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    • 81. 发明授权
    • Compounds for the treatment of metabolic disorders
    • 用于治疗代谢紊乱的化合物
    • US07820721B2
    • 2010-10-26
    • US12160854
    • 2007-01-22
    • Shalini SharmaReid W. von Borstel
    • Shalini SharmaReid W. von Borstel
    • A61K31/12A61K31/075A01N35/00A01N31/14C07C49/00C07C41/00C07C43/02C07C43/20
    • C07C49/84A61K31/138C07C43/23
    • Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. wherein n is 1 or 2; m is 0, 1, 2, 3, or 4; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R3 and R4 is hydrogen or hydroxy and the other is hydrogen; or R3 and R4 together are ═O; R5 is hydrogen or alkyl having one, two, three, four or five carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon. Alternatively, the. agent can be a pharmaceutically acceptable salt of the compound of Formula I.
    • 公开了可用于治疗各种代谢紊乱(例如胰岛素抵抗综合征,糖尿病,多囊卵巢综合征,高脂血症,脂肪肝疾病,恶病质,肥胖症,动脉粥样硬化和动脉硬化)的药剂。 其中n为1或2; m为0,1,2,3或4; q为0或1; t为0或1; R1是具有1至3个碳原子的烷基; R2是氢,卤素,具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基; R3和R4之一是氢或羟基,另一个是氢; 或R3和R4一起为= O; R5是氢或具有一个,两个,三个,四个或五个碳原子的烷基; A是未取代的或被1或2个选自:卤素,羟基,具有1或2个碳原子的烷基,全氟甲基,具有1或2个碳原子的烷氧基和全氟甲氧基取代的苯基; 或具有3至6个环碳原子的环烷基,其中环烷基是未取代的或一个或两个环碳独立地被甲基或乙基单取代; 或具有1或2个选自N,S和O的环杂原子的5或6元杂芳环,杂芳环通过环碳与式I化合物的其余部分共价结合。 或者, 药剂可以是式I化合物的药学上可接受的盐。
    • 86. 发明授权
    • Chemical compounds
    • US07589123B2
    • 2009-09-15
    • US11773952
    • 2007-07-05
    • Daryl David ReesPhillip James GunningAntonia OrsiPatrick A. HowsonPaul BarracloughNoelle Callizot
    • Daryl David ReesPhillip James GunningAntonia OrsiPatrick A. HowsonPaul BarracloughNoelle Callizot
    • A61K31/12C07C49/00C07C69/78
    • A61K31/12C07C45/455C07C45/62C07C45/673C07C45/68C07C45/74C07C49/255C07C49/577C07C49/84C07C69/738C07C217/22C07C255/56C07C2601/02C07C2601/10C07C2601/14C07F7/1804Y02P20/582
    • Compounds of general formula I: wherein: R1 and R2 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, optionally substituted —CO—(C1-10alkyl), optionally substituted C3-10cycloalkyl, optionally substituted —CO—(C3-10cycloalkyl), optionally substituted C2-10alkenyl, optionally substituted —CO—(C2-10alkenyl), optionally substituted aryl, and optionally substituted —CO-aryl, or R1 and R2 together represent an optionally substituted saturated or unsaturated C1-10alkylidene group, or an optionally substituted saturated or unsaturated C3-10cycloalkylidene group, or R1 and R2 together with the carbon atom to which they are attached represent an optionally substituted saturated or unsaturated organic ring containing 3, 4, 5, 6, 7 or 8 ring carbon atoms and optionally 1, 2 or 3 ring heteroatoms selected from O, N and S; R3, which may be the same as, or different from, either of R1 and R2, is selected from optionally substituted C1-10alkyl, optionally substituted C3-10cycloalkyl, optionally substituted C2-10alkenyl, and optionally substituted aryl; R4, R5 and R6 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, OH, optionally substituted C1-10 alkoxy, halo, optionally substituted aryloxy, optionally substituted (C1-10alkyl)-S(O)n— where n=0, 1 or 2, optionally substituted aryl-S(O)n— where n=0, 1 or 2, or R4 is hydrogen and R5 and R6 together represent an optionally substituted saturated or unsaturated organic chain containing 1, 2, 3, 4, 5, 6 or 7 chain carbon atoms and optionally 1, 2 or 3 chain heteroatoms selected from O, N and S, provided that the chain is at least 3 atoms long; with the proviso that, when R1═R2=hydrogen, then any optionally substituted C1-10alkyl or optionally substituted C2-10alkenyl for R3 must have a branch point at one or more of the α and β positions counted from the carbonyl group (or tautomeric form thereof) to which R3 is attached; or a physiologically acceptable salt, complex or prodrug thereof; are disclosed per se and for use in the treatment or prophylaxis of hypersensitivity, smooth muscle disorders, spasmodic conditions, allergic conditions, inflammatory conditions and/or pain.
