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1. 发明授权

US07202238B2 Diazabicyclo alkane derivatives with NK1 antagonistic activity 有权
标题翻译：具有NK1拮抗活性的二氮杂双环烷烃衍生物
公开(公告)号：US07202238B2
公开(公告)日：2007-04-10
申请号：US10490364
申请日：2003-04-02
申请人： Dirk de Boer , Hein K. A. C. Coolen , Mayke B. Hesselink , Wouter I. Iwema Bakker , Gijsbert D. Kuil , Jan H. van Maarseveen , Andrew C. McCreary , Gustaaf J. M. van Scharrenburg
发明人： Dirk de Boer , Hein K. A. C. Coolen , Mayke B. Hesselink , Wouter I. Iwema Bakker , Gijsbert D. Kuil , Jan H. van Maarseveen , Andrew C. McCreary , Gustaaf J. M. van Scharrenburg
IPC分类号： A01N43/00 , A01N43/58 , A01N43/50 , A61K31/55 , C07D241/36
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-NK1 receptor antagonistic activity represented by the general formula (1) wherein: R1 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), R2 and R3 independently represent halogen, H, OCH3, CH3 and CF3, R4, R5 and R6 independently represent H, OH, O-alkyl(1–4C), CH2OH, NH2, 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; R4 and R5 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）表示的具有感兴趣的神经激肽NK 1受体拮抗作用的独特的二氮杂双环烷烃衍生物组，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，该基团可被卤素或烷基（1-3C），R 2和R 2 > 3个独立地表示卤素，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 （1-3C）N，吡咯烷-1-基，哌啶-1-基，吗啉-4-基或被一个或两个甲基或甲氧基甲基取代的吗啉-4-基，吗啉代 - 吡啶-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 5一起可以表示酮基，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，当n分别为1,2或3时，a为非对称碳原子8a，9a或10a。本发明还涉及一种制备新化合物的方法以及含有这些化合物中的至少一种作为活性成分的药物组合物

2. 发明授权

US07094779B2 Piperazine oxime dervatives having NK-1 receptor antagonistic activity 有权
标题翻译：具有NK-1受体拮抗活性的哌嗪肟衍生物
公开(公告)号：US07094779B2
公开(公告)日：2006-08-22
申请号：US10480542
申请日：2002-07-03
申请人： Wouter I. Iwema Bakker , Jan H. van Maarseveen , Hein K. A. C. Coolen , Martinus Th. M. Tulp , Arnoldus H. J. Herremans , Andrew C. Mccreary , Gustaaf J. M. van Scharrenburg , Adrianus van den Hoogenband
发明人： Wouter I. Iwema Bakker , Jan H. van Maarseveen , Hein K. A. C. Coolen , Martinus Th. M. Tulp , Arnoldus H. J. Herremans , Andrew C. Mccreary , Gustaaf J. M. van Scharrenburg , Adrianus van den Hoogenband
IPC分类号： A61K31/496 , C07D403/06 , C07D413/14 , C07D471/04
CPC分类号： C07D401/14 , C07D241/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D471/04
摘要： The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein: X represents phenyl or pyridyl substituted with 1 or 2 substituents from the group CH3, CF3, OCH3, halogen, cyano and 5-CF3-tetrazol-1-yl; Y represents 2- or 3-indolyl, phenyl, 7-aza-indol-3-yl or 3-indazolyl, 2-naphthyl, 3-benzo[b]thiophenyl, 2-benzofuranyl, which groups may be substituted with one or more halogen or alkyl (1–3C); n has the value 0–3; m has the value 0–2; R1 represents NH2, NH-alkyl (1–3C), dialkyl (1–3C)N, morpholino or morpholino substituted with one or two methyl and/or methoxymethyl groups, thiomorpholino, 1,1-dioxothiomorpholino, 2-, 3- or 4-pyridyl or 4-CH3-piperazinyl; R2 is hydrogen, alkyl (1–4C) or phenyl, or R2 together with (CH2)m wherein m is 1, and the intermediate carbon, nitrogen and oxygen atoms forms an isoxazolyl or a 4,5-dihydroisoxazolyl group; R3 and R4 independently represent hydrogen or methyl, or R3 and R4 together are oxygen. The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions comprising compounds with formula (1) as an active ingredient and the use of these compounds for the treatment of disorders in which neurokinin-1 receptors are involved
摘要翻译：本发明涉及一组具有有趣的NK-1拮抗活性的新型哌嗪肟衍生物。本发明涉及通式（1）的化合物，其中：X表示苯基或被1或2个取代基取代的吡啶基，其中CH 3，CF 3，OCH 3， N 3，卤素，氰基和5-CF 3 - 四唑-1-基; Y代表2-或3-吲哚基，苯基，7-氮杂 - 吲哚-3-基或3-吲唑基，2-萘基，3-苯并[b]噻吩基，2-苯并呋喃基，它们可以被一个或多个卤素或烷基（1-3C）; n的值为0-3; m的值为0-2; R 1表示NH 2，NH-烷基（1-3C），（1-3C）二烷基，吗啉代或吗啉基，被一或两个甲基和/或甲氧基甲基基团，硫代吗啉代，1,1-二氧代硫代吗啉代，2-，3-或4-吡啶基或4- CH 3 - 哌嗪基; R 2是氢，烷基（1-4C）或苯基，或R 2和（CH 2 CH 2）m，其中m为1，中间碳，氮和氧原子形成异恶唑基或4,5-二氢异恶唑基; R 3和R 4独立地代表氢或甲基，或R 3和R 4一起是氧。本发明还涉及一种制备新化合物的方法，以及包含式（1）化合物作为活性成分的药物组合物，以及这些化合物用于治疗涉及神经激肽-1受体的疾病的用途

