公开(公告)号：WO2012127385A1

公开(公告)日：2012-09-27

申请号：PCT/IB2012/051263

申请日：2012-03-16

申请人： LUPIN LIMITED ,  SHUKLA, Manojkumar, Ramprasad ,  ANKUSH, Sarde, Gangaram ,  VIPUL, Pachpute, Dilip ,  KULKARNI, Sanjeev, Anant ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, Kumar

发明人： SHUKLA, Manojkumar, Ramprasad ,  ANKUSH, Sarde, Gangaram ,  VIPUL, Pachpute, Dilip ,  KULKARNI, Sanjeev, Anant ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, Kumar

IPC分类号： C07D413/04 ,  C07D265/36 ,  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 (Ca SR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (Ca SR) receptors of Formula (I).

摘要翻译： 式（I）的化合物及其制备方法，其可用于治疗，治疗和/或减轻与钙感觉（Ca SR）受体调节相关的疾病，病症，综合征或病症。 治疗，治疗和/或减轻与调节式（I）的钙敏感（Ca SR））受体相关的疾病，病症，综合征或病症的方法。

公开(公告)号：WO2012104782A1

公开(公告)日：2012-08-09

申请号：PCT/IB2012/050442

申请日：2012-01-31

申请人： LUPIN LIMITED ,  SINHA, Neelima ,  JANA, Gourhari ,  KARCHE, Navnath, Popat ,  ADURKAR, Shridhar, Keshav ,  HATNAPURE, Girish, Dhanraj ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, Kumar

发明人： SINHA, Neelima ,  JANA, Gourhari ,  KARCHE, Navnath, Popat ,  ADURKAR, Shridhar, Keshav ,  HATNAPURE, Girish, Dhanraj ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, Kumar

IPC分类号： C07D401/04 ,  C07D405/04 ,  C07D207/333 ,  A61K31/402 ,  A61K31/4025 ,  A61K31/435 ,  A61P23/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

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a7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a7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：WO2012076966A1

公开(公告)日：2012-06-14

申请号：PCT/IB2011/002954

申请日：2011-12-07

申请人： LUPIN LIMITED ,  SINDKHEDKAR, Milind, Dattatraya ,  SAHA, Nabendu, Nilmani ,  DEEPAK, Ukirde ,  SACHCHIDANAND, Sachchidanand ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, KUMAR

发明人： SINDKHEDKAR, Milind, Dattatraya ,  SAHA, Nabendu, Nilmani ,  DEEPAK, Ukirde ,  SACHCHIDANAND, Sachchidanand ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, KUMAR

IPC分类号： C07D513/04 ,  A61P3/04 ,  A61P3/10 ,  A61K31/4985

CPC分类号： C07D513/04

摘要： The invention relates to thieno[3,4-b]pyrazine derivatives of Formula (I) and their pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the compounds of the invention. The invention also relates to methods for treating, preventing and/or managing diseases, disorders, syndromes or conditions associated with inadequate insulin secretion such as diabetes, related disorders and metabolic syndrome. The invention also relates to methods for treating, preventing and/or managing diseases, disorders, syndromes or conditions which are affected or facilitated by the modulation of GLP-1 receptor. The invention also relates to processes for the preparation of the compounds of Formula (I).

摘要翻译： 本发明涉及式（I）的噻吩并[3,4-b]吡嗪衍生物及其药学上可接受的盐，其含有本发明化合物的药物组合物。 本发明还涉及用于治疗，预防和/或控制与胰岛素分泌不足相关的疾病，病症，综合征或病症的方法，例如糖尿病，相关病症和代谢综合征。 本发明还涉及用于治疗，预防和/或控制受GLP-1受体调节影响或促进的疾病，病症，综合征或病症的方法。 本发明还涉及制备式（I）化合物的方法。

