[go: up one dir, main page]

AR055212A1 - Compuestos heterociclicos como bloqueantes del canal ionico p2x7 - Google Patents

Compuestos heterociclicos como bloqueantes del canal ionico p2x7

Info

Publication number
AR055212A1
AR055212A1 ARP040102578A ARP040102578A AR055212A1 AR 055212 A1 AR055212 A1 AR 055212A1 AR P040102578 A ARP040102578 A AR P040102578A AR P040102578 A ARP040102578 A AR P040102578A AR 055212 A1 AR055212 A1 AR 055212A1
Authority
AR
Argentina
Prior art keywords
integer
alkyl
aryl
alkoxy
hydrogen
Prior art date
Application number
ARP040102578A
Other languages
English (en)
Original Assignee
Aventis Pharma 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 Aventis Pharma Inc filed Critical Aventis Pharma Inc
Publication of AR055212A1 publication Critical patent/AR055212A1/es

Links

Classifications

    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61P25/28—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
    • 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
    • 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/22—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/24—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/42—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/44—Nitrogen atoms not forming part of a nitro radical
    • C07D233/46—Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/44—Nitrogen atoms not forming part of a nitro radical
    • C07D233/48—Nitrogen atoms not forming part of a nitro radical with acyclic hydrocarbon or substituted acyclic hydrocarbon radicals, attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/10—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 carbon chain containing aromatic rings