    • 88. 发明授权
    • Trifunctional photoinitiators
    • 三功能光引发剂
    • US07462650B2
    • 2008-12-09
    • US10552952
    • 2004-05-04
    • Reinhard H. SommerladeRinaldo HüslerStephan IlgAndré FuchsSouâd BoulmaâzJean-Luc Birbaum
    • Reinhard H. SommerladeRinaldo HüslerStephan IlgAndré FuchsSouâd BoulmaâzJean-Luc Birbaum
    • C08F2/46C07C49/00
    • G03F7/0295B33Y70/00C07C45/46C07C45/63C07C45/64C07C45/71C07C49/784C07C49/813C07C49/83C07C49/84C07C225/22C07C271/20C07C2601/14C08F2/50G03F7/029G03F7/031
    • The Invention relates to novel ketones of formulae (I) and (II) wherein R1, R2, R3 and R4 are, for example, C1-C8alkyl, R5 is, for example, hydrogen, A is CI, Br, -0-R7, —NR8R9 or —S—R16, A′ is —O—, —NH— or —NR8—, X and Y are each independently of the other —O—R10 or —N(R11)(R12), n is an integer from 1 to 10, R6 is, for example, an n-valent radical of linear or branched C2-C20alkyl the carbon chain of which may be interrupted by cyclohexanediyl, phenylene, —CH(OH)—, —C(C2H5)(CH2—CH2—OH)—, —C(CH3)(CH2—CH2—OH)—, —C(CH2—CH2—OH)2—, —N(CH3)—, —N(C2H5)—, —N(CH2—CH2—OH)—, —CO—O—, —O—CO—, —P(CH2—CH2—OH)—, —P(O)(CH2—CH2—OH)—, -0-P(O—CH2—CH2—OH)—O—, -0-P(O)(0-CH2—CH2—OH)—O—, —O-cyclohexanediyl-C(CH3)2-Cyclohexanediyl-O—, —O-phenylene-C(CH3)2-phenylene-O—, —O-phenylene-CH2-phenylene-O—, —Si(CH3)2—, -0-Si(CH3)2—O—, —O—Si(CH3)(0-CH3)—O—, —Si(CH3)(R17)—O—Si(CH3)(R18)—, 5-(2-hydroxyethyl)-[1,3,5]triazinane-2,4,6-trione-1,3-diyl and/or by from one to nine oxygen atoms.
    • 本发明涉及式(I)和(II)的新型酮,其中R 1,R 2,R 3和R 4是例如C 1 -C 8烷基,R 5是例如氢,A是Cl,Br,-O-R 7 ,-NR 8 R 9或-S-R 16,A'为-O-,-NH-或-NR 8 - ,X和Y各自独立地为O-R 10或-N(R 11)(R 12),n为 R 1为例如直链或支链C 2 -C 20烷基的n价基团,其碳链可以被环己二基,亚苯基,-CH(OH) - , - C(C 2 H 5)( CH 2 -CH 2 -OH) - , - C(CH 3)(CH 2 -CH 2 -OH) - , - C(CH 2 -CH 2 OH)2 - , - N(CH 3) - , - N(C 2 H 5) (CH2-CH2-OH) - , - CO-O - , - O-CO-,-P(CH2-CH2-OH) - ,-P(O)(CH2-CH2-OH) (O-CH 2 -CH 2 -OH)-O-,-O-P(O)(O-CH 2 -CH 2 -OH)-O-,-O-环己二基-C(CH 3)2 - 环己烷二基-O-, - O-亚苯基-C(CH 3)2 - 亚苯基-O - , - 亚苯基-CH 2 - 亚苯基-O-,-Si(CH 3)2 - , - O-Si(CH 3)2 -O-,-O- Si(CH 3)(O-CH 3)-O-,-Si(CH 3)(R 17)-O-Si(CH 3)(R 18) - ,5-(2-羟乙基) - [1,3,5] 2,4,6-三酮-1,3-二基和/或1-9个氧原子。