公开(公告)号：US08933132B2

公开(公告)日：2015-01-13

申请号：US13979830

申请日：2012-01-19

申请人： David Norton ,  Daniele Andreotti ,  Simon E. Ward ,  Roberto Profeta ,  Simone Spada ,  Helen Susanne Price

发明人： David Norton ,  Daniele Andreotti ,  Simon E. Ward ,  Roberto Profeta ,  Simone Spada ,  Helen Susanne Price

IPC分类号： A61K31/10 ,  C07C317/32 ,  C07D471/14 ,  C07D487/14

CPC分类号： C07D471/14 ,  C07D487/14

摘要： The invention relates to novel piperazine compounds of formula (I): to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial, i.e. in particular to treat pain.

摘要翻译： 本发明涉及式（I）的新型哌嗪化合物：其制备方法; 含有该化合物的药物组合物; 以及在治疗中使用化合物治疗阻断Cav2.2钙通道的疾病是有益的，即特别是治疗疼痛。

公开(公告)号：US20140038976A1

公开(公告)日：2014-02-06

申请号：US13979830

申请日：2012-01-19

申请人： David Norton ,  Daniele Andreotti ,  Simon E. Ward ,  Roberto Profeta ,  Simone Spada ,  Helen Susanne Price

发明人： David Norton ,  Daniele Andreotti ,  Simon E. Ward ,  Roberto Profeta ,  Simone Spada ,  Helen Susanne Price

IPC分类号： C07D471/14

CPC分类号： C07D471/14 ,  C07D487/14

摘要： The invention relates to novel piperazine compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial, i.e. in particular to treat pain.

摘要翻译： 本发明涉及新型哌嗪化合物; 进行准备; 包含该化合物的药物组合物; 以及在治疗中使用化合物治疗阻断Cav2.2钙通道的疾病是有益的，即特别是治疗疼痛。

公开(公告)号：US20080167351A1

公开(公告)日：2008-07-10

申请号：US11816284

申请日：2006-02-13

申请人： Daniele Andreotti ,  Luca Arista ,  Francesca Cardullo ,  Simone Spada ,  Kevin Michael Thewlis ,  Simon Edward Ward

发明人： Daniele Andreotti ,  Luca Arista ,  Francesca Cardullo ,  Simone Spada ,  Kevin Michael Thewlis ,  Simon Edward Ward

IPC分类号： A61K31/44 ,  C07D213/02 ,  C07C311/01 ,  A61K31/18 ,  C07D333/02 ,  A61K31/381 ,  A61P25/18

CPC分类号： C07D277/64 ,  C07D213/42 ,  C07D213/61 ,  C07D213/65 ,  C07D317/58 ,  C07D333/20

摘要： This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.

摘要翻译： 本发明涉及通过新的式（I）化合物增强谷氨酸受体：本发明还涉及该衍生物在治疗由谷氨酸受体增强介导的疾病和病症中的用途，含有衍生物的组合物及其制备方法 。

公开(公告)号：US20090023757A1

公开(公告)日：2009-01-22

申请号：US11910990

申请日：2006-04-06

申请人： Daniele Andreotti ,  Sergio Bacchi ,  Monica Delpogetto ,  Simone Guelfi ,  Alcide Perboni ,  Arianna Ribecai ,  Simone Spada ,  Paolo Stabile ,  Marsia Tampieri

发明人： Daniele Andreotti ,  Sergio Bacchi ,  Monica Delpogetto ,  Simone Guelfi ,  Alcide Perboni ,  Arianna Ribecai ,  Simone Spada ,  Paolo Stabile ,  Marsia Tampieri

IPC分类号： A61K31/519 ,  C07D471/04 ,  A61P1/00 ,  C07D207/14

CPC分类号： C07D471/04 ,  C07D207/22

摘要： The present invention relates to a novel process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper.

