公开(公告)号：US20190275012A9

公开(公告)日：2019-09-12

申请号：US16320902

申请日：2017-07-28

申请人： Lupin Limited

发明人： Gagan Kukreja ,  Nageswara Rao Irlapati ,  Arun Rangnath Jagdale ,  Gokul Keruji Deshmukh ,  Vinod Popatrao Vyavahare ,  Kiran Chandrashekhar Kulkarni ,  Neelima Sinha ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： A61K31/429 ,  A61P35/02 ,  A61P37/00 ,  A61P11/00

摘要： Disclosed are compounds of the general formula (I), wherein R1-R3 are as defined herein, for use as MALT1 inhibitors in the treatment of autoimmune and inflammatory diseases or disorders. Methods of synthesizing the compounds are also disclosed. Also disclosed are pharmaceutical compositions containing a compound of the invention and a method of treating a patient for an autoimmune or an inflammatory disease or disorder, for example, a cancer, by administering a compound of the invention.

公开(公告)号：US09944639B2

公开(公告)日：2018-04-17

申请号：US15323565

申请日：2015-07-01

申请人： Lupin Limited

发明人： Manojkumar Ramprasad Shukla ,  Nirmal Kumar Jana ,  Sachin Jaysing Mahangare ,  Prashant Popatrao Vidhate ,  Dipak Raychand Lagad ,  Anand Jagannath Tarage ,  Sanjeev Anant Kulkarni ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D519/00 ,  A61K31/52 ,  A61K31/519 ,  C07D471/04 ,  C07D473/34 ,  C07D473/16 ,  C07D513/04

CPC分类号： C07D471/04 ,  C07D473/16 ,  C07D473/34 ,  C07D513/04 ,  C07D519/00

摘要： Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, wherein R1-R4, and n are as defined in the specification, pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PI3K enzyme of a subject.

公开(公告)号：US09573944B2

公开(公告)日：2017-02-21

申请号：US14385106

申请日：2013-03-11

申请人： LUPIN LIMITED

发明人： Bhavesh Dave ,  Rakesh Kumar Banerjee ,  Samiron Phukan ,  Abhijit Datta Khoje ,  Rajkumar Hangarge ,  Jitendra Sambhaji Jadhav ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  A61N5/10

CPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  A61N5/10

摘要： The present invention is related to heteroaryl compounds as MEK inhibitors. The invention includes heteroaryl compounds of formula I, their tautomers and pharmaceutically acceptable salts, 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.

摘要翻译： 本公开涉及作为MEK抑制剂的杂芳基化合物。 这些化合物包括式I的杂芳基化合物，其药学上可接受的盐，与合适的药物的组合及其药物组合物。 本公开还包括制备化合物的方法及其在治疗方法中的用途。 本文公开的化合物具有下式（I）：

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：US09399638B2

公开(公告)日：2016-07-26

申请号：US14398154

申请日：2013-05-01

申请人： LUPIN LIMITED

发明人： Nageswara Rao Irlapati ,  Zubair Abdul Wajid Shaikh ,  Vijay Pandurang Karche ,  Gokul Keruji Deshmukh ,  Neelima Sinha ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D413/04 ,  C07D417/14 ,  C07D413/14

CPC分类号： C07D413/14 ,  C07D413/04 ,  C07D417/14

摘要： The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release-activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I) and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.

摘要翻译： 本发明涉及调节钙释放活化的钙（CRAC）通道的活性的式（I）化合物及其药学上可接受的盐。 本发明还描述了式（I）的化合物和含有其化合物的药物组合物，用于治疗，治疗和/或降低与调节钙释放激活的钙（CRAC）相关的疾病，病症，综合征或病症的严重性， 渠道。

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：US20150111925A1

公开(公告)日：2015-04-23

申请号：US14398161

申请日：2013-05-01

申请人： LUPIN LIMITED

发明人： Nageswara Rao Irlapati ,  Gokul Keruji Deshmukh ,  Nilesh Raghunath Khedkar ,  Kiran Chandrashekhar Kulkarni ,  Zubair Abdul Wajid Shaikh ,  Neelima Sinha ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D413/14 ,  C07D401/14

CPC分类号： C07D413/14 ,  C07D401/14

摘要： The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release-activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I) and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.

摘要翻译： 本发明涉及调节钙释放活化的钙（CRAC）通道的活性的式（I）化合物及其药学上可接受的盐。 本发明还描述了式（I）化合物和含有其化合物的药物组合物，用于治疗，控制和/或降低与调节钙释放激活的钙（CRAC）相关的疾病，病症，综合征或病症的严重性， 渠道。

公开(公告)号：US10239869B2

公开(公告)日：2019-03-26

申请号：US15757103

申请日：2016-09-03

申请人： LUPIN LIMITED

发明人： Vidya Ramdas ,  Rajeshkumar Maganlal Loriya ,  Moloy Banerjee ,  Pradeep Rangrao Patil ,  Advait Arun Joshi ,  Laxmikant Shamlal Datrange ,  Deepak Sahebrao Walke ,  Talha Hussain Khan ,  Amit Kumar Das ,  Ganesh Navinchandra Gote ,  Vaibhav Madhukar Kalhapure ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61P29/00

摘要： The present invention relates to sulfonamide compounds Formula (I) wherein the substituents are as described herein, and their use in a medicine for the treatment of diseases, disorders associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. It further relates to the compounds herein and their pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof useful in treating diseases, disorders, syndromes and/or conditions associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. The invention also relates to process for the preparation of the compounds of the invention.

公开(公告)号：US09737534B2

公开(公告)日：2017-08-22

申请号：US14840118

申请日：2015-08-31

申请人： LUPIN LIMITED

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 ,  A61P19/02 ,  A61K31/497 ,  C07D261/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/423 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/496

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).

公开(公告)号：US20170137421A1

公开(公告)日：2017-05-18

申请号：US15323565

申请日：2015-07-01

申请人： Lupin Limited

发明人： Manojkumar Ramprasad Shukla ,  Nirmal Kumar Jana ,  Sachin Jaysing Mahangare ,  Prashant Popatrao Vidhate ,  Dipak Raychand Lagad ,  Anand Jagannath Tarage ,  Sanjeev Anant Kulkarni ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D471/04 ,  C07D473/16 ,  C07D513/04 ,  C07D473/34

CPC分类号： C07D471/04 ,  C07D473/16 ,  C07D473/34 ,  C07D513/04 ,  C07D519/00

摘要： Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, wherein R1-R4, and n are as defined in the specification, pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PI3K enzyme of a subject.