se elige entre el grupo formado por hidrogeno, alquilo C1-7, halogeno-alquilo C1-7, cicloalquilo C3-7 o cicloalquil C3-7-alquilo C1-7, dicho cicloalquilo C3-7 está sin sustituir o sustituido por carboxil-alquilo C1-7 o alcoxi C1-7-carbonilo; heterociclilo, heterociclil-alquilo C1-7, heteroarilo, heteroaril-alquilo C1-7, carboxil-alquilo C1-7, alcoxi C1-7-carbonil-alquilo C1-7, alcoxi C1-7-carboniloxi-alquilo C1-7, alquil C1-7-sulfonilo, fenilo, dicho fenilo está sin sustituir o sustituido por carboxil-alquilo C1-7 o alcoxi C1-7-carbonilo, fenilcarbonilo, dicho fenilo está sin sustituir o sustituido por carboxil-alquilo C1-7 o alcoxi C1-7-carbonilo y fenilsulfonilo, dicho fenilo está sin sustituir o sustituido por carboxil-alquilo C1-7 o alcoxi C1-7-carbonilo, o R21 y R17 juntos son -(CH2)3- y forman parte de un anillo, o R21 junto con un par de R17 y R18 son -CH=CH-CH= y forman parte de un anillo; y n es el numero 1, 2 o 3; B1 es N o N+-O; B2 es CR7 o N; R5, R6 y R7 con independencia entre sí se eligen entre el grupo formado por hidrogeno, halogeno, alquilo C1-7, alcoxi C1-7, halogeno-alquilo C1-7, halogeno-alcoxi C1-7 y ciano; y R8, R9, R10, R11 y R12 se eligen con independencia entre sí entre el grupo formado por hidrogeno, alquilo C1-7, alquenilo C2-7, alquinilo C2-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, hidroxi, hidroxi-alcoxi C1-7, hidroxi-alquilo C1-7, hidroxi-alquenilo C3-7, hidroxi-alquinilo C37, ciano, carboxilo, alcoxi C1-7-carbonilo, aminocarbonilo, carboxil-alquilo C1-7, carboxil-alquenilo C2-7, carboxil-alquinilo C2-7, alcoxi C1-7-carbonil-alquilo C1-7, alcoxi C1-7-carbonil-alquenilo C2-7, alcoxi C1-7-carbonil-alquinilo C2-7, carboxil-alcoxi C1-7, alcoxi C1-7-carbonil-alcoxi C1-7, carboxil-alquil C1-7-aminocarbonilo, carboxil-alquil C1-7-alquil C1-7-amino-carbonilo, alcoxi C1-7-carbonil-alquil C1-7-aminocarbonilo, alcoxi C1-7-carbonil-alquil C1-7-alquil C1-7-amino-carbonilo, carboxil-alquil C1-7-aminocarbonil-alquilo C1-7, carboxil-alquil C1-7-alquil C1-7-amino-carbonil-alquilo C1-7, alcoxi C1-7-carbonil-alquil C1-7-aminocarbonil-alquilo C1-7, alcoxi C1-7-carbonil-alquil C1-7-alquil C1-7-amino-carbonil-alquilo C1-7, hidroxi-alquil C1-7-aminocarbonilo, di-hidroxi-alquil C1-7-aminocarbonilo, aminocarbonil-alquil C1-7-amino-carbonilo, hidroxisulfonil-alquil C1-7-aminocarbonilo, hidroxisulfonil-alquil C1-7-alquil C1-7-amino-carbonilo, di-alcoxi C1-7-carbonil-alquil C1-7-metilaminocarbonilo, fenilo, dicho fenilo está sin sustituir o sustituido de una a tres veces por restos elegidos entre halogeno, alcoxi C1-7, carboxilo y alcoxi C1-7-carbonilo, fenil-carbonilo, dicho fenilo está sin sustituir o sustituido de una a tres veces por restos elegidos entre halogeno, alcoxi C1-7, carboxilo y alcoxi C1-7-carbonilo, fenil-aminocarbonilo, dicho fenilo está sin sustituir o sustituido de una a tres veces por restos elegidos entre halogeno, alcoxi C1-7, carboxilo y alcoxi C1-7-carbonilo, fenil-alquilo C17, dicho fenilo está sin sustituir o sustituido de una a tres veces por restos elegidos entre halogeno, alcoxi C1-7, carboxilo y alcoxi C1-7-carbonilo, fenil-alquinilo C2-7, dicho fenilo está sin sustituir o sustituido de una a tres veces por restos elegidos entre halogeno, alcoxi C1-7, carboxilo y alcoxi C1-7-carbonilo, heteroarilo, dicho heteroarilo está sin sustituir o sustituido de una a tres veces por restos elegidos entre halogeno, alcoxi C1-7, carboxilo y alcoxi C1-7-carbonilo, heteroaril-carbonilo, dicho heteroarilo está sin sustituir o sustituido de una a tres veces por restos elegidos entre halogeno, alcoxi C1-7, carboxilo y alcoxi C1-7-carbonilo, heteroaril-aminocarbonilo, dicho heteroarilo está sin sustituir o sustituido de una a tres veces por restos elegidos entre halogeno, alcoxi C1-7, carboxilo y alcoxi C1-7-carbonilo, heteroaril-alquilo C1-7, dicho heteroarilo está sin sustituir o sustituido de una a tres veces por restos elegidos entre halogeno, alquilo C1-7, alcoxi C1-7, carboxilo y alcoxi C1-7-carbonilo, heteroaril-alquil C1-7-aminocarbonilo, dicho heteroarilo está sin sustituir o sustituido de una a tres veces por restos elegidos entre halogeno, alcoxi C1-7, carboxilo y alcoxi C1-7-carbonilo y heteroaril-carbonil-alquilo C1-7, fenilo está sin sustituir o sustituido de una a tres veces por restos elegidos entre halogeno, alcoxi C1-7, carboxilo y alcoxi C1-7-carbonilo; o las sales farmacéuticamente aceptables de los mismos.
ARP110100173A 2010-01-21 2011-01-19 Compuestos de 4-- fenoxi -nicotinamida o 4- fenoxi -pirimidina - 5- carboxamida AR079938A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10151319 2010-01-21