3. 发明授权

US07244734B2 Hexa- and octahydro-pyrido[1,2-a]pyrazine derivatives with NK1 antagonistic activity 失效
标题翻译：具有NK1拮抗活性的六氢和八氢吡啶并[1,2-a]吡嗪衍生物
公开(公告)号：US07244734B2
公开(公告)日：2007-07-17
申请号：US10946176
申请日：2004-09-22
申请人： Wouter I. Iwema Bakker , Gustaaf J. M. Van Scharrenburg , Adrianus Van Den Hoogenband , Andrew C. McCreary
发明人： Wouter I. Iwema Bakker , Gustaaf J. M. Van Scharrenburg , Adrianus Van Den Hoogenband , Andrew C. McCreary
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D401/00
CPC分类号： C07D471/04
摘要： The invention relates to hexahydro-pyrido[1,2-a]pyrazine derivatives having interesting neurokinin-NK1 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-NN1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。

4. 发明授权

US08796262B2 Fused heterocyclic derivatives as S1P modulators 有权
标题翻译：稠合杂环衍生物作为S1P调节剂
公开(公告)号：US08796262B2
公开(公告)日：2014-08-05
申请号：US13808908
申请日：2011-07-08
申请人： Pieter Smid , Wouter I. Iwema Bakker , Hein K. A. C. Coolen , Leonardus A. J. M. Sliedregt , Maria J. P. van Dongen , Jacobus A. J. den Hartog , Adrian Hobson
发明人： Pieter Smid , Wouter I. Iwema Bakker , Hein K. A. C. Coolen , Leonardus A. J. M. Sliedregt , Maria J. P. van Dongen , Jacobus A. J. den Hartog , Adrian Hobson
IPC分类号： A01N43/00 , A01N43/46 , A61K31/55 , C07D495/04 , C07D513/04 , C07D491/048 , C07D487/04 , C07D471/04 , C07D491/04 , C07D498/04
CPC分类号： C07D491/048 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： This invention relates to new fused heterocyclic derivatives having affinity to S1P receptors, a pharmaceutical composition containing said compounds, as well as the use of said compounds for the preparation of a medicament for treating, alleviating or preventing diseases and conditions in which any S1P receptor is involved or in which modulation of the endogenous S1P signaling system via any S1P receptor is involved.
摘要翻译：本发明涉及对S1P受体具有亲和性的新的稠合杂环衍生物，含有所述化合物的药物组合物，以及所述化合物在制备用于治疗，缓解或预防任何S1P受体是涉及或参与通过任何S1P受体调节内源性S1P信号传导系统。

