公开(公告)号：US20140057888A1

公开(公告)日：2014-02-27

申请号：US13989600

申请日：2011-11-25

Applicant: Senthilkumar Udayampalayam Palanisamy ,  Maneesh Paul-Satyaseela ,  Shridhar Narayanan ,  Gopalan Balasubramanian ,  Aravind Appu ,  Senthilnathan Manickam ,  Hariharam Periasamy

Inventor： Senthilkumar Udayampalayam Palanisamy ,  Maneesh Paul-Satyaseela ,  Shridhar Narayanan ,  Gopalan Balasubramanian ,  Aravind Appu ,  Senthilnathan Manickam ,  Hariharam Periasamy

IPC: A61K31/431 ,  C12Q1/44 ,  A61K31/496 ,  A61K31/542 ,  A61K31/4025 ,  C07D499/00 ,  A61K31/397

CPC classification number: A61K31/431 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/496 ,  A61K31/542 ,  C07D499/00 ,  C07D499/883 ,  C12Q1/44

Abstract: Described herein are compounds and their use in the treatment of infections. The compound of formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, solvates, pharmaceutically acceptable salts and pharmaceutical compositions described herein are also useful as β-lactamase inhibitors, which restore or enhance the antibiotic spectrum of a suitable antibiotic agent. The compounds of formula (I) act as inhibitors of β-lactamases. These compounds restore/potentiate the activities of β-lactam antibiotics against carbapenemases. These compounds find use in diagnostic method for detecting β-lactamases.Formula (I)

Abstract translation: 本文描述的是化合物及其在治疗感染中的用途。 本文所述的式（I）化合物，其衍生物，类似物，互变异构体形式，立体异构体，多晶型物，溶剂合物，药学上可接受的盐和药物组合物也可用作β-内酰胺酶抑制剂，其恢复或增强合适的抗生素的抗生素谱 代理商 式（I）化合物作为β-内酰胺酶的抑制剂。 这些化合物恢复/增强β-内酰胺抗生素对碳青霉烯酶的活性。 这些化合物可用于检测β-内酰胺酶的诊断方法。 式（I）

公开(公告)号：US08580795B2

公开(公告)日：2013-11-12

申请号：US13143480

申请日：2010-01-21

Applicant: Gopalan Balasubramanian ,  Sukunath Narayanan ,  Ganapavarapu Veera Raghava Sharma ,  Lavanya Andiappan ,  Shridhar Narayanan ,  Sanjeev Saxena ,  Sridharan Rajagopal ,  Santosh Lolaknath Vishwakarma ,  Saravanan Thirunavukkarasu

Inventor： Gopalan Balasubramanian ,  Sukunath Narayanan ,  Ganapavarapu Veera Raghava Sharma ,  Lavanya Andiappan ,  Shridhar Narayanan ,  Sanjeev Saxena ,  Sridharan Rajagopal ,  Santosh Lolaknath Vishwakarma ,  Saravanan Thirunavukkarasu

IPC: A61K31/496 ,  C07D405/14

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

Abstract: Compounds of the formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, N-oxides, metabolites and prodrugs thereof. These compounds are phosphodiesterase type 4 (PDE4) inhibitors. They are useful in the treatment of a variety of allergic or inflammatory diseases including asthma, COPD, chronic bronchitis, atopic dermatitis, allergic rhinitis, allergic conjunctivitis, vernal conjuctivitis, psoriasis, rheumatoid arthritis, ulcerative colitis, Crohn's disease, uveitis, NASH and lupus.

Abstract translation: 式（I）化合物，其衍生物，类似物，互变异构体，区域异构体，立体异构体，多晶型物，溶剂合物，中间体，药学上可接受的盐，药物组合物，N-氧化物，代谢物和前药。 这些化合物是磷酸二酯酶4型（PDE4）抑制剂。 它们可用于治疗各种过敏或炎性疾病，包括哮喘，COPD，慢性支气管炎，特应性皮炎，过敏性鼻炎，过敏性结膜炎，春季结膜炎，牛皮癣，类风湿性关节炎，溃疡性结肠炎，克罗恩病，葡萄膜炎，NASH和狼疮 。

公开(公告)号：US20110269753A1

公开(公告)日：2011-11-03

申请号：US13143480

申请日：2010-01-21

Applicant: Gopalan Balasubramanian ,  Sukunath Narayanan ,  Ganapavarapu Veera Raghava Sharma ,  Lavanya Andiappan ,  Shridhar Narayanan ,  Sanjeev Saxena ,  Sridharan Rajagopal ,  Santosh Lolaknath Vishwakarma ,  Saravanan Thirunavukkarasu

