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    • 1. 发明申请
    • METHOD AND APPARATUS FOR PRODUCING HEAT ENERGY AND CARBON DIOXIDE
    • 生产热能和二氧化碳的方法和装置
    • WO2010117323A1
    • 2010-10-14
    • PCT/SE2010/050375
    • 2010-04-06
    • ASTRAZENECA ABBOSTRÖM, JonasCHENG, LeifengFEX, TomasKARLE, MichaelPETTERSEN, DanielSCHELL, Peter
    • BOSTRÖM, JonasCHENG, LeifengFEX, TomasKARLE, MichaelPETTERSEN, DanielSCHELL, Peter
    • C07D413/04A61K31/4523A61P7/04
    • C07D413/04
    • Formula I or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.
    • 式I或其药学上合适的盐,其中R 1和R 2独立地是氢,氘,芳基,杂芳基,任选被一个或多个取代基独立地被R 3取代的C 1 -C 8烷基,R 3是芳基,杂芳基, 氟,含有一个或多个氟的C 1 -C 6烷基,含有一个或多个氘的C 1 -C 6烷基,含羟基的C 1 -C 6烷基,任选被一个或多个卤素取代的芳基和杂芳基,氟化 烷氧基,氟化烷基,磺酰基,一个或多个氘,C 1-6烷基,C 1-6烷氧基,腈或R 3是任选被一个或多个下列基团取代的C 1-6烷基:COOR 4, OCOR4,CONR5R6,NR5COR6,OR4; 其中,R4为任选被一个或多个氟,氘,烷氧基,芳基羧酸酯,羧酸烷基酯取代的C 1-10烷基; R 5和R 6独立地选自氢,烷基或它们可以一起形成4-8元碳环; 或R 1和R 2形成任选地包含O或N并任选被C 1-10烷基或芳基取代的3-10元碳环,任选被R 3取代的杂芳基。
    • 5. 发明申请
    • PYRAZOLE DERIVATIVES AS CBl MODULATORS
    • 作为CBI调节剂的吡唑衍生物
    • WO2007010217A1
    • 2007-01-25
    • PCT/GB2006/002631
    • 2006-07-17
    • ASTRAZENECA ABASTRAZENECA UK LIMITEDCHENG, LeifengJONFORSEN, MariaSCHELL, Peter
    • CHENG, LeifengJONFORSEN, MariaSCHELL, Peter
    • C07D401/12C07D231/14A61P3/04A61P25/28A61P25/18
    • C07D231/14C07D401/12
    • The present invention relates to compounds of formula (I) wherein R 1 represents a group R 5 O- in which R 5 represents a C 3-7 alkyl group substituted by one or more fluoro or R 5 represents a C 3-7 alkylsulphonyl group which is optionally substituted by one or more fluoro; R 2 represents a C 1-4 alkyl group, hydroxy, fluoro, chloro or cyano wherein each R 2 is independently selected when n is >1; R 3 represents a) cyclohexyl optionally substituted by one or more of the following: hydroxy, fluoro, amino, mono or diC 1-3 alkylamino, carboxy or a C 1-4 alkoxycarbonyl group b) piperidino substituted by one or more hydroxy c) unsubstituted piperidino but only when one of the following applies: R 4 represents cyano or R 1 represents 3-fluoropropylsulphonyloxy or R 1 represents 3,3,3-trifluoropropoxy or R 1 represents 3-fluoropropoxy or R 2 is methyl d) phenyl substituted by one or more of the following: hydroxy, halo or a C 1-4 alkyl group e) pyridyl substituted by a C 1-4 alkyl group or f) a C 4-9 alkyl group; R 4 represents cyano or methyl; and n is 1, 2 or 3 and pharmaceutically acceptable salts thereof and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    • 本发明涉及式(I)的化合物,其中R 1表示基团R 5 O,其中R 5表示C 1〜 被一个或多个氟或R 5取代的C 3-7烷基表示任选被一个或多个氟取代的C 3-7烷基磺酰基 氟; R 2表示C 1-4烷基,羟基,氟,氯或氰基,其中当n是>时独立地选择每个R 2, 1; R 3表示a)任选被以下一个或多个取代的环己基:羟基,氟,氨基,单或二-C 1-3烷基氨基,羧基或C 代表3-氟丙基磺酰氧基或R 1代表3,3,3-三氟丙氧基或R 1代表3-氟丙氧基或R 2是 甲基d)被一个或多个下列基团取代的苯基:羟基,卤素或C 1-4烷基; e)被C 1-4烷基取代的吡啶基 或f)C 4-9烷基; R 4表示氰基或甲基; 和n为1,2或3及其药学上可接受的盐及其制备方法,它们在治疗肥胖症,精神病学和神经障碍中的应用,以及其治疗用途的方法和含有它们的药物组合物。