公开(公告)号：WO2012049555A1

公开(公告)日：2012-04-19

申请号：PCT/IB2011/002392

申请日：2011-10-12

申请人： LUPIN LIMITED ,  PADIYA, Kamlesh, Jyotindra ,  NAIR, Prathap, S. ,  PAL, Ravindra, Ramsurat ,  CHAURE, Ganesh, Shankar ,  GUDADE, Ganesh, Bhausaheb ,  PARKALE, Santosh, Sadashiv ,  MANOJKUMAR, Vishwanath, Lohar ,  SWAPNIL, Ramesh, Bajare ,  SMITA, Aditya, Bhoskar ,  SACHIN, Dilip, Survase ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, Kumar

发明人： PADIYA, Kamlesh, Jyotindra ,  NAIR, Prathap, S. ,  PAL, Ravindra, Ramsurat ,  CHAURE, Ganesh, Shankar ,  GUDADE, Ganesh, Bhausaheb ,  PARKALE, Santosh, Sadashiv ,  MANOJKUMAR, Vishwanath, Lohar ,  SWAPNIL, Ramesh, Bajare ,  SMITA, Aditya, Bhoskar ,  SACHIN, Dilip, Survase ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, Kumar

IPC分类号： C07D491/10 ,  C07D491/20 ,  C07D491/22 ,  A61K31/407 ,  A61P25/00 ,  A61P29/00

CPC分类号： C07D491/10 ,  C07D491/20 ,  C07D491/22

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 modulated by VGSCs. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions by modulators of VGSC 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/或治疗由VGSC调节的疾病，病症，综合征或病症。 本发明还涉及通过式（I）的VGSC的调节剂治疗，预防治疗和/或减轻疾病，病症，综合征或病症的方法。

公开(公告)号：WO2013005168A3

公开(公告)日：2013-04-25

申请号：PCT/IB2012053407

申请日：2012-07-04

申请人： LUPIN LTD ,  KULKARNI SANJEEV ANANT ,  MADAN SACHIN ,  JANA NIRMAL KUMAR ,  TALE PRASHANT VITTHALRAO ,  CHEEMALA NARASIMHA MURTHY ,  MAHANGARE SACHIN JAYSING ,  VIDHATE PRASHANT POPATRAO ,  KULKARNI CHAITANYA PRABHAKAR ,  PATEL SAPANA SURESH ,  PATIL AMOLSING DATTU ,  ZADE SEEMA PRABHAKAR ,  SHINDE ROHAN MAHADEV ,  PALLE VENKATA P ,  KAMBOJ RAJENDER KUMAR

发明人： KULKARNI SANJEEV ANANT ,  MADAN SACHIN ,  JANA NIRMAL KUMAR ,  TALE PRASHANT VITTHALRAO ,  CHEEMALA NARASIMHA MURTHY ,  MAHANGARE SACHIN JAYSING ,  VIDHATE PRASHANT POPATRAO ,  KULKARNI CHAITANYA PRABHAKAR ,  PATEL SAPANA SURESH ,  PATIL AMOLSING DATTU ,  ZADE SEEMA PRABHAKAR ,  SHINDE ROHAN MAHADEV ,  PALLE VENKATA P ,  KAMBOJ RAJENDER KUMAR

IPC分类号： A61K31/4725 ,  A61K31/5377 ,  A61K31/541 ,  C07C237/48 ,  C07D213/40 ,  C07D217/14 ,  C07D217/22 ,  C07D217/26 ,  C07D265/30 ,  C07D309/04 ,  C07D401/06 ,  C07D405/12 ,  C07D413/06 ,  C07D471/08 ,  C07D491/08

CPC分类号： C07D217/26 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/541 ,  C07C237/48 ,  C07D209/52 ,  C07D213/40 ,  C07D213/53 ,  C07D217/14 ,  C07D217/22 ,  C07D217/24 ,  C07D265/30 ,  C07D295/16 ,  C07D295/192 ,  C07D309/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/06 ,  C07D417/06 ,  C07D471/08 ,  C07D487/10 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

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 cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).