Inventor： Gopalan Balasubramanian ,  Sukunath Narayanan ,  Ganapavarapu Veera Raghava Sharma ,  Lavanya Andiappan ,  Shridhar Narayanan ,  Sanjeev Saxena ,  Sridharan Rajagopal ,  Santosh Lolaknath Vishwakarma ,  Saravanan Thirunavukkarasu

IPC: A61K31/4439 ,  C07D407/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D498/04 ,  C07D498/14 ,  A61K31/427 ,  A61K31/506 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/422 ,  A61K31/423 ,  A61K31/437 ,  A61P29/00 ,  A61P37/00 ,  A61P11/06 ,  A61P11/00 ,  A61P11/08 ,  A61P17/00 ,  A61P27/14 ,  A61P17/06 ,  A61P1/04 ,  A61P1/00 ,  A61P27/02 ,  A61P19/04 ,  C07D417/14

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

Abstract: Compounds of the formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, N-oxides, metabolites and prodrugs thereof. These compounds are phosphodiesterase type 4 (PDE4) inhibitors. They are useful in the treatment of a variety of allergic or inflammatory diseases including asthma, COPD, chronic bronchitis, atopic dermatitis, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, psoriasis, rheumatoid arthritis, ulcerative colitis, Crohn's disease, uveitis, NASH and lupus.

Abstract translation: 式（I）化合物，其衍生物，类似物，互变异构体，区域异构体，立体异构体，多晶型物，溶剂合物，中间体，药学上可接受的盐，药物组合物，N-氧化物，代谢物和前药。 这些化合物是磷酸二酯酶4型（PDE4）抑制剂。 它们可用于治疗各种过敏或炎性疾病，包括哮喘，COPD，慢性支气管炎，特应性皮炎，过敏性鼻炎，过敏性结膜炎，春季结膜炎，牛皮癣，类风湿性关节炎，溃疡性结肠炎，克罗恩病，葡萄膜炎，NASH和狼疮 。

公开(公告)号：US20110257164A1

公开(公告)日：2011-10-20

申请号：US13140997

申请日：2010-01-07

Applicant: Gopalan Balasubramanian ,  Sukumar Sakamuri ,  Gajendra Singh ,  Sivanesan Dharmalingam ,  Franklin Pooppady Xavier ,  Shridhar Narayanan ,  Jeyamurugan Mookkan ,  Jeganatha Sivakumar Balasubramanian ,  Agneeswari Rajalingam ,  Jayanarayan Kulathingal

Inventor： Gopalan Balasubramanian ,  Sukumar Sakamuri ,  Gajendra Singh ,  Sivanesan Dharmalingam ,  Franklin Pooppady Xavier ,  Shridhar Narayanan ,  Jeyamurugan Mookkan ,  Jeganatha Sivakumar Balasubramanian ,  Agneeswari Rajalingam ,  Jayanarayan Kulathingal

IPC: A61K31/541 ,  A61K31/4196 ,  C07D405/12 ,  A61K31/4025 ,  A61K31/46 ,  C07D413/12 ,  A61K31/4245 ,  C07D413/14 ,  A61K31/497 ,  A61K31/4439 ,  C07D207/00 ,  A61K31/40 ,  C07D401/12 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/41 ,  C07D417/12 ,  A61P3/10 ,  A61P3/04 ,  A61P3/06 ,  A61P9/00 ,  A61P1/00 ,  A61P25/00 ,  A61P25/28 ,  C07D403/12

CPC classification number: C07D417/12 ,  C07D207/10 ,  C07D207/12 ,  C07D211/46 ,  C07D213/12 ,  C07D401/12 ,  C07D403/12

Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.

Abstract translation: 描述了式（I）的新化合物，其衍生物，类似物，互变异构体，区域异构体，立体异构体，多晶型物，溶剂合物，中间体，药学上可接受的盐，药物组合物，代谢物和前药。 这些化合物有效降低血糖，血清胰岛素，游离脂肪酸，胆固醇，甘油三酯水平; 治疗肥胖，炎症，自身免疫性疾病如多发性硬化，类风湿性关节炎; 治疗和/或预防II型糖尿病。 这些化合物更特别是二肽基肽酶（DPP IV）抑制剂。

公开(公告)号：US20070232608A1

公开(公告)日：2007-10-04

申请号：US11675157

申请日：2007-02-15

Applicant: Abraham Thomas ,  Gopalan Balasubramanian ,  V.S. Lingam ,  Daisy Shah

