公开(公告)号：US09072731B2

公开(公告)日：2015-07-07

申请号：US14000829

申请日：2012-02-22

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

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

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 analogs, 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 analogs. 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：US20080242676A1

公开(公告)日：2008-10-02

申请号：US12137170

申请日：2008-06-11

申请人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

发明人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

IPC分类号： A61K31/496 ,  C07D403/02 ,  C12N1/00 ,  C12N1/20 ,  A61P31/04

CPC分类号： C07D207/335 ,  C07D207/32 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).

摘要翻译： 式（I）的新型吡咯衍生物及其药学上可接受的酸加成盐对临床敏感性以及抗结核分枝杆菌菌株具有优异的抗分枝杆菌活性，并且与已知化合物相比具有较小的毒性。 使用式（I）的新化合物用于治疗潜在结核病，包括多药耐药性结核病（MDR TB）。 制备新化合物的方法，含有新化合物的药物组合物和通过施用式（I）化合物治疗MDR TB的方法。

公开(公告)号：US20140018327A1

公开(公告)日：2014-01-16

申请号：US14007458

申请日：2012-03-27

申请人： Neelima Sinha ,  Gourhari Jana ,  Ajay Ramchandra Tilekar ,  Navnath Popat Karche ,  Venkata P. Palle ,  Rajender Kumar Kamboj

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

IPC分类号： C07D207/34 ,  A61K45/06 ,  C07D207/335 ,  A61K31/635

CPC分类号： C07D207/34 ,  A61K31/402 ,  A61K31/635 ,  A61K45/06 ,  C07D207/333 ,  C07D207/335 ,  Y02A50/411 ,  A61K2300/00

摘要： Disclosed is a compound of formula (I) wherein ‘a’ and R1-R5 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 thereofs, 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“a”和R1-R5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 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：US07763602B2

公开(公告)日：2010-07-27

申请号：US12137170

申请日：2008-06-11

申请人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

发明人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

IPC分类号： A01N43/00 ,  A01N43/36 ,  A01N43/50 ,  A01N43/62 ,  A01N43/76 ,  A61K31/00 ,  A61K31/40 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  A61K31/445 ,  A61K31/497 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55

CPC分类号： C07D207/335 ,  C07D207/32 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).

摘要翻译： 式（I）的新型吡咯衍生物及其药学上可接受的酸加成盐对临床敏感性以及抗结核分枝杆菌菌株具有优异的抗分枝杆菌活性，并且与已知化合物相比具有较小的毒性。 使用式（I）的新化合物用于治疗潜在结核病，包括多药耐药性结核病（MDR TB）。 制备新化合物的方法，含有新化合物的药物组合物和通过施用式（I）化合物治疗MDR TB的方法。

公开(公告)号：US07691837B2

公开(公告)日：2010-04-06

申请号：US10497615

申请日：2002-09-20

申请人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

发明人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

IPC分类号： A01N43/00 ,  A01N43/40 ,  A61K31/33 ,  A61K31/55 ,  A61K31/497 ,  A61K31/435 ,  C07D223/00 ,  C07D243/00 ,  C07D241/04 ,  C07D295/00 ,  C07D213/00

CPC分类号： C07D207/335 ,  C07D207/32 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).

公开(公告)号：US09187420B2

公开(公告)日：2015-11-17

申请号：US14007458

申请日：2012-03-27

申请人： Neelima Sinha ,  Gourhari Jana ,  Ajay Ramchandra Tilekar ,  Navnath Popat Karche ,  Venkata P. Palle ,  Rajender Kumar Kamboj

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

IPC分类号： C07D207/333 ,  C07D207/34 ,  A61K31/402 ,  A61K45/06 ,  A61K31/635 ,  C07D207/335

CPC分类号： C07D207/34 ,  A61K31/402 ,  A61K31/635 ,  A61K45/06 ,  C07D207/333 ,  C07D207/335 ,  Y02A50/411 ,  A61K2300/00

摘要： Disclosed is a compound of formula (I) wherein ‘a’ and R1-R5 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the α7 subtype, in a subject in need thereof, as well as analogs, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereofs, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogs. 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“a”和R1-R5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 类似物，代谢物，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，用于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：US20130331387A1

