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

Applicant: 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

Inventor： 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: 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 classification number: 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

Abstract: 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).

Abstract translation: 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

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

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

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

CPC classification number: 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

Abstract: 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.

Abstract translation: 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

Applicant: 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

Inventor： 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: C07D265/36 ,  C07D413/04 ,  A61K31/538 ,  A61P5/18

CPC classification number: C07D265/36 ,  A61K31/538 ,  C07D413/04

Abstract: 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).

Abstract translation: 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：WO2012038944A1

公开(公告)日：2012-03-29

申请号：PCT/IB2011/054229

申请日：2011-09-26

Applicant: RANBAXY LABORATORIES LIMITED ,  KHERA, Manoj Kumar ,  PALLE, Venkata P. ,  SATTIGERI, Viswajanani ,  SATTIGERI, Jitendra ,  SONI, Ajay ,  RAUF, Abdul Rehman Abdul ,  SIVAKUMAR, R. ,  REDDY, Ranadheer R. ,  MUSIB, Arpita ,  CLIFFE, Ian A. ,  BHATNAGAR, Pradip Kumar ,  RAY, Abhijit ,  SRIVASTAVA, Punit ,  DASTIDAR, Sunanda Ghosh

Inventor： KHERA, Manoj Kumar ,  PALLE, Venkata P. ,  SATTIGERI, Viswajanani ,  SATTIGERI, Jitendra ,  SONI, Ajay ,  RAUF, Abdul Rehman Abdul ,  SIVAKUMAR, R. ,  REDDY, Ranadheer R. ,  MUSIB, Arpita ,  CLIFFE, Ian A. ,  BHATNAGAR, Pradip Kumar ,  RAY, Abhijit ,  SRIVASTAVA, Punit ,  DASTIDAR, Sunanda Ghosh

IPC: C07D209/48 ,  C07D253/04 ,  C07D401/12 ,  C07C271/28 ,  A61K31/27 ,  A61K31/4035 ,  A61K31/53 ,  A61P11/00 ,  A61P19/02 ,  A61P35/00

CPC classification number: C07D253/04 ,  C07C271/28 ,  C07D209/48 ,  C07D401/12

Abstract: The present invention relates to methyl sulfonamides and N-formamides derivatives of formula (I) and to processes for their syntheses. The invention also relates to pharmacological compositions containing these derivatives and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatie arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, dry eye, neointimal proliferation which leads to restenosis and ischemic heart failure, stroke, renal disease, tumor metastasis, and other inflammatory disorders characterized by over expression and over activation of an matrix metalloproteinase using the compounds.

Abstract translation: 本发明涉及式（I）的甲基磺酰胺和N-甲酰胺衍生物及其合成方法。 本发明还涉及含有这些衍生物的药物组合物和治疗哮喘，类风湿性关节炎，COPD，鼻炎，骨关节炎，银屑病关节炎，牛皮癣，肺纤维化，肺部炎症，急性呼吸窘迫综合征，牙周炎，多发性硬化，牙龈炎，动脉粥样硬化， 干眼症，新生内膜增生，其导致再狭窄和缺血性心力衰竭，中风，肾脏疾病，肿瘤转移和其他以使用该化合物过度表达和过度活化基质金属蛋白酶为特征的炎症性疾病。

公开(公告)号：WO2008035315A3

公开(公告)日：2008-12-04

申请号：PCT/IB2007053854

申请日：2007-09-22

Applicant: RANBAXY LAB LTD ,  RUDRA SONALI ,  GUPTA NIDHI ,  BAREGAMA LALIT KUMAR ,  AGARWAL RITU ,  KHAIRNAR VINAYAK VASANTRAO ,  CHAKLADAR SASWATI ,  RAMAIAH MANDADAPU RAGHU ,  MUTHUKAMAL NAGARAJAN ,  BALACHANDRAN SARLA ,  RAMNANI SARIKA ,  PALLE VENKATA P ,  DASTIDAR SUNANDA G ,  RAY ABHIJIT ,  VIJAYKRISHNAN LALITHA ,  SATTIGERI JITENDRA

