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1. 发明申请

WO2012004375A1 BISARYL (THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS 审中-公开
标题翻译： BISARYL（THIO）MORPHOLINE衍生物作为S1P调节剂
公开(公告)号：WO2012004375A1
公开(公告)日：2012-01-12
申请号：PCT/EP2011/061590
申请日：2011-07-08
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , IWEMA BAKKER, Wouter I. , BRONGER, Raymond
发明人： IWEMA BAKKER, Wouter I. , BRONGER, Raymond
IPC分类号： C07D265/30 , C07D413/10 , A61K31/5375 , A61K31/5377 , A61P25/00
CPC分类号： A61K31/5375 , A61K31/5377 , A61K31/54 , C07D265/30 , C07D295/15 , C07D413/10
摘要： The present invention relates to bisaryl (thio)morpholine derivatives of the formula (I) wherein R1 is an aryl substitutent selected from phenyl, pyridyl, pyrimidinyl, biphenyl and naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, -SO 2 -(1-4C)alkyl, -CO-(1-4C)alkyl, -CO-O-(1-4C)alkyl and -NH-CO-(1-4C)alkyl, or substituted with phenoxy, benzyl, benzyloxy, phenylethyl or morpholinyl, each optionally substituted with (1-4C)alkyl, and (8-10C)bicyclic group, bicyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms or oxo; A is selected from -CO-, -NH-, -O-, -S-, -SO- or -SO 2 -; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, or halogen; and R3 is (1-4C)alkylene-R6 wherein the alkylene group may be substituted with (CH 2 ) 2 to form a cyclopropyl moiety or with one or more halogen atoms, or R3 is (3-6C)cycloalkylene-R5 or -CO-CH 2 -R6, wherein R6 is -OH, -PO 3 H 2 , -OPO 3 H 2 , -COOH, -COO(1-4C)alkyl or tetrazol-5-yl; R4 is H or (1-4C)alkyl; R5 is one or more substituents independently selected from H, (1-4C)alkyl or oxo; W is -O-, -S-, -SO- or -SO 2 -; or a pharmaceutically acceptable salt, a solvate or hydrate thereof, with the proviso that the derivative of formula (I) is not 2-[4-(4-chlorophenoxy)-2-chloro-phenyl]-4-morpholineethanol. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
摘要翻译：本发明涉及式（I）的二芳基（硫代）吗啉衍生物，其中R 1是选自苯基，吡啶基，嘧啶基，联苯基和萘基的芳基取代基，各自任选被一个或多个独立地选自卤素的取代基取代任选被一个或多个氟原子取代的（1-4C）烷氧基，氨基，二（1-4C）烷基氨基，-SO 2 - （1-4C）烷基，-CO - （1-4C）烷基，-CO-O-（1-4C）烷基和-NH-CO-（1-4C）烷基，或被苯氧基，苄基，苄氧基，苯基乙基或吗啉基取代，各自任选被（ 1-4C）烷基和（8-10C）双环基团，各自任选被（1-4C）烷基任意地被一个或多个氟原子或氧代取代的烷基取代; A选自-CO - ， - NH - ， - O - ， - S - ， - SO-或-SO 2 - ; 环结构B任选地含有一个氮原子; R2是H，任选被一个或多个氟原子取代的（1-4C）烷基，（1-4C）任选被一个或多个氟原子取代的烷氧基或卤素; 并且R 3是（1-4C）亚烷基-R 6，其中亚烷基可以被（CH 2）2取代以形成环丙基部分或与一个或多个卤素原子，或者R 3是（3-6C）亚环烷基-R 5或-CO -CH 2 -R 6，其中R 6是-OH，-PO 3 H 2，-OPO 3 H 2，-COOH，-COO（1-4C）烷基或四唑-5-基; R4是H或（1-4C）烷基; R5是一个或多个独立地选自H，（1-4C）烷基或氧代的取代基; W是-O - ， - S - ， - SO-或-SO 2 - ; 或其药学上可接受的盐，溶剂合物或水合物，条件是式（I）的衍生物不是2- [4-（4-氯苯氧基）-2-氯 - 苯基] -4-吗啉乙醇。本发明的化合物对S1P受体具有亲和性，可用于治疗，缓解或预防S1P受体介导的疾病和病症。

