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1. 发明授权

US06492348B1 Adenosine derivatives 有权
标题翻译：腺苷衍生物
公开(公告)号：US06492348B1
公开(公告)日：2002-12-10
申请号：US09736018
申请日：2001-03-06
申请人： David Edmund Bays , Richard Peter Charles Cousins , Hazel Joan Dyke , Colin David Eldred , Brian David Judkins , Martin Pass , Andrew Michael Kenneth Pennell
发明人： David Edmund Bays , Richard Peter Charles Cousins , Hazel Joan Dyke , Colin David Eldred , Brian David Judkins , Martin Pass , Andrew Michael Kenneth Pennell
IPC分类号： A61K3170
CPC分类号： C07D473/00 , C07H19/16
摘要： A compound of formula (I) which is an agonist at the adenosine Al receptor, wherein Y, Z, and W represent heteroatoms, and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof for use in therapy.
摘要翻译：作为腺苷A1受体的激动剂的式（I）化合物，其中Y，Z和W表示杂原子，以及其盐和溶剂化物，特别是用于治疗的生理学上可接受的溶剂合物及其盐。

2. 发明授权

US06677316B2 Adenosine derivatives and methods of administration 有权
标题翻译：腺苷衍生物和给药方法
公开(公告)号：US06677316B2
公开(公告)日：2004-01-13
申请号：US10217107
申请日：2002-08-13
申请人： David Edmund Bays , Richard Peter Charles Cousins , Hazel Joan Dyke , Colin David Eldred , Brian David Judkins , Martin Pass , Andrew Michael Kenneth Pennell
发明人： David Edmund Bays , Richard Peter Charles Cousins , Hazel Joan Dyke , Colin David Eldred , Brian David Judkins , Martin Pass , Andrew Michael Kenneth Pennell
IPC分类号： A61K3170
CPC分类号： C07D473/00 , C07H19/16
摘要： A method of treating a patient suffering from or susceptible to ischemic heart disease, peripheral vascular disease or stroke or which subject is suffering pain, a CNS disorder or sleep apnea which comprises administering a therapeutically effective amount of an adenosine derivative which is an agonist at the adenosine A1 receptor and which exhibits little or no agonist activity of the A3 receptor. The adenosine derivative has a general formula (I) as follows:
摘要翻译：治疗患有或易患缺血性心脏病，外周血管疾病或中风或受试者患有疼痛，CNS病症或睡眠呼吸暂停症的患者的方法，其包括给予治疗有效量的作为激动剂的腺苷衍生物腺苷A1受体并且其表现出很少或没有A3受体的激动剂活性。腺苷衍生物具有如下通式（I）：

3. 发明授权

US06610665B1 2-(purin-9-yl)-tetrahydrofuran-3, 4-diol derivatives 失效
标题翻译： 2-（嘌呤-9-基） - 四氢呋喃-3,4-二醇衍生物
公开(公告)号：US06610665B1
公开(公告)日：2003-08-26
申请号：US09622313
申请日：2000-08-29
申请人： David Edmund Bays , Chuen Chan , Caroline Mary Cook , Brian Cox , Richard Peter Charles Cousins , Hazel Joan Dyke , Frank Ellis , Joanna Victoria Geden , Stephen Swanson
发明人： David Edmund Bays , Chuen Chan , Caroline Mary Cook , Brian Cox , Richard Peter Charles Cousins , Hazel Joan Dyke , Frank Ellis , Joanna Victoria Geden , Stephen Swanson
IPC分类号： A61K3170
CPC分类号： C07H19/16
摘要： There are disclosed according to the invention, compounds of formula (I) wherein R1, R2 and R3 are defined in the specification. Additionally, processes of preparing the compounds of formula (I), formulations containing same, and the administration of said compounds or formulations thereof in the treatment of inflammatory diseases are also disclosed.
摘要翻译：根据本发明公开了式（I）化合物，其中R1，R2和R3在说明书中定义。此外，还公开了制备式（I）化合物，含有其的制剂，以及所述化合物或其制剂在治疗炎性疾病中的用途的方法。