Inventor： RUDRA SONALI ,  GUPTA NIDHI ,  BAREGAMA LALIT KUMAR ,  AGARWAL RITU ,  KHAIRNAR VINAYAK VASANTRAO ,  CHAKLADAR SASWATI ,  RAMAIAH MANDADAPU RAGHU ,  MUTHUKAMAL NAGARAJAN ,  BALACHANDRAN SARLA ,  RAMNANI SARIKA ,  PALLE VENKATA P ,  DASTIDAR SUNANDA G ,  RAY ABHIJIT ,  VIJAYKRISHNAN LALITHA ,  SATTIGERI JITENDRA

IPC: C07D261/04 ,  A61K31/41 ,  A61P29/00 ,  C07D261/20 ,  C07D498/10

CPC classification number: C07D498/10 ,  C07D261/04 ,  C07D261/20

Abstract: The present invention relates to catechol derivatives of formula (I), which can be used as inhibitors of phosphodiesterase (PDPI) type 4 or type 7, Compounds disclosed herein can be useful in the treatment of CNS disorders, inflammatory diseases such as, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and their use as phosphodiesterase (PDE) type 4 or type 7 inhibitors.

Abstract translation: 本发明涉及式（I）的儿茶酚衍生物，其可用作4型或7型磷酸二酯酶（PDPI）的抑制剂。本文公开的化合物可用于治疗CNS疾病，炎性疾病如AIDS， 哮喘，关节炎，支气管炎，慢性阻塞性肺疾病（COPD），牛皮癣，过敏性鼻炎，休克，特应性皮炎，克罗恩病，成人呼吸窘迫综合征（ARDS），嗜酸性肉芽肿，过敏性结膜炎，骨关节炎，溃疡性结肠炎等炎症性疾病 在人类 提供了制备所公开化合物的方法，以及含有所公开化合物的药物组合物及其作为4型或7型抑制剂的磷酸二酯酶（PDE）的用途。

公开(公告)号：WO2008035316A3

公开(公告)日：2008-11-27

申请号：PCT/IB2007053855

申请日：2007-09-22

Applicant: RANBAXY LAB LTD ,  BALACHANDRAN SARALA ,  GUPTA NIDHI ,  KHAIRNAR VINAYAK VASANTRAO ,  RUDRA SONALI ,  PALLE VENKATA P ,  DASTIDAR SUNANDA G

Inventor： BALACHANDRAN SARALA ,  GUPTA NIDHI ,  KHAIRNAR VINAYAK VASANTRAO ,  RUDRA SONALI ,  PALLE VENKATA P ,  DASTIDAR SUNANDA G

IPC: C07D413/04 ,  A61K31/42

CPC classification number: C07D261/18 ,  C07D413/04

Abstract: The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Compounds disclosed herein can be useful in the treatment of CNS diseases, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and their use as PDE type IV selective inhibitors, are provided.

Abstract translation: 本发明涉及磷酸二酯酶（PDE）IV型选择性抑制剂。 本文公开的化合物可用于治疗CNS疾病，AIDS，哮喘，关节炎，支气管炎，慢性阻塞性肺疾病（COPD），牛皮癣，过敏性鼻炎，休克，特应性皮炎，克罗恩病，成人呼吸窘迫综合征（ARDS） 嗜酸粒细胞性肉芽肿，过敏性结膜炎，骨关节炎，溃疡性结肠炎和其他炎性疾病，特别是人类。 提供制备所公开化合物的方法，含有所公开化合物的药物组合物及其作为PDE IV型选择性抑制剂的用途。

公开(公告)号：WO2008117229A1

公开(公告)日：2008-10-02

申请号：PCT/IB2008/051088

申请日：2008-03-24

Applicant: RANBAXY LABORATORIES LIMITED ,  KUMAR, Naresh ,  KAUR, Kirandeep ,  GARG, Malvika ,  PALLE, Venkata, P. ,  SALMAN, Mohammad ,  RAY, Abhijit ,  GUPTA, Suman ,  MALHOTRA, Shivani ,  SHIRUMALLA, Rajkumar