摘要翻译： 式（I）化合物及其制备方法可用于治疗，控制和/或减轻与大麻素（CB）受体调节相关的疾病，病症，综合征或病症。 治疗，处理和/或减轻与调节式（I）的大麻素（CB）受体相关的疾病，病症，综合征或病症的方法。

公开(公告)号：WO2013005153A1

公开(公告)日：2013-01-10

申请号：PCT/IB2012/053347

申请日：2012-07-02

申请人： LUPIN LIMITED ,  SINHA, Neelima ,  KARCHE, Navnath, Popat ,  HATNAPURE, Girish, Dhanraj ,  HAJARE, Anil, Kashiram ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, Kumar

发明人： SINHA, Neelima ,  KARCHE, Navnath, Popat ,  HATNAPURE, Girish, Dhanraj ,  HAJARE, Anil, Kashiram ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, Kumar

IPC分类号： C07D277/28 ,  C07D277/30 ,  C07D333/22 ,  C07D207/335 ,  A61K31/381 ,  A61K31/401 ,  A61K31/4025 ,  A61K31/426

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', Έ', 'm', 'n' and R 1 -R 4 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'，α'，'m'，'n'和R1-R4如本文所述，作为烟碱乙酰胆碱受体的调节剂，特别是a7亚型， 其需要，以及类似物，前药，同位素替代的类似物，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，可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。 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：WO2012127388A1

公开(公告)日：2012-09-27

申请号：PCT/IB2012/051268

申请日：2012-03-16

申请人： LUPIN LIMITED ,  SHUKLA, Manojkumar, Ramprasad ,  ANKUSH, Sarde, Gangaram ,  VIPUL, Pachpute, Dilip ,  SAYYED, Majid, Bashir ,  TRYAMBAKE, Mahadeo, Bhaskar ,  PAWAR, Chetan, Sanjay ,  GOTE, Ganesh, Navinchandra ,  KULKARNI, Sanjeev, Anant ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, Kumar

发明人： SHUKLA, Manojkumar, Ramprasad ,  ANKUSH, Sarde, Gangaram ,  VIPUL, Pachpute, Dilip ,  SAYYED, Majid, Bashir ,  TRYAMBAKE, Mahadeo, Bhaskar ,  PAWAR, Chetan, Sanjay ,  GOTE, Ganesh, Navinchandra ,  KULKARNI, Sanjeev, Anant ,  PALLE, Venkata, P. ,  KAMBOJ, Rajender, Kumar

IPC分类号： C07D265/36 ,  C07D413/04 ,  A61K31/538 ,  A61P5/18

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).

摘要翻译： 式（I）的化合物及其制备方法，其可用于治疗，控制和/或减轻与钙感觉（CaSR）受体调节相关的疾病，病症，综合征或病症。 治疗，控制和/或减轻与调节式（I）的钙敏感（CaSR）受体相关的疾病，病症，综合征或病症的方法。

公开(公告)号：WO2011018796A1

公开(公告)日：2011-02-17

申请号：PCT/IN2010/000276

申请日：2010-04-28

申请人： LUPIN LIMITED ,  ROY, Bhairab, Nath ,  KAMBOJ, Rajender, Kumar ,  GEORGE, Shaji, K. ,  VENUGOPAL, Spinvin, C. ,  SHANMUGVADIVELU, Muthu, Kumaran ,  SINHA, Neelima

发明人： ROY, Bhairab, Nath ,  KAMBOJ, Rajender, Kumar ,  GEORGE, Shaji, K. ,  VENUGOPAL, Spinvin, C. ,  SHANMUGVADIVELU, Muthu, Kumaran ,  SINHA, Neelima

IPC分类号： C07D451/02

CPC分类号： C07D451/02

摘要： An improved process for the synthesis of intermediates like Alkyl/Aralkyl (2S)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof which are useful in the synthesis of Dipeptidyl peptidase-IV (DPPIV) inhibitors.

