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1. 发明申请

WO2006094843A1 PIPERAZINE DERIVATIVES AS GLYT1 INHIBITORS 审中-公开
标题翻译：哌嗪衍生物作为GLYT1抑制剂
公开(公告)号：WO2006094843A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/002485
申请日：2006-03-09
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
IPC分类号： C07D295/18 , C07D239/42 , C07D241/44 , C07D215/38 , C07D487/04 , C07D213/85 , C07D213/73 , C07D213/75 , A61P25/00 , A61K31/495 , A61K31/5377 , A61K31/4709 , A61K31/444 , A61K31/437 , A61K31/498
CPC分类号： C07D213/73 , C07D213/75 , C07D213/85 , C07D215/38 , C07D239/42 , C07D241/44 , C07D295/192 , C07D487/04
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R 1 , n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
摘要翻译：本发明提供式（I）化合物或其盐或溶剂化物：其中R 1，n，X，Y和Z如说明书中所定义，以及这些化合物的用途。该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍，包括精神分裂症。

2. 发明申请

WO2010142652A1 IMIDAZOBENZAZEPINE COMPOUNDS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM (CNS) DISEASES 审中-公开
标题翻译：用于治疗中枢神经系统（CNS）的IMIDAZOBENZAZEPINE化合物
公开(公告)号：WO2010142652A1
公开(公告)日：2010-12-16
申请号：PCT/EP2010/057948
申请日：2010-06-08
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , GIANOTTI, Massimo , LESLIE, Colin Philip , STASI, Luigi Piero
发明人： DI FABIO, Romano , GIANOTTI, Massimo , LESLIE, Colin Philip , STASI, Luigi Piero
IPC分类号： C07D487/04 , A61K31/55 , A61P25/00
CPC分类号： C07D487/04 , A61K31/55 , A61K45/06 , A61K2300/00
摘要： This invention relates to novel novel imidazobenzazepine derivatives of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.
摘要翻译：本发明涉及用于治疗中枢神经系统（CNS）的疾病和病症，特别是睡眠障碍的式（I）的新颖的咪唑并氮吖庚因衍生物或其药学上可接受的盐。

3. 发明申请

WO2005014552A1 QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING AFFINITY FOR 5HT1-TYPE RECEPTORS 审中-公开
标题翻译：具有5HT1型受体亲和力的喹啉和喹唑啉衍生物
公开(公告)号：WO2005014552A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008000
申请日：2004-07-15
申请人： GLAXO GROUP LIMITED , BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BROMIDGE, Steven Mark , FALCHI, Alessandro , LESLIE, Colin Philip , MERLO, Giancarlo , PIZZI, Domenica Antonia , RINALDI, Marilisa , STASI, Luigi Piero , TIBASCO, Jessica , VONG, Antonio, Kuok, Keong , WARD, Simon, Edward
发明人： BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BROMIDGE, Steven Mark , FALCHI, Alessandro , LESLIE, Colin Philip , MERLO, Giancarlo , PIZZI, Domenica Antonia , RINALDI, Marilisa , STASI, Luigi Piero , TIBASCO, Jessica , VONG, Antonio, Kuok, Keong , WARD, Simon, Edward
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , C04B35/632
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R 1 , m, X, R 2 , n, W, p, Y, Z, R 3 , R 4 , R 5 and q have the meanings as defined in the description. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression or anxiety, are also disclosed.
摘要翻译：提供式（I）化合物及其药学上可接受的盐：其中R1，m，X，R2，n，W，p，Y，Z，R3，R4，R5和q具有如说明书中所定义的含义。还公开了其治疗方法及其在治疗中的用途，特别是CNS疾病如抑郁或焦虑症。

4. 发明申请

WO2013004291A1 CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR AGONISTS 审中-公开
标题翻译：循环胺衍生物作为EP4受体激动剂
公开(公告)号：WO2013004291A1
公开(公告)日：2013-01-10
申请号：PCT/EP2011/061229
申请日：2011-07-04
申请人： ROTTAPHARM S.P.A. , BORRIELLO, Manuela , PUCCI, Sabrina , STASI, Luigi Piero , ROVATI, Lucio
发明人： BORRIELLO, Manuela , PUCCI, Sabrina , STASI, Luigi Piero , ROVATI, Lucio
IPC分类号： A61K31/401 , C07D207/10 , A61P19/10
CPC分类号： C07F1/02 , C07D207/16 , C07D211/60
摘要： There is described a group of novel cyclic amine derivative compounds having an EP 4 receptor agonistic activity. Specifically, the compounds according to the invention are provided with analgesic, antiinflammatory, antiglaucoma activity, and also with anti-osteoporosis and antiulcerative activity. The present invention therefore relates to novel cyclic amine derivative compounds, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as pain, glaucoma, ulcerative colitis and osteoporosis.
摘要翻译：描述了一组具有EP4受体激动活性的新型环胺衍生物化合物。具体地说，根据本发明的化合物具有止痛，抗炎，抗青光眼活性，并具有抗骨质疏松和抗溃疡活性。因此，本发明涉及新型环胺衍生物化合物，其制备方法，含有它们的药物组合物及其作为药物的用途，特别是用于治疗或缓解前列腺素E介导的疾病如疼痛，青光眼，溃疡性结肠炎和骨质疏松症。

