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    Novel organic trithio oxides and method for the preparation thereof
    1.
    发明授权
    Novel organic trithio oxides and method for the preparation thereof 失效
    新型有机三氧化硫及其制备方法

    公开(公告)号：US4643994A

    公开(公告)日：1987-02-17

    申请号：US682435

    申请日：1984-12-17

    Applicant: Eric Block ,  Saleem Ahmad

    Inventor： Eric Block ,  Saleem Ahmad

    IPC: A61K31/095 ,  A61K31/105 ,  C07C323/65 ,  C07C381/00 ,  C07C381/04 ,  A61K31/60 ,  C07C149/12

    CPC classification number: A61K31/095 ,  A61K31/105 ,  C07C323/65 ,  C07C381/00 ,  C07C381/04

    Abstract: This invention relates to novel organic trithio oxides of the formula:R.sup.1 --X --R--X.sup.1 --R.sup.1wherein R is selected from --CH.sub.2 CH.dbd.CH--, ##STR1## and (CH.sub.2).sub.3 ; X is selected from ##STR2## X.sup.1 is selected from --S--S, ##STR3## and, each R.sup.1 is independently selected from carboxyalkyl, alkoxy, alkylthio, amino, alkylamino and acyl substituted and unsubstituted lower alkyl, lower alkenyl, lower alkynyl, phenyl and lower alkylphenyl; provided when R is --CH.sub.2 CH.dbd.CH--, X is ##STR4## and X.sup.1 is --S--S--, then R.sup.1 is not in both instances --CH.sub.2 CH.dbd.CH.sub.2.This invention also relates to a method of preparing the above-identified compounds by heating and further oxidizing various oxides of organic disulfides and to antithrombotic uses of the compounds.

    Abstract translation: 本发明涉及下式的新型有机三氧化硫：R1-X-R-X1-R1其中R选自-CH2CH = CH-，和（CH2）3; X选自，X 1选自-SS，，每个R 1独立地选自羧基烷基，烷氧基，烷硫基，氨基，烷基氨基和酰基取代和未取代的低级烷基，低级烯基，低级炔基，苯基和 低级烷基苯基; 当R是-CH 2 CH = CH-，X是X，且X 1是-S-S-时，则R 2不在两个实例-CH 2 CH = CH 2中。 本发明还涉及通过加热和进一步氧化各种有机二硫化物的氧化物和化合物的抗血栓形成方法来制备上述化合物的方法。

    Dihydroquinazolinones as 5HT modulators
    5.
    发明申请
    Dihydroquinazolinones as 5HT modulators 有权
    二氢喹唑啉酮作为5HT调节剂

    公开(公告)号：US20060178386A1

    公开(公告)日：2006-08-10

    申请号：US11350997

    申请日：2006-02-09

    Applicant: Saleem Ahmad ,  Khehyong Ngu

    Inventor： Saleem Ahmad ,  Khehyong Ngu

    IPC: A61K31/519 ,  C07D487/14

    CPC classification number: C07D487/04

    Abstract: The present application provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.

    Abstract translation: 本申请提供5-羟色胺受体的调节剂，含有这种调节剂的药物组合物和用于治疗与调节血清素受体相关的各种疾病，病症和病症的方法，所述调节剂包括但不限于肥胖，糖尿病， 糖尿病并发症，动脉粥样硬化，葡萄糖耐量异常和血脂异常; 包括但不限于焦虑，抑郁，强迫症，惊恐障碍，精神病，精神分裂症，睡眠障碍，性障碍和社交恐惧症的中枢神经系统疾病; 头痛 偏头痛 和使用这些化合物和组合物的胃肠道疾病。

    Pyrrolo(oxo)isoquinolines as 5HT ligands
    6.
    发明申请
    Pyrrolo(oxo)isoquinolines as 5HT ligands 有权
    吡咯（氧代）异喹啉作为5HT配体

    公开(公告)号：US20060014777A1

    公开(公告)日：2006-01-19

    申请号：US11180268

    申请日：2005-07-13

    Applicant: John Fevig ,  Jianxin Feng ,  Saleem Ahmad

    Inventor： John Fevig ,  Jianxin Feng ,  Saleem Ahmad

    IPC: A61K31/4745 ,  C07D471/02

    CPC classification number: C07D471/04

    Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions, comprising at least one compound according to Formula I and optionally at least one additional therapeutic agent and methods of treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using compounds according to Formula I or pharmaceutically acceptable salt forms thereof, wherein A, B, D, E, m, n, R3, R7, R8, R9, R10, R11 and X are described herein.

