公开(公告)号：US09504680B2

公开(公告)日：2016-11-29

申请号：US14898773

申请日：2014-06-16

申请人： Lupin Limited

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Shridhar Keshav Adurkar ,  Dnyaneshwar Changdeo Bhanage ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： A61K31/4439 ,  C07D207/333 ,  C07D401/04 ,  A61K31/40 ,  A61K45/06 ,  C07D401/06

CPC分类号： A61K31/4439 ,  A61K31/40 ,  A61K45/06 ,  C07D207/333 ,  C07D401/04 ,  C07D401/06

摘要： Disclosed are compounds of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and m are as described herein, as modulators of the nicotinic acetylcholine receptors, particularly the α7 subtype, their tautomeric forms, stereoisomers, and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and combinations thereof with suitable other medicaments. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and/or treatment of disorders such as Alzheimer's disease, mild cognitive impairment, and senile dementia.

公开(公告)号：US09388196B2

公开(公告)日：2016-07-12

申请号：US14379134

申请日：2013-02-22

申请人： Lupin Limited

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Anil Kashiram Hajare ,  Shridhar Keshav Adurkar ,  Bikramjit Singh Lairikyengbam ,  Firoj Aftab Raje ,  Ajay Ramchandra Tilekar ,  Baban Rupaji Thube ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： A61K31/5377 ,  A61K31/5386 ,  A61K31/454 ,  A61K31/439 ,  A61K31/427 ,  C07D417/14 ,  C07D417/06 ,  C07D417/04 ,  C07D498/08 ,  C07D277/56 ,  C07D221/22 ,  A61K45/06

CPC分类号： C07D498/08 ,  A61K31/427 ,  A61K31/439 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/5386 ,  A61K45/06 ,  C07D221/22 ,  C07D277/56 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14

摘要： Disclosed is a compound of formula (I) wherein Y, Ring D, m and R1-R4 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the α7 subtype, in a subject in need thereof, as well as pharmaceutically acceptable salts, polymorphs, solvates, and isomers thereofs, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.

摘要翻译： 公开了其中Y，环D，m和R 1 -R 4如本文所述的式（I）化合物，作为需要其的受试者中烟碱乙酰胆碱受体，特别是α7亚型的调节剂，以及药学上可接受的盐 ，多晶型物，溶剂合物和异构体，单独使用或与合适的其它药物组合使用，以及含有这些化合物的药物组合物。 还公开了化合物的制备方法及其在治疗中的用途，特别是在诸如阿尔茨海默氏病，轻度认知障碍，老年痴呆等疾病的预防和治疗中。

公开(公告)号：US09617211B2

公开(公告)日：2017-04-11

申请号：US14655878

申请日：2014-01-13

申请人： Lupin Limited

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Anil Kashiram Hajare ,  Baban Rupaji Thube ,  Dnyaneshwar Changdeo Bhanage ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D207/333 ,  A61K45/06 ,  A61K31/403 ,  A61K31/40 ,  C07D403/06 ,  C07D207/33 ,  C07D207/416

CPC分类号： C07D207/333 ,  A61K31/40 ,  A61K31/403 ,  A61K45/06 ,  C07D207/33 ,  C07D207/416 ,  C07D403/06 ,  Y02A50/411

摘要： Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and m are as described herein, as a modulator of nicotinic acetylcholine receptors particularly α7 subtype, its tautomeric forms, its stereoisomers, its pharmaceutically acceptable salts, its pharmaceutical composition, and its combinations with suitable medicaments. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.

公开(公告)号：US20160107990A1

公开(公告)日：2016-04-21

申请号：US14894803

申请日：2014-06-02

申请人： LUPIN LIMITED

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Ajay Ramchandra Tilekar ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D207/335 ,  A61K45/06 ,  A61K31/40

CPC分类号： C07D207/335 ,  A61K31/40 ,  A61K45/06 ,  C07D207/333

摘要： Disclosed are an alpha 7 nAChR receptor modulator compound, 4-(5-(4-chlorophenyl)-2-(2-cyclopropylacetyl)-1,4-dimethyl-1H-pyrrol-3-yljbenzenesulfonamide, its tautomeric form, its pharmaceutically acceptable salts, pharmaceutical compositions comprising the compound or a salt thereof, and a method of treating various diseases, disorders or conditions, for example, Alzheimer's disease, mild cognitive impairment, senile dementia, vascular dementia, dementia of Parkinson's disease, and attention deficit disorder.

