公开(公告)号：US20100222393A1

公开(公告)日：2010-09-02

申请号：US12159505

申请日：2006-12-21

申请人： Naresh Kumar ,  Jaskiran Kaur ,  Venkata P. Palle ,  Beenu Bhatt ,  Shelly Jindal ,  Anita Chugh ,  Suman Gupta ,  Abhijit Ray ,  Shivani Malhotra ,  Raj Kumar Shirumalla

发明人： Naresh Kumar ,  Jaskiran Kaur ,  Venkata P. Palle ,  Beenu Bhatt ,  Shelly Jindal ,  Anita Chugh ,  Suman Gupta ,  Abhijit Ray ,  Shivani Malhotra ,  Raj Kumar Shirumalla

IPC分类号： A61K31/4439 ,  C07D233/54 ,  A61K31/4164 ,  C07D401/02 ,  A61P11/00 ,  A61P13/00 ,  A61P1/00 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D233/54 ,  C07D233/14 ,  C07D233/56 ,  C07D233/64 ,  C07D401/12

摘要： Compounds of Formula (I), wherein represents a single bond when G is —OH and double bond when G is —O; R1 and R2 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, heterocyclylalkyl or heteroarylalkyl; R3 is selected from the group selected from hydrogen, hydroxy, alkoxy, alkenyloxy or alkynyloxy; X is selected from oxygen, —NH, —NR (wherein R is alkyl, alkenyl, alkenyl, alkynyl or aryl), sulphur or no atom; Het is heterocyclyl or heteroaryl; n is an integer from 1 to 6; are muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and 4 i gastrointestinal systems mediated through muscarinic receptors.

摘要翻译： 式（I）的化合物，当G为-OH时，当G为-O时，表示单键; R 1和R 2独立地选自氢，烷基，烯基，炔基，芳烷基，环烷基，芳基，杂芳基，杂环基，杂环基烷基或杂芳基烷基; R3选自氢，羟基，烷氧基，烯氧基或炔氧基; X选自氧，-NH，-NR（其中R是烷基，烯基，烯基，炔基或芳基），硫或无原子; Het是杂环基或杂芳基; n是1至6的整数; 是毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，尿和4I胃肠系统的各种疾病，以及其它用途。

公开(公告)号：US20100144772A1

公开(公告)日：2010-06-10

申请号：US12528770

申请日：2008-02-25

申请人： Kasim A. Mookhtiar ,  Debnath Bhuniya ,  Bhavesh Dave ,  Gobind S. Kapkoti ,  Sujay Basu ,  Anita Chugh ,  Siddhartha De ,  Venkata P. Palle

发明人： Kasim A. Mookhtiar ,  Debnath Bhuniya ,  Bhavesh Dave ,  Gobind S. Kapkoti ,  Sujay Basu ,  Anita Chugh ,  Siddhartha De ,  Venkata P. Palle

IPC分类号： A61K31/427 ,  C07D417/12 ,  C07D277/38 ,  C07D239/22 ,  A61K31/4439 ,  A61K31/426 ,  A61K31/505 ,  A61P3/10 ,  A61P3/04 ,  C12Q1/48

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

摘要： 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.

摘要翻译： 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：US20090306129A1

公开(公告)日：2009-12-10

申请号：US12067013

申请日：2006-09-11

申请人： Venkata P. Palle ,  Sarala Balachandran ,  Nidhi Gupta ,  Vinayak Vasantrao Khairnar ,  Mandadapu Raghuramaiah ,  Abhijit Ray ,  Sunanda Ghose Dastidar

发明人： Venkata P. Palle ,  Sarala Balachandran ,  Nidhi Gupta ,  Vinayak Vasantrao Khairnar ,  Mandadapu Raghuramaiah ,  Abhijit Ray ,  Sunanda Ghose Dastidar

IPC分类号： A61K31/415 ,  C07D231/10 ,  C07D471/04 ,  A61K31/437 ,  A61P11/06 ,  A61P25/00 ,  A61P17/00 ,  A61P29/00 ,  A61P19/02

CPC分类号： C07D471/04

摘要： The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided. Prepared compounds correspond to structure XIV Formula (XIV).