5. 发明申请

WO2013004290A1 CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：循环胺衍生物作为EP4受体拮抗剂
公开(公告)号：WO2013004290A1
公开(公告)日：2013-01-10
申请号：PCT/EP2011/061226
申请日：2011-07-04
申请人： ROTTAPHARM S.P.A. , BORRIELLO, Manuela , PUCCI, Sabrina , STASI, Luigi, Piero , ROVATI, Lucio
发明人： BORRIELLO, Manuela , PUCCI, Sabrina , STASI, Luigi, Piero , ROVATI, Lucio
IPC分类号： C07D207/16 , C07D209/52 , C07D209/54 , C07D211/60 , C07D221/04 , C07D453/06 , A61K31/453 , A61P29/00 , A61K31/40
CPC分类号： C07F1/02 , C07D205/04 , C07D207/16 , C07D209/52 , C07D209/54 , C07D211/34 , C07D211/60 , C07D221/04 , C07D221/20 , C07D401/06 , C07D453/06 , C07D471/08 , C07F7/1852 , C07F7/1856
摘要： There is described a novel group of cyclic amine derivative compounds, having an EP 4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP 4 subtype of PGE 2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
摘要翻译：描述了具有EP4受体拮抗活性的新型一组环胺衍生物化合物，特别是可用于治疗或缓解前列腺素E介导的疾病的药物化合物。因此，本发明涉及作为具有止痛和抗炎活性的PGE 2受体的EP4亚型的选择性拮抗剂的新化合物，其制备方法，含有它们的药物组合物及其作为药物的用途，尤其用于治疗或缓解前列腺素E 介导的疾病如急性和慢性疼痛，骨关节炎，作为关节炎的炎症相关疾病，类风湿性关节炎，癌症，偏头痛和子宫内膜异位症。

6. 发明申请

WO2012104338A1 SPIRO AMINIC COMPOUNDS WITH NK1 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有NK1拮抗剂活性的SPIRO氨基化合物
公开(公告)号：WO2012104338A1
公开(公告)日：2012-08-09
申请号：PCT/EP2012/051661
申请日：2012-02-01
申请人： ROTTAPHARM S.P.A. , STASI, Luigi Piero , ROVATI, Lucio
发明人： STASI, Luigi Piero , ROVATI, Lucio
IPC分类号： C07D401/12 , C07D401/14 , A61K31/438 , A61K31/444 , A61P1/00
CPC分类号： A61K31/506 , A61K31/444 , C07D401/12 , C07D401/14
摘要： The invention concerns a spiro-amino compound of Formula (I), wherein A is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring containing 1 to 3 nitrogen atom; X is a substituent selected from the group consisting of (C 1 -C 3 )alkyl and halogen, Y is a substituent selected from the group consisting of halogen and trifluoromethyl or a pharmaceutically acceptable salt thereof for use in the treatment of pathologies which require an antagonist of the NK1 receptor.
摘要翻译：本发明涉及式（I）的螺 - 氨基化合物，其中A选自5或6元芳环和含有1至3个氮原子的5或6元杂芳环; X是选自（C 1 -C 3）烷基和卤素的取代基，Y是选自卤素和三氟甲基的取代基或其药学上可接受的盐，其用于治疗需要拮抗剂 NK1受体。

7. 发明申请

WO2011006960A1 SPIRO AMINO COMPOUNDS SUITABLE FOR THE TREATMENT OF INTER ALIA SLEEP DISORDERS AND DRUG ADDICTION 审中-公开
标题翻译：适用于治疗间歇性睡眠障碍和药物治疗的SPIRO AMINO化合物
公开(公告)号：WO2011006960A1
公开(公告)日：2011-01-20
申请号：PCT/EP2010/060206
申请日：2010-07-15
申请人： ROTTAPHARM S.P.A. , STASI, Luigi, Piero , ROVATI, Lucio
发明人： STASI, Luigi, Piero , ROVATI, Lucio
IPC分类号： C07D401/12 , C07D401/14 , C07D417/06 , C07D417/14 , A61K31/438 , A61P25/30
CPC分类号： C07D417/14 , C07D401/12 , C07D401/14 , C07D417/06
摘要： The invention concerns a spiro-amino compound of Formula (Vl) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O e N, such ring being substituted with one or two substituents selected from the group consisting of (C 1 -C 3 )alkyl, halogen, (C 3 -C 5 )cycloalkyloxy, (C 1 -C 3 )alkylcarbonyl, phenyl optionally substituted with one or more halogen atoms, a 5- or 6-membered heterocycle comprising at least one nitrogen atom; P is a substituent Q or COQ, wherein Q is selected from the group consisting of phenyl, pyridil, pyrimidil, quinolyl, isoquinolyl, quinoxalyl, benzofuranyl, imidazotriazolyl, being such Q optionally substituted with one or more substituents selected from the group consisting of (C 1 -C 3 )alkyl, halogen, trifluoromethyl, carbammido, methylcarbammido, carboxy, methylcarboxy or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式（VI）的螺 - 氨基化合物，其中m为1或2或3，n为1或2，R选自5-或6-元芳环和5-或6-元杂芳族环，其包含1至3个选自S，O e N的杂原子，该环被一个或两个选自（C 1 -C 3）烷基，卤素，（C 3 -C 5）环烷氧基，（C 1 -C 3）烷基羰基，任选被一个或多个卤素原子取代的苯基，含有至少一个氮原子的5-或6-元杂环; P是取代基Q或COQ，其中Q选自苯基，吡啶基，嘧啶基，喹啉基，异喹啉基，喹喔啉基，苯并呋喃基，咪唑并三唑基，任选地被一个或多个选自以下的取代基取代： C 1 -C 3）烷基，卤素，三氟甲基，碳酰氨基，甲基氨基甲酰基，羧基，甲基羧基或其药学上可接受的盐。