2. 发明申请

WO2012004378A1 SPIRO-CYCLIC AMINE DERIVATIVES AS S1P MODULATORS 审中-公开
标题翻译：作为S1P调节剂的螺旋环胺衍生物
公开(公告)号：WO2012004378A1
公开(公告)日：2012-01-12
申请号：PCT/EP2011/061599
申请日：2011-07-08
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , STOIT, Axel , IWEMA BAKKER, Wouter, I. , COOLEN, Hein K.A.C. , VAN DONGEN, Maria J.P. , LEFLEMME, Nicolas J.-L.D.
发明人： STOIT, Axel , IWEMA BAKKER, Wouter, I. , COOLEN, Hein K.A.C. , VAN DONGEN, Maria J.P. , LEFLEMME, Nicolas J.-L.D.
IPC分类号： C07D265/36 , C07D491/107 , C07D491/20 , A61K31/407 , A61K31/4355 , A61K31/5386 , A61P25/00
CPC分类号： C07D491/107 , C07D265/34 , C07D265/36 , C07D491/20 , C07F9/6561
摘要： The present invention relates spiro- cyclic amine derivatives of the formula (I) wherein R1; R2; R3; Q; -W-T-; R5; Z; and A have the definitions provided in the claims; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor (s) is (are) involved.
摘要翻译：本发明涉及式（I）的螺环胺衍生物，其中R1; R2; R3; Q; -W-T-; R5; Z者除外; 和A具有权利要求中提供的定义; 或其药学上可接受的盐，溶剂合物或水合物或其一种或多种N-氧化物。本发明的化合物对S1P受体具有亲和力，可用于治疗，缓解或预防（a）S1P受体涉及的疾病和病症。

