公开(公告)号：WO2006051390A1

公开(公告)日：2006-05-18

申请号：PCT/IB2005/003359

申请日：2005-11-09

Applicant: GLENMARK PHARMACEUTICALS S.A. ,  KHAIRATKAR-JOSHI, Neelima ,  BALASUBRAMANIAN, Gopalan ,  GHARAT, Laxmikant, Atmaram

Inventor： KHAIRATKAR-JOSHI, Neelima ,  BALASUBRAMANIAN, Gopalan ,  GHARAT, Laxmikant, Atmaram

IPC: C07D405/12 ,  C07D405/14 ,  A61K31/33 ,  A61P11/06 ,  A61P37/08

CPC classification number: C07D405/12 ,  C07D405/14

Abstract: The present invention relates to new phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) and analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, N-oxides, pharmaceutically acceptable solvates and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, and methods of treating allergic and inflammatory diseases, such as asthma or chronic obstructive pulmonary disease (COPD), with them.

Abstract translation: 本发明涉及式（1）的新型磷酸二酯酶4型（PDE4）抑制剂及其类似物，互变异构体，对映异构体，非对映体，区域异构体，立体异构体，多晶型物，N-氧化物，药学上可接受的溶剂合物及其药学上可接受的盐， 他们以及治疗过敏性和炎性疾病如哮喘或慢性阻塞性肺疾病（COPD）的方法。

公开(公告)号：WO2012070071A9

公开(公告)日：2012-05-31

申请号：PCT/IN2011/000813

申请日：2011-11-25

Applicant: ORCHID RESEARCH LABORATORIES LTD ,  UDAYAMPALAYAM PALANISAMY, Senthilkumar ,  PAUL-SATYASEELA, Maneesh ,  NARAYANAN, Shridhar ,  BALASUBRAMANIAN, Gopalan ,  APPU, Aravind ,  MANICKAM, Senthilnathan ,  PERIASAMY, Hariharan

Inventor： UDAYAMPALAYAM PALANISAMY, Senthilkumar ,  PAUL-SATYASEELA, Maneesh ,  NARAYANAN, Shridhar ,  BALASUBRAMANIAN, Gopalan ,  APPU, Aravind ,  MANICKAM, Senthilnathan ,  PERIASAMY, Hariharan

IPC: A61K31/34 ,  C07D507/00 ,  A61P31/00

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：WO2012070071A1

公开(公告)日：2012-05-31

申请号：PCT/IN2011000813

申请日：2011-11-25

Applicant: ORCHID RES LAB LTD ,  UDAYAMPALAYAM PALANISAMY SENTHILKUMAR ,  PAUL-SATYASEELA MANEESH ,  NARAYANAN SHRIDHAR ,  BALASUBRAMANIAN GOPALAN ,  APPU ARAVIND ,  MANICKAM SENTHILNATHAN ,  PERIASAMY HARIHARAN

Inventor： UDAYAMPALAYAM PALANISAMY SENTHILKUMAR ,  PAUL-SATYASEELA MANEESH ,  NARAYANAN SHRIDHAR ,  BALASUBRAMANIAN GOPALAN ,  APPU ARAVIND ,  MANICKAM SENTHILNATHAN ,  PERIASAMY HARIHARAN

IPC: A61K31/34 ,  A61P31/00 ,  C07D507/00

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 ß -lactamase inhibitors, which restore or enhance the antibiotic spectrum of a suitable antibiotic agent. The compounds of formula (I) act as inhibitors of ß-lactamases. These compounds restore/potentiate the activities of ß-lactam antibiotics against carbapenemases. These compounds find use in diagnostic method for detecting ß-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 剂。 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。 这些化合物用于检测β-内酰胺酶的诊断方法。 式（I）

公开(公告)号：WO2010084402A3

公开(公告)日：2010-07-29

申请号：PCT/IB2010/000094

申请日：2010-01-21

Applicant: ORCHID RESEARCH LABORATORIES LTD. ,  BALASUBRAMANIAN, Gopalan ,  NARAYANAN, Sukunath ,  SHARMA, Ganapavarapu, vEERA, rAGHAVA ,  ANDIAPPAN, Lavanya ,  NARAYANAN, Shridhar ,  SAXENA, Sanjeev ,  RAJAGOPAL, Sridharan ,  VISHWAKARMA, Lolaknath, Santosh ,  THIRUNAVUKKARASU, Saravanan

Inventor： BALASUBRAMANIAN, Gopalan ,  NARAYANAN, Sukunath ,  SHARMA, Ganapavarapu, vEERA, rAGHAVA ,  ANDIAPPAN, Lavanya ,  NARAYANAN, Shridhar ,  SAXENA, Sanjeev ,  RAJAGOPAL, Sridharan ,  VISHWAKARMA, Lolaknath, Santosh ,  THIRUNAVUKKARASU, Saravanan

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

Abstract: Described are 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.