Publications (1)

Publication Number Publication Date
AR079938A1 true AR079938A1 (es) 2012-02-29

Family

ID=43825182

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110100173A AR079938A1 (es) 2010-01-21 2011-01-19 Compuestos de 4-- fenoxi -nicotinamida o 4- fenoxi -pirimidina - 5- carboxamida

Country Status (14)

Country Link
US (2) US8420647B2 (es)
EP (1) EP2526096B1 (es)
JP (1) JP5600184B2 (es)
KR (1) KR101472647B1 (es)
CN (1) CN102712620B (es)
AR (1) AR079938A1 (es)
BR (1) BR112012018098A2 (es)
CA (1) CA2786162A1 (es)
ES (1) ES2537810T3 (es)
HK (1) HK1172018A1 (es)
MX (1) MX2012007582A (es)
RU (1) RU2565077C2 (es)
TW (1) TW201129554A (es)
WO (1) WO2011089099A1 (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102850321A (zh) * 2011-06-28 2013-01-02 中国科学院上海药物研究所 芳香氧基嘧啶甲酰胺或芳香氧基吡啶甲酰胺类化合物及其制备方法、药物组合物和用途
EP2794576A1 (en) * 2011-12-21 2014-10-29 Ardelyx, Inc. Non-systemic tgr5 agonists
WO2014117292A1 (zh) * 2013-01-31 2014-08-07 中国科学院上海药物研究所 酰胺类化合物及其制备方法、药物组合物和用途
ES2860695T3 (es) 2013-11-18 2021-10-05 Forma Therapeutics Inc Composiciones de tetrahidroquinolina como inhibidores de bromodominio BET
RU2720237C2 (ru) 2013-11-18 2020-04-28 Форма Терапеутикс, Инк. Композиции, содержащие бензопиперазин, в качестве ингибиторов бромодоменов вет
CN104181252B (zh) * 2014-09-01 2015-12-02 广东东阳光药业有限公司 一种分离检测安塞曲匹及其异构体的方法
WO2016187544A1 (en) * 2015-05-20 2016-11-24 The Regents Of The University Of Michigan Compositions and methods for treating and preventing cancer
KR101850607B1 (ko) * 2015-07-23 2018-04-19 서울대학교산학협력단 인돌리지노[3,2-ｃ]퀴놀린계 형광 프로브
KR101936054B1 (ko) 2017-06-23 2019-01-11 한국과학기술연구원 항염증 활성을 가지는 6-페녹시피리미딘 유도체, 이의 제조방법 및 이를 활성성분으로 하는 약학 조성물
EP3651752A1 (en) 2017-07-11 2020-05-20 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
CN112794844B (zh) * 2019-11-13 2023-03-21 中国科学院上海药物研究所 酯类化合物及其制备方法和应用、酯类软药