摘要翻译： 本发明涉及磷酸二酯酶（PDE）IV型选择性抑制剂。 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。 制备的化合物对应于结构XIV式（XIV）。

公开(公告)号：US20090221515A1

公开(公告)日：2009-09-03

申请号：US11574465

申请日：2005-08-31

申请人： Viswajanani Jitendra Sattigeri ,  Sudershan K. Arora ,  Venkata P. Palle ,  Mohammad Salman ,  Abhijit Ray ,  Raj Kumar Shirumalla ,  Abdul Rehaman Abdul Rauf

发明人： Viswajanani Jitendra Sattigeri ,  Sudershan K. Arora ,  Venkata P. Palle ,  Mohammad Salman ,  Abhijit Ray ,  Raj Kumar Shirumalla ,  Abdul Rehaman Abdul Rauf

IPC分类号： A61K31/7008 ,  C07H5/04

CPC分类号： C07H15/18

摘要： The present invention relates to monosaccharide derivatives as anti-inflammatory agents. The compounds disclosed herein can be useful for inhibition and prevention of inflammation and associated pathologies, including inflammatory and autoimmune diseases such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection, psoriasis, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis or allergic rhinitis. Pharmacological compositions containing the compounds of the present invention and the methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, type I diabetes, psoriasis, allograft rejection, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis, allergic rhinitis and other inflammatory and/or autoimmune disorders, using the compounds are also provided.

摘要翻译： 本发明涉及作为抗炎剂的单糖衍生物。 本文公开的化合物可用于抑制和预防炎症和相关病理学，包括炎症和自身免疫性疾病如支气管哮喘，类风湿性关节炎，I型糖尿病，多发性硬化，同种异体移植排斥，牛皮癣，炎性肠病，溃疡性结肠炎，痤疮 ，动脉粥样硬化，癌症，瘙痒症或过敏性鼻炎。 包含本发明化合物的药物组合物，治疗支气管哮喘，慢性阻塞性肺病，类风湿性关节炎，多发性硬化，I型糖尿病，牛皮癣，同种异体移植排斥，炎性肠病，溃疡性结肠炎，痤疮，动脉粥样硬化，癌症， 还提供了使用该化合物的瘙痒症，过敏性鼻炎和其它炎性和/或自身免疫性疾病。

公开(公告)号：US20090048247A1

公开(公告)日：2009-02-19

申请号：US11815695

申请日：2006-02-13

申请人： Venkata P. Palle ,  Sarala Balachandran ,  Nidhi Gupta ,  Nagarajan Muthukamal ,  Mandadapu Raghu Ramaiah ,  Manoj Kumar Khera ,  Lailt Kumar Baregama ,  Vinayak Vasantrao Khairnar ,  Abhijit Ray ,  Sunanda G. Dastidar

发明人： Venkata P. Palle ,  Sarala Balachandran ,  Nidhi Gupta ,  Nagarajan Muthukamal ,  Mandadapu Raghu Ramaiah ,  Manoj Kumar Khera ,  Lailt Kumar Baregama ,  Vinayak Vasantrao Khairnar ,  Abhijit Ray ,  Sunanda G. Dastidar

IPC分类号： A61K31/5377 ,  C07D498/10 ,  A61K31/424 ,  A61P31/18

CPC分类号： C07D261/20

摘要： 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.

摘要翻译： 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。

公开(公告)号：US09382216B2

公开(公告)日：2016-07-05

申请号：US14003853

申请日：2012-03-09

申请人： Manojkumar Ramprasad Shukla ,  Vinod Dinkar Chaudhari ,  Majid Bashir Sayyed ,  Ramesh Dattatraya Phadtare ,  Navnath Bajirao Walke ,  Sanjeev Anant Kulkarni ,  Venkata P. Palle ,  Rajender Kumar Kamboj

发明人： Manojkumar Ramprasad Shukla ,  Vinod Dinkar Chaudhari ,  Majid Bashir Sayyed ,  Ramesh Dattatraya Phadtare ,  Navnath Bajirao Walke ,  Sanjeev Anant Kulkarni ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D265/30 ,  C07D265/32 ,  C07D413/04

CPC分类号： A61K31/5375 ,  C07D265/30 ,  C07D265/32 ,  C07D413/04

摘要： 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).