5. 发明授权

US10179791B2 Spiro-cyclic amine derivatives as S1P modulators 有权
公开(公告)号：US10179791B2
公开(公告)日：2019-01-15
申请号：US13808903
申请日：2011-07-08
申请人： Axel Stoit , Wouter I. Iwema Bakker , Hein K. A. C. Coolen , Maria J. P. van Dongen , Nicolas J.-L. D. Leflemme , Adrian Hobson
发明人： Axel Stoit , Wouter I. Iwema Bakker , Hein K. A. C. Coolen , Maria J. P. van Dongen , Nicolas J.-L. D. Leflemme , Adrian Hobson
IPC分类号： C07D491/107 , C07D265/36 , C07D491/20 , A61K31/44 , C07D401/00 , C07D265/34 , C07F9/6561
摘要： The present invention relates to spiro-cyclic amine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (3-6C)cycloalkyl, or phenyl optionally substituted with (1-4C)alkyl or halogen, and bicyclic heterocycle optionally substituted with halogen or (1-4C)alkyl optionally substituted with one or more fluoro atoms; —Y—(Cn-alkylene)-X— is a linking group wherein Y is attached to R1 and selected from a bond, —O—, —CO—, —S—, —SO—, —SO2—, —NH—, —CH═CH—, —C(CF3)═CH—, —C≡C—, —CH2—O—, —O—CO—, —CO—O—, —CO—NH—, —NH—CO—, and trans-cyclopropylene; n is an integer from 0 to 10; and X is attached to the phenylene/pyridyl moiety and selected from a bond, —O—, —S—, —SO—, —SO2—, —NH—, —CO—, —CH═CH—, and trans-cyclopropylene; R2 is H or independently selected from one or more substituents selected from halogen, (1-4C)alkoxy and (1-4C)alkyl optionally substituted with one or more fluor atoms; and R3 is (1-4C)alkylene-R4 wherein the alkylene group may be substituted with one or more halogen atoms or with (CH2)2 to form a cyclopropyl moiety, or R3 is (3-6C)cycloalkylene-R4, —CH2-(3-6C)cycloalkylene-R4, (3-6C)cycloalkylene-CH2—R4 or —CO—CH2—R4, wherein R4 is —OH, —PO3H2, —OPO3H2, —COOH, —COO(1-4C)alkyl or tetrazol-5-yl; Q is a bond or —O—; —W-T- is selected from —CH═CH—, —CH2—CH2—, —CH2—O—, —O—CH2—, —O—CH2—CH2—, and —CO—O—; R5 is H or independently selected from one or more halogens; Z is CH, CR2 or N; and A represents a morpholine ring structure or a 5-, 6- or 7-membered cyclic amine; 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.

6. 发明授权

US09045441B2 (Thio)morpholine derivatives as S1P modulators 有权
标题翻译：（Thio）吗啉衍生物作为S1P调节剂
公开(公告)号：US09045441B2
公开(公告)日：2015-06-02
申请号：US13393497
申请日：2010-08-27
申请人： Wouter I. Iwema Bakker , Hein K. A. C. Coolen , Axel Stoit , Harmen Mons , Eric Ronken , Elizabeth Van Der Kam , Jurjen Frankena , Adrian Hobson
发明人： Wouter I. Iwema Bakker , Hein K. A. C. Coolen , Axel Stoit , Harmen Mons , Eric Ronken , Elizabeth Van Der Kam , Jurjen Frankena , Adrian Hobson
IPC分类号： C07D265/32 , C07D265/30 , C07D279/12 , C07D413/04 , A61K31/5375 , A61K31/5377 , C07D413/06 , C07D413/12 , C07D417/12 , C07D471/04 , C07F9/6533
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 disclosure relates to (thio)morpholine derivatives of the formula (I) 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 disclosure 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：本公开涉及式（I）的（硫代）吗啉衍生物或其药学上可接受的盐，其溶剂合物或水合物; 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。本公开的化合物对S1P受体具有亲和力，并且可用于治疗，缓解或预防S1P受体介导的疾病和病症。

7. 发明申请

US20110046171A1 ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS 有权
标题翻译：作为5-HT6拮抗剂的芳基磺酰基吡唑烷酮衍生物
公开(公告)号：US20110046171A1
公开(公告)日：2011-02-24
申请号：US12933182
申请日：2009-03-17
申请人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Axel Stoit , Agatha A.M. Rensink , Jennifer Venhorst , Martina A.W. Van Der Neut , Martin De Haan , Cornelis G. Kruse
发明人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Axel Stoit , Agatha A.M. Rensink , Jennifer Venhorst , Martina A.W. Van Der Neut , Martin De Haan , Cornelis G. Kruse
IPC分类号： A61K31/438 , C07D231/54 , C07D231/06 , C07D491/10 , C07D403/12 , C07D471/10 , A61K31/415 , A61K31/416 , A61K31/4162 , A61K31/4155 , A61P25/16 , A61P25/14 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/08 , A61P25/06 , A61P25/28 , A61P25/00 , A61P25/20 , A61P3/00 , A61P3/04 , A61P25/30 , A61P1/00 , A61P3/10
CPC分类号： C07D231/06 , A61K31/415 , A61K31/4155 , A61K31/4162 , A61K31/435 , A61K31/635 , A61K45/06 , C07D231/00 , C07D231/54 , C07D403/12 , C07D471/10 , C07D491/10 , C07D491/107
摘要： This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 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受体的拮抗剂的芳基磺酰基吡唑啉甲脒衍生物，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

