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1. 发明授权

US06329534B1 Glucocorticoid receptor antagonists for treatment of diabetes 失效
标题翻译：用于治疗糖尿病的糖皮质激素受体拮抗剂
公开(公告)号：US06329534B1
公开(公告)日：2001-12-11
申请号：US09654322
申请日：2000-09-01
申请人： Philip R. Kym , Benjamin C. Lane , John K. Pratt , Tom Von Geldern , Martin Winn , Jehrod Brenneman , Jyoti R. Patel , David L. Arendsen , Irini Akritopoulou-Zanze
发明人： Philip R. Kym , Benjamin C. Lane , John K. Pratt , Tom Von Geldern , Martin Winn , Jehrod Brenneman , Jyoti R. Patel , David L. Arendsen , Irini Akritopoulou-Zanze
IPC分类号： C07D31180
CPC分类号： C07D407/04 , C07D311/80 , C07D409/04
摘要： Compounds of formula I are useful for treating type II diabetes, obesity, hyperglycemia, inadequate glucose clearance, hyperinsulinemia, hypertriglyceridemia, and high-circulating glucocorticoid levels, preparations of the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：式I化合物可用于治疗II型糖尿病，肥胖症，高血糖症，葡萄糖清除率不足，高胰岛素血症，高甘油三酯血症和高循环糖皮质激素水平，化合物的制剂，含该化合物的组合物，以及使用该化合物的治疗方法。

2. 发明授权

US5140039A Aminomethyl-thiochroman compounds 失效
标题翻译：氨基甲基 - 二氢苯并噻喃化合物
公开(公告)号：US5140039A
公开(公告)日：1992-08-18
申请号：US786140
申请日：1991-10-31
申请人： John F. DeBernardis , David L. Arendsen , Robert E. Zelle
发明人： John F. DeBernardis , David L. Arendsen , Robert E. Zelle
IPC分类号： C07D311/16 , C07D311/58 , C07D311/64 , C07D335/06 , C07D405/06 , C07D409/06 , C07D493/04
CPC分类号： C07D335/06 , C07D311/16 , C07D311/58 , C07D311/64 , C07D405/06 , C07D409/06 , C07D493/04
摘要： The present invention includes compounds represented by the formula: ##STR1## wherein X is O or S; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, hydroxy, halo, loweralkoxy, thioalkoxy and loweralkyl; or R.sub.1 and R.sub.2 taken together can form a methylenedioxy or ethylenedioxy bridge;R.sub.3 is loweralkyl;R.sub.4 is selected from ##STR2## wherein Y is O or S, R.sub.6 is hydrogen, methoxy or halo and m is 0 or 1; R.sub.5 is hydrogen, loweralkyl, phenyl or substituted phenyl wherein the phenyl ring is substituted with one, two or three substituents independently selected from loweralkyl, halo, hydroxy, loweralkoxy, amino and thioalkoxy; andR.sub.8 hydrogen or R.sub.3 and R.sub.8 taken together form a pyrrolidine ring; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明包括由下式表示的化合物：其中X是O或S; R 1和R 2独立地选自氢，羟基，卤素，低级烷氧基，硫代烷氧基和低级烷基; 或者R1和R2一起可以形成亚甲二氧基或亚乙二氧基桥; R3是低级烷基; R4选自其中Y是O或S，R6是氢，甲氧基或卤素，m是0或1; R5是氢，低级烷基，苯基或取代苯基，其中苯环被一个，两个或三个独立地选自低级烷基，卤素，羟基，低级烷氧基，氨基和硫代烷氧基的取代基取代; R8氢或R3和R8一起形成吡咯烷环; 或其药学上可接受的盐。