公开(公告)号：WO2009095773A2

公开(公告)日：2009-08-06

申请号：PCT/IB2009/000157

申请日：2009-01-30

Applicant: ORCHID RESEARCH LABORATORIES LIMITED ,  ORCHID RESEARCH LABORATORIES LIMITED ,  SRINIVAS, Visweswara, Akella, Satya, Surya ,  TADIPARTHI, Ravikumar ,  SHARMA, Ganapavarapu, Veera, Raghava ,  SAPPANIMUTHU, Thirunavukkarasu ,  BHAKIARAJ, Durairaj, Peter ,  KACHHADIA, Virendra ,  NARASIMHAN, Kilambi ,  THARA, Sathya, Narayana ,  RAJAGOPAL, Sriram ,  NARAYANAN, Sukunath ,  PARAMESWARAN, Venkatesan ,  JANARTHANAM, Venkatesan ,  NARAYANAM, Maruthikumar ,  GADDE, Sathyanarayana ,  RAMACHANDRAN, Uma ,  BALASUBRAMANIAN, Gopalan ,  SURENDRAN, Narayanan ,  NARAYANAN, Shridhar ,  VISHWAKARMA, Lolaknath, Santosh ,  SAXENA, Sanjeev

Inventor： SRINIVAS, Visweswara, Akella, Satya, Surya ,  TADIPARTHI, Ravikumar ,  SHARMA, Ganapavarapu, Veera, Raghava ,  SAPPANIMUTHU, Thirunavukkarasu ,  BHAKIARAJ, Durairaj, Peter ,  KACHHADIA, Virendra ,  NARASIMHAN, Kilambi ,  THARA, Sathya, Narayana ,  RAJAGOPAL, Sriram ,  NARAYANAN, Sukunath ,  PARAMESWARAN, Venkatesan ,  JANARTHANAM, Venkatesan ,  NARAYANAM, Maruthikumar ,  GADDE, Sathyanarayana ,  RAMACHANDRAN, Uma ,  BALASUBRAMANIAN, Gopalan ,  SURENDRAN, Narayanan ,  NARAYANAN, Shridhar ,  VISHWAKARMA, Lolaknath, Santosh ,  SAXENA, Sanjeev

IPC: C07D403/04 ,  C07D401/04 ,  C07D239/26

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性疾病，炎症，疼痛障碍，类风湿性关节炎; 骨质疏松症; 多发性骨髓瘤 uveititis; 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 过敏性反应; 接触性皮炎; 肌肉退化; 哮喘; 慢性阻塞性肺病; 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：WO2006129178A8

公开(公告)日：2007-01-11

申请号：PCT/IB2006001437

申请日：2006-06-01

Applicant: GLENMARK PHARMACEUTICALS SA ,  MUTHUPPALANIAPPAN MEYYAPPAN ,  BALASUBRAMANIAN GOPALAN ,  GULLAPALLI SRINIVAS ,  JOSHI NEELIMA KHAIRATKAR ,  NARAYANAN SHRIDHAR

Inventor： MUTHUPPALANIAPPAN MEYYAPPAN ,  BALASUBRAMANIAN GOPALAN ,  GULLAPALLI SRINIVAS ,  JOSHI NEELIMA KHAIRATKAR ,  NARAYANAN SHRIDHAR

IPC: C07D231/54 ,  A61K31/416

CPC classification number: C07D231/54

Abstract: The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CBl) 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 ，饮食失调，减肥或控制，以及肥胖）。

公开(公告)号：WO2006011035A1

公开(公告)日：2006-02-02

申请号：PCT/IB2005/002146

申请日：2005-07-22

Applicant: GLENMARK PHARMACEUTICALS LTD. ,  THOMAS, Abraham ,  BALASUBRAMANIAN, Gopalan ,  LINGAM, Prasada, Rao, V., S. ,  SHAH, Daisy, Manish

Inventor： THOMAS, Abraham ,  BALASUBRAMANIAN, Gopalan ,  LINGAM, Prasada, Rao, V., S. ,  SHAH, Daisy, Manish