Inventor： Abraham Thomas ,  Gopalan Balasubramanian ,  V.S. Lingam ,  Daisy Shah

IPC: A61K31/40 ,  C07D207/04

CPC classification number: C07D235/06 ,  C07C271/24 ,  C07C309/66 ,  C07C2601/08 ,  C07C2601/10 ,  C07D207/16 ,  C07D207/325 ,  C07D207/34 ,  C07D209/08 ,  C07D209/42 ,  C07D209/44 ,  C07D211/62 ,  C07D217/04 ,  C07D231/12 ,  C07D233/54 ,  C07D233/68 ,  C07D233/90 ,  C07D233/95 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D277/04 ,  C07D295/135 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

Abstract: The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein.

公开(公告)号：US07205323B2

公开(公告)日：2007-04-17

申请号：US11250195

申请日：2005-10-12

Applicant: Abraham Thomas ,  Gopalan Balasubramanian ,  V. S. Prasada Rao Lingam ,  Daisy Manish Shah

Inventor： Abraham Thomas ,  Gopalan Balasubramanian ,  V. S. Prasada Rao Lingam ,  Daisy Manish Shah

IPC: C07D277/06 ,  C07D275/03 ,  A61K31/427 ,  A61K31/415 ,  A61K31/4178

CPC classification number: C07D235/06 ,  C07C271/24 ,  C07C309/66 ,  C07C2601/08 ,  C07C2601/10 ,  C07D207/16 ,  C07D207/325 ,  C07D207/34 ,  C07D209/08 ,  C07D209/42 ,  C07D209/44 ,  C07D211/62 ,  C07D217/04 ,  C07D231/12 ,  C07D233/54 ,  C07D233/68 ,  C07D233/90 ,  C07D233/95 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D277/04 ,  C07D295/135 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

Abstract: The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein.

Abstract translation: 本发明涉及可用作下式的二肽基肽酶IV（DPP-IV）抑制剂的新化合物：

公开(公告)号：US20060178418A1

公开(公告)日：2006-08-10

申请号：US10532273

申请日：2003-10-08

Applicant: Gopalan Balasubramanian ,  Laxmikant Gharat ,  Aftab Lakdawala ,  Raghu Anupindi

Inventor： Gopalan Balasubramanian ,  Laxmikant Gharat ,  Aftab Lakdawala ,  Raghu Anupindi

IPC: A61K31/403 ,  A61K31/381 ,  A61K31/343

CPC classification number: C07D307/91 ,  C07D209/88 ,  C07D333/76 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12

Abstract: The present invention relates to novel tricyclic compounds useful for the treatment of inflammatory conditions, diseases of the central nervous and insulin resistant diabetes.

Abstract translation: 本发明涉及可用于治疗炎性病症，中枢神经和胰岛素抵抗性糖尿病的新型三环化合物。

公开(公告)号：US10201532B2

公开(公告)日：2019-02-12

申请号：US13989600

申请日：2011-11-25

Applicant: Senthilkumar Udayampalayam Palanisamy ,  Maneesh Paul-Satyaseela ,  Shridhar Narayanan ,  Gopalan Balasubramanian ,  Aravind Appu ,  Senthilnathan Manickam ,  Hariharan Periasamy

Inventor： Senthilkumar Udayampalayam Palanisamy ,  Maneesh Paul-Satyaseela ,  Shridhar Narayanan ,  Gopalan Balasubramanian ,  Aravind Appu ,  Senthilnathan Manickam ,  Hariharan Periasamy

IPC: A61K31/431 ,  C07D499/883 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/496 ,  A61K31/542 ,  C07D499/00 ,  C12Q1/44

Abstract: Described herein are compounds and their use in the treatment of infections. The compound of formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, solvates, pharmaceutically acceptable salts and pharmaceutical compositions described herein are also useful as β-lactamase inhibitors, which restore or enhance the antibiotic spectrum of a suitable antibiotic agent. The compounds of formula (I) act as inhibitors of β-lactamases. These compounds restore/potentiate the activities of β-lactam antibiotics against carbapenemases. These compounds find use in diagnostic method for detecting β-lactamases.Formula (I)