    Abstract translation: 本申请描述了根据式I的化合物，药物组合物，其包含至少一种根据式I的化合物和任选的至少一种另外的治疗剂和治疗与调节血清素受体相关的各种疾病，病症和病症的方法，例如 糖尿病并发症，动脉粥样硬化，葡萄糖耐量异常和血脂异常等代谢疾病，包括但不限于肥胖，糖尿病，糖尿病并发症，动脉粥样硬化， 包括但不限于焦虑，抑郁，强迫症，惊恐障碍，精神病，精神分裂症，睡眠障碍，性障碍和社交恐惧症的中枢神经系统疾病; 头痛 偏头痛 和使用根据式I的化合物或其药学上可接受的盐形式的胃肠道疾病，其中A，B，D，E，m，n，R 3，R 7，R 本文描述了本发明的第8，第9，第十十，第十一和第十七和第十七。

    Lactam derivatives as antiarrhythmic agents
    8.
    发明授权
    Lactam derivatives as antiarrhythmic agents 有权
    内酰胺衍生物作为抗心律失常药

    公开(公告)号：US06664250B2

    公开(公告)日：2003-12-16

    申请号：US10267466

    申请日：2002-10-09

    Applicant: Karnail S. Atwal ,  Saleem Ahmad ,  Francis N. Ferrara

    Inventor： Karnail S. Atwal ,  Saleem Ahmad ,  Francis N. Ferrara

    IPC: C07D48700

    CPC classification number: C07D223/16 ,  A61K31/472 ,  A61K31/4725 ,  C07D217/24

    Abstract: Lactam derivatives of the formula where X is —C(═O)NR3′—, —NR3′C(═O)—, —C(═NCN)NR3′—, —NR3′C(═NCN)—, —CH2NR3′—, —CH(alkyl)NR3′—, —CH(COOalkyl)NR3′—, —CH(CH2OH)NR3′—, —C(CH2Oalkyl)—; R1 is halo, alkyl, cycloalkyl, alkyl(cycloalkyl), aryl, (aryl)alkyl, (aryl)alkenyl, (aryl)alkynyl, O-alkyl, O-alkenyl, O-aryl, O-alky(aryl), O-alkyl(heterocyclo), COO-alkyl, C)-alkyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(aryl), NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(aryl), N(alkyl)CO-alkyl(heterocyclo); R2 is hydrogen, alkyl, halo, aryl, (aryl)alkyl, O-alkyl, amino, substituted amino; R3 and R3′ are the same or different and are independently selected from hydrogen, alkyl or alkyl(aryl); R4 which can be bonded to a ring carbon or nitrogen, is selected from hydrogen, alkyl, alkenyl, alky(aryl), alkyl(heterocyclo), cycloalkyl, alkyl(cycloalkyl), alkyl-(amino), alkyl-(substituted amino), alkyl-NHCO(alkyl), alkyl-NHCO(aryl), alkyl-NHCO(heterocyclo), alkyl-NHCO(alkylaryl), alkyl-NHCO(alkylheterocyclo); and n is an integer of 0 to 2. These compounds have been found to be useful in the treatment of arrhythmia.

    Abstract translation: 式（2）的内酰胺衍生物是-C（= O）NR 3 - ，-NR 3 C（= O） - ， - C（= NCN）NR 3 - C（= NCN） - ， - CH 2 NR 3 - ， - CH（烷基）NR 3 - ， - CH（COO烷基）NR 3 - ， - CH（CH 2 OH）NR 3 - ， - C（CH 2 O烷基） - ; R 1是卤素，烷基，环烷基，烷基（环烷基），芳基，（芳基）烷基，（芳基）烯基，（芳基）炔基，O-烷基，O-链烯基， O-芳基，O-烷基（芳基），O-烷基（杂环），COO-烷基，C） - 烷基，CO-氨基，CO取代的氨基，烷基-CO-氨基，烷基-CO-取代的氨基，NHCO - 烷基，NHCO-芳基，NHCO-烷基（芳基），NHCO-烷基（杂环），N（烷基）CO-烷基，N（烷基）CO-芳基，N（烷基）CO-杂环，N（烷基） - 烷基（芳基），N（烷基）CO-烷基（杂环）; R 2是氢，烷基，卤素，芳基，（芳基）烷基，O-烷基，氨基，取代的氨基; R 3和R “3”可以相同或不同，独立地选自氢，烷基或烷基（芳基）;可以与环碳或氮键合的R 4选自氢，烷基，烯基，烷基（芳基 ），烷基（杂环），环烷基，烷基（环烷基），烷基 - （氨基） （烷基），烷基-NHCO（芳基），烷基-NHCO（杂环），烷基-NHCO（烷基芳基），烷基-NHCO（烷基杂环））。 并且n是0至2的整数。已经发现这些化合物可用于治疗心律失常。

    Aza pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
    10.
    发明授权
    Aza pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists 有权
    可用作黑色素浓缩激素受体-1拮抗剂的氮杂吡啶酮类似物

    公开(公告)号：US08278316B2

    公开(公告)日：2012-10-02

    申请号：US13255170

    申请日：2010-03-09

    Applicant: Saleem Ahmad

    Inventor： Saleem Ahmad

    IPC: A01N43/54 ,  A61K31/505

    CPC classification number: C07D239/36 ,  C07D239/47 ,  C07D239/54 ,  C07D239/56

    Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.

    Abstract translation: 提供具有以下式I的MCHR1拮抗剂：其中所有变量在本文中定义。 这些化合物可用于治疗MCHR1介导的疾病，例如肥胖症，糖尿病，IBD，抑郁症和焦虑症。

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