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    BENZOAZOLYPIPERAZINE DERIVATIVES HAVING MGLUR1- AND MGLUR5-ANTAGONISTIC ACTIVITY
    82.
    发明公开
    BENZOAZOLYPIPERAZINE DERIVATIVES HAVING MGLUR1- AND MGLUR5-ANTAGONISTIC ACTIVITY 有权
    具有MGLUR1-和MGLUR5-拮抗活性的苯并氮杂哌嗪衍生物

    公开(公告)号：EP1583763A1

    公开(公告)日：2005-10-12

    申请号：EP03814351.7

    申请日：2003-12-22

    申请人： Euro-Celtique S.A.

    发明人： SUN, Qun ,  TAFESSE, Laykea ,  VICTORY, Sam

    IPC分类号： C07D417/12 ,  C07D413/12 ,  C07D403/12 ,  C07D401/12 ,  A61K31/495 ,  A61P29/00 ,  A61P13/00

    CPC分类号： C07D417/12 ,  A61K31/495 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

    摘要： A compound of formula (I) wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson’s disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, retricted brain function, Huntington’s chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of Benzoazolylpiperazine Compound are disclosed.

    摘要翻译： 其中Ar 1，A，R 3，x和m如本文所公开且Ar 2为苯并噻唑基，苯并恶唑基或苯并咪唑基或其药学上可接受的盐（“苯并唑基哌嗪化合物”）的组合物， 苯并唑基哌嗪化合物，以及治疗或预防疼痛，UI，溃疡，IBD，IBS，成瘾性病症，帕金森病，帕金森病，焦虑症，癫痫症，中风，惊厥，瘙痒症状，精神病，认知障碍，记忆 公开了在动物中施用有效量的苯并唑基哌嗪化合物，包括向有需要的动物给药，包括给予有效量的苯并唑基哌嗪化合物，其中所述化合物包含有效量的苯并咪唑基哌嗪化合物或其药学可接受的盐。

    The use of carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones as sodium channel blockers
    83.
    发明公开
    The use of carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones as sodium channel blockers 失效
    通过碳环和杂环取代的缩氨基脲和缩氨基硫脲及它们作为钠通道阻断剂的使用

    公开(公告)号：EP1568690A1

    公开(公告)日：2005-08-31

    申请号：EP04030775.3

    申请日：1998-04-22

    申请人： Euro-Celtique S.A.

    发明人： Wang, Yan ,  Cai, Sui Xiong ,  Lan, Nancy C. ,  Ilyin, Victor I. ,  Keana, John F. W. ,  Weber, Eckard

    IPC分类号： C07D211/06 ,  C07D213/02 ,  C07D215/02 ,  C07D239/02 ,  C07D309/02 ,  A61K31/35 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61K31/505 ,  C07D213/64

    CPC分类号： C07D213/643 ,  C07C281/14 ,  C07C323/48 ,  C07C337/08 ,  C07D209/14 ,  C07D211/46 ,  C07D213/68 ,  C07D215/12 ,  C07D215/20 ,  C07D239/34 ,  C07D307/91 ,  C07D309/12 ,  C07D317/50 ,  C07D317/62 ,  C07D317/64 ,  C07D319/18

    摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by formula (I), or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R 1 , R 21 , R 22 and R 23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R 22 and R 23 , together with the N, form a heterocycle; A 1 and A 2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR 24 , CR 25 R 26 , C(O), NR 24 C(O), C(O)NR 24 , SO, SO 2 or a covalent bond; where R 24 , R 25 and R 26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention is also directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyiotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.

    摘要翻译： 本发明涉及碳环和杂环取代的缩氨基脲和缩氨基硫脲，式（I）表示的，或者其药学上可接受的盐或其前药，worin：Y是氧或硫; R1，R21，R22和R23独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基; 或R22和R23与N一起形成杂环; A1和A2为unabhängig芳基，杂芳基，饱和或部分不饱和的羰周期或饱和或部分不饱和杂环，任何的所有其任选substituiertem; X是一种或O，S，NR24，CR25R26，C（O），NR24C（O），C（O）NR24，SO，SO 2或共价键; 其中R24，R25和R26独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。 因此，本发明涉及使用碳氮化周期和杂环substituiertem缩氨基脲和缩氨基硫脲的对神经元损伤的以下全局和局部缺血的治疗，用于治疗或预防的神经退行性病症：诸如amyiotrophic侧索硬化症（ALS），用于治疗和预防 的otoneurotoxicity和眼部疾病涉及谷氨酸毒性以及用于治疗，预防或改善疼痛，如抗惊厥药，和抗躁狂抑制剂，局部麻醉剂，抗心律不齐和糖尿病性神经病变和尿失禁的治疗或预防。