3. 发明授权

US5185364A Aminomethyl-chroman and -thiochroman compounds 失效
标题翻译：氨基甲基 - 苯并二氢吡喃并 - 二氢苯并噻喃化合物
公开(公告)号：US5185364A
公开(公告)日：1993-02-09
申请号：US786150
申请日：1991-10-31
申请人： John F. DeBernardis , David L. Arendsen , Robert E. Zelle
发明人： John F. DeBernardis , David L. Arendsen , Robert E. Zelle
IPC分类号： C07D311/16 , C07D311/58 , C07D311/64 , C07D335/06 , C07D405/06 , C07D409/06 , C07D493/04
CPC分类号： C07D335/06 , C07D311/16 , C07D311/58 , C07D311/64 , C07D405/06 , C07D409/06 , C07D493/04
摘要： The present invention includes compounds represented by the formula: ##STR1## wherein X is O or S;R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, hydroxy, halo, loweralkoxy, thioalkoxy and loweralkyl; or R.sub.1 and R.sub.2 taken together can form a methylenedioxy or ethylenedioxy bridge;R.sub.3 is loweralkyl;R.sub.4 is selected from ##STR2## wherein Y is O or S, R.sub.6 is hydrogen, methoxy or halo and m is 0 or 1l R.sub.5 is hydrogen, loweralkyl, phenyl or substituted phenyl wherein the phenyl ring is substituted with one, two or three substituents independently selected from loweralkyl, halo, hydroxy, loweralkoxy, amino and thioalkoxy; andR.sub.8 is hydrogen or R.sub.3 and R.sub.8 taken together form a pyrrolidine ring; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明包括由下式表示的化合物：其中X是O或S; R 1和R 2独立地选自氢，羟基，卤素，低级烷氧基，硫代烷氧基和低级烷基; 或者R1和R2一起可以形成亚甲二氧基或亚乙二氧基桥; R3是低级烷基; R4选自其中Y是O或S，R6是氢，甲氧基或卤素，m是0或者R1是氢，低级烷基，苯基或取代的苯基，其中苯环被一个，两个或三个取代基取代卤素，羟基，低级烷氧基，氨基和硫代烷氧基; 并且R 8是氢或R 3和R 8一起形成吡咯烷环; 或其药学上可接受的盐。

4. 发明授权

US4234594A Pyrazolyl amino imidazolines as antihypertensive agents 失效
标题翻译：吡唑基氨基咪唑啉作为抗高血压药
公开(公告)号：US4234594A
公开(公告)日：1980-11-18
申请号：US36884
申请日：1979-05-07
申请人： Martin Winn , Carl W. Nordeen , David L. Arendsen
发明人： Martin Winn , Carl W. Nordeen , David L. Arendsen
IPC分类号： C07D231/38 , C07D231/40 , A61K31/40 , A61K31/415 , A61K31/435 , A61K31/47
CPC分类号： C07D231/38 , C07D231/40
摘要： Described is a method of treating hypertensive by administering to mammalian patients compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, loweralkyl, lowercycloalkyl, aralkyl, aryl, pyridyl, isoquinolyl, phthalazinyl, or aryl substituted by one or more hydrogen, halo, loweralkyl, lowercycloalkyl, haloloweralkyl, haloloweralkyl, aminosulfonyl, nitro, hydroxy, alkoxy, carboxy, alkoxycarbonyl, cycloalkoxy carbonyl, aminocarbonyl, diloweralkylaminocarbonyl or ##STR2## wherein n is 4 or 5.R.sub.3 is hydrogen, halogen, loweralkyl or aryl, andR.sub.4 is hydrogen, acyl, amino or loweralkyl, and the pharmaceutically acceptable acid addition salts thereof.
摘要翻译：描述了通过向哺乳动物患者施用式IMA的化合物治疗高血压的方法，其中R 1和R 2是氢，低级烷基，低级环烷基，芳烷基，芳基，吡啶基，异喹啉基，酞嗪基或被一个或多个氢取代的芳基，卤素低级烷基，低级环烷基，卤代低级烷基，卤代低级烷基，氨基磺酰基，硝基，羟基，烷氧基，羧基，烷氧羰基，环烷氧基羰基，氨基羰基，二低级烷基氨基羰基或其中n为4或5.R 3为氢，卤素，低级烷基或芳基，是氢，酰基，氨基或低级烷基，及其药学上可接受的酸加成盐。