摘要翻译： 公开了α7nAChR受体调节剂化合物，4-（5-（4-氯苯基）-2-（2-环丙基乙酰基）-1,4-二甲基-1H-吡咯-3-基]苯磺酰胺，其互变异构形式，其药学上可接受的 盐，包含该化合物或其盐的药物组合物，以及治疗各种疾病，病症或病症例如阿尔茨海默病，轻度认知障碍，老年痴呆，血管性痴呆，帕金森病痴呆和注意缺陷障碍的方法。

公开(公告)号：US20150344422A1

公开(公告)日：2015-12-03

申请号：US14655476

申请日：2014-03-12

申请人： LUPIN LIMITED

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Shridhar Keshav Adurkar ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D207/323 ,  A61K45/06 ,  A61K31/401

CPC分类号： C07D207/323 ,  A61K31/401 ,  A61K45/06 ,  C07D207/34 ,  C07D401/04 ,  C07D403/06

摘要： Disclosed are compounds of the Formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and m are as described herein, as modulators of the nicotinic acetylcholine receptors, particularly the α7 subtype, their tautomeric forms, stereoisomers, and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and combinations thereof with suitable other medicaments. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and/or treatment of disorders such as Alzheimer's disease, mild cognitive impairment, and senile dementia.

摘要翻译： 公开了式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和m如本文所述，作为烟碱乙酰胆碱受体的调节剂，特别是α7亚型，其互变异构体形式，立体异构体， 及其药学上可接受的盐，药物组合物及其与合适的其它药物的组合。 还公开了化合物的制备方法及其在治疗中的预期用途，特别是在诸如阿尔茨海默氏病，轻度认知障碍和老年痴呆症的疾病的预防和/或治疗中。

公开(公告)号：US09617210B2

公开(公告)日：2017-04-11

申请号：US14655476

申请日：2014-03-12

申请人： Lupin Limited

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Shridhar Keshav Adurkar ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D207/323 ,  A61K45/06 ,  A61K31/401 ,  C07D401/04 ,  C07D403/06 ,  C07D207/34

CPC分类号： C07D207/323 ,  A61K31/401 ,  A61K45/06 ,  C07D207/34 ,  C07D401/04 ,  C07D403/06

摘要： Disclosed are compounds of the Formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and m are as described herein, as modulators of the nicotinic acetylcholine receptors, particularly the α7 subtype, their tautomeric forms, stereoisomers, and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and combinations thereof with suitable other medicaments. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and/or treatment of disorders such as Alzheimer's disease, mild cognitive impairment, and senile dementia.

公开(公告)号：US09393247B2

公开(公告)日：2016-07-19

申请号：US14705144

申请日：2015-05-06

申请人： Lupin Limited

发明人： Neelima Sinha ,  Gourhari Jana ,  Sachchidanand Sachchidanand ,  Sanjay Pralhad Kurhade ,  Navnath Popat Karche ,  Anil Kashiram Hajare ,  Ajay Ramchandra Tilekar ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： A61K31/40 ,  A61K31/381 ,  A61K31/341 ,  A61K31/5377 ,  A61K31/4535 ,  A61K45/06

CPC分类号： A61K31/5377 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/4436 ,  A61K31/4535 ,  A61K31/496 ,  A61K45/06 ,  C07D207/32 ,  C07D207/333 ,  C07D207/337 ,  C07D307/68 ,  C07D333/22 ,  C07D333/26 ,  C07D333/36 ,  C07D333/38 ,  C07D409/04 ,  A61K2300/00

摘要： Disclosed is a compound of formula I: wherein Z, m and R1-R6 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the α7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.

