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    • 5. 发明申请
    • NOVEL USE OF ORGANIC COMPOUNDS
    • 有机化合物的新用途
    • WO2007134867A2
    • 2007-11-29
    • PCT/EP2007004627
    • 2007-05-24
    • DSM IP ASSETS BVD ORAZIO DANIELRAEDERSTORFF DANIELSCHUELER GOEDEWANG-SCHMIDT YINGWERTZ KARINWOLFRAM SWEN
    • D ORAZIO DANIELRAEDERSTORFF DANIELSCHUELER GOEDEWANG-SCHMIDT YINGWERTZ KARINWOLFRAM SWEN
    • A61P21/00A23L1/30A61K31/12A61K31/166A61K31/352A61P1/00A61P9/00A61P9/10A61P19/02
    • A23K20/111A23L2/52A23L33/10A23V2002/00A61K31/12A61K31/166A61K31/352A23V2200/316A23V2200/328A23V2200/326A23V2200/318A23V2200/32
    • The present invention refers to compounds of the general formulae Ia to Ie as defined above for use as/in a composition (especially foods and dietary supplements, cosmetic, as well as pharmaceutical compositions) for the prevention and improvement of muscular disorders and for the improvement of muscle function. Other fields of use are disorders connected to impaired lipid metabolism, impaired glucose metabolism and impaired insulin action, obesity, overweight conditions, eating disorders such as bulimia and anorexia nervosa, cardiovascular diseases, atherosclerosis, vascular diseases, heart failure, inflammatory disorders such as arthritis, rheumatoid arthritis, osteoarthritis, gout, gastrointestinal disorders such as inflammatory bowel syndrome, Crohn's disease, gastritis, irritable bowel syndrome and ulcerative colitis, skin related conditions such as psoriasis, eczema, burns, dermatitis, and allergy,, respiratory disorders such as asthma, chronic obstructive pulmonary disease (COPD), allergic diseases, and/or bone disorders such as osteoporosis and osteopenia. The compounds may also be used for bodyshaping, for improving the muscle : fat ratio or for accelerating skin wound healing. The present invention is also directed to dietary compositions such as (fortified) food, beverages, (fortified) feed, food additives, beverage additives, feed additives, clinical nutrition, dietary supplements, functional food, functional feed and nutraceuticals and to pharmaceutical compositions containing such compounds, to methods of treating the above mentioned disorders/diseases in mammals including humans and to the compounds of the formula I themselves. Another object of the present invention is the use of such compounds for the manufacture of a composition for the treatment of such disorders/diseases as mentioned above.
    • 本发明涉及如上定义的用于预防和改善肌肉疾病和改善的组合物(特别是食品和膳食补充剂,化妆品以及药物组合物)中的上述通式Ia至Ie的化合物 的肌肉功能。 其他使用领域是与脂质代谢受损,葡萄糖代谢受损和胰岛素作用受损,肥胖症,超重症状,进食障碍如贪食症和神经性厌食症,心血管疾病,动脉粥样硬化,血管疾病,心力衰竭,炎症性疾病如关节炎相关的疾病 ,类风湿性关节炎,骨关节炎,痛风,胃肠道疾病如肠炎综合征,克罗恩病,胃炎,肠易激综合征和溃疡性结肠炎,皮肤相关病症如牛皮癣,湿疹,烧伤,皮炎和过敏,呼吸系统疾病如哮喘 ,慢性阻塞性肺疾病(COPD),过敏性疾病和/或骨骼疾病如骨质疏松症和骨质减少。 这些化合物也可用于体脂整形,用于改善肌肉:脂肪比例或用于加速皮肤伤口愈合。 本发明还涉及饮食组合物,例如(强化)食品,饮料,(强化)饲料,食品添加剂,饮料添加剂,饲料添加剂,临床营养,膳食补充剂,功能性食品,功能性饲料和营养食品,以及含有 这些化合物,涉及治疗哺乳动物(包括人)和式I本身化合物的上述疾病/疾病的方法。 本发明的另一个目的是使用这些化合物来制备用于治疗如上所述的这种疾病/疾病的组合物。
    • 6. 发明申请
    • LIGUSTILIDE DERIVATIVES FOR THE TREATMENT OF DISORDERS OF THE CENTRAL NERVOUS SYSTEM
    • 用于治疗中枢神经系统疾病的LIGESTILIDE衍生物
    • WO2008017491A8
    • 2009-05-07
    • PCT/EP2007007086
    • 2007-08-10
    • DSM IP ASSETS BVDE SAIZIEU ANTOINEGORALCZYK REGINASCHUELER GOEDE
    • DE SAIZIEU ANTOINEGORALCZYK REGINASCHUELER GOEDE
    • A61K31/343A61P25/22A61P25/24
    • A61K31/343
    • The present invention refers to compounds of the general formula (I) wherein R1 is hydrogen or hydroxy; R2 is butyl or butyryl if R1 is hydroxy, but R2 is butyl if R1 is hydrogen; or R1 and R2 taken together are 1-propylidene or 1-butylidene optionally substituted by hydroxy, methyl, or 3-(a,ß-dimethylacryloyloxy); the dotted line is an optional bond; X is an optionally substituted aliphatic C4- residue selected from the group consisting of X1, X2, X3, X4, and X5; wherein X is X2, X3 or X5 if the dotted line in formula (I) is absent; and X is Xl, X4 or X5 if the dotted line signifies a bond in formula (I) above; R3 and R4 are, independently from each other, hydrogen or hydroxy; and R5 is hydroxy or butyryl, for use in the treatment of disorders connected to impaired neurotransmission, as well as to dietary and pharmaceutical compositions containing such compounds, and their uses.