4. 发明授权

US06534486B1 2-(purin-9-yl)-Tetrahydrofuran-3,4-diol derivatives 失效
标题翻译： 2-（嘌呤-9-基） - 四氢呋喃-3,4-二醇衍生物
公开(公告)号：US06534486B1
公开(公告)日：2003-03-18
申请号：US09720193
申请日：2001-02-28
申请人： David George Allen , Chuen Chan , Caroline Mary Cook , Richard Peter Charles Cousins , Brian Cox , Hazel Joan Dyke , Frank Ellis , Joanna Victoria Geden , Heather Hobbs , Suzanne Elaine Keeling , Alison Judith Redgrave , Stephen Swanson , Caroline Whitworth , David Bays
发明人： David George Allen , Chuen Chan , Caroline Mary Cook , Richard Peter Charles Cousins , Brian Cox , Hazel Joan Dyke , Frank Ellis , Joanna Victoria Geden , Heather Hobbs , Suzanne Elaine Keeling , Alison Judith Redgrave , Stephen Swanson , Caroline Whitworth , David Bays
IPC分类号： A01N4304
CPC分类号： C07H19/16 , Y10S514/826 , Y10S514/851 , Y10S514/921 , Y10S514/925
摘要： A series of 2-(Purin-9-yl)-tetrahydrofuran-3,4-diol derivatives with broad anti-inflammatory properties which inhibit leukocyte recruitment and activation and which are agonists of the adenosine 2a receptor are described.
摘要翻译：描述了一系列具有抑制白细胞募集和活化并且是腺苷2a受体激动剂的广泛抗炎性质的2-（嘌呤-9-基） - 四氢呋喃-3,4-二醇衍生物。

5. 发明授权

US09365564B2 3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (β)-HSD1 有权
标题翻译： 3,3-二取代 - （8-氮杂 - 双环[3.2.1]辛-8-基） - [5-（1H-吡唑-4-基） - 噻吩-3-基] - 甲酮作为11 ＆bgr;） - HSD1
公开(公告)号：US09365564B2
公开(公告)日：2016-06-14
申请号：US13642963
申请日：2011-03-10
申请人： Scott Peter Webster , Jonathan Robert Seckl , Brian Robert Walker , Peter Ward , Thomas David Pallin , Hazel Joan Dyke , Trevor Robert Perrior
发明人： Scott Peter Webster , Jonathan Robert Seckl , Brian Robert Walker , Peter Ward , Thomas David Pallin , Hazel Joan Dyke , Trevor Robert Perrior
IPC分类号： C07D451/06 , C07D451/02 , C07D409/14 , C07D451/04
CPC分类号： C07D451/06 , C07D409/14 , C07D451/02 , C07D451/04
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3-disubstituted-(6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4,4-disubstituted piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
摘要翻译：本发明一般涉及治疗化合物领域。更具体地，本发明涉及某些3,3-二取代 - （8-氮杂 - 双环[3.2.1]辛-8-基） - [5-（1H-吡唑-4-基） - 噻吩-3-基 ] - 甲酮，3,3-二取代 - （6-氮杂 - 双环[3.1.1]庚-6-基） - [5-（1H-吡唑-4-基） - 噻吩-3-基] - 甲酮，和4,4-二取代哌啶-1-基） - [5-（1H-吡唑-4-基） - 噻吩-3-基] - 甲酮化合物，其特别是抑制11-羟基类固醇脱氢酶类型1（11＆bgr; -HSD1）。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制1型的1β-羟基类固醇脱氢酶; 治疗通过抑制11型β-羟基类固醇脱氢酶1改善的病症; 治疗代谢综合征，其包括诸如2型糖尿病和肥胖症的疾病，以及包括胰岛素抵抗，高血压，脂质障碍和心血管疾病如缺血性（冠心病）心脏病的相关疾病; 治疗CNS疾病如轻度认知障碍和早期痴呆，包括阿尔茨海默氏病; 等等

