公开(公告)号：US20140155433A1

公开(公告)日：2014-06-05

申请号：US14130815

申请日：2012-07-02

申请人： Neelima Sinha ,  Navnath Popat Karche ,  Girish Dhanraj Hatnapure ,  Anil Kashiram Hajare ,  Venkata P. Palle ,  Rajender Kumar Kamboj

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Girish Dhanraj Hatnapure ,  Anil Kashiram Hajare ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D277/56 ,  A61K31/381 ,  A61K31/454 ,  C07D417/12 ,  A61K45/06 ,  C07D277/28 ,  A61K31/426 ,  C07D207/335 ,  A61K31/40 ,  C07D333/22 ,  A61K31/427

CPC分类号： C07D277/56 ,  A61K31/381 ,  A61K31/40 ,  A61K31/401 ,  A61K31/4025 ,  A61K31/4164 ,  A61K31/426 ,  A61K31/427 ,  A61K31/454 ,  A61K45/06 ,  C07D207/335 ,  C07D277/28 ,  C07D277/30 ,  C07D333/22 ,  C07D417/12 ,  A61K2300/00

摘要： Disclosed is a compound of formula (I): wherein ‘D’, ‘E’, ‘m’, ‘n’ 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 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）的化合物：其中'D'，'E'，'m'，'n'和R1-R4如本文所述，作为烟草乙酰胆碱受体的调节剂，特别是α7亚型， 需要它们以及类似物，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，以及药物组合物 含有这些化合物和类似物。 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：US08946432B2

公开(公告)日：2015-02-03

申请号：US14130815

申请日：2012-07-02

申请人： Neelima Sinha ,  Navnath Popat Karche ,  Girish Dhanraj Hatnapure ,  Anil Kashiram Hajare ,  Venkata P. Palle ,  Rajender Kumar Kamboj

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Girish Dhanraj Hatnapure ,  Anil Kashiram Hajare ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D207/335 ,  C07D277/28 ,  C07D333/22 ,  C07D417/12 ,  C07D277/56 ,  A61K31/381 ,  A61K31/401 ,  A61K31/4025 ,  A61K31/426 ,  C07D277/30 ,  A61K45/06 ,  A61K31/4164 ,  A61K31/40 ,  A61K31/427 ,  A61K31/454

CPC分类号： C07D277/56 ,  A61K31/381 ,  A61K31/40 ,  A61K31/401 ,  A61K31/4025 ,  A61K31/4164 ,  A61K31/426 ,  A61K31/427 ,  A61K31/454 ,  A61K45/06 ,  C07D207/335 ,  C07D277/28 ,  C07D277/30 ,  C07D333/22 ,  C07D417/12 ,  A61K2300/00

摘要： Disclosed is a compound of formula (I): wherein ‘D’, ‘E’, ‘m’, ‘n’ 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 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）的化合物：其中'D'，'E'，'m'，'n'和R1-R4如本文所述，作为烟草乙酰胆碱受体的调节剂，特别是α7亚型， 需要它们以及类似物，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，以及药物组合物 含有这些化合物和类似物。 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：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：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：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：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：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：US20130225600A1

公开(公告)日：2013-08-29

申请号：US13882567

申请日：2011-10-31

申请人： Nageswara Rao Irlapati ,  Gokul Keruji Deshmukh ,  Vijay Pandurang Karche ,  Santosh Madhukar Jachak ,  Neelima Sinha ,  Venkata P. Palle ,  Rajender Kumar Kamboj

发明人： Nageswara Rao Irlapati ,  Gokul Keruji Deshmukh ,  Vijay Pandurang Karche ,  Santosh Madhukar Jachak ,  Neelima Sinha ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D417/14 ,  C07D261/12 ,  C07D413/14 ,  C07D413/10

CPC分类号： A61K31/497 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/496 ,  C07D261/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14

摘要： The present invention relates to compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).

摘要翻译： 本发明涉及式（I）化合物及其制备方法，其可用于治疗，预防和/或控制与调节CRAC相关的疾病，病症，综合征或病症。 本发明还涉及治疗，预防管理和/或减轻与调节式（I）的CRAC相关的疾病，病症，综合征或病症的方法。

公开(公告)号：US09169242B2

公开(公告)日：2015-10-27

申请号：US13882567

申请日：2011-10-31

申请人： Nageswara Rao Irlapati ,  Gokul Keruji Deshmukh ,  Vijay Pandurang Karche ,  Santosh Madhukar Jachak ,  Neelima Sinha ,  Venkata P. Palle ,  Rajender Kumar Kamboj

发明人： Nageswara Rao Irlapati ,  Gokul Keruji Deshmukh ,  Vijay Pandurang Karche ,  Santosh Madhukar Jachak ,  Neelima Sinha ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D271/113 ,  A61K31/4245 ,  A61P17/06 ,  A61P19/02 ,  A61P35/00 ,  C07D261/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  A61K31/497

CPC分类号： A61K31/497 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/496 ,  C07D261/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14

摘要： The present invention relates to compounds that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC and to processes for preparing these compounds. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC by these compounds.

摘要翻译： 本发明涉及可用于治疗，预防和/或治疗与调节CRAC相关的疾病，病症，综合征或病症的化合物及其制备方法。 本发明还涉及治疗，预防和/或减轻与这些化合物调节CRAC相关的疾病，病症，综合征或病症的方法。

公开(公告)号：US09464063B2

公开(公告)日：2016-10-11

申请号：US14005944

申请日：2012-03-16

申请人： Manojkumar Ramprasad Shukla ,  Sarde Gangaram Ankush ,  Pachpute Dilip Vipul ,  Majid Bashir Sayyed ,  Mahadeo Bhaskar Tryambake ,  Chetan Sanjay Pawar ,  Ganesh Navinchandra Gote ,  Sanjeev Anant Kulkarni ,  Venkata P. Palle ,  Rajender Kumar Kamboj

发明人： Manojkumar Ramprasad Shukla ,  Sarde Gangaram Ankush ,  Pachpute Dilip Vipul ,  Majid Bashir Sayyed ,  Mahadeo Bhaskar Tryambake ,  Chetan Sanjay Pawar ,  Ganesh Navinchandra Gote ,  Sanjeev Anant Kulkarni ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D265/36 ,  C07D413/04 ,  A61K31/538

CPC分类号： C07D265/36 ,  A61K31/538 ,  C07D413/04

摘要： Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I).