摘要翻译： 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，治疗和/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：US20140155433A1

公开(公告)日：2014-06-05

申请号：US14130815

申请日：2012-07-02

申请人： Neelima Sinha ,  Navnath Popat Karche ,  Girish Dhanraj Hatnapure ,  Anil Kashiram Hajare ,  Venkata P. Palle ,  Rajender Kumar Kamboj

发明人： Neelima Sinha ,  Navnath Popat Karche ,  Girish Dhanraj Hatnapure ,  Anil Kashiram Hajare ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D277/56 ,  A61K31/381 ,  A61K31/454 ,  C07D417/12 ,  A61K45/06 ,  C07D277/28 ,  A61K31/426 ,  C07D207/335 ,  A61K31/40 ,  C07D333/22 ,  A61K31/427

CPC分类号： 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

摘要： Disclosed is a compound of formula (I): wherein ‘D’, ‘E’, ‘m’, ‘n’ 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 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.

摘要翻译： 公开了式（I）的化合物：其中'D'，'E'，'m'，'n'和R1-R4如本文所述，作为烟草乙酰胆碱受体的调节剂，特别是α7亚型， 需要它们以及类似物，前药，同位素取代的类似物，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，单独使用或与合适的其它药物组合使用，以及药物组合物 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：US20140018327A1

公开(公告)日：2014-01-16

申请号：US14007458

申请日：2012-03-27

申请人： Neelima Sinha ,  Gourhari Jana ,  Ajay Ramchandra Tilekar ,  Navnath Popat Karche ,  Venkata P. Palle ,  Rajender Kumar Kamboj

发明人： Neelima Sinha ,  Gourhari Jana ,  Ajay Ramchandra Tilekar ,  Navnath Popat Karche ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D207/34 ,  A61K45/06 ,  C07D207/335 ,  A61K31/635

CPC分类号： C07D207/34 ,  A61K31/402 ,  A61K31/635 ,  A61K45/06 ,  C07D207/333 ,  C07D207/335 ,  Y02A50/411 ,  A61K2300/00

摘要： Disclosed is a compound of formula (I) wherein ‘a’ and R1-R5 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 thereofs, 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.

摘要翻译： 公开了式（I）化合物，其中“a”和R1-R5如本文所述，作为有需要的受试者中烟碱乙酰胆碱受体，特别是α7亚型的调节剂，以及类似物，前药，同位素取代 类似物，代谢产物，药学上可接受的盐，多晶型物，溶剂化物，异构体，包合物和共结晶，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：US20130245000A1

公开(公告)日：2013-09-19

申请号：US13989611

申请日：2011-11-24

申请人： Rajesh Thotapally ,  Onkar Gangaram Kachi ,  Atish Harishchandra Rodge ,  Ashok Bhau Pathak ,  Bhavana Shrirang Kardile ,  Milind Dattatraya Sindkhedkar ,  Venkata P. Palle ,  Rajender Kumar Kamboj

发明人： Rajesh Thotapally ,  Onkar Gangaram Kachi ,  Atish Harishchandra Rodge ,  Ashok Bhau Pathak ,  Bhavana Shrirang Kardile ,  Milind Dattatraya Sindkhedkar ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D471/04 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/155 ,  A61K31/454 ,  A61K31/437 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D401/12

CPC分类号： C07D471/04 ,  A61K31/155 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/08

摘要： The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).

摘要翻译： 本发明涉及可用于治疗，预防和/或控制与调节GPR119受体活性相关的疾病，病症，综合征或病症的式（I）化合物。 本发明还涉及制备化合物的方法及其药物组合物。 本发明还涉及通过单独使用或以式（I）的组合来治疗，预防和/或治疗与调节GPR119受体相关的疾病，病症综合征或病症的方法。

公开(公告)号：US07915286B2

公开(公告)日：2011-03-29

申请号：US12067013

申请日：2006-09-11

申请人： Venkata P. Palle ,  Sarala Balachandran ,  Nidhi Gupta ,  Vinayak Vasantrao Khairnar ,  Mandadapu Raghuramaiah ,  Abhijit Ray ,  Sunanda Ghose Dastidar

发明人： Venkata P. Palle ,  Sarala Balachandran ,  Nidhi Gupta ,  Vinayak Vasantrao Khairnar ,  Mandadapu Raghuramaiah ,  Abhijit Ray ,  Sunanda Ghose Dastidar

IPC分类号： A61K31/415 ,  A61K31/437 ,  C07D231/10 ,  C07D471/04 ,  A61P11/06 ,  A61P25/00 ,  A61P17/00 ,  A61P29/00 ,  A61P19/02

CPC分类号： C07D471/04

摘要： The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided. Prepared compounds correspond to structure XIV Formula (XIV).

摘要翻译： 本发明涉及磷酸二酯酶（PDE）IV型选择性抑制剂。 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。 制备的化合物对应于结构XIV式（XIV）。