3. 发明申请

WO2011023795A1 (THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS 审中-公开
标题翻译：（THIO）吗啉衍生物作为S1P调节剂
公开(公告)号：WO2011023795A1
公开(公告)日：2011-03-03
申请号：PCT/EP2010/062552
申请日：2010-08-27
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , IWEMA BAKKER, Wouter, I. , COOLEN, Hein K.A.C. , MONS, Harmen , STOIT, Axel , RONKEN, Eric , KAM, VAN DER, Elizabeth , FRANKENA, Jurjen
发明人： IWEMA BAKKER, Wouter, I. , COOLEN, Hein K.A.C. , MONS, Harmen , STOIT, Axel , RONKEN, Eric , KAM, VAN DER, Elizabeth , FRANKENA, Jurjen
IPC分类号： C07D265/30 , C07D265/32 , C07D413/12 , C07D419/12 , C07D471/04 , A61K31/5377 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , C07D279/12 , C07D417/12 , C07D487/04
CPC分类号： C07D295/15 , C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/12 , C07D471/04 , C07F9/6533
摘要： The present invention relates to (thio)morpholine derivatives of the formula (I), wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyloptionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms,amino, di(1-4C)alkylamino, -SO 2 -(1-4C)alkyl, -CO-(1-4C)alkyl, -CO-O-(1-4C)alkyl, -NH-CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from -CO-O-, -O-CO-, -NH-CO-, -CO-NH, -C=C-, -CCH 3 -O- and the linking group –Y-(CH 2 ) n -X- wherein Y is attached to R1 and selected from a bond, -O-, -S-, -SO-, -SO 2 -, -CH 2 -O-, -CO-, -O-CO-, -CO-O-, -CO-NH-, -NH-CO-, -C=C-and -C≡C-; n is an integer from 1 to 10; and X is attached to the phenylene / pyridyl group and selected from a bond, -O-, -S-, -SO-, -SO 2 -, -NH, -CO-, -C=C-and -C≡C-; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, or halogen; and R3 is (1-4C)alkylene-R5 wherein the alkylene group may be substituted with (CH 2 ) 2 to form a cyclopropyl moiety or one or two halogen atoms, or R3 is is (3-6C)cycloalkylene-R5 or -CO-CH 2 -R5, wherein R5 is -OH, -PO 3 H 2 , -OPO 3 H 2 , -COOH, -COO(1-4C)alkyl or tetrazol-5-yl; R4 is H or (1-4C)alkyl; R6 is one or more substituents independently selected from H, (1-4C)alkyl or oxo; W is -O-, -S-, -SO- or -SO 2 -; or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
摘要翻译：本发明涉及式（I）的（硫代）吗啉衍生物，其中R 1选自氰基，（2-4C）炔基，（1-4C）烷基，（3-6C）环烷基，（4-6C）环烷基，（6-8C）双环烷基，（8-10C）双环基团，各自任选被（1-4C）烷基，苯基，联苯基，萘基取代，各自任选被一个或多个独立地选自卤素，（1- 氨基，二（1-4C）烷基氨基，-SO 2 - （1-4C）烷氧基，被一个或多个氟原子烷基取代的（2-4C）炔基，任选被一个或多个氟原子取代的（1-4C）） - （1-4C）烷基，-CO-O-（1-4C）烷基，-NH-CO-（1-4C）烷基和（3-6C）环烷基，被苯氧基取代的苯基（1-4C）烷基或任选被（1-4C）烷基任意取代的苯基的单环杂环，和任选被取代的（1-4C）烷基的双环杂环，与（1-4C）烷基; A选自-CO-O-，-O-CO-，-NH-CO-，-CO-NH，-C = C-，-CCH 3 -O-和连接基-Y-（CH 2）n X- 其中Y连接到R 1并且选自-O - ， - S - ， - SO - ， - SO 2 - ， - CH 2 -O-，-CO-，-O-CO-，-CO-O-， -CO-NH-，-NH-CO-，-C≡C-和-C = C-; n为1〜10的整数，并且X连接到亚苯基/吡啶基上，并且选自-O - ， - S - ， - SO - ， - SO 2 - ， - NH，-CO - ， - C = C - 和-C = C- ; 环结构B任选地含有一个氮原子; R2是H，任选被一个或多个氟原子取代的（1-4C）烷基，（1-4C）任选被一个或多个氟原子取代的烷氧基或卤素; 并且R 3是（1-4C）亚烷基-R 5，其中亚烷基可以被（CH 2）2取代以形成环丙基部分或一个或两个卤素原子，或者R 3是（3-6C）亚环烷基-R 5或-CO -CH 2 -R 5，其中R 5是-OH，-PO 3 H 2，-OPO 3 H 2，-COOH，-COO（1-4C）烷基或四唑-5-基; R4是H或（1-4C）烷基; R6是一个或多个独立地选自H，（1-4C）烷基或氧代的取代基; W是-O - ， - S - ， - SO-或-SO 2 - ; 或其药学上可接受的盐，溶剂合物或水合物; 条件是式（I）的衍生物不是2-（4-乙基苯基）-4-吗啉代乙醇或4- [4-（2-羟乙基）-2-吗啉基]苯乙腈或其药学上可接受的盐，溶剂合物或水合物。本发明的化合物对S1P受体具有亲和力，可用于治疗，缓解或预防S1P受体介导的疾病和病症。

