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    Cephalosporin derivatives
    52.
    发明授权
    Cephalosporin derivatives 失效
    CEPHALOSPORIN衍生物

    公开(公告)号：US5055572A

    公开(公告)日：1991-10-08

    申请号：US179199

    申请日：1988-04-08

    申请人： Andre Furlenmeier ,  Erwin Gotschi ,  Paul Hebeisen ,  Werner Hofheinz ,  Helmut Link

    发明人： Andre Furlenmeier ,  Erwin Gotschi ,  Paul Hebeisen ,  Werner Hofheinz ,  Helmut Link

    IPC分类号： C07D519/06 ,  A61K31/545 ,  A61P31/04 ,  C07D501/36 ,  C07D501/46 ,  C07D519/00

    CPC分类号： C07D501/36 ,  C07D519/00 ,  Y02P20/55

    摘要： Acyl derivatives of the formula ##STR1## in which R is an acyl group, excluding those acyl groups of the formula ##STR2## in which A is a group of the formulae --NHCO--, --NHCONHCO--, --NHCOCH.dbd.CH--, ##STR3## wherein R.sup.6 is hydrogen or lower alkyl; R.sup.1 and R.sup.2 are hydrogen or a protecting group, X is hydrogen, halogen, lower alkoxy, nitro or --OR.sup.2, n is 1 or 2, R.sup.4 and R.sup.5 are hydrogen or together represent an additional bond and Z is a direct bond or carbonyl (where R.sup.4 and R.sup.5 both represent hydrogen) or a group of the formula --O--B-- (where R.sup.4 and R.sup.5 together represent an additional bond) in which B is a straight-chain, branched or cyclic lower alkylene;and wherein R.sup.3 is a substituted bicyclic group of the formulae ##STR4## wherein R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl or trifluoromethyl or, in formulae (a), (b), (e) and (f) together represent alkylene with 3 or 4 carbon atoms, and R', R" and R"' are independently hydrogen, lower alkyl or lower cycloalkyl; wherein compounds of formula I in which R.sup.4 and R.sup.5 together represent an additional bond are present in the syn-isomeric form or as a mixture with the anti-isomeric form in which the syn-isomeric form predominates,as well as readily hydrolyzable esters and salts of these compounds and hydrates of the compounds of formula I or of their esters and salts.These compounds are useful as antibiotics.

    摘要翻译： 除了那些其中A是式-NHCO-，-NHCONHCO-，-NHCOCH = CH-的基团的式“IMAGE”的酰基之外，其中R是酰基的式Ⅰ的酰基衍生物， 其中R6是氢或低级烷基; R1和R2是氢或保护基，X是氢，卤素，低级烷氧基，硝基或-OR2，n是1或2，R4和R5是氢或一起代表另外的键，Z是直接键或羰基（ 其中R4和R5都表示氢）或式-BB-（其中R4和R5一起代表附加键）的基团，其中B是直链，支链或环状低级亚烷基; 并且其中R 3是下式的取代的双环基团：其中R 7和R 8独立地是氢，低级烷基或三氟甲基，或者在式（a），（b）中， ），（e）和（f）共同表示具有3或4个碳原子的亚烷基，R'，R“和R”'独立地是氢，低级烷基或低级环烷基; 其中R 4和R 5一起代表另外的键的式Ⅰ化合物以顺式异构形式存在，或作为其中顺式异构体形式占优势的抗异构体形式的混合物以及容易水解的酯和盐 的这些化合物和式I化合物的水合物或它们的酯和盐。 这些化合物可用作抗生素。

    Derivatives of 3-(2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl)-cephams
    53.
    发明授权
    Derivatives of 3-(2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl)-cephams 有权
    3-（2-氧代 - [1,3']联吡咯烷基-3-亚甲基甲基） - 头孢的衍生物

    公开(公告)号：US06232306B1

    公开(公告)日：2001-05-15

    申请号：US09332811

    申请日：1999-06-14

    申请人： Paul Hebeisen ,  Christian Hubschwerlen ,  Jean-Luc Specklin

    发明人： Paul Hebeisen ,  Christian Hubschwerlen ,  Jean-Luc Specklin

    IPC分类号： C07D50124

    CPC分类号： C07D501/00

    摘要： The present invention provides compounds of formula I wherein R1 is hydrogen, C1-6-alkyl, C1-6-alkyl substituted by fluoro, or C3-6-cycloalkyl; R2 is hydrogen or a substituent selected from the group consisting of —CH2C(═CHR)—COOR, —CH2OCOR, —CH(R)OCOR, —CH(R)OCOOR, —CH(OCOR)OCOR, —CH2COCH2OCOR and R3 is hydrogen or a substituent selected from the group consisting of —CH2C(═CH2)—COOR, —COOCH2C(═CHR)—COOR, —COOCH2OCOR, —COOCH(R)OCOR, —COOCH(R)OCOOR, —COOCH(OCOR)OCOR, —COOCH2COCH2OCOR, and  with the proviso that one of R2 and R3 is hydrogen and the other is not hydrogen, R is hydrogen or C1-6-alkyl; R4 is hydrogen or hydroxy, R5 is hydrogen or &ohgr;-hydroxyalkyl; and X is CH or N, pharmaceutically acceptable salts of the compounds and hydrates of the compounds and of their salts.