IPC: C07D207/16

CPC classification number: C07D213/70 ,  C07C233/62 ,  C07C233/78 ,  C07C235/50 ,  C07C271/24 ,  C07C311/05 ,  C07C311/18 ,  C07C317/14 ,  C07C323/67 ,  C07C2601/08 ,  C07C2603/74 ,  C07D207/16 ,  C07D207/34 ,  C07D209/42 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention relates to novel organic compounds, more particularly, novel Dipeptidyl peptidase IV (DPP-IV) inhibitors of general formula (I) wherein: Y is -S(O) m -, -CH 2 -, -CHF-, or -CF 2 ; X and Z are independently -C(=O)-, -NR 3 -, - O- or -S(O) m -; each occurrence of m is independently 0, 1 or 2; a is 0, 1 or 2; b is 0, 1 or 2; the dotted line [----] in the carbocyclic ring represents an optional double bond; R 1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic ring, substituted or unsubstituted heterocyclylalkyl, or substituted or unsubstituted heteroarylalkyl; R 2 is hydrogene, nitrile (-CN), COOH, or an isostere of carboxylic; or analogs, tautomers, enantiomers, diastereomers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, N-oxides, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

Abstract translation: 本发明涉及新的有机化合物，更具体地说，涉及通式（I）的新型二肽基肽酶IV（DPP-IV）抑制剂，其中：Y是-S（O）

公开(公告)号：WO2004037805A1

公开(公告)日：2004-05-06

申请号：PCT/IB2003/004442

申请日：2003-10-08

Applicant: GLENMARK PHARMACEUTICALS LTD. ,  BALASUBRAMANIAN, Gopalan ,  GHARAT, Laxmikant, Atmaram ,  LAKDAWALA, Aftab, Dawoodbhai ,  ANUPINDI, Raghu, Ram

Inventor： BALASUBRAMANIAN, Gopalan ,  GHARAT, Laxmikant, Atmaram ,  LAKDAWALA, Aftab, Dawoodbhai ,  ANUPINDI, Raghu, Ram

IPC: C07D307/91

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：WO2010079413A3

公开(公告)日：2010-12-02

申请号：PCT/IB2010000008

申请日：2010-01-07

Applicant: ORCHID RES LAB LTD ,  BALASUBRAMANIAN GOPALAN ,  SAKAMURI SUKUMAR ,  SINGH GAJENDRA ,  DHARMALINGAM SIVANESAN ,  POOPPADY XAVIER FRANKLIN ,  NARAYANAN SHRIDHAR ,  MOOKKAN JEYAMURUGAN ,  BALASUBRAMANIAN JEGANATHA SIVAKUMAR ,  RAJALINGAM AGNEESWARI ,  KULATHINGAL JAYANARAYAN

Inventor： BALASUBRAMANIAN GOPALAN ,  SAKAMURI SUKUMAR ,  SINGH GAJENDRA ,  DHARMALINGAM SIVANESAN ,  POOPPADY XAVIER FRANKLIN ,  NARAYANAN SHRIDHAR ,  MOOKKAN JEYAMURUGAN ,  BALASUBRAMANIAN JEGANATHA SIVAKUMAR ,  RAJALINGAM AGNEESWARI ,  KULATHINGAL JAYANARAYAN

IPC: C07D207/10

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：WO2010079413A2

公开(公告)日：2010-07-15

申请号：PCT/IB2010/000008

申请日：2010-01-07

Applicant: ORCHID RESEARCH LABORATORIES LTD. ,  BALASUBRAMANIAN, Gopalan ,  SAKAMURI, Sukumar ,  SINGH, Gajendra ,  DHARMALINGAM, Sivanesan ,  POOPPADY XAVIER, Franklin ,  NARAYANAN, Shridhar ,  MOOKKAN, Jeyamurugan ,  BALASUBRAMANIAN, Jeganatha, Sivakumar ,  RAJALINGAM, Agneeswari ,  KULATHINGAL, Jayanarayan

Inventor： BALASUBRAMANIAN, Gopalan ,  SAKAMURI, Sukumar ,  SINGH, Gajendra ,  DHARMALINGAM, Sivanesan ,  POOPPADY XAVIER, Franklin ,  NARAYANAN, Shridhar ,  MOOKKAN, Jeyamurugan ,  BALASUBRAMANIAN, Jeganatha, Sivakumar ,  RAJALINGAM, Agneeswari ,  KULATHINGAL, Jayanarayan

IPC: C07D207/10

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）的新型化合物，其衍生物，类似物，互变异构形式，区域异构体，立体异构体，多晶型物，溶剂化物，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; 治疗肥胖症，炎症，自身免疫性疾病如多发性硬化症，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。