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    • 1. 发明公开
    • CALCIUM RECEPTOR MODULATING COMPOUND AND USE THEREOF
    • CALRIUM-REZEPTOR-MODULIERENDE VERBINDUNG UND IHRE VERWENDUNG
    • EP1572113A2
    • 2005-09-14
    • EP03793273.8
    • 2003-08-21
    • Takeda Pharmaceutical Company Limited
    • YASUMA, TsuneoMORI, AkiraKAWASE, MasahiroKIMURA, HiroyukiYOSHIDA, MasatoGYORKOS, Albert, CharlesPRATT, Scott, AlanCORRETTE, Christopher, Peter
    • A61K6/00
    • C07D487/04
    • There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7- membered ring; ring B is an optionally substituted 5- to 7- membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and --- is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7- membered ring; Q is C, CR5 or N; R8, R9,R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.
    • 提供了包含式(I)化合物的钙受体调节剂:其中环A是任选取代的5-至7-元环; 环B是任选取代的5-至7-元杂环; X1是CR1,CR1R2,N或NR13; X2为N或NR3; Y为C,CR4或N,Z为CR5,CR5R6,N或NR7; Ar是任选取代的环状基团; R为H,任选取代的烃基等; < img id =“CUSTOM-CHARACTER-00001”he =“3.13mm”wi =“8.47mm”file =“US20090215746A1-20090827-P00001.TIF”img-content =“character”img-format =“tif”/ >是单键或双键; R 1,R 2,R 3,R 4,R 5,R 6,R 7和R 13独立地为H,任选取代的烃基; 或其盐或其前药。 式(II)和(III)的化合物:其中环A是任选取代的5-至7-元环; Q为C,CR5或N; R8,R9,R10,R11和R12独立地为H,任意取代的烃基等,或其盐。 也如前所述,在式(II)和(III)中指定X1,R3,R1,Y和X3。
    • 2. 发明公开
    • FIVE-MEMBERED HETEROCYCLIC COMPOUNDS
    • F NFGLIEDRIGE HETEROCYCLISCHE VERBINDUNGEN
    • EP1541564A1
    • 2005-06-15
    • EP03795338.7
    • 2003-09-09
    • Takeda Pharmaceutical Company Limited
    • MOMOSE, YuTAKAKURA, NobuyukiMAEKAWA, TsuyoshiODAKA, HiroyukiKIMURA, Hiroyuki
    • C07D263/32C07D413/12C07D413/14C07D417/14C07D417/12C07D401/14C07D403/12C07F7/18C07F9/6558A61K31/422A61K31/4439A61K31/427A61K31/4245A61K31/454A61K31/5377A61K31/675A61K31/695A61K31/662A61P3/06A61P3/04A61P3/10
    • C07D263/32C07F9/6558C07F9/65583
    • The present invention provides a compound represented by the formula:
      wherein R 1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is -(CH 2 ) n -Z 1 - or -Z 1 -(CH 2 ) n - (n is an integer of 0 to 8, Z 1 is a bond, an oxygen atom, a sulfur atom and the like); ring B is a nitrogen-containing heterocycle optionally further having 1 to 3 substituents; W is a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R 2 is a hydrogen atom, a cyano group, -PO(OR 9 )(OR 10 ) (R 9 and R 10 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and R 9 and R 10 are optionally bonded to form an optionally substituted ring) and the like, or a salt thereof, which has a superior adipose tissue weight decreasing action, a hypoglycemic action and a hypolipidemic action, and which is useful as an agent for the prophylaxis or treatment of obesity, diabetes mellitus, hyperlipidemia, impaired glucose tolerance, hypertension and the like.
    • 本发明提供由下式表示的化合物:其中R 1为任选取代的5元杂环基; X,Y和V相同或不同,各自为键,氧原子,硫原子等; Q为碳原子数为1〜20的二价烃基; 环A是任选进一步具有1至3个取代基的芳环; Z是 - (CH 2)n Z 1 - 或-Z 1 - (CH 2)n - (n是0至8的整数,Z 1是键,氧原子,硫原子和 喜欢); 环B是任选还含有1至3个取代基的含氮杂环; W是碳原子数为1〜20的键或二价烃基; R 2是氢原子,氰基,-PO(OR 9)(OR 10)(R 9和R 10)相同或不同,各自为氢原子或 任选取代的烃基,R 9和R 10任选地键合以形成任选取代的环)等,或其盐具有优异的脂肪组织重量减轻作用,降血糖作用和降血脂症 作为预防或治疗肥胖症,糖尿病,高脂血症,葡萄糖耐量降低,高血压等的作用剂。