    摘要翻译： 本发明提供式I化合物，其中R 1是氢，C 1-6 - 烷基，被氟取代的C 1-6 - 烷基或C 3-6 - 环烷基; R 2是氢或选自-CH 2 C（= CHR ）-COOR，-CH 2 OCOR，-CH（R）OCOR，-CH（R）OCOOR，-CH（OCOR）OCOR，-CH 2 COCH 2 OCOR和R 3是氢或选自-CH 2 C（= CH 2）-COOR ，-COOCH 2 C（= CHR）-COOR，-COOCH 2 OCOR，-COOCH（R）OCOR，-COOCH（R）OCOOR，-COOCH（OCOR）OCOR，-COOCH 2 COCH 2 OCOR，条件是R 2和R 3之一为氢， 另一个不是氢，R是氢或C 1-6 - 烷基; R 4是氢或羟基，R 5是氢或ω-羟基烷基; 和X是CH或N，化合物及其盐的化合物和水合物的药学上可接受的盐。

    1-carba-(dethia)-cephalosporin derivatives
    55.
    发明授权
    1-carba-(dethia)-cephalosporin derivatives 失效
    1-卡巴（dethia） - 头孢菌素衍生物

    公开(公告)号：US5939410A

    公开(公告)日：1999-08-17

    申请号：US929248

    申请日：1997-09-10

    申请人： Peter Angehrn ,  Paul Hebeisen ,  Ingrid Heinze-Krauss ,  Malcolm Page

    发明人： Peter Angehrn ,  Paul Hebeisen ,  Ingrid Heinze-Krauss ,  Malcolm Page

    IPC分类号： C07D463/14 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/445 ,  A61K31/4545 ,  A61P31/04 ,  C07D463/00

    CPC分类号： C07D463/22 ,  Y02P20/55

    摘要： Compounds of formula I whereinR.sup.1 is hydrogen, lower alkyl which is unsubstituted or substituted by fluoro, aralkyl, cycloalkyl, --COR.sup.4 or --C(R.sup.5 R.sup.6)CO.sub.2 R.sup.7 --C(R.sup.5 R.sup.6)CONHR.sup.7 ; where R.sup.5 and R.sup.6 are each independently hydrogen or lower alkyl, or R.sup.5 and R.sup.6 taken together form a cycloalkyl group; R.sup.4 is hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group;R.sup.2 is hydrogen, hydroxy, lower alkyl-Q.sub.m, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl-Q.sub.m, aryl-Q.sub.m, aryloxy, aralkoxy, a heterocyclic ring or heterocyclyl lower alkyl, the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic ring being unsubstituted or substituted with at least one group selected from carboxy, amino, nitro, cyano, lower alkyl which is unsubstituted or substituted by fluoro, lower alkoxy, hydroxy, halogen, --COR.sup.6, --C(R.sup.5 R.sup.6)CO.sub.2 R.sup.7, --C(R.sup.5 R.sup.6)CONR.sup.5 R.sup.8, --CONR.sup.5 R.sup.6, --N(R.sup.6)COOR.sup.10, R.sup.6 OCO-- or R.sup.6 COO-- where R.sup.5 and R.sup.6 are hydrogen or lower alkyl; R.sup.7 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group; R.sup.8 is hydrogen, lower alkyl or phenyl which is unsubstituted or substituted with at least one halogen, hydroxy, amino, lower alkyl, or lower alkoxy; R.sup.10 is lower alkyl, lower alkenyl or a carboxylic acid protecting group;Q is --CHR--, --CO-- or --SO.sub.2 --;R is hydrogen or lower alkyl;R.sup.3 is hydroxy, --O--, lower alkoxy, --OM and M represents an alkali metal;m is 0 or 1;n is 0, 1 or 2;x is CH or Nas well as readily hydrolysable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts are provided. These compounds have valuable antiinfective properties.