6. 发明申请

US20140080822A1 Tricyclic Pyrazole Sulphonamide Compounds and Methods of Making and Using Same 有权
标题翻译：三环吡唑磺酰胺化合物及其制备和使用方法
公开(公告)号：US20140080822A1
公开(公告)日：2014-03-20
申请号：US14116029
申请日：2012-05-07
申请人： Susan Mary Cramp , Hazel Joan Dyke , Thomas David Pallin , Robert Zahler
发明人： Susan Mary Cramp , Hazel Joan Dyke , Thomas David Pallin , Robert Zahler
IPC分类号： C07D498/14 , C07D471/04
CPC分类号： A61K31/5383 , A61K9/0053 , A61K31/4745 , C07D471/04 , C07D498/04 , C07D498/14
摘要： The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
摘要翻译：本发明提供三环磺酰胺化合物及其在治疗医学疾病如肥胖症中的用途。提供制备各种三环化合物的药物组合物和方法。化合物被认为具有抗甲硫氨酰氨基肽酶2的活性。

7. 发明申请

US20140073623A1 Tricyclic Sulfonamide Compounds and Methods of Making and Using Same 有权
标题翻译：三环磺酰胺化合物及其制备和使用方法
公开(公告)号：US20140073623A1
公开(公告)日：2014-03-13
申请号：US14116026
申请日：2012-05-07
申请人： Susan Mary Cramp , Hazel Joan Dyke , Thomas David Pallin , Robert Zahler
发明人： Susan Mary Cramp , Hazel Joan Dyke , Thomas David Pallin , Robert Zahler
IPC分类号： C07D498/04 , C07D487/04
CPC分类号： A61K31/5383 , A61K9/0053 , A61K31/407 , A61K31/4188 , A61K31/4745 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
摘要翻译：本发明提供三环磺酰胺化合物及其在治疗医学疾病如肥胖症中的用途。提供制备各种三环化合物的药物组合物和方法。化合物被认为具有抗甲硫氨酰氨基肽酶2的活性。

8. 发明授权

US08461328B2 Tricyclic heterocyclic compounds, compositions and methods of use thereof 失效
标题翻译：三环杂环化合物，其组合物及其使用方法
公开(公告)号：US08461328B2
公开(公告)日：2013-06-11
申请号：US13004808
申请日：2011-01-11
申请人： Srinivasan Babu , Phillippe Bergeron , Peter Dragovich , Hazel Joan Dyke , Paul Gibbons , Stefan Gradl , Emily Hanan , Christopher Hurley , Tony Johnson , Michael Koehler , Janusz Kulagowski , Sharada Labadie , Joseph Lyssikatos , Rohan Mendonca , Rebecca Pulk , Stuart Ward , Bohdan Waszkowycz , Mark Zak
发明人： Srinivasan Babu , Phillippe Bergeron , Peter Dragovich , Hazel Joan Dyke , Paul Gibbons , Stefan Gradl , Emily Hanan , Christopher Hurley , Tony Johnson , Michael Koehler , Janusz Kulagowski , Sharada Labadie , Joseph Lyssikatos , Rohan Mendonca , Rebecca Pulk , Stuart Ward , Bohdan Waszkowycz , Mark Zak
IPC分类号： A61P11/06 , A61P17/06 , A61P19/02 , A61P37/06 , C07D413/14 , C07D471/14
CPC分类号： C07D471/14 , C07D487/10
摘要： The invention provides novel compounds of formula I having the general formula: wherein R1, R2, R3, X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
摘要翻译：本发明提供具有以下通式的新颖的式I化合物：其中R1，R2，R3，X和Y如本文所述。因此，化合物可以以药学上可接受的组合物提供，并用于治疗免疫学或过度增殖性疾病。