    • 本发明涉及通式(I)的化合物,其中R 1是氢或羟基; 如果R 1是羟基,则R 2是丁基或丁酰基,但如果R 1是氢,则R 2是丁基; 或R 1和R 2一起为1-羟基,甲基或3-(a,β-二甲基丙烯酰氧基)任意取代的1-亚丙基或1-亚丁基; 虚线是可选的键; X是选自X 1,X 2,X 3,X 4和X 5的任选取代的脂族C 4 - 残基; 其中如果式(I)中的虚线不存在,X是X 2,X 3或X 5; 如果虚线表示上述式(I)中的键,X为X 1,X 4或X 5; R 3和R 4彼此独立地为氢或羟基; 和R5是羟基或丁酰基,用于治疗与受损的神经传递相关的疾病,以及含有这些化合物的饮食和药物组合物及其用途。
    • 7. 发明申请
    • NOVEL USE OF ORGANIC COMPOUNDS
    • 有机化合物的新用途
    • WO2006125651A2
    • 2006-11-30
    • PCT/EP2006005005
    • 2006-05-24
    • DSM IP ASSETS BVFOWLER ANNRAEDERSTORFF DANIELSCHUELER GOEDESCHWAGER JOSEPH
    • FOWLER ANNRAEDERSTORFF DANIELSCHUELER GOEDESCHWAGER JOSEPH
    • A61K31/343A61P11/00A61P19/02A61P19/06A61P29/00
    • A61K31/343
    • The present invention relates to the use of compounds of the formula (I) wherein the clotted line is an optional bond; R 1 is butyl or butyryl if R 2 is hydroxyl but is butyl if R 2 is hydrogen; or R 1 and R 2 taken together are 1-butylidene optionally substituted by hydroxyl, methyl, or 3- (a,ß-dimethylacrylyloxy)-pentylidenyl; X is a residue selected from the group consisting of X1 , X2, X3, X4, and X5; wherein X is X2, X3or X5 if the dotted line in formula (I) is absent ;and X is X1 , X4 or X5 if the dotted line signifies a bond in formula (I) above; R 3 is hydroxyl or butyryl; and n is 1 or 2, as agents for the prevention, control and treatment of conditions requiring modulation of inflammation in mammals. In another aspect, the present invention relates to the use of compounds of the formula (I) as active ingredients in the manufacture of medicaments/compositions for the prevention, control and treatment of conditions requiring modulation of inflammation. The compounds of formula (I) as defined above may also be useful (for the manufacture of a composition) for the management of pain, fever and injuries, especially sport injuries. Moreover, the compounds of formula (I) as defined above may also be useful (for the manufacture of a composition) for the maintenance and regeneration of articular cartilage.
    • 本发明涉及式(I)化合物的用途,其中凝血线是任选的键; 如果R 2是羟基,则R 1是丁基或丁酰基,如果R 2是氢,则是丁基; 或R 1和R 2一起是任选被羟基,甲基或3-(a,β-二甲基丙烯酰氧基) - 戊酰基取代的1-亚丁基; X是选自X1,X2,X3,X4和X5的残基; 其中,如果不存在式(I)中的虚线,X为X 2,X 3或X 5;如果虚线表示上述式(I)中的键,X为X 1,X 4或X 5; R 3是羟基或丁酰基; 和n为1或2,作为预防,控制和治疗需要调节哺乳动物炎症的病症的药剂。 另一方面,本发明涉及式(I)化合物作为活性成分在制备用于预防,控制和治疗需要调节炎症的病症的药物/组合物中的用途。 如上定义的式(I)化合物也可用于治疗疼痛,发烧和损伤,特别是运动损伤(用于制造组合物)。 此外,如上定义的式(I)化合物也可用于维持和再生关节软骨(用于制备组合物)。