US20080311179A1 SULFONYLPYRAZOLE AND SULFONYLPYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS 有权
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：US20080311179A1
公开(公告)日：2008-12-18
申请号：US11859323
申请日：2007-09-21
申请人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Hiskias G. Keizer , Jan Zorgdrager , Martina A.W. Van Der Neut , Cornelis G. Kruse
发明人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Hiskias G. Keizer , Jan Zorgdrager , Martina A.W. Van Der Neut , Cornelis G. Kruse
IPC分类号： A61K9/12 , C07D403/12 , C07D409/12 , C07D413/14 , A61K9/48 , A61P3/00 , A61P1/00 , A61P25/00 , A61K9/70 , A61K31/4155 , A61K31/4245
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 compounds of the general formula (1). and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from 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.
摘要翻译：本发明涉及通式（1）的化合物。及其衍生物，其为5-HT 6受体的拮抗剂，其中符号具有说明书中给出的含义。本发明还涉及制备这些化合物的方法，可用于其合成的新型中间体，以及这些化合物和组合物的用途，特别是它们在将它们给予患者以达到治疗至少在疾病或病症上的治疗效果选自帕金森病，亨廷顿氏舞蹈病，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫症，强迫症，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，注意缺陷障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯二氮卓类药物的疼痛，疼痛，与脊髓创伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征肠综合征，肥胖症和2型糖尿病。

9. 发明授权

US09029371B2 Bisaryl (thio)morpholine derivatives as S1P modulators 有权
标题翻译：二芳基（硫代）吗啉衍生物作为S1P调节剂
公开(公告)号：US09029371B2
公开(公告)日：2015-05-12
申请号：US13808900
申请日：2011-07-08
申请人： Wouter I. Iwema Bakker , Raymond Bronger
发明人： Wouter I. Iwema Bakker , Raymond Bronger
IPC分类号： C07D295/15 , C07D265/30 , C07D413/10 , A61K31/5377 , A61K31/5375
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) 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-chlorophenyl]-4 -morpholineethanol. The compounds of the invention have affinity to S1 Preceptors and may be used in the treatment, alleviation or prevention of S1 Preceptor 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S1受体具有亲和力，可用于治疗，缓解或预防S1受体介导的疾病和病症。

10. 发明授权

US08722887B2 Sulfonylpyrazole and sulfonylpyrazoline carboxamidine derivatives as 5-HT6 antagonists 有权
标题翻译：磺酰基吡唑和磺酰吡唑啉甲脒衍生物作为5-HT6拮抗剂
公开(公告)号：US08722887B2
公开(公告)日：2014-05-13
申请号：US12706279
申请日：2010-02-16
申请人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Hiskias G. Keizer , Jan Zorgdrager , Martina A. W. Van Der Neut , Cornelis G. Kruse
发明人： Arnold Van Loevezijn , Wouter I. Iwema Bakker , Hiskias G. Keizer , Jan Zorgdrager , Martina A. W. Van Der Neut , Cornelis G. Kruse
IPC分类号： C07D231/06 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/10
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 compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from 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.
摘要翻译：本发明涉及作为5-HT 6受体的拮抗剂的通式（1）的化合物及其衍生物，其中符号具有说明书中给出的含义。本发明还涉及制备这些化合物的方法，可用于其合成的新型中间体，以及这些化合物和组合物的用途，特别是它们在将它们给予患者以达到治疗至少在疾病或病症上的治疗效果选自帕金森病，亨廷顿氏舞蹈病，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫症，强迫症，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，注意缺陷障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯二氮卓类药物的疼痛，疼痛，与脊髓创伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征肠综合征，肥胖症和2型糖尿病。

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