5. 发明授权

US06579882B2 Cell adhesion-inhibiting antiinflammatory compounds 失效
标题翻译：细胞粘附抑制性抗炎化合物
公开(公告)号：US06579882B2
公开(公告)日：2003-06-17
申请号：US09799729
申请日：2001-03-06
申请人： Andrew O. Stewart , Steven A. Boyd , David L. Arendsen , Pramila Bhatia , Kevin R. Condroski , Jennifer C. Freeman , Indrani W. Gunawardana , Gui-Dong Zhu , Kraig Lartey , Catherine M. McCarty , Nicholas A. Mort , Meena V. Patel , Michael A. Staeger , David M. Stout
发明人： Andrew O. Stewart , Steven A. Boyd , David L. Arendsen , Pramila Bhatia , Kevin R. Condroski , Jennifer C. Freeman , Indrani W. Gunawardana , Gui-Dong Zhu , Kraig Lartey , Catherine M. McCarty , Nicholas A. Mort , Meena V. Patel , Michael A. Staeger , David M. Stout
IPC分类号： A61K31519
CPC分类号： C07D493/04 , C07D495/04 , C07D513/04
摘要： Compounds having Formula I are useful for treating inflammation. Also disclosed are pharmaceutical compositions comprising compounds of Formula I, and methods of inhibiting/treating inflammatory diseases in a mammal.
摘要翻译：具有式Iare的化合物可用于治疗炎症。还公开了包含式I化合物的药物组合物，以及哺乳动物抑制/治疗炎性疾病的方法。

6. 发明授权

US06232320B1 Cell adhesion-inhibiting antiinflammatory compounds 有权
标题翻译：细胞粘附抑制性抗炎化合物
公开(公告)号：US06232320B1
公开(公告)日：2001-05-15
申请号：US09325336
申请日：1999-06-03
申请人： Andrew O. Stewart , Steven A. Boyd , David L. Arendsen , Pramila Bhatia , Kevin R. Condroski , Jennifer C. Freeman , Indrani W. Gunawardana , Gui-Dong Zhu , Kraig Lartey , Catherine M. McCarty , Nicholas A. Mort , Meena V. Patel , Michael A. Staeger , David M. Stout
发明人： Andrew O. Stewart , Steven A. Boyd , David L. Arendsen , Pramila Bhatia , Kevin R. Condroski , Jennifer C. Freeman , Indrani W. Gunawardana , Gui-Dong Zhu , Kraig Lartey , Catherine M. McCarty , Nicholas A. Mort , Meena V. Patel , Michael A. Staeger , David M. Stout
IPC分类号： A61K314365
CPC分类号： C07D493/04 , C07D495/04 , C07D513/04
摘要： Compounds having Formula I are useful for treating inflammation. Also disclosed are pharmaceutical compositions comprising compounds of Formula I, and methods of inhibiting/treating inflammatory diseases in a mammal.
摘要翻译：具有式Iare的化合物可用于治疗炎症。还公开了包含式I化合物的药物组合物，以及哺乳动物抑制/治疗炎性疾病的方法。