4. 发明申请

WO2008034863A2 SULFONYLPYRAZOLE AND SULFONYLPYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS 审中-公开
标题翻译：作为5-HT6拮抗剂的磺酰基吡唑和磺酰基吡唑烷酮衍生物
公开(公告)号：WO2008034863A2
公开(公告)日：2008-03-27
申请号：PCT/EP2007/059944
申请日：2007-09-20
申请人： SOLVAY PHARMACEUTICALS B.V. , IWEMA BAKKER, Wouter I. , KEIZER, Hiskias G. , NEUT, VAN DER, Martina A.W. , KRUSE, Cornelis G. , LOEVEZIJN, VAN, Arnold , ZORGDRAGER, Jan
发明人： IWEMA BAKKER, Wouter I. , KEIZER, Hiskias G. , NEUT, VAN DER, Martina A.W. , KRUSE, Cornelis G. , LOEVEZIJN, VAN, Arnold , ZORGDRAGER, Jan
IPC分类号： C07D231/06 , C07D401/12 , C07D409/12 , C07D513/04 , C07D417/12 , C07D403/12 , C07D231/12 , A61K31/415 , A61K31/4155 , A61P25/00 , C07D401/04 , C07D407/04
CPC分类号： C07D513/04 , A61K9/0019 , A61K9/0031 , A61K9/1652 , A61K9/2054 , C07D231/06 , C07D231/12 , C07D231/54 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/10 , C07D491/10 , C07D491/107 , C07D519/00
摘要： This invention concerns sulfonylpyrazoline carboxamidine derivatives as antagonists of 5-HT 6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1), wherein the symbols have the meanings given in the description.
摘要翻译：本发明涉及作为5-HT 6受体拮抗剂的磺酰吡唑啉甲脒衍生物，涉及制备这些化合物的方法和用于它们合成的新型中间体。本发明还涉及这些化合物和组合物的用途，特别是它们在给予患者以在帕金森病，亨廷顿氏舞蹈症，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫，强迫症中的治疗效果方面的用途，情绪障碍，偏头痛，阿尔茨海默病，年龄相关认知衰退，轻度认知障碍，睡眠障碍，进食障碍，厌食症，贪食症，暴饮暴食症，惊恐发作，静坐不动，注意力缺陷多动障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯并二氮杂，疼痛，与脊髓损伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征，肥胖症和2型糖尿病。化合物具有通式（1），其中符号具有说明书中给出的含义。

5. 发明申请

WO2006089861A2 ANETHOLE DITHIOLETHIONE AND OTHER DITHIOLETHIONES FOR THE TREATMENT OF CONDITIONS ASSOCIATED WITH DYSFUNCTION OF MONOAMINE NEUROTRANSMISSION 审中-公开
标题翻译： ANETHOLE DITHIOLETHIONE和其他二硫烯酮治疗与单胺神经传导功能障碍有关的病症
公开(公告)号：WO2006089861A2
公开(公告)日：2006-08-31
申请号：PCT/EP2006/060060
申请日：2006-02-17
申请人： SOLVAY PHARMACEUTICALS B.V. , DRUKARCH, Benjamin , SCHOFFELMEER, Anton, N., M. , FEENSTRA, Roelof, W. , CHRISTEN, Marie-odile , BURGOT, Jean-louise , CHOLLET, Marylene , IWEMA BAKKER, Wouter, I. , VAN VLIET, Bernard, J. , TULP, Martinus, Th. M.
发明人： DRUKARCH, Benjamin , SCHOFFELMEER, Anton, N., M. , FEENSTRA, Roelof, W. , CHRISTEN, Marie-odile , BURGOT, Jean-louise , CHOLLET, Marylene , IWEMA BAKKER, Wouter, I. , VAN VLIET, Bernard, J. , TULP, Martinus, Th. M.
IPC分类号： C07D339/04 , A61K31/385
CPC分类号： C07D409/12 , A61K31/385 , C07D339/04
摘要： The invention relates to dithiolethiones derivatives as monoamino oxidase inhibitors, in particular MAO-B inhibitors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said dithiolethiones derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. In embodiments of the invention specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment, amelioration or prevention of conditions associated with dysfunction of monoamine neurotransmission. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及作为单氨基氧化酶抑制剂的二硫代硫醇衍生物，特别是MAO-B抑制剂，涉及制备这些化合物的方法和涉及用于合成所述二硫代硫醇衍生物的新型中间体。本发明还涉及本文公开的化合物用于制造产生有益效果的药物的用途。在本发明的实施方案中，本文公开的具体化合物用于制造用于治疗，改善或预防与单胺神经传递功能障碍相关的病症的药物。该化合物具有通式（1），其中符号具有说明书中给出的含义。