公开(公告)号：US20100329998A1

公开(公告)日：2010-12-30

申请号：US12863796

申请日：2009-01-30

Applicant: Visweswara Akella Satya Surya Srinivas ,  Ravikumar Tadiparthi ,  Ganapavarapu Veera Raghava Sharma ,  Thirunavukkarasu Sappanimuthu ,  Durairaj Peter Bhakiaraj ,  Virendra Kachhadia ,  Kilambi Narasimhan ,  Sathya Narayana Thara ,  Sriram Rajagopal ,  Om Gaddam ,  Nishikanth Reddy Gaddam ,  Sukunath Narayanan ,  Venkatesan Parameswaran ,  Venkatesan Janarthanam ,  Maruthikumar Narayanam ,  Sathyanarayana Gadde ,  Uma Ramachandran ,  Gopalan Balasubramanian ,  Narayanan Surendran ,  Shridhar Narayanan ,  Lolaknath Santosh Vishwakarma ,  Sanjeev Saxena

Inventor： Visweswara Akella Satya Surya Srinivas ,  Ravikumar Tadiparthi ,  Ganapavarapu Veera Raghava Sharma ,  Thirunavukkarasu Sappanimuthu ,  Durairaj Peter Bhakiaraj ,  Virendra Kachhadia ,  Kilambi Narasimhan ,  Sathya Narayana Thara ,  Sriram Rajagopal ,  Om Gaddam ,  Nishikanth Reddy Gaddam ,  Sukunath Narayanan ,  Venkatesan Parameswaran ,  Venkatesan Janarthanam ,  Maruthikumar Narayanam ,  Sathyanarayana Gadde ,  Uma Ramachandran ,  Gopalan Balasubramanian ,  Narayanan Surendran ,  Shridhar Narayanan ,  Lolaknath Santosh Vishwakarma ,  Sanjeev Saxena

IPC: A61K9/12 ,  A61K31/505 ,  C07D239/02 ,  C07D401/14 ,  A61K31/506 ,  A61K31/497 ,  C07D417/04 ,  C07D403/04 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/54 ,  A61P37/00 ,  A61P29/00 ,  A61P19/02 ,  A61P19/10 ,  A61P35/02 ,  A61P35/04 ,  A61P9/00 ,  A61P1/00 ,  A61P11/00

CPC classification number: C07D239/42 ,  A61K31/5377 ,  C07D265/28 ,  C07D401/04

Abstract: Described are novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are useful in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; ARDS; psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever. More particularly these compounds are useful as PDE4 inhibitors and are useful for treating PDE4 mediated diseases.

Abstract translation: 描述了通式（I）的新型杂环化合物，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，溶剂合物，药学上可接受的盐，药物组合物，代谢物和前药。 这些化合物可用于治疗免疫疾病，炎症，疼痛障碍，类风湿性关节炎; 骨质疏松症 多发性骨髓瘤 葡萄膜炎 急性和慢性粒细胞白血病; 动脉粥样硬化 癌症; 恶病质 缺血诱导的细胞损伤; 胰腺β细胞破坏; 骨关节炎 类风湿性脊柱炎; 痛风性关节炎 炎症性肠病; ARDS; 银屑病; 克罗恩病; 过敏性鼻炎; 溃疡性结肠炎 过敏反应 接触性皮炎; 肌肉退化; 哮喘; COPD; 骨吸收疾病; 多发性硬化症 败血症 败血性休克 中毒性休克综合征和发烧。 更特别地，这些化合物可用作PDE4抑制剂，并且可用于治疗PDE4介导的疾病。

公开(公告)号：US20080200501A1

公开(公告)日：2008-08-21

申请号：US11934186

申请日：2007-11-02

Applicant: Meyyappan Muthuppalaniappan ,  Kumar Sukeerthi ,  Gopalan Balasubramanian ,  Srinivas Gullapalli ,  Neelima Khairatkar Joshi ,  Shridhar Narayanan ,  Pallavi V. Kamik

Inventor： Meyyappan Muthuppalaniappan ,  Kumar Sukeerthi ,  Gopalan Balasubramanian ,  Srinivas Gullapalli ,  Neelima Khairatkar Joshi ,  Shridhar Narayanan ,  Pallavi V. Kamik

IPC: A61K31/416 ,  A61P3/00 ,  C07D413/02 ,  C07D231/54 ,  A61K31/4245 ,  A61K31/422 ,  C07D471/00 ,  A61K31/4709 ,  A61K31/4725

CPC classification number: C07D401/06 ,  C07D231/54 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04

Abstract: The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenative disorders, eating disorders, weight loss or control, and obesity).

Abstract translation: 本发明涉及新型大麻素受体调节剂，特别是大麻素1（CB1）或大麻素2（CB2）受体调节剂及其用于治疗由大麻素受体调节的疾病，病症和/或障碍的用途（例如疼痛，神经发生疾病 ，进食障碍，减肥或控制，以及肥胖）。