Landscapes

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

Abstract

Métodos para preparar estos compuestos. Dichos compuestos son bloqueadores del canal ionico P2X7 y por lo tanto son utiles como agentes farmacéuticos, especialmente en el tratamiento y/o prevencion de una variedad de enfermedades que tienen un componente inflamatorio, incluyendo la enfermedad intestinal inflamatoria, artritis reumatoidea, y afecciones asociadas con el sistema nervioso central, tales como apoplejía, enfermedad de Alzheimer, etc. Reivindicacion 1: Un compuesto que incluye enantiomeros, estereoisomeros, rotomeros y tautomeros de dicho compuesto y sus sales, solvatos o derivados aceptables desde el punto de vista farmacéutico, caracterizado porque dicho compuesto tiene la estructura general que se muestra en la formula (1), en la cual: R is hidrogeno, alquilo C1-6, acilo C2-6, alcoxicarbonilo C1-6, o ariloxicarbonilo C6-12; Rl y R3 son iguales o diferentes y cada uno de se selecciona independientemente de: cicloalquilo C5-8, heterociclo, seleccionado de morfolinilo, piperidinilo, piperazinilo, pirrolidinilo, tetrahidrofuranilo, tetrahidropiranilo, tetrahidrotiofenilo o tiazolinilo, arilo, seleccionado de fenilo, bifenilo o naftilo, heteroarilo, seleccionado de benzoimidazolilo, benzofuranilo, benzoxazolilo, furanilo, imidazolilo, indolilo, isoxazolilo, isoquinolilo, isotiazolilo, oxadiazolilo, oxazolilo, pirazinilo, pirazolilo, piridilo, pirimidilo, pirrolilo, quinolilo, tetrazolilo, tiazidazolilo, tiazolilo, tienilo o triazolilo, arilalquilo C1-4, cicloalquilC5-8-alquiloC1-4, heteroarilalquilo Cl-4, donde arilo y heteroarilo son como se definieron anteriormente, y donde cicloalquilo C5-8, arilo o heteroarilo está opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo integrado por halogeno, alquilo C1-4, fluoroalquilo o fluoroalcoxi formula CnHxFy o OCnHxFy, donde n es un entero de 1 a 4, x es un entero de 0 a 8, y es un entero de 1 a 9 y suma de x e y es 2n + 1, , alcoxi C1-4, tioalquilo C1-4, hidroxi, aciloxi C1-4, nitro, amino, alquilamino C1-4, dialquilamino C1-4, aminoalquilo Cl-4, alquilaminoCl-4-alquiloCl-4, dialquilaminoCl-4-alquiloCl-4, -CN, -CO2H, -CO2-alquiloCl-4, fenilo, fenoxi y benciloxi; o R1 y R3 tomados juntos con los átomos de carbono a los cuales están unidos forman un ciclopentano, ciclohexano, cicloheptano o ciclooctano; R2 y R4 son iguales o diferentes y cada uno se selecciona independientemente de: hidrogeno, alquilo C1-6 o fluoroalquilo de formula CnHXFy, donde n es un entero de 1 a 4, x es un entero de 0 a 8, y es un entero de 1 a 9 y la suma de x e y es 2n + l; R5 es hidrogeno, cicloalquilo C3-8, alquinilo C2-4, heterociclo, seleccionado de morfolinilo, piperidinilo, piperazinilo, pirrolidinilo, piridinonilo, tetrahidrofuranilo, tetrahidropiranilo, dioxanilo, benzopiranilo, dihidrobenzodioxanilo, tetrahidrotiofenilo o tiazolinilo, arilo, seleccionado de fenilo, bifenilo, naftilo o antracenilo, heteroarilo, seleccionado de benzoimidazolilo, benzofuranilo, benzoxazolilo, furanilo, imidazolilo, indolilo, isoxazolilo, isoquinolilo, isotiazolilo, oxadiazolilo, oxazolilo, pirazinilo, pirazolilo, piridilo, pirimidilo, pirrolilo, quinolilo, tetrazolilo, tiazidazolilo, tiazolilo, tienilo o triazolilo, donde cicloalquilo C5-8, heterociclilo, arilo o heteroarilo está opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo integrado por halogeno, alquilo C1-4, fluoroalquilo fluoroalcoxi de formula CnHXFy o OCnHXFy, donde n es un entero de 1 a 4, x es un entero de 0 a 8, y es un entero de 1 a 9 y la suma de x e y es 2n + 1, alcoxi C1-4, tioalquilo C1-4, hidroxi, aciloxi C1-4, nitro, amino, alquilamino C1-4, dialquilamino Cl-4, aminoalquilo C1-4, alquilaminoC1-4-alquiloC1-4, dialquilaminoC1-4-alquiloC1-4, -CN,-CO2H, y-CO2alquiloC1-4, fenilo, fenoxi y benciloxi; X-Y es -(CH2)-Z-(CH2)b-, -(CH2)a-Z-(CH2)b-Z1- o -NHCO-, donde (CH2) está opcionalmente sustituido con uno o más grupos seleccionados independientemente de: hidroxi, alcoxi C1-6, arilaminocarboniloxi, cicloalquilo C3-8, alquilo C1-4 o fluoroalquilo de formula CnHxFy, donde n es un entero de 1 a 4, x, es un entero de 0 a 8, y es un entero de 1 a9 y la suma de x e y es 2n + 1, donde dicho alcoxi o alquilo o fluoroalquilo está opcionalmente sustituido con al menos un sustituyente seleccionado del grupo integrado por hidroxi, -SH, alcoxi C1-4, tioalquilo C1-4, aciloxi C1-4, nitro, amino, alquilamino C1-4, dialquilamino C1-4, -CN, -CO2H, y -CO2-alquiloC1-4, arilo; Z y Z1 son iguales o diferentes y cada uno se selecciona independientemente de: O, S, NR6, NR6-NR6, -OCONH-, -NH-CO-NH, -SO2-NH-, -(NR6)SO2-, o un enlace; donde R6 se selecciona de: hidrogeno, alcoxi C1-6, alquilo C1-6, o fluoroalquilo de formula CnHxFy, donde n es un entero de 1 a 4, x es un entero de 0 a 8, y es un entero de 1 a 9 y la suma de x e y es 2n + 1, donde dicho alcoxi o alquilo o fluoroalquilo está opcionalmente sustituido con al menos un sustituyente seleccionado del grupo integrado por: hidroxi, -SH, alcoxi c1-4, tioalquilo C1-4, aciloxi c1-4, nitro, amino, alquilamino C1-4, dialquilamino C1-4, -CN, -CO2H, y -CO2-alquiloC1-4, arilo; a es un entero de 0 a 2 y b es un entero de 0 a 4 siempre que la suma de a y b sea al menos 1; y con la salvedad de que: cuando X-y sea -(CH2)aZ-(CH2)b-, cuando Z sea S, R, R2, y R4 sean hidrogeno, R1 y R3 sean fenilo o p-Cl-fenilo, a sea 0 y b sea 1, R5 no sea hidrogeno o fenilo; y cuando X-Y sea -(CH2)a-Z-(CH2)b-, cuando Z sea un enlace, R, R2, y R4 sean hidrogeno, R1 y R3 sean fenilo, a sea 0 y b sea 1, R5 no sea hidrogeno.
ARP040102578A 2003-07-21 2004-07-21 Compuestos heterociclicos como bloqueantes del canal ionico p2x7 AR055212A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US48924603P 2003-07-21 2003-07-21