摘要翻译： 合成中间体如（2S）-2-（叔丁氧基羰基） - 氨基-2- [-8-氮杂双环[3.2.1]辛-3-基] - 乙酸乙酯和类似物的中间体的改进方法 它们可用于合成二肽基肽酶-IV（DPPIV）抑制剂。

公开(公告)号：WO2010146597A1

公开(公告)日：2010-12-23

申请号：PCT/IN2009/000478

申请日：2009-09-01

申请人： LUPIN LIMITED ,  SINHA, Neelima ,  NAIR, Prathap ,  KARCHE, Navnath ,  SAHA, Nabendu ,  GOEL, Rajan ,  KAMBOJ, Rajender Kumar

发明人： SINHA, Neelima ,  NAIR, Prathap ,  KARCHE, Navnath ,  SAHA, Nabendu ,  GOEL, Rajan ,  KAMBOJ, Rajender Kumar

IPC分类号： C07D451/02 ,  A61K31/439 ,  A61P3/00

CPC分类号： A61K31/46 ,  C07D451/02

摘要： The present invention is related to novel 2-Amino-2- [8-(dimethyl carbamoyl)- 8-aza- bicyclo [3.2.1] oct-3-yl]-exo-ethanoyl derivatives of the general formula (A), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods of making of the above compounds, and their use as Dipeptidyl Peptidase-IV (DPP-IV) Inhibitors, which are useful in the treatment or prevention of diseases particularly Type II diabetes, other complications related to diabetes and other pathogenic conditions in which DPP IV enzyme is involved.

摘要翻译： 本发明涉及通式（A）的新型2-氨基-2- [8-（二甲基氨基甲酰基）-8-氮杂 - 双环[3.2.1]辛-3-基] - 异 - 乙酰基衍生物， 它们的互变异构形式，其立体异构体，其药学上可接受的盐，含有它们的药物组合物，制备上述化合物的方法，以及它们作为二肽基肽酶-IV（DPP-IV）抑制剂的用途，其可用于治疗或预防疾病 特别是II型糖尿病，与糖尿病有关的其他并发症和涉及DPP IV酶的其他致病条件。

公开(公告)号：WO2013021337A1

公开(公告)日：2013-02-14

申请号：PCT/IB2012/054007

申请日：2012-08-06

申请人： LUPIN LIMITED ,  RAMDAS, Vidya ,  JOSHI, Advait, Arun ,  WALKE, Deepak, Sahebrao ,  BANERJEE, Moloy, MANOJ ,  PALLE, Venkata, P ,  KAMBOJ, Rajender, Kumar

发明人： RAMDAS, Vidya ,  JOSHI, Advait, Arun ,  WALKE, Deepak, Sahebrao ,  BANERJEE, Moloy, MANOJ ,  PALLE, Venkata, P ,  KAMBOJ, Rajender, Kumar

IPC分类号： C07D403/14 ,  C07D491/044 ,  A61K31/4184 ,  A61K31/4188 ,  A61P31/14

CPC分类号： C07D491/044 ,  C07D403/14

摘要： Compounds of the general formula I, their tautomeric forms, their stereoisomers, their analogs, their prodrugs, their isotopes, their N-oxides, their metabolites, their pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament, pharmaceutical compositions containing them, methods of making of the above compounds, and their use as antiviral candidate, more specifically as anti-HCV are disclosed.

摘要翻译： 通式I的化合物，其互变异构形式，其立体异构体，其类似物，其前药，其同位素，其N-氧化物，其代谢物，其药学上可接受的盐，多晶型物，溶剂合物，旋光异构体，包合物，共晶体，组合 公开了具有合适的药物，含有它们的药物组合物，制备上述化合物的方法及其作为抗病毒候选物的用途，更具体地作为抗HCV。