8. 发明申请

WO2009124956A1 PYRIDINE DERIVATIVES USED TO TREAT OREXIN RELATED DISORDERS 审中-公开
标题翻译：用于治疗OREXIN相关疾病的吡啶衍生物
公开(公告)号：WO2009124956A1
公开(公告)日：2009-10-15
申请号：PCT/EP2009/054189
申请日：2009-04-08
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , AMANTINI, David , STASI, Luigi, Piero
发明人： ALVARO, Giuseppe , AMANTINI, David , STASI, Luigi, Piero
IPC分类号： C07D401/12 , A61K31/4545 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/30
CPC分类号： C07D401/12
摘要： This invention relates to pyridinamine methyl substituded piperidinyl derivatives I and their use as pharmaceuticals.
摘要翻译：本发明涉及吡啶胺甲基取代哌啶衍生物I及其作为药物的用途。

9. 发明申请

WO2006094840A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2006094840A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/002480
申请日：2006-03-09
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
IPC分类号： C07D295/18 , A61P25/00 , A61K31/495
CPC分类号： C07D295/192
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R 1 , n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
摘要翻译：本发明提供式（I）化合物或其盐或溶剂化物：其中R 1，n，X，Y和Z如说明书中所定义，以及这些化合物的用途。该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍，包括精神分裂症。

10. 发明申请

WO2012076063A1 PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡啶酰胺衍生物作为EP4受体拮抗剂
公开(公告)号：WO2012076063A1
公开(公告)日：2012-06-14
申请号：PCT/EP2010/069355
申请日：2010-12-10
申请人： ROTTAPHARM S.P.A. , BORRIELLO, Manuela , ROVATI, Lucio , STASI, Luigi Piero , BUZZI, Benedetta , COLACE, Fabrizio
发明人： BORRIELLO, Manuela , ROVATI, Lucio , STASI, Luigi Piero , BUZZI, Benedetta , COLACE, Fabrizio
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , A61K31/4439 , A61P29/00
CPC分类号： C07D413/14 , C07D401/04 , C07D401/14
摘要： The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is -O-, -O(C1-C3 alkyl)-; -(C1-C3 alkyl)O-; -C(O)-; -C(=N-O(C1-C3 alkyl))-; -NH- or -NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, -NH(C1-C3alkyl)-; -N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is convalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-membered heteroaromatic ring containing 1 to 3 heteroatoms selected from S, O e N, such heteroaromatic ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl. The compounds of the invention could be used for manufacturing a medicament for the treatment of pathologies which require the use of an antagonist of the EP4 receptor, such as the treatment of acute and chronic pain, inflammatory pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid artrhritis, cancer, endometriosis and migraine.
摘要翻译：本发明涉及式（I）的吡啶酰胺衍生物或其药学上可接受的盐，其中R 1和R 2独立地为氢，直链或支链（C 1 -C 3）烷基或连接在一起形成环丙基环; R独立地选自卤素和三氟甲基，p是1,2或3; A是C或N; E是式（B）或（C）的基团，其中B是C（O）OH，C（O）O（C1-C3）烷基，C选自式（I） 1,2或3，n为0或1，W为-O - ， - O（C 1 -C 3烷基） - ; - （C 1 -C 3烷基）O-; -C（O） - ; -C（= N-O（C 1 -C 3烷基）） - ; -NH-或-NH（C 1 -C 3烷基） - ; Ar是任选被一个或多个选自卤素，三氟甲基，三氟甲氧基，甲基，-NH（C 1 -C 3烷基） - 的取代基取代的苯基。 -N（C 1 -C 3烷基）（C 1 -C 3烷基） - ，含有一个与Ar共价结合的氮原子的5至7元杂环，并任选地含有一个或两个选自N，O和S的杂原子; 和含有1至3个选自S，O e N的杂原子的5或6元杂芳环，所述杂芳环被一个或两个选自（C 1 -C 3）烷基，（C 3 -C 5））环烷基氧基，（C1-C3）烷基羰基。本发明的化合物可用于制备用于治疗需要使用EP4受体拮抗剂的病症的药物，例如治疗急性和慢性疼痛，炎性疼痛，骨关节炎，炎症相关疾病作为关节炎，类风湿性肾炎，癌症，子宫内膜异位症和偏头痛。

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