Inventor： KUMAR, Naresh ,  KAUR, Kirandeep ,  GARG, Malvika ,  PALLE, Venkata, P. ,  SALMAN, Mohammad ,  RAY, Abhijit ,  GUPTA, Suman ,  MALHOTRA, Shivani ,  SHIRUMALLA, Rajkumar

IPC: C07D451/00 ,  A61K31/439 ,  A61P11/00 ,  A61P13/00

CPC classification number: C07D451/00

Abstract: The present invention relates to muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors. Also provided herein are pharmaceutical compositions comprising one or more muscarinic receptor antagonists and at least one or more therapeutic agent selected from histamine antagonists, corticosteroids, beta agonists, leukotriene antagonists, EGFR kinase inhibitors, PAF antagonists, 5-lipoxygenase inhibitors, chemokine inhibitors, PDE-4 inhibitors or p38 MAP Kinase inhibitors.

Abstract translation: 本发明涉及毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病，以及其它用途。 本发明还涉及制备所公开的化合物的方法，含有所公开的化合物的药物组合物，以及用于治疗通过毒蕈碱受体介导的疾病的方法。 本文还提供了包含一种或多种毒蕈碱受体拮抗剂和至少一种或多种选自组胺拮抗剂，皮质类固醇，β激动剂，白细胞三烯拮抗剂，EGFR激酶抑制剂，PAF拮抗剂，5-脂肪氧合酶抑制剂，趋化因子抑制剂，PDE -4抑制剂或p38 MAP激酶抑制剂。

公开(公告)号：WO2008104994A2

公开(公告)日：2008-09-04

申请号：PCT/IN2008/000109

申请日：2008-02-25

Applicant: ADVINUS THERAPEUTICS PRIVATE LIMITED ,  MOOKHTIAR, Kasim, A. ,  BHUNIYA, Debnath ,  DAVE, Bhavesh ,  KAPKOTI, Gobind, S. ,  BASU, Sujay ,  CHUGH, Anita ,  DE, Siddartha ,  PALLE, Venkata, P.

Inventor： MOOKHTIAR, Kasim, A. ,  BHUNIYA, Debnath ,  DAVE, Bhavesh ,  KAPKOTI, Gobind, S. ,  BASU, Sujay ,  CHUGH, Anita ,  DE, Siddartha ,  PALLE, Venkata, P.

IPC: C07D213/40 ,  C07D213/75 ,  C07D213/80 ,  C07D213/82 ,  C07D239/42 ,  C07D257/06 ,  C07D261/06

CPC classification number: C07D277/46 ,  C07D213/40 ,  C07D213/75 ,  C07D213/76 ,  C07D213/80 ,  C07D213/82 ,  C07D239/42 ,  C07D257/06 ,  C07D261/14 ,  C07D277/82 ,  C07D285/135 ,  C07D417/12

Abstract: Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators.

Abstract translation: 本公开的化合物是可用作葡糖苷酶活化剂的式（I）的2,2,2-三取代乙酰胺衍生物，其多晶型物，立体异构体，前药，溶剂化物，药学上可接受的盐和制剂。 本发明还描述了其制备方法。 本公开还描述了表征部分葡糖激酶激活剂的方法。

公开(公告)号：WO2008023336A2

公开(公告)日：2008-02-28

申请号：PCT/IB2007/053340

申请日：2007-08-21

Applicant: RANBAXY LABORATORIES LIMITED ,  SATTIGERI, Viswajanani, J. ,  PALLE, Venkata, P. ,  KHERA, Manoj, Kumar ,  REDDY, Ranadheer ,  TIWARI, Manoj, Kumar ,  SONI, Ajay ,  RAUF, Abdul, Rehman, Abdul ,  JOSEPH, Sony ,  MUSIB, Arpita ,  DASTIDAR, Sunanda, G. ,  SRIVASTAVA, Punit, Kumar