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4223465A1 (de) * 1992-07-16 1994-01-20 Bayer Ag Herbizide Mittel auf Basis von Heteroaryloxyacetamiden
JP3686718B2 (ja) 1995-12-27 2005-08-24 ポリプラスチックス株式会社 液晶性ポリマー組成物および成形体
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
BR9914091A (pt) * 1998-10-06 2001-11-27 Dainippon Pharmaceutical Co Derivados de piridina 2,3-di-substituìda, processopara preparação dos mesmos, composições dedroga contendo os mesmos e intermediários paraa preparação
MXPA01009814A (es) 1999-03-29 2002-04-24 Hoffmann La Roche Activadores de la glucoquinasa.
JP2004238361A (ja) * 2003-02-07 2004-08-26 Tosoh Corp ピリミジン−５−カルボキサミド誘導体、その中間体及びそれらの製造方法
US20040204450A1 (en) * 2003-03-28 2004-10-14 Pfizer Inc Quinoline and quinoxaline compounds
CN1795177A (zh) * 2003-03-28 2006-06-28 辉瑞产品公司 作为治疗动脉粥样硬化和肥胖症的cetp抑制剂的 1 , 2 , 4 , －取代的1，2，3，4，－四氢－和1，2二氢－喹啉以及1， 2 , 3 ， 4－四氢－喹喔啉衍生物
US7504396B2 (en) 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
GB0317472D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors
ATE490251T1 (de) 2005-06-16 2010-12-15 Janssen Pharmaceutica Nv Tricyclische opioidmodulatoren
KR20090021313A (ko) * 2006-07-17 2009-03-02 노파르티스 아게 면역조절제로서 사용하기 위한 담즙산 아미드의 술포닐아미노카르보닐 유도체
WO2008125627A1 (en) * 2007-04-13 2008-10-23 Novartis Ag Pyridazine-, pyridine- and pyrane-derivatives as gpbar1 agonisis
WO2010049302A1 (en) 2008-10-29 2010-05-06 F. Hoffmann-La Roche Ag Novel phenyl amide or pyridil amide derivatives and their use as gpbar1 agonists

Also Published As

Publication number Publication date
JP5600184B2 (ja) 2014-10-01
TW201129554A (en) 2011-09-01
HK1172018A1 (es) 2013-04-12
ES2537810T3 (es) 2015-06-12
US8420647B2 (en) 2013-04-16
KR20120097425A (ko) 2012-09-03
EP2526096A1 (en) 2012-11-28
BR112012018098A2 (pt) 2016-05-03
US20130150372A1 (en) 2013-06-13
RU2565077C2 (ru) 2015-10-20
CA2786162A1 (en) 2011-07-28
EP2526096B1 (en) 2015-04-22
KR101472647B1 (ko) 2014-12-15
JP2013517313A (ja) 2013-05-16
CN102712620A (zh) 2012-10-03
US8729091B2 (en) 2014-05-20
RU2012134093A (ru) 2014-02-27
WO2011089099A1 (en) 2011-07-28
US20110178089A1 (en) 2011-07-21
MX2012007582A (es) 2012-07-30
CN102712620B (zh) 2014-02-26

Similar Documents

Publication Publication Date Title
AR079938A1 (es) Compuestos de 4-- fenoxi -nicotinamida o 4- fenoxi -pirimidina - 5- carboxamida
AR073990A1 (es) Derivados de fenilamida y piridilamida
AR082138A1 (es) 1-hidroxiimino-3-fenil-propanos
CY1124855T1 (el) 2-(μορφολιν-4-υλ)-1,7-ναφθυριδινες
ECSP14004812A (es) Triazolopiridinas sustituidas
PE20190174A1 (es) Moduladores del receptor espiro-lactama n-metil-d-aspartato y usos de los mismos
AR082574A1 (es) Compuestos de 1,4,5,6-tetrahidro-pirimidin-2-ilamina, composiciones farmaceuticas en base al compuesto y procedimiento para la obtencion del compuesto
ECSP14013217A (es) 4-imidazopiridazin-1-il-benzamidas y 4-imidazotriazin-1-il-benzamidas como inhibidores de btk.
ECSP13013011A (es) Triazolopiridinas
CO6650348A2 (es) Triazolopiridinas sustituidas
NI201300068A (es) Moduladores del receptor de glucagón
AR087668A1 (es) Derivados de oxazina y su uso en el tratamiento de enfermedades
CL2011000378A1 (es) Uso de edta asociado a trometamina o sales de edta oftalmologicamente aceptables asociadas a trometamina, y/o uno o mas fotointensificadores escogidos entre; amarillo de acridina, amarillo de quinidina, azul de metileno, eritrosina; composicion oftalmologica.
BR112014031091A2 (pt) Derivados de piperidina para agonista de gpr119
AR100137A1 (es) Compuestos 4-amino-imidazoquinolina
ECSP12011935A (es) Triazolopiridinas
AR062357A1 (es) Derivados de fenilo, piridina y quinolina, composiciones farmaceuticas y su utilizacion como medicamentos
AR092860A1 (es) Formulacion oftalmica y metodo para mejorar la presbicia
AR093244A1 (es) Compuestos de benceno sustituidos utilizables en el tratamiento de trastornos mediados por ezh2
AR085039A1 (es) DERIVADOS DE PURINA, COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN Y SU USO EN LA PREPARACION DE MEDICAMENTOS PARA TRATAR ENFERMEDADES MODULADAS POR LA INHIBICION DE LA PI3K DE CLASE I Y/O mTOR
PA8828201A1 (es) Compuestos triazina como inhibidores mtor y quinasa p13
AR084849A1 (es) Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
AR090590A1 (es) COMPUESTOS 1,3,4-OXADIAZOL Y 1,3,4-TIADIAZOL COMO INHIBIDORES DE b-LACTAMASA
CR20130560A (es) Compuestos de bezotiazol y su uso farmacéutico
BR112014029868A2 (pt) compostos, e, composição farmacêutica

Legal Events

Date Code Title Description
FB Suspension of granting procedure