6. 发明申请

WO2003084955A1 DIAZABICYCLO ALKANE DERIVATIVES WITH NK1 ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有NK1拮抗活性的DIAZABICYCLO ALKANE衍生物
公开(公告)号：WO2003084955A1
公开(公告)日：2003-10-16
申请号：PCT/EP2003/050086
申请日：2003-04-02
申请人： SOLVAY PHARMACEUTICALS B.V. , DE BOER, Dirk , COOLEN, Hein, K.A.C. , HESSELINK, Mayke, B. , IWEMA BAKKER, Wouter, I. , KUIL, Gijsbert, D. , VAN MAARSEVEEN, Jan, H. , MCCREARY, Andrew, C. , VAN SCHARRENBURG, Gustaaf, J.M.
发明人： DE BOER, Dirk , COOLEN, Hein, K.A.C. , HESSELINK, Mayke, B. , IWEMA BAKKER, Wouter, I. , KUIL, Gijsbert, D. , VAN MAARSEVEEN, Jan, H. , MCCREARY, Andrew, C. , VAN SCHARRENBURG, Gustaaf, J.M.
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to a group of unique diazabicyclo alkane derivatives having interesting neurokinin-NK 1 receptor antagonistic activity represented by the general formula (1) wherein: R 1 represents phenyl, 2-indolyl, 3-indolyl, 3-indazolyl or benzo[b]thiophen-3-yl, which groups may be substituted with halogen or alkyl (1-3C), R 2 and R 3 independently represent halogen, H, OCH 3, CH 3 and CF 3 , R 4 , R 5 and R 6 independently represent H, OH, O-alkyl(1-4C), CH 2 OH, NH 2 , dialkyl(1-3C)N, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or morpholin-4-yl substituted with one or two methyl or methoxymethyl groups, morpholin-4-ylamino, morpholin-4-ylmethyl, imidazol-1-yl, thiomorpholin-4-yl, 1, 1-dioxothiomorpholin-4-yl or 3-oxa-8-azabicyclo[3.2.1]oct-8-yl; R 4 and R 5 together may represent a keto, a 1,3-dioxan-2-yl or a 1,3-dioxolan-2-yl group, X represents either O or S, n has the value of 1, 2 or 3, a is the asymmetrical carbon atom 8a, 9a or 10a when n equals 1, 2 or 3 respectively The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions containing at least one of these compounds as an active ingredient.
摘要翻译：本发明涉及具有由通式（1）表示的感兴趣的神经激肽-N NK受体拮抗作用的独特的二氮杂双环烷烃衍生物，其中：R 1表示苯基，2-吲哚基，3-吲哚基，3-吲唑基或苯并 [b]噻吩-3-基，该基团可以被卤素或烷基（1-3C）取代，R 2和R 3独立地表示卤素，H，OCH 3，CH 3和CF 3，R 4， R 5和R 6独立地表示H，OH，O-烷基（1-4C），CH 2 OH，NH 2，二烷基（1-3C）N，吡咯烷-1-基，哌啶-1-基，吗啉 - 被一个或两个甲基或甲氧基甲基取代的吗啉-4-基或吗啉-4-基氨基，吗啉-4-基甲基，咪唑-1-基，硫代吗啉-4-基，1,1-二氧代硫代吗啉-4 - 基或3-氧杂-8-氮杂双环[3.2.1]辛-8-基; R 4和R 5一起可以表示酮，1,3-二氧杂环戊烷-2-基或1,3-二氧戊环-2-基，X表示O或S，n的值为 1,2或3中，a是当n等于1,2或3时不对称碳原子8a，9a或10a。本发明还涉及制备新化合物的方法，以及含有至少一种这些化合物作为活性成分。