摘要翻译： 本发明涉及通过由铜催化的偶联反应制备式（I）的中间体化合物来制备作为促肾上腺皮质激素释放因子（CRF）受体的有效和特异性拮抗剂的式（IA）化合物的新方法。

公开(公告)号：US07790758B2

公开(公告)日：2010-09-07

申请号：US11816284

申请日：2006-02-13

申请人： Daniele Andreotti ,  Luca Arista ,  Francesca Cardullo ,  Simone Spada ,  Kevin Michael Thewlis ,  Simon Edward Ward

发明人： Daniele Andreotti ,  Luca Arista ,  Francesca Cardullo ,  Simone Spada ,  Kevin Michael Thewlis ,  Simon Edward Ward

IPC分类号： C07D333/20 ,  C07D317/58 ,  C07D277/64 ,  C07D213/61 ,  C07D213/42 ,  C07D213/647 ,  C07D213/64 ,  C07D213/65 ,  C07C311/08 ,  A61K31/4418 ,  A61K31/428 ,  A61K31/381 ,  A61K31/36 ,  A61K31/277 ,  A61K31/18

CPC分类号： C07D277/64 ,  C07D213/42 ,  C07D213/61 ,  C07D213/65 ,  C07D317/58 ,  C07D333/20

摘要： This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.

摘要翻译： 本发明涉及通过新的式（I）化合物增强谷氨酸受体：本发明还涉及该衍生物在治疗由谷氨酸受体增强介导的疾病和病症中的用途，含有衍生物的组合物及其制备方法 。

公开(公告)号：US08778939B2

公开(公告)日：2014-07-15

申请号：US13498975

申请日：2010-09-27

申请人： Paula Louise Nichols ,  Andrew John Eatherton ,  Paul Bamborough ,  Karamjit Singh Jandu ,  Oliver James Philps ,  Daniele Andreotti

发明人： Paula Louise Nichols ,  Andrew John Eatherton ,  Paul Bamborough ,  Karamjit Singh Jandu ,  Oliver James Philps ,  Daniele Andreotti

IPC分类号： A61K31/5377 ,  A61K31/4406 ,  C07C235/56 ,  A61K31/167 ,  C07D237/20 ,  A61K31/50 ,  A61K31/4402 ,  C07D239/42 ,  A61K31/505

CPC分类号： C07C235/64 ,  C07D213/75 ,  C07D231/40 ,  C07D237/20 ,  C07D261/14 ,  C07D263/48 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.

摘要翻译： 本发明涉及抑制LRRK2激酶活性的新化合物，其制备方法，含有它们的组合物及其用于治疗特征为LRRK2激酶活性，特别是帕金森病和阿尔茨海默病的疾病的用途。

公开(公告)号：US5138048A

公开(公告)日：1992-08-11

申请号：US578949

申请日：1990-09-07

申请人： Bruno Tamburini ,  Alcide Perboni ,  Tino Rossi ,  Daniele Donati ,  Daniele Andreotti ,  Giovanni Gaviraghi ,  Stefano Biondi ,  Claudio Bismara

发明人： Bruno Tamburini ,  Alcide Perboni ,  Tino Rossi ,  Daniele Donati ,  Daniele Andreotti ,  Giovanni Gaviraghi ,  Stefano Biondi ,  Claudio Bismara

IPC分类号： C07D487/04 ,  A61K31/395 ,  A61K31/397 ,  A61K31/40 ,  A61K31/407 ,  A61P31/04 ,  C07C45/71 ,  C07C49/753 ,  C07D205/08 ,  C07D477/00 ,  C07D487/00 ,  C07F7/18

CPC分类号： C07D477/00 ,  C07C45/71 ,  C07C49/753 ,  C07D205/08 ,  C07F7/186 ,  Y02P20/55

摘要： Compounds of the general formula (I) ##STR1## in which: R.sub.1 represents a hydroxyl protecting group; andR.sub.2 represents a hydrogen or halogen atom, an azido group, a C.sub.1-3 alkyl group, a group (CH.sub.2).sub.m OR.sub.3 wherein m is zero or one and R.sub.3 represents a hydrogen atom or a hydroxyl protecting group, an azidoethoxy group, a protected hydroxyethoxy group or a group XR.sub.4 in which X is an oxygen atom or the group S(O).sub.n in which n is zero, 1 or 2 and R.sub.4 represents a C.sub.1-5 alkyl, C.sub.3-7 cycloalkyl or phenyl group or when X is oxygen or sulphur then R.sub.4 may also represent the group AlkNR.sub.5 R.sub.6 in which Alk represents a C.sub.2-6 straight or branched alkylene chain and R.sub.5 and R.sub.6 independently represent a hydrogen atom or C.sub.1-4 alkyl group or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached form a pyrrolidino or piperidino ring or the group NR.sub.5 R.sub.6 represents a protected amino group, or R.sub.2 represents the group (CH.sub.2).sub.m NR.sub.7 R.sub.8 in which m is zero or 1 and R.sub.7 and R.sub.8 independently represent a hydrogen atom or a C.sub.1-4 alkyl group or NR.sub.7 R.sub.8 represents a protected amino group, or R.sub.2 and the carbon atom to which it is attached represent a keto group or a ketal derivative thereof; and acid addition salts of such compounds containing basic centers.

