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    BENZOTHIAZOLE AND BENZOXAZOLE DERIVATIVES AND METHODS OF USE
    99.
    发明专利
    BENZOTHIAZOLE AND BENZOXAZOLE DERIVATIVES AND METHODS OF USE 未知

    公开(公告)号：NZ586301A

    公开(公告)日：2012-10-26

    申请号：NZ58630108

    申请日：2008-12-18

    Applicant: ABBOTT LAB

    Inventor： BLACK LAWRENCE A ,  COWART MARLON D ,  GFESSER GREGORY A ,  WAKEFIELD BRIAN D ,  ALTENBACH ROBERT J ,  LIU HUAQING ,  ZHAO CHEN ,  HSIEH GIN C

    IPC: C07D413/14 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61P3/10 ,  A61P25/00 ,  C07D277/82 ,  C07D417/14

    Abstract: Disclosed are 2-(pyrrolidin-1-yl)benzo[d]thiazole derivatives as represented by the general formula (I), wherein Z is sulfur; n is an integer from 0 to 2; p is an integer from 0 to 1; and wherein the remaining substituents are as defined herein; and radiolabelled analogues thereof. Representative compounds include 6-(1-methyl-1H-pyrazol-4-yl)-2-(3-(piperidin-1-yl)azetidin-1-yl)benzo[d]thiazole, (R)-4-(2-(1,3'-bipyrrolidin-1'-yl)benzo[d]thiazol-6-yl)benzonitrile, (R)-6-(1-(11C)methyl-1H-pyrazol-4-yl)-2-(3-(piperidin-1-yl)pyrrolidin-1-yl)benzo[d]thiazole, (R)-6-(1-methyl-1H-pyrazol-4-yl)-2-(3-(4-(18F)fluoro-piperidin-1-yl)pyrrolidin-1-yl)benzo[d]thiazole, (R)-2-(2-(3-(4-(18F)fluoro-piperidin-1-yl)pyrrolidin-1-yl)benzo[d]thiazol-6-yl)pyridazin-3(2R)-one; (R)-3-(2-(3-(4-(18F)fluoro-piperidin-1-yl)pyrrolidin-1-yl)benzo[d]thiazol-6-yl)oxazolidin-2-one, (S)-3-hydroxy-1-(2-((R)-3-(4-(18F)fluoro-piperidin-1-yl)pyrrolidin-1-yl)benzo[d]thiazol-6-yl)pyrrolidin-2-one and (R)-N-(2-(18F)fluoroethyl)-2-(3-(piperidin-1-yl)pyrrolidin-1-yl)benzo[d]thiazole-6-carboxamide. Further disclosed is a pharmaceutical composition comprising a therapeutically effective amount of a compound as defined above in combination with a pharmaceutically acceptable carrier for treating a condition or disorder modulated by the histamine-3 receptors selected from acute myocardial infarction, Alzheimer's disease, asthma, attention-deficit hyperactivity disorder, bipolar disorder, cognitive dysfunction, cognitive deficits in psychiatric disorders, deficits of memory, deficits of learning, dementia, cutaneous carcinoma, drug abuse, diabetes, type II diabetes, depression, epilepsy, gastrointestinal disorders, inflammation, insulin resistance syndrome, jet lag, medullary thyroid carcinoma, melanoma, Meniere's disease, metabolic syndrome, mild cognitive impairment, migraine, mood and attention alteration, motion sickness, narcolepsy, neurogenic inflammation, obesity, obsessive compulsive disorder, pain, neuropathic pain, osteoarthritis pain, Parkinson's disease, polycystic ovary syndrome, schizophrenia, cognitive deficits of schizophrenia, seizures, septic shock, Syndrome X, Tourette's syndrome, vertigo, and sleep disorders.

    Octahydro-pyrrolo[3,4-b]pyrrole derivatives and their use as histamine-3 receptor ligands
    100.
    发明专利
    Octahydro-pyrrolo[3,4-b]pyrrole derivatives and their use as histamine-3 receptor ligands 未知

    公开(公告)号：NZ570235A

    公开(公告)日：2011-10-28

    申请号：NZ57023507

    申请日：2007-02-16

    Applicant: ABBOTT LAB

    Inventor： COWART MARLON D ,  ZHAO CHEN ,  SUN MINGHUA ,  BLACK LAWRENCE A ,  ZHENG GUO ZHU ,  GREGG ROBERT J ,  ZHANG GEOFF G

    IPC: C07D487/04 ,  A61K31/407 ,  A61K31/501 ,  C07D237/14

    Abstract: Disclosed are 1-phenyl-pyrrolo[3,4-b]pyrrole derivatives as represented by the general formula (I), wherein R1 is alkyl, cycloalkyl, or (cycloalkyl)methyl; R2a-R2f each are independently hydrogen, methyl, or fluoromethyl; R3a-R3d are each independently hydrogen, alkyl, fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile; L1 is a bond, oxygen, sulfur, carbonyl, alkylene, alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, or NR4; L2 is a bond, oxygen, sulphur, carbonyl, alkylene, alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR5, -C(=O)NR5-, or -NR5C(=O)-; Cy1 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; Cy2 is aryl, cycloalkyl, cycloalkenyl, heteroaryl or heterocycle, wherein the heteroaryl or heterocycle moiety has 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur, provided that at least one heteroatom is nitrogen; and wherein the other substituents are as defined herein. Of particular importance are the compounds 2-{ 4'-[(3aR,6aR)-5- methylhexahydropyrrolo[3,4-b]pyrrol-1(2H)-yl]-1,1'-biphenyl-4-yl} pyridazin-3(2H)-one, 2-(5-{ 4-[(3aR,6aR)-5-methylhexahydropyrrolo[3,4-b]pyrrol-1(2H)-yl]phenyl} pyridin-2-yl)pyridazin-3(2H)-one and 2-(6-{ 4-[(3aR,6aR)-5-methylhexahydropyrrolo[3,4-b]pyrrol-1(2H)-yl]phenyl} pyridin-3-yl)pyridazin-3(2H)-one. Further disclosed is a harmaceutical composition which comprises a compound as defined above and a pharmaceutically acceptable carrier.

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