7. 发明申请

WO2008034863A3 SULFONYLPYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS 审中-公开
标题翻译：作为5-HT6拮抗剂的磺酰基吡唑烷酮衍生物
公开(公告)号：WO2008034863A3
公开(公告)日：2008-05-08
申请号：PCT/EP2007059944
申请日：2007-09-20
申请人： SOLVAY PHARM BV , IWEMA BAKKER WOUTER I , KEIZER HISKIAS G , NEUT VAN DER MARTINA A W , KRUSE CORNELIS G , LOEVEZIJN VAN ARNOLD , ZORGDRAGER JAN
发明人： IWEMA BAKKER WOUTER I , KEIZER HISKIAS G , NEUT VAN DER MARTINA A W , KRUSE CORNELIS G , LOEVEZIJN VAN ARNOLD , ZORGDRAGER JAN
IPC分类号： C07D231/06 , A61K31/415 , A61K31/4155 , A61P25/00 , C07D231/12 , C07D401/04 , C07D401/12 , C07D403/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/12 , C07D513/04
CPC分类号： C07D513/04 , A61K9/0019 , A61K9/0031 , A61K9/1652 , A61K9/2054 , C07D231/06 , C07D231/12 , C07D231/54 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/10 , C07D491/10 , C07D491/107 , C07D519/00
摘要： This invention concerns sulfonylpyrazoline carboxamidine derivatives as antagonists of 5-HT 6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1), wherein the symbols have the meanings given in the description.
摘要翻译：本发明涉及作为5-HT 6受体拮抗剂的磺酰吡唑啉甲脒衍生物，涉及制备这些化合物的方法和用于它们合成的新型中间体。本发明还涉及这些化合物和组合物的用途，特别是它们在给予患者以在帕金森病，亨廷顿氏舞蹈症，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫，强迫症中的治疗效果方面的用途，情绪障碍，偏头痛，阿尔茨海默病，年龄相关认知衰退，轻度认知障碍，睡眠障碍，进食障碍，厌食症，贪食症，暴饮暴食症，惊恐发作，静坐不动，注意力缺陷多动障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯并二氮杂，疼痛，与脊髓损伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征，肥胖症和2型糖尿病。化合物具有通式（1），其中符号具有说明书中给出的含义。

8. 发明申请

WO2006089861A3 ANETHOLE DITHIOLETHIONE AND OTHER DITHIOLETHIONES FOR THE TREATMENT OF CONDITIONS ASSOCIATED WITH DYSFUNCTION OF MONOAMINE NEUROTRANSMISSION 审中-公开
标题翻译：用于治疗与单胺神经递质功能异常有关的病症的单胺二脱氧胆碱和其他脱乙酰
公开(公告)号：WO2006089861A3
公开(公告)日：2006-10-26
申请号：PCT/EP2006060060
申请日：2006-02-17
申请人： SOLVAY PHARM BV , DRUKARCH BENJAMIN , SCHOFFELMEER ANTON N M , FEENSTRA ROELOF W , CHRISTEN MARIE-ODILE , BURGOT JEAN-LOUISE , CHOLLET MARYLENE , IWEMA BAKKER WOUTER I , VAN VLIET BERNARD J , TULP MARTINUS TH M
发明人： DRUKARCH BENJAMIN , SCHOFFELMEER ANTON N M , FEENSTRA ROELOF W , CHRISTEN MARIE-ODILE , BURGOT JEAN-LOUISE , CHOLLET MARYLENE , IWEMA BAKKER WOUTER I , VAN VLIET BERNARD J , TULP MARTINUS TH M
IPC分类号： C07D339/04 , A61K31/385
CPC分类号： C07D409/12 , A61K31/385 , C07D339/04
摘要： The invention relates to dithiolethiones derivatives as monoamino oxidase inhibitors, in particular MAO-B inhibitors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said dithiolethiones derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. In embodiments of the invention specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment, amelioration or prevention of conditions associated with dysfunction of monoamine neurotransmission. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及二硫代硫代乙烯衍生物作为单氨基氧化酶抑制剂，特别是MAO-B抑制剂，涉及制备这些化合物的方法和用于合成所述二硫代硫代衍生物的新型中间体。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。在本发明的实施方案中，本文公开的具体化合物用于制备可用于治疗，改善或预防与单胺神经传递功能障碍相关的病症的药物。化合物具有通式（1），其中符号具有说明书中给出的含义。