Publications (1)

Publication Number Publication Date
AR055212A1 true AR055212A1 (es) 2007-08-15

Family

ID=29712371

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040102578A AR055212A1 (es) 2003-07-21 2004-07-21 Compuestos heterociclicos como bloqueantes del canal ionico p2x7

Country Status (16)

Country Link
US (2) US7326792B2 (es)
EP (1) EP1651613B1 (es)
JP (1) JP2006528178A (es)
KR (1) KR20060041255A (es)
CN (1) CN1826325A (es)
AR (1) AR055212A1 (es)
AT (1) ATE469130T1 (es)
AU (1) AU2004263491A1 (es)
BR (1) BRPI0412897A (es)
CA (1) CA2532910A1 (es)
DE (1) DE602004027382D1 (es)
GB (1) GB0324498D0 (es)
IL (1) IL173146A0 (es)
MX (1) MXPA05013331A (es)
TW (1) TW200519093A (es)
WO (1) WO2005014555A1 (es)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20010001203A1 (en) * 2000-04-04 2001-05-17 Mccall Don C. Fuel dispensing system
WO2007049532A1 (ja) 2005-10-25 2007-05-03 Shionogi & Co., Ltd. アミノジヒドロチアジン誘導体
KR100694181B1 (ko) * 2005-11-25 2007-03-12 연세대학교 산학협력단 근원세포 또는 근섬유로부터 신경세포 분화를 유도하는화합물, 이를 포함하는 약학적 조성물, 신경세포 분화를유도하는 방법 및 신경세포 분화를 유도하는 화합물을검색하는 스크리닝 방법
GB0705882D0 (en) 2007-03-27 2007-05-02 Glaxo Group Ltd Novel compounds
JP2010522710A (ja) * 2007-03-29 2010-07-08 グラクソ グループ リミテッド Ｐ２ｘ７調節因子としてのオキサゾリジンおよびモルホリンカルボキサミド誘導体
BRPI0809930A2 (pt) * 2007-04-03 2014-10-07 Glaxo Group Ltd Derivados de carboxamida imidazolidina como moduladores de p2x7
TW200902526A (en) 2007-04-24 2009-01-16 Shionogi & Amp Co Ltd Aminodihydrothiazin derivative substituted with a cyclic group
JP5383483B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
EA022505B1 (ru) 2008-03-25 2016-01-29 Эффектис Фармасьютиклз Аг Новые p2x7r антагонисты и их применение
TWI431004B (zh) * 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
EP2298778A4 (en) 2008-06-12 2011-10-05 Daiichi Sankyo Co Ltd IMIDAZOTHIAZOLE DERIVATE HAVING A CYCLIC STRUCTURE OF 4,7-DIAZASPIRO®2.5OCITANE
CA2727859C (en) 2008-06-13 2016-11-01 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY
WO2010047372A1 (ja) 2008-10-22 2010-04-29 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２－アミノピリミジン－４－オンおよび２－アミノピリジン誘導体
WO2010082612A1 (ja) 2009-01-16 2010-07-22 第一三共株式会社 プロリン環構造を有するイミダゾチアゾール誘導体
DK2243772T3 (da) 2009-04-14 2012-02-13 Affectis Pharmaceuticals Ag Hidtil ukendte P2X7R-antagonister og deres anvendelse
US9914465B2 (en) * 2009-05-29 2018-03-13 L.B. Foster Rail Technologies, Inc. Top of rail resilient bar
EP2322149A1 (en) 2009-11-03 2011-05-18 Universidad del Pais Vasco Methods and compositions for the treatment of ischemia
CN102834102B (zh) 2009-12-08 2015-01-14 范德比尔特大学 用于静脉采集和自体移植的改进的方法和组合物
CA2783958A1 (en) 2009-12-11 2011-06-16 Shionogi & Co., Ltd. Oxazine derivative
WO2011091152A1 (en) * 2010-01-22 2011-07-28 Pablo Gastaminza Inhibitors of hepatitis c virus infection
WO2011109833A2 (en) 2010-03-05 2011-09-09 President And Fellows Of Harvard College Induced dendritic cell compositions and uses thereof
JP2013526496A (ja) 2010-05-14 2013-06-24 アフェクティス ファーマシューティカルズ アーゲー Ｐ２ｘ７ｒ拮抗剤の新規調製方法
WO2012007426A1 (en) 2010-07-13 2012-01-19 Basf Se Azoline substituted isoxazoline benzamide compounds for combating animal pests
US9018219B2 (en) 2010-10-29 2015-04-28 Shionogi & Co., Ltd. Fused aminodihydropyrimidine derivative
AU2011321427A1 (en) 2010-10-29 2013-05-02 Shionogi & Co., Ltd. Naphthyridine derivative
WO2012110190A1 (en) 2011-02-17 2012-08-23 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
CN103608345A (zh) 2011-04-26 2014-02-26 盐野义制药株式会社 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂
WO2012163792A1 (en) 2011-05-27 2012-12-06 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
WO2012163456A1 (en) 2011-05-27 2012-12-06 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
US9343413B2 (en) 2012-05-18 2016-05-17 Globalfoundries Singapore Pte. Ltd. ESD protection for high voltage applications
JP2016501827A (ja) 2012-10-24 2016-01-21 塩野義製薬株式会社 Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体
CN104072421B (zh) * 2014-07-14 2017-02-15 郑州大学 一种手性咪唑啉硫配体及其合成方法
CN113939521A (zh) * 2019-03-29 2022-01-14 巴黎大学 作为cxcr4调节剂的咪唑啉衍生物
WO2020227159A2 (en) 2019-05-03 2020-11-12 Flagship Pioneering Innovations V, Inc. Methods of modulating immune activity
EP3993793A4 (en) * 2019-07-01 2023-06-28 Ligang Qian P2x7r antagonists
GB201915826D0 (en) * 2019-10-31 2019-12-18 Fu Rui Chiral guanidines, methods of making chiral guanidines and uses of chiral guanidines in the preparation of enantiomerically pure amino acids
EP4334298A1 (en) 2021-06-14 2024-03-13 Scorpion Therapeutics, Inc. Urea derivatives which can be used to treat cancer