公开(公告)号：US20120184553A1

公开(公告)日：2012-07-19

申请号：US13498975

申请日：2010-09-27

申请人： Paula Louise Nichols ,  Andrew John Eatherton ,  Paul Bamborough ,  Karamjit Singh Jandu ,  Oliver James Philps ,  Daniele Andreotti

发明人： Paula Louise Nichols ,  Andrew John Eatherton ,  Paul Bamborough ,  Karamjit Singh Jandu ,  Oliver James Philps ,  Daniele Andreotti

IPC分类号： A61K31/5377 ,  A61K31/4406 ,  C07C235/56 ,  A61K31/167 ,  C07D237/20 ,  A61K31/50 ,  A61K31/4402 ,  C07D239/42 ,  A61K31/505 ,  C07D401/12 ,  A61K31/4545 ,  A61K31/496 ,  C07D413/12 ,  A61P25/16 ,  C07D213/75

CPC分类号： C07C235/64 ,  C07D213/75 ,  C07D231/40 ,  C07D237/20 ,  C07D261/14 ,  C07D263/48 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.

摘要翻译： 本发明涉及抑制LRRK2激酶活性的新化合物，其制备方法，含有它们的组合物及其用于治疗特征为LRRK2激酶活性，特别是帕金森病和阿尔茨海默病的疾病的用途。

公开(公告)号：US06900183B2

公开(公告)日：2005-05-31

申请号：US10450886

申请日：2001-12-20

申请人： Daniele Andreotti ,  Stefano Biondi ,  Sergio Lociuro

发明人： Daniele Andreotti ,  Stefano Biondi ,  Sergio Lociuro

IPC分类号： A01N25/34 ,  A01N43/22 ,  A01N63/02 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  A61K31/70

CPC分类号： C07H17/08 ,  A61K9/0019 ,  A61K9/2018

摘要： 11,12 γ lactone ketolides of the following formula: and pharmaceutically acceptable salts and solvates thereof, wherein R, R1, R2, and R3 are as described herein. The disclosure also relates to processes for the preparation of such compounds, to compositions containing them, and to their use in the therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.

摘要翻译： 具有下式的11,12个γ-内酯酮内酯及其药学上可接受的盐和溶剂合物，其中R 1，R 2，R 2和R 3， SUB>如本文所述。 本公开还涉及制备这些化合物的方法，含有它们的组合物及其在治疗或预防人或动物体内的全身或局部细菌感染中的用途。

公开(公告)号：US06531466B2

公开(公告)日：2003-03-11

申请号：US09781292

申请日：2001-02-13

申请人： Tino Rossi ,  Daniele Andreotti ,  Giovanna Tedesco ,  Luca Tarsi ,  Emiliangelo Ratti ,  Aldo Feriani ,  Domenica Antonia Pizzi ,  Giovanni Gaviraghi ,  Stefano Biondi ,  Gabriella Finizia

发明人： Tino Rossi ,  Daniele Andreotti ,  Giovanna Tedesco ,  Luca Tarsi ,  Emiliangelo Ratti ,  Aldo Feriani ,  Domenica Antonia Pizzi ,  Giovanni Gaviraghi ,  Stefano Biondi ,  Gabriella Finizia

IPC分类号： C07D47714

CPC分类号： C07D477/00

摘要： A compound of formula (I), salts and metabolically labile esters thereof, wherein R represents optionally substituted aryl or heteroaryl group; A represents a propylene chain or A is a chain of 3 members one of which is selected from an oxygen or sulphur atom or the group NH or a substituted derivative thereof and the other two members are methylene groups, having antibacterial activity, processes for their preparation and to their use in medicine.

摘要翻译： 式（I）的化合物，其盐和代谢不稳定的酯，其中R表示任选取代的芳基或杂芳基; A表示丙烯链或A是3个成员的链，其中一个选自氧或硫原子，或NH基或其取代衍生物，另外两个成员是具有抗菌活性的亚甲基，其制备方法 并用于医学。