公开(公告)号：US20230049917A1

公开(公告)日：2023-02-16

申请号：US17789343

申请日：2020-12-26

Applicant: Lupin Limited

Inventor： Rajender Kumar Kamboj ,  Dhananjay Sadashiv Bakhle ,  Chirag Anilkumar Shah

IPC: A61K31/5375 ,  A61K9/20 ,  A61K31/352 ,  A61K31/195 ,  A61K31/137 ,  A61P5/20

Abstract: The invention provides for a compound having the structure of Formula (I) to Formula (VI), including Compounds 1 to 6, their pharmaceutically acceptable salts, and compositions comprising thereof. This invention further includes methods of their use for the treatment of diseases or disorders associated with the modulation of calcium sensing receptors (CaSRs), including secondary hyperparathyroidism associated with chronic kidney disease in a subject in need thereof. This disclosure further relates to a process for the preparation of said pharmaceutical compositions.

公开(公告)号：US20190275012A9

公开(公告)日：2019-09-12

申请号：US16320902

申请日：2017-07-28

Applicant: Lupin Limited

Inventor： 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: A61K31/429 ,  A61P35/02 ,  A61P37/00 ,  A61P11/00

Abstract: 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

Applicant: Lupin Limited

Inventor： 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: C07D519/00 ,  A61K31/52 ,  A61K31/519 ,  C07D471/04 ,  C07D473/34 ,  C07D473/16 ,  C07D513/04

CPC classification number: C07D471/04 ,  C07D473/16 ,  C07D473/34 ,  C07D513/04 ,  C07D519/00

Abstract: 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

Applicant: LUPIN LIMITED

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

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

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  A61N5/10

Abstract: 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.

Abstract translation: 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

Applicant: Lupin Limited

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

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

CPC classification number: A61K31/4439 ,  A61K31/40 ,  A61K45/06 ,  C07D207/333 ,  C07D401/04 ,  C07D401/06

Abstract: 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

Applicant: LUPIN LIMITED

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

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

CPC classification number: C07D413/14 ,  C07D413/04 ,  C07D417/14

Abstract: 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.

Abstract translation: 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

Applicant: Lupin Limited

Inventor： 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: 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 classification number: C07D498/08 ,  A61K31/427 ,  A61K31/439 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/5386 ,  A61K45/06 ,  C07D221/22 ,  C07D277/56 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14

Abstract: 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.

Abstract translation: 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

Applicant: LUPIN LIMITED

Inventor： 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: C07D413/14 ,  C07D401/14

CPC classification number: C07D413/14 ,  C07D401/14

Abstract: 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.

Abstract translation: 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：US20240366608A1

公开(公告)日：2024-11-07

申请号：US18262155

申请日：2022-01-19

Applicant: Lupin Limited

Inventor： Mandar Ramesh Bhonde ,  Sukanya Patra ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC: A61K31/519 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/7068 ,  A61P35/00

Abstract: This disclosure relates to pharmaceutical combinations for treating and/or preventing cancer and methods and uses thereof. More particularly, provided is a pharmaceutical combination comprising a SOS1 Inhibitor and an additional active ingredient selected from a KRAS inhibitor such as a KRAS G12C inhibitor and a KRASG12D inhibitor, KRAS G13C inhibitor, and panKRAS inhibitor; an EGFR inhibitor; an ERK1/2 inhibitor; a BRAF inhibitor; a pan-RAF inhibitor; a MEK inhibitor; a AKT inhibitor; a SHP2 inhibitor; protein arginine methyltransferases (PRMTs) inhibitor such as a PRMT5 inhibitor and Type 1 PRMT inhibitor; a PI3K inhibitor; a cyclin-dependent kinase (CDK) inhibitor such as CDK4/6 inhibitor; a FGFR inhibitor; a c-Met inhibitor; a RTK inhibitor; a non-receptor tyrosine kinase inhibitor; a histone methyltransferases (HMTs) inhibitor; a DNA methyltransferases (DNMTs) inhibitor; a Focal Adhesion Kinase (FAK) inhibitor; a Bcr-Abl tyrosine kinase inhibitor; a mTOR inhibitor; a PD1 inhibitor; a PD-L1 inhibitor; CTLA4 inhibitor; and chemotherapeutic agents such as gemcitabine, doxorubicin, cisplatin, carboplatin, paclitaxel, docetaxel, topotecan, irinotecan and temozolomide.

公开(公告)号：US10239869B2

公开(公告)日：2019-03-26

申请号：US15757103

申请日：2016-09-03

Applicant: LUPIN LIMITED

Inventor： 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: C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61P29/00

Abstract: 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.