9. 发明授权

US08299063B2 Amido-thiophene compounds and their use 有权
标题翻译：酰胺 - 噻吩化合物及其用途
公开(公告)号：US08299063B2
公开(公告)日：2012-10-30
申请号：US12920774
申请日：2009-03-13
申请人： Scott Peter Webster , Jonathan Robert Seckl , Brian Robert Walker , Peter Ward , Thomas David Pallin , Hazel Joan Dyke , Trevor Robert Perrior
发明人： Scott Peter Webster , Jonathan Robert Seckl , Brian Robert Walker , Peter Ward , Thomas David Pallin , Hazel Joan Dyke , Trevor Robert Perrior
IPC分类号： A61K31/55 , A61K31/551 , A61K31/541 , A61K31/5355 , A61K31/536 , A61K31/496 , A61K31/498 , A61K31/4709 , A61K31/451 , A61K31/4535 , A61K31/4402 , A61K31/4155 , C07D243/08 , C07D401/14 , C07D403/14 , C07D265/36 , C07D265/30 , C07D279/12 , C07D231/12 , C07D239/04
CPC分类号： C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D487/04 , C07D487/08
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
摘要翻译：本发明一般涉及治疗化合物领域。更具体地说，本发明涉及某些特别是抑制11型β-羟基类固醇脱氢酶（11＆amp; bgr-HSD1）的酰氨基噻吩化合物。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制1型的1β-羟基类固醇脱氢酶; 治疗通过抑制11型β-羟基类固醇脱氢酶1改善的病症; 治疗代谢综合征，其包括诸如2型糖尿病和肥胖症的疾病，以及包括胰岛素抵抗，高血压，脂质障碍和心血管疾病如缺血性（冠心病）心脏病的相关疾病; 治疗CNS疾病如轻度认知障碍和早期痴呆，包括阿尔茨海默氏病; 等等

10. 发明申请

US20120095046A1 Amido-Isothiazole Compounds and Their Use as Inhibitors of 11Beta-HSD1 for the Treatment of Metabolic Syndrome and Related Disorders 审中-公开
标题翻译：酰胺 - 异噻唑化合物及其作为11Beta-HSD1抑制剂用于治疗代谢综合征和相关疾病的用途
公开(公告)号：US20120095046A1
公开(公告)日：2012-04-19
申请号：US13377611
申请日：2010-06-14
申请人： Scott Peter Webster , Jonathan Robert Seckl , Brian Robert Walker , Peter Ward , Thomas David Pallin , Hazel Joan Dyke , Trevor Robert Perrior
发明人： Scott Peter Webster , Jonathan Robert Seckl , Brian Robert Walker , Peter Ward , Thomas David Pallin , Hazel Joan Dyke , Trevor Robert Perrior
IPC分类号： A61K31/4709 , C07D417/14 , A61K31/427 , C12N9/99 , A61P43/00 , A61P3/10 , A61P3/08 , A61P3/04 , A61P3/06 , A61P9/10 , A61P9/00 , A61P3/00 , A61P1/16 , A61P25/00 , A61P25/18 , A61P25/28 , A61P25/16 , A61P1/18 , A61P27/06 , A61P25/22 , A61P25/24 , A61P29/00 , A61P19/10 , A61P9/12 , A61P27/02 , A61P11/06 , A61P11/00 , A61P17/00 , A61P1/00 , A61P19/02 , C07D413/06
CPC分类号： C07D417/14 , C07D417/06
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-isothiazole compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
摘要翻译：本发明一般涉及治疗化合物领域。更具体地，本发明涉及某些特别是抑制11型β-羟基类固醇脱氢酶（11＆amp; bgr-HSD1）的酰胺 - 异噻唑化合物。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制1型的1β-羟基类固醇脱氢酶; 治疗通过抑制11型β-羟基类固醇脱氢酶1改善的病症; 治疗代谢综合征，其包括诸如2型糖尿病和肥胖症的疾病，以及包括胰岛素抵抗，高血压，脂质障碍和心血管疾病如缺血性（冠心病）心脏病的相关疾病; 治疗CNS疾病如轻度认知障碍和早期痴呆，包括阿尔茨海默氏病; 等等

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