摘要翻译： 公开了式I化合物：其中Z，m和R 1 -R 6如本文所述，作为有需要的受试者中烟碱乙酰胆碱受体，特别是α7亚型的调节剂，以及类似物，前药，同位素取代的类似物 ，代谢产物，药学上可接受的盐，多晶型物，溶剂化物，异构体，包合物和共结晶，单独使用或与合适的其它药物组合使用，以及含有这些化合物和类似物的药物组合物。 还公开了化合物的制备方法及其在治疗中的用途，特别是在诸如阿尔茨海默氏病，轻度认知障碍，老年痴呆等疾病的预防和治疗中。

公开(公告)号：US20150361041A1

公开(公告)日：2015-12-17

申请号：US14655878

申请日：2014-01-13

申请人： LUPIN LIMITED

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Anil Kashiram Hajare ,  Baban Rupaji Thube ,  Dnyaneshwar Changdeo Bhanage ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D207/333 ,  A61K45/06 ,  A61K31/403 ,  A61K31/40 ,  C07D403/06

CPC分类号： C07D207/333 ,  A61K31/40 ,  A61K31/403 ,  A61K45/06 ,  C07D207/33 ,  C07D207/416 ,  C07D403/06 ,  Y02A50/411

摘要： Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and m are as described herein, as a modulator of nicotinic acetylcholine receptors particularly α7 subtype, its tautomeric forms, its stereoisomers, its pharmaceutically acceptable salts, its pharmaceutical composition, and its combinations with suitable medicaments. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.

摘要翻译： 公开了式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和m如本文所述，作为烟碱型乙酰胆碱受体的调节剂，特别是α7亚型，其互变异构形式，其立体异构体，其 药学上可接受的盐，其药物组合物及其与合适药物的组合。 还公开了化合物的制备方法及其在治疗中的用途，特别是在诸如阿尔茨海默氏病，轻度认知障碍，老年痴呆等疾病的预防和治疗中。

公开(公告)号：US20150299178A1

公开(公告)日：2015-10-22

申请号：US14439120

申请日：2013-11-11

申请人： LUPIN LIMITED

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Anil Kashiram Hajare ,  Baban Rupaji Thube ,  Firoj Aftab Raje ,  Dnyaneshwar Changdeo Bhanage ,  Sudhakar Maruti Balgude ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D417/06 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/439 ,  C07D277/24 ,  A61K31/426

CPC分类号： C07D417/06 ,  A61K31/426 ,  A61K31/439 ,  A61K31/4439 ,  A61K45/06 ,  C07D277/24 ,  C07D277/26 ,  C07D277/46 ,  C07D277/56 ,  C07D417/04

摘要： Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5 and m are as described herein, as a modulator of nicotinic acetylcholine receptors particularly α7 subtype, its tautomeric forms, its stereoisomers, its pharmaceutically acceptable salts, its pharmaceutical composition, and its combinations with suitable medicaments. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.

摘要翻译： 公开了式（I）化合物，其中R 1，R 2，R 3，R 4，R 5和m如本文所述，作为烟碱乙酰胆碱受体，特别是α7亚型，其互变异构形式，其立体异构体，其药学上可接受的盐， 其药物组合物及其与合适药物的组合。 还公开了化合物的制备方法及其在治疗中的用途，特别是在诸如阿尔茨海默氏病，轻度认知障碍，老年痴呆等疾病的预防和治疗中。

公开(公告)号：US09447037B2

公开(公告)日：2016-09-20

申请号：US14894803

申请日：2014-06-02

申请人： Lupin Limited

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Ajay Ramchandra Tilekar ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D207/335 ,  C07D207/333 ,  A61K31/40 ,  A61K45/06

CPC分类号： C07D207/335 ,  A61K31/40 ,  A61K45/06 ,  C07D207/333

摘要： Disclosed are an alpha 7 nAChR receptor modulator compound, 4-(5-(4-chlorophenyl)-2-(2-cyclopropylacetyl)-1,4-dimethyl-1H-pyrrol-3-yljbenzenesulfonamide, its tautomeric form, its pharmaceutically acceptable salts, pharmaceutical compositions comprising the compound or a salt thereof, and a method of treating various diseases, disorders or conditions, for example, Alzheimer's disease, mild cognitive impairment, senile dementia, vascular dementia, dementia of Parkinson's disease, and attention deficit disorder.

摘要翻译： 公开了α7nAChR受体调节剂化合物，4-（5-（4-氯苯基）-2-（2-环丙基乙酰基）-1,4-二甲基-1H-吡咯-3-基]苯磺酰胺，其互变异构形式，其药学上可接受的 盐，包含该化合物或其盐的药物组合物，以及治疗各种疾病，病症或病症例如阿尔茨海默病，轻度认知障碍，老年痴呆，血管性痴呆，帕金森病痴呆和注意缺陷障碍的方法。