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS54112864A (en) 1978-02-22 1979-09-04 Teijin Ltd Novel imidazole derivative, its mineral acid salt, and their preparation
US4308277A (en) * 1978-08-10 1981-12-29 Ciba-Geigy Corporation 2,4,5-Trisubstituted imidazolines and pharmaceutical compositions containing same
JPH0283372A (ja) 1988-09-19 1990-03-23 Taisho Pharmaceut Co Ltd シクロヘキシルイミダゾール誘導体
US5106845A (en) * 1990-01-10 1992-04-21 Merrell Dow Pharmaceuticals Inc. Calcium antagonists
SE9704544D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
SE9704545D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
SE9704546D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
US6476233B1 (en) * 1998-11-12 2002-11-05 The Penn State Research Foundation Transition metal-catalyzed reactions based on chiral amine oxazolinyl ligands and related compounds
NZ514477A (en) 1999-04-09 2003-04-29 Astrazeneca Ab Adamantane derivatives
SE9904652D0 (sv) * 1999-12-17 1999-12-17 Astra Pharma Prod Novel Compounds
SE9904738D0 (sv) * 1999-12-22 1999-12-22 Astra Pharma Prod Novel compounds

Also Published As

Publication number Publication date
GB0324498D0 (en) 2003-11-26
IL173146A0 (en) 2006-06-11
WO2005014555A1 (en) 2005-02-17
DE602004027382D1 (de) 2010-07-08
EP1651613B1 (en) 2010-05-26
US20050026916A1 (en) 2005-02-03
EP1651613A1 (en) 2006-05-03
KR20060041255A (ko) 2006-05-11
CA2532910A1 (en) 2005-02-17
US7741493B2 (en) 2010-06-22
BRPI0412897A (pt) 2006-10-03
US7326792B2 (en) 2008-02-05
US20080132550A1 (en) 2008-06-05
CN1826325A (zh) 2006-08-30
AU2004263491A1 (en) 2005-02-17
ATE469130T1 (de) 2010-06-15
TW200519093A (en) 2005-06-16
MXPA05013331A (es) 2006-03-17
JP2006528178A (ja) 2006-12-14