    摘要翻译： 式I化合物，其中R 1是氢，未被取代或被氟取代的低级烷基，芳烷基，环烷基，-COR 4或-C（R 5 R 6）CO 2 R 7 -C（R 5 R 6）CONHR 7; 其中R 5和R 6各自独立地为氢或低级烷基，或者R 5和R 6一起形成环烷基; R4是氢或低级烷基，R7是氢，低级烷基，低级烯基或羧酸保护基; R2是氢，羟基，低级烷基-Qm，环烷基，低级烷氧基，低级烯基，环烯基，低级炔基，芳烷基-Qm，芳基-Qm，芳氧基，芳烷氧基，杂环或杂环基低级烷基，低级烷基，环烷基， 低级烷氧基，低级烯基，环烯基，低级炔基，芳烷基，芳基，芳氧基，芳烷氧基，杂环是未取代的或被至少一个选自羧基，氨基，硝基，氰基，未被取代或被氟取代的低级烷基 ，低级烷氧基，羟基，卤素，-COR6，-C（R5R6）CO2R7，-C（R5R6）CONR5R8，-CONR5R6，-N（R6）COOR10，R6OCO-或R6COO-，其中R5和R6是氢或低级烷基; R7是氢，低级烷基，低级烯基或羧酸保护基; R8是氢，低级烷基或未取代的或被至少一个卤素，羟基，氨基，低级烷基或低级烷氧基取代的苯基; R 10为低级烷基，低级烯基或羧酸保护基; Q是-CHR-，-CO-或-SO 2 - ; R是氢或低级烷基; R3是羟基，-O-，低级烷氧基，-OM，M代表碱金属; m为0或1; n为0,1或2; x是CH或N，以及其易水解的酯，所述化合物的药学上可接受的盐和式I化合物的水合物及其酯和盐。 这些化合物具有有价值的抗感染性。

    Process for the preparation of DNA gyrase inhibitors
    56.
    发明授权
    Process for the preparation of DNA gyrase inhibitors 失效
    DNA促旋酶抑制剂的制备方法

    公开(公告)号：US5486466A

    公开(公告)日：1996-01-23

    申请号：US339442

    申请日：1994-11-14

    申请人： Mikio Arisawa ,  Erwin Gotschi ,  Paul Hebeisen ,  Tsutomu Kamiyama ,  Helmut Link ,  Raffaello Masciadri ,  Hisao Shimada ,  Junko Watanabe

    发明人： Mikio Arisawa ,  Erwin Gotschi ,  Paul Hebeisen ,  Tsutomu Kamiyama ,  Helmut Link ,  Raffaello Masciadri ,  Hisao Shimada ,  Junko Watanabe

    IPC分类号： A61K31/395 ,  A61K31/42 ,  A61K31/425 ,  A61K38/00 ,  A61P31/04 ,  C07C317/24 ,  C07C317/28 ,  C07C317/46 ,  C07C317/48 ,  C07C323/56 ,  C07C323/58 ,  C07C323/64 ,  C07D291/08 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D419/04 ,  C07D419/12 ,  C07K5/02 ,  C07K5/078 ,  C07K5/097 ,  C07K5/103 ,  C07K7/06 ,  C12P13/04 ,  C12N1/20

    CPC分类号： C07D419/04 ,  C07D291/08 ,  C07K5/0202 ,  C07K5/06139 ,  C07K5/0821 ,  C07K5/1008 ,  C07K7/06 ,  A61K38/00 ,  Y10S435/886

    摘要： Bicyclic derivatives of the general formula ##STR1## wherein X.sup.1 is --S-- or --SO--;X.sup.2 is --CO-- or --CS--;R.sup.1 is hydrogen, halogen or lower alkyl optionally substituted by halogen or lower alkoxy;R.sup.2 and R.sup.3 are each independently hydrogen, lower alkyl, halogen, amino, lower alkylamino, di-lower alkylamino, acylamino, lower alkexy, lower alkoxymethoxy or a group OR.sup.4 ;R.sup.4 is hydrogen or an easily hydrolyzable group;R.sup.5 is hydrogen, optionally esterified carboxy or amidated (thio)carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted acyl or heterocyclyl;R.sup.6 and R.sup.7a are each independently hydrogen or lower alkyl;R.sup.7b is hydrogen, optionally substituted hydroxy, --NR--A or --N.dbd.B, in which R is hydrogen or lower alkyl, A is hydrogen, optionally substituted alkyl, lower cycloalkyl, iminoyl, (thio)acyl, esterified carboxy or amidated (thio)carboxy and B is lower alkylidene;R.sup.7a and R.sup.7b together represent oxo, lower alkoxycarbonylmethylidene or optionally substituted hydroxyimino; andR.sup.8 is hydrogen, optionally substituted alkyl, optionally esterified carboxy or amidated (thio)carboxy; provided that no more than two of R.sup.1 -R.sup.3 are nitrogen-containing groups; no more than two of R.sup.1 -R.sup.3 are oxygen containing groups and no more than two of R.sup.1 -R.sup.3 are either nitrogen containing or oxygen containing groups;and pharmaceutically acceptable salts of the compounds of formula I carrying an acidic and/or basic substituent.The products are antimicrobially active.