    ANTIBODIES THAT BIND CELL-ASSOCIATED CA 125/0722P AND METHODS OF USE THEREOF
    87.
    发明公开
    ANTIBODIES THAT BIND CELL-ASSOCIATED CA 125/0722P AND METHODS OF USE THEREOF 有权
    抗体与细胞相关的CA 125 / 0722P结合和申请流程。

    公开(公告)号：EP1551876A2

    公开(公告)日：2005-07-13

    申请号：EP03789713.9

    申请日：2003-10-15

    申请人： Euro-Celtique S.A.

    发明人： ALBONE, Earl, F. ,  SOLTIS, Daniel, A.

    IPC分类号： C07K16/00 ,  A61K39/395 ,  C12N5/12 ,  C07H21/04 ,  G01N33/53

    CPC分类号： C07K16/3069 ,  A61K47/6869 ,  A61K2039/505 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/732

    摘要： The present invention provides fusion proteins of antibodies, and antigen-binding fragments of antibodies, that preferentially bind cell-associated CA 125/0772P polypeptides relative to shed CA 125/0772P polypeptides. They comprise a heterologous agent such as a detectable agent or a therapeutic agent. The present disclsoure further provides methods of preventing, managing, treating or ameliorating one or more symptoms associated with a CA 125/0772P-related disorder. In particular, the present disclosure provides methods of preventing, managing, treating, or ameliorating one or more symptoms associated with a cell proliferative disorder, such as cancer, e.g., ovarian cancer. The present disclosure still further provides methods for diagnosing a CA 125/0772P-related disorder or predisposition to developing such a disorder, as well as methods for identifying antibodies, and antigen-binding fragments of antibodies, that preferentially bind cell-associated CA 125/0772P polypeptides relative to shed CA 125/0772P polypeptides.

    N-SUBSTITUTED HYDROMORPHONES AND THE USE THEREOF
    88.
    发明公开
    N-SUBSTITUTED HYDROMORPHONES AND THE USE THEREOF 有权
    N-取代氢吗啡酮及其应用

    公开(公告)号：EP1543010A1

    公开(公告)日：2005-06-22

    申请号：EP03754837.7

    申请日：2003-09-24

    申请人： Euro-Celtique S.A.

    发明人： KYLE, Donald, J.

    IPC分类号： C07D489/02 ,  A61K31/44

    CPC分类号： C07D489/04 ,  C07D489/02

    摘要： This invention relates to N-substituted hydromorphones of Formula I or a pharmaceutically acceptable salt thereof. These compounds act as µ opioid receptor agonists. The invention is also directed to the use of compounds of Formula I for the treatment, prevention or amelioration of both acute and chronic pain.

    ARYL SUBSTITUTED BENZIMIDAZOLES AND THEIR USE AS SODIUM CHANNEL BLOCKERS
    89.
    发明公开
    ARYL SUBSTITUTED BENZIMIDAZOLES AND THEIR USE AS SODIUM CHANNEL BLOCKERS 审中-公开
    芳基取代的苯并咪唑及其作为钠通道阻滞剂

    公开(公告)号：EP1532119A2

    公开(公告)日：2005-05-25

    申请号：EP03772101.6

    申请日：2003-07-31

    申请人： Euro-Celtique S.A.

    发明人： SUN, Qun ,  ZHOU, Xiaoming ,  KYLE, Donald, J.

    IPC分类号： C07D235/00

    CPC分类号： C07D403/06 ,  C07D235/08 ,  C07D235/12

    摘要： This invention relates aryl substituted benzimidazoles of Formula (I) or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1, R2, R10 and n are defined in the specification. The invention is also directed to the use of compounds of Formula (I) for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.