9. 发明申请

WO2005030214A1 HEXA- AND OCTAHYDRO-PYRIDO[1,2-a]PYRAZINE DERIVATIVES WITH NK1 ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有NK1拮抗活性的HEXA-和OCTAHYDRO-PYRIDO [1,2-a]吡嗪衍生物
公开(公告)号：WO2005030214A1
公开(公告)日：2005-04-07
申请号：PCT/EP2004/052277
申请日：2004-09-23
申请人： SOLVAY PHARMACEUTICALS B.V. , IWEMA BAKKER, Wouter I. , VAN SCHARRENBURG, Gustaaf J.M. , VAN DEN HOOGENBAND, Adrianus , MCCREARY, Andrew C.
发明人： IWEMA BAKKER, Wouter I. , VAN SCHARRENBURG, Gustaaf J.M. , VAN DEN HOOGENBAND, Adrianus , MCCREARY, Andrew C.
IPC分类号： A61K31/4985
CPC分类号： C07D471/04
摘要： The invention relates to hexahydro-pyrido[1,2-a]pyrazine derivatives having interesting neurokinin-NK 1 receptor antagonistic activity. The invention also relates to methods for the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient, as well as to the use of these compositions for the treatment of disorders in which neurokinin receptors are involved. The invention relates to compounds represented by the general formula (1) wherein the symbols have the meanings as given in the description.
摘要翻译：本发明涉及具有感兴趣的神经激肽NK1受体拮抗活性的六氢 - 吡啶并[1,2-a]吡嗪衍生物。本发明还涉及制备这些化合物的方法，含有药理学活性量的这些化合物中的至少一种作为活性成分的药物组合物，以及这些组合物用于治疗神经激肽受体参与。本发明涉及由通式（1）表示的化合物，其中符号具有说明书中给出的含义。

10. 发明申请

WO2012004373A1 FUSED HETEROCYCLIC DERIVATIVES AS S1P MODULATORS 审中-公开
标题翻译：作为S1P调节剂的熔融杂环衍生物
公开(公告)号：WO2012004373A1
公开(公告)日：2012-01-12
申请号：PCT/EP2011/061586
申请日：2011-07-08
申请人： ABBOTT HEALTHCARE PRODUCTS B.V. , SMID, Pieter , IWEMA BAKKER, Wouter, I. , COOLEN, Hein, K.A.C. , SLIEDREGT, Leonardus, A.J.M. , VAN DONGEN, Maria, J.P. , DEN HARTOG, Jacobus, A.J.
发明人： SMID, Pieter , IWEMA BAKKER, Wouter, I. , COOLEN, Hein, K.A.C. , SLIEDREGT, Leonardus, A.J.M. , VAN DONGEN, Maria, J.P. , DEN HARTOG, Jacobus, A.J.
IPC分类号： C07D487/04 , C07D491/04 , C07D498/04 , C07D513/04 , A61P25/28 , A61K31/429 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/55
CPC分类号： C07D491/048 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified substructures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
摘要翻译：本发明涉及式（I）的稠合杂环衍生物。变量R1-R4，z，A，Q，X和Y如权利要求中所定义。以下杂环是式（I）的亚结构：式（I）化合物是S1P受体（鞘氨醇-1-磷酸受体）的调节剂，更具体地说，它们是S1P5的激动剂。该化合物在治疗认知障碍，与年龄有关的认知衰退和痴呆方面具有治疗用途。

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