    摘要翻译： 通式为其中X 1为-S-或-SO-的通式为其的双环衍生物; X2是-CO-或-CS-; R 1为氢，卤素或任选被卤素或低级烷氧基取代的低级烷基; R2和R3各自独立地为氢，低级烷基，卤素，氨基，低级烷基氨基，二低级烷基氨基，酰氨基，低级烷基，低级烷氧基甲氧基或基团OR4; R4是氢或易水解基团; R 5为氢，任选酯化的羧基或酰胺基（硫代）羧基，任选取代的烷基，任选取代的烯基，任选取代的酰基或杂环基; R6和R7a各自独立地为氢或低级烷基; R7b是氢，任选取代的羟基，-NR-A或-N = B，其中R是氢或低级烷基，A是氢，任选取代的烷基，低级环烷基，亚氨酰基，（硫代）酰基，酯化的羧基或酰胺基（ 硫代）羧基，B是低级亚烷基; R7a和R7b一起代表氧代，低级烷氧基羰基亚甲基或任选取代的羟基亚氨基; 和R 8是氢，任选取代的烷基，任选酯化的羧基或酰胺基（硫代）羧基; 条件是R1-R3中不超过两个为含氮基团; R1-R3中不超过两个为含氧基团，R1-R3中不超过两个为含氮基团或含氧基团; 和具有酸性和/或碱性取代基的式I化合物的药学上可接受的盐。 该产品具有抗微生物活性。

    Process for producing allyl aminothiazole acetate intermediates
    57.
    发明授权
    Process for producing allyl aminothiazole acetate intermediates 失效
    制备烯丙基氨基噻唑乙酸酯中间体的方法

    公开(公告)号：US4888429A

    公开(公告)日：1989-12-19

    申请号：US258062

    申请日：1988-10-17

    申请人： Paul Hebeisen

    发明人： Paul Hebeisen

    IPC分类号： C07D499/04 ,  C07D205/08 ,  C07D277/20 ,  C07D277/32 ,  C07D277/40 ,  C07D417/12 ,  C07D499/10 ,  C07D499/64 ,  C07D499/70 ,  C07D501/04 ,  C07D501/20

    CPC分类号： C07D277/587 ,  C07D417/12

    摘要： There is described a process for the manufacture of a compound of the formula ##STR1## wherein R.sup.1 is lower alkyl, lower alkanoyl, lower alkenyl or the group --CH.sub.2 COOR.sup.2 or --C(CH.sub.3).sub.2 COOR.sup.2 and R.sup.2 is a readily cleavable group, by reacting a compound of the formula ##STR2## wherein R is lower alkyl, with an alkali metal allylate and reacting the resulting compound of the formula ##STR3## wherein M is an alkali metal atom, with a compound of the formula R.sup.1 -X, wherein X is a leaving group. This process can be used to manufacture antimicrobially active mono-.beta.-lactam, cephalosporin and penicillin derivatives.

    摘要翻译： 描述了制备式IV的化合物的方法，其中R 1是低级烷基，低级烷酰基，低级烯基或基团-CH 2 COOR 2或-C（CH 3）2 COOR 2，并且R 2是容易切割的基团，通过 使其中R为低级烷基的式II化合物与碱金属烯丙基酯反应，并使所得的其中M为碱金属原子的式I化合物与式R1-X的化合物 ，其中X是离去基团。 该方法可用于制备抗微生物活性单β-内酰胺，头孢菌素和青霉素衍生物。

    Aza- indolyl derivatives for treating obesity
    59.
    发明授权
    Aza- indolyl derivatives for treating obesity 失效
    用于治疗肥胖症的氮杂吲哚基衍生物

    公开(公告)号：US06583134B2

    公开(公告)日：2003-06-24

    申请号：US09794491

    申请日：2001-02-27

    申请人： Jonathan Mark Bentley ,  Paul Hebeisen ,  Sven Taylor

    发明人： Jonathan Mark Bentley ,  Paul Hebeisen ,  Sven Taylor

    IPC分类号： A61K3155

    CPC分类号： C07D471/14 ,  C07D487/14

    摘要： Novel compounds of formula (I): wherein X1, X2, X3 and X4, n, R1, R2 and R3 are defined in the specification, and pharmaceutically acceptable salts and prodrugs of the compounds of formula (I) have therapeutic uses. These compounds are useful for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea. They are particularly useful for the treatment of obesity.

    摘要翻译： 式（I）的新型化合物：其中X 1，X 2，X 3和X 4，n，R 1，R 2和R 3在说明书中定义，并且式（I）化合物的药学上可接受的盐和前药具有治疗用途。 这些化合物可用于治疗中枢神经系统疾病; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症和睡眠呼吸暂停。 它们对治疗肥胖特别有用。