公开(公告)日：2013-12-12

申请号：US14000829

申请日：2012-02-22

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

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： C07D409/04 ,  A61K31/381 ,  A61K45/06 ,  C07D333/26 ,  A61K31/5377 ,  A61K31/341 ,  A61K31/4436 ,  A61K31/404 ,  C07D207/333 ,  A61K31/40 ,  A61K31/4535 ,  C07D307/68 ,  C07D333/22 ,  A61K31/496

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，代谢物，药学上可接受的盐，多晶型物，溶剂合物，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：US20130310419A1

公开(公告)日：2013-11-21

申请号：US13983362

申请日：2012-01-31

申请人： Neelima Sinha ,  Gourhari Jana ,  Navnath Popat Karche ,  Shridhar Keshav Adurkar ,  Girish Dhanraj Hatnapure ,  Venkata P. Palle ,  Rajender Kumar Kamboj

发明人： Neelima Sinha ,  Gourhari Jana ,  Navnath Popat Karche ,  Shridhar Keshav Adurkar ,  Girish Dhanraj Hatnapure ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D207/333 ,  A61K31/4025 ,  A61K31/4709 ,  A61K31/402 ,  C07D401/04 ,  A61K31/4725 ,  C07D405/04 ,  A61K45/06

CPC分类号： C07D207/333 ,  A61K31/402 ,  A61K31/4025 ,  A61K31/4709 ,  A61K31/4725 ,  A61K45/06 ,  C07D401/04 ,  C07D405/04

摘要： The present invention is related to pyrrole derivatives of formula I as the modulators of nicotinic acetylcholine receptors particularly the α7 subtype. The invention includes pyrrole derivatives, analogues, their prodrugs, their isotopes, their metabolites, pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament and pharmaceutical compositions thereof. The present invention also includes process of preparation of the said compounds and intended use in therapy of them. Owing to the modulatory activity of the pyrrole derivatives on the nicotinic acetylcholine receptors, the invention finds application in the prophylaxis and therapy of disorders encompassing the involvement of cholinergic transmission in the central and peripheral nervous system. The invention relates to the ability of pyrrole derivatives to modulate the cholinergic transmission and efficacy of the endogenous neurotransmitter ACh thorough the nicotinic acetylcholine receptors particularly the α7 subtype.

摘要翻译： 本发明涉及式I的吡咯衍生物作为烟碱乙酰胆碱受体的调节剂，特别是α7亚型。 本发明包括吡咯衍生物，类似物，其前药，其同位素，其代谢物，药学上可接受的盐，多晶型物，溶剂合物，旋光异构体，包合物，共晶体，与合适的药物的组合及其药物组合物。 本发明还包括制备所述化合物的方法和用于治疗它们的预期用途。 由于吡咯衍生物对烟碱乙酰胆碱受体的调节活性，本发明可用于预防和治疗包括胆碱能传递在中枢和周围神经系统中的疾病。 本发明涉及吡咯衍生物通过烟碱乙酰胆碱受体，特别是α7亚型调节内源性神经递质ACh的胆碱能传递和功效的能力。

公开(公告)号：US20050107370A1

公开(公告)日：2005-05-19

申请号：US10497615

申请日：2002-09-20

申请人： Sudershan Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Sinha

发明人： Sudershan Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Sinha

IPC分类号： A61P31/06 ,  C07D207/32 ,  C07D207/335 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06 ,  C07D417/02 ,  A61K31/4025 ,  A61K31/426 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  C07D413/02 ,  C07D43/02

CPC分类号： C07D207/335 ,  C07D207/32 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).

摘要翻译： 式（I）的新型吡咯衍生物及其药学上可接受的酸加成盐对临床敏感性以及抗结核分枝杆菌菌株具有优异的抗分枝杆菌活性，并且与已知化合物相比具有较小的毒性。 使用式（I）的新化合物用于治疗潜在结核病，包括多药耐药性结核病（MDR TB）。 制备新化合物的方法，含有新化合物的药物组合物和通过施用式（I）化合物治疗MDR TB的方法。