Inventor： SATTIGERI, Viswajanani, J. ,  PALLE, Venkata, P. ,  KHERA, Manoj, Kumar ,  REDDY, Ranadheer ,  TIWARI, Manoj, Kumar ,  SONI, Ajay ,  RAUF, Abdul, Rehman, Abdul ,  JOSEPH, Sony ,  MUSIB, Arpita ,  DASTIDAR, Sunanda, G. ,  SRIVASTAVA, Punit, Kumar

IPC: C07D209/48 ,  C07D401/06 ,  A61K31/4035 ,  A61P29/00

CPC classification number: A61K31/4155 ,  A61K31/4035 ,  A61K31/41 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/502 ,  A61K31/506 ,  A61K31/517 ,  A61K31/53 ,  A61K31/536 ,  A61K45/06 ,  C07D209/44 ,  C07D209/48 ,  C07D253/08 ,  C07D265/26 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/10 ,  C07D409/06 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10

Abstract: The present invention relates to β-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure β-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over- activation of a matrix metalloproteinase using the compounds.

Abstract translation: 本发明涉及作为基质金属蛋白酶抑制剂，特别是非对映异构体纯的β-羟基羧酸的β-羟基和氨基取代的羧酸，相应的合成方法以及含有该化合物的药物组合物 的本发明。 本发明化合物可用于治疗各种炎性，自身免疫和变应性疾病，例如治疗哮喘，类风湿性关节炎，COPD，鼻炎，骨关节炎，银屑病关节炎，牛皮癣，肺纤维化，伤口愈合障碍，肺部炎症， 急性呼吸窘迫综合征，牙周炎，多发性硬化症，牙龈炎，动脉粥样硬化，新内膜增殖，其导致再狭窄和缺血性心力衰竭，中风，肾脏疾病，肿瘤转移和其他炎症性疾病，其特征在于过度表达和过度激活 基质金属蛋白酶使用这些化合物。

公开(公告)号：WO2006085212A2

公开(公告)日：2006-08-17

申请号：PCT/IB2006/000285

申请日：2006-02-13

Applicant: RANBAXY LABORATORIES LIMITED ,  PALLE, Venkata, P. ,  BALACHANDRAN, Sarala ,  GUPTA, Nidhi ,  MUTHUKAMAL, Nagarajan ,  RAMAIAH, Mandadapu, Raghu ,  KHERA, Manoj, Kumar ,  BAREGAMA, Lailt, Kumar ,  KAHIRNAR, Vinayak, Vasantrao ,  RAY, Abhijit ,  DASTIDAR, Sunanda, G.

Inventor： PALLE, Venkata, P. ,  BALACHANDRAN, Sarala ,  GUPTA, Nidhi ,  MUTHUKAMAL, Nagarajan ,  RAMAIAH, Mandadapu, Raghu ,  KHERA, Manoj, Kumar ,  BAREGAMA, Lailt, Kumar ,  KAHIRNAR, Vinayak, Vasantrao ,  RAY, Abhijit ,  DASTIDAR, Sunanda, G.

IPC: C07D498/10 ,  C07D261/20 ,  C07D498/04 ,  A61K31/423 ,  A61K31/424 ,  A61P11/00 ,  A61P31/18

CPC classification number: C07D261/20

Abstract: The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.

Abstract translation: 本发明涉及异恶唑啉衍生物，其可用作IV型磷酸二酯酶（PDE）的选择性抑制剂。 特别地，本文公开的化合物可用于治疗AIDS，哮喘，关节炎，支气管炎，慢性阻塞性肺病（COPD），牛皮癣，过敏性鼻炎，休克，特应性皮炎，克罗恩病，成人呼吸窘迫综合征（ARDS） 嗜酸粒细胞肉芽肿，过敏性结膜炎，骨关节炎，溃疡性结肠炎和其他炎性疾病，特别是在人类中。 本发明还涉及制备所公开的化合物及其药物组合物及其作为磷酸二酯酶（PDE）IV型抑制剂的用途的方法。