Similar Documents

Publication Publication Date Title
AR055212A1 (es) Compuestos heterociclicos como bloqueantes del canal ionico p2x7
AR079689A1 (es) Derivados de imidazo[1,2a]piridina, composiciones farmaceuticas que los comprenden y uso de los mismos en trastornos mieloproliferativos, leucemia y enfermedades inmunologicas e inflamatorias.
EA201590092A1 (ru) АЗОТСОДЕРЖАЩИЕ 5-ЧЛЕННЫЕ ГЕТЕРОЦИКЛЫ, ЗАМЕЩЕННЫЕ КАРБОКСАМИДОМ ИЛИ СУЛЬФОНАМИДОМ, В КАЧЕСТВЕ МОДУЛЯТОРОВ ДЛЯ ЯДЕРНОГО ОРФАНОВОГО РЕЦЕПТОРА RORγ
EA200702200A1 (ru) Дигидротиенопиримидины для лечения воспалительных заболеваний
AR064561A1 (es) Derivados de 2-aza-biciclo[3.1.0]hexano y su uso en la preparacion de un medicamento para el tratamiento de enfermedades relacionadas con disfunciones generales del sistema de la orexina.
EA201791271A1 (ru) ТИАЗОЛЫ, ЗАМЕЩЕННЫЕ КАРБОКСАМИДОМ ИЛИ СУЛЬФОНАМИДОМ, И РОДСТВЕННЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ ДЛЯ ОРФАННОГО ЯДЕРНОГО РЕЦЕПТОРА RORγ
AR043700A1 (es) Derivados de 3-substituida-4-pirimidona
CY1118572T1 (el) Παραγωγο κυκλοαλκανιου
AR081994A1 (es) Derivados de [1,8]naftiridina, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para el tratamiento de enfermedades inducidas por quinasas, en particular diferentes tipos de canceres
AR052887A1 (es) Derivados de tiazol, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para tratar enfermedades mediadas por la inhibicion de la protein quinasa
AR054890A1 (es) Derivados de quinolina como agentes antibacterianos
RS52953B (en) PYRIDOPINIDINONSKI INHIBITORI PI3 KALFA
RU2012120288A (ru) Новые производные нафтиридина и их применение в качестве ингибиторов киназы
NO20073357L (no) 5-karboksamid substituerte tiazol derivater som reagerer med ionekanaler, i saerdeleshet med ionekanaler fra Kv familien
AR070459A1 (es) Derivados de 2-aza-biciclo- [2,2,1] heptano
AR043111A1 (es) Derivados monoacilados de o-fenilendiaminas
CO6160288A2 (es) Composiciones farmaceuticas que comprenden nilotinib o su sal
AR070502A1 (es) Derivado de sulfonilmalonamida, su uso farmaceutico y composiciones que los comprenden
AR043434A1 (es) Derivados de piperizacina acilados como agonistas del receptor de melanocortina-4. composiciones farmaceuticas y usos
AR071120A1 (es) Derivados de diosmetina, su procedimiento de preparacion, las composiciones farmaceuticas que los contienen y su uso en el tratamiento de las enfermedades venosas cronicas.
AR061792A1 (es) Derivados heterociclicos y su uso en el tratamiento o prevencion de enfermedades psiquiatricas donde se requiere un aumento de las respuestas sinapticas mediadas por receptores ampa
EA202192900A1 (ru) Модуляторы пути интегрированной реакции на стресс
BRPI0608216A2 (pt) agente terapêutico para um tumor, método para tratar um tumor, e, uso de um composto de benzoìla, uma pró-groga do mesmo ou um sal farmaceuticamente aceitável do mesmo
EA201270359A1 (ru) Терапевтическое средство от расстройств настроения
EA201070839A1 (ru) Новые производные ацилцианопирролидинов

Legal Events

Date Code Title Description
FA Abandonment or withdrawal