7. 发明授权

US4473586A Aminoalkyl dihydronaphthalenes 失效
标题翻译：氨基烷基二氢萘
公开(公告)号：US4473586A
公开(公告)日：1984-09-25
申请号：US374352
申请日：1982-05-03
申请人： John F. Debernardis , David L. Arendsen , Martin Winn
发明人： John F. Debernardis , David L. Arendsen , Martin Winn
IPC分类号： A61K31/135 , A61K31/18 , C07C317/22 , C07D295/096 , C07D317/70 , C07D319/20 , A61K31/165 , C07C143/72
CPC分类号： C07D295/096 , C07C323/00 , C07D317/70 , C07D319/20
摘要： Disclosed herein are 1-aminoalkyl-3,4-dihydronaphthalenes represented by the formula ##STR1## wherein n is 1 or 2; R, R.sub.1, and R.sub.2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, thiomethyl, halo, or ##STR2## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula ##STR3## wherein R.sub.7 is loweralkyl of 1 to 4 carbon atoms; or R and R.sub.1, or R.sub.1 and R.sub.2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R.sub.1 or R.sub.2 must be other than hydrogen; and R.sub.3 and R.sub.4 are independently selected from hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula ##STR4## wherein m is 0, 1 or 2, p is 0 or 1, R.sub.8 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R.sub.9 and R.sub.10 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1 to 4 carbon atoms, or halo, or R.sub.9 and R.sub.10 can be taken together to form a methylenedioxy or ethylenedioxy bridge; or 1,4-benzodioxan of the formula ##STR5## wherein q is 1, 2 or 3, and R.sub.11 is hydrogen, methoxy, or halo; or R.sub.3 and R.sub.4 can be taken together to form a piperazino, piperidino or morpholino moiety; and the pharmaceutically acceptable salts thereof. Also disclosed are novel intermediates useful in the preparation of these compounds.
摘要翻译：本文公开了由式（I）表示的1-氨基烷基-3,4-二氢萘，其中n为1或2; R 1，R 2和R 2独立地选自氢，羟基，1至3个碳原子的低级烷氧基，1至3个碳原子的低级链烯氧基，硫代甲基，卤素或者其中R 5和R 6独立地选自氢， 1至4个碳原子的磺酰基或下式的其中R 7为1至4个碳原子的低级烷基; 或R和R 1，或R 1和R 2可以一起形成亚甲二氧基或亚乙二氧基桥; 条件是R，R 1或R 2中的至少一个必须不是氢; 并且R 3和R 4独立地选自氢; 1至4个碳原子的低级烷基; 1至4个碳原子的卤素取代的低级烷基; 其中m为0,1或2，p为0或1，R 8为氢或1至4个碳原子的低级烷基，R 9和R 10独立地选自氢，羟基，甲氧基，低级烷基1 至4个碳原子，或卤素，或R 9和R 10可以一起形成亚甲二氧基或亚乙二氧基桥; 或其中q为1,2或3，且R 11为氢，甲氧基或卤素的式“IMAGE”的1,4-苯并二恶烷; 或者R 3和R 4可以一起形成哌嗪基，哌啶子基或吗啉代部分; 及其药学上可接受的盐。还公开了可用于制备这些化合物的新型中间体。

8. 发明授权

US4226877A Pyrazoles active in the central nervous system 失效
标题翻译：吡唑类在中枢神经系统中活跃
公开(公告)号：US4226877A
公开(公告)日：1980-10-07
申请号：US39015
申请日：1979-05-14
申请人： David L. Arendsen
发明人： David L. Arendsen
IPC分类号： C07D231/16 , C07D231/20 , A61K31/415 , C07D403/12
CPC分类号： C07D231/20 , C07D231/16
摘要： Disclosed are pyrazoles of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, or phenyl, R.sub.2 is hydrogen or lower alkyl, R.sub.3 is alkoxy or hydroxy, R.sub.4 is lower alkyl, and the pharmaceutically acceptable acid addition salts thereof. The compounds are useful primarily as antipsychotic agents. As an example, they exhibit central nervous system activity as antischizophrenic agents.
摘要翻译：公开了式IMA的吡唑，其中R 1是氢，低级烷基或苯基，R 2是氢或低级烷基，R 3是烷氧基或羟基，R 4是低级烷基，和其药学上可接受的酸加成盐。该化合物主要用作抗精神病药。作为示例，它们表现出作为抗精神分裂症药剂的中枢神经系统活性。

9. 发明授权

US06583180B2 Glucocorticoid receptor modulators 失效
标题翻译：糖皮质激素受体调节剂
公开(公告)号：US06583180B2
公开(公告)日：2003-06-24
申请号：US10072548
申请日：2002-02-08
申请人： James T. Link , Bryan K. Sorensen , Jyoti R. Patel , David L. Arendsen , Gaoquan Li
发明人： James T. Link , Bryan K. Sorensen , Jyoti R. Patel , David L. Arendsen , Gaoquan Li
IPC分类号： A61K3118
CPC分类号： C07D295/088 , C07C307/10 , C07C311/08 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are novel glucocorticoid receptor modulators and are useful for treating type II diabetes in a mammal.
摘要翻译：式（I）化合物或其药学上可接受的盐是新型糖皮质激素受体调节剂，可用于治疗哺乳动物的II型糖尿病。

10. 发明授权

US4505932A Method of producing .alpha..sub.2 -adrenergic receptor agonist activity 失效
标题翻译：产生α2-肾上腺素能受体激动剂活性的方法
公开(公告)号：US4505932A
公开(公告)日：1985-03-19
申请号：US590938
申请日：1984-03-19
申请人： John F. DeBernardis , David L. Arendsen
发明人： John F. DeBernardis , David L. Arendsen
IPC分类号： C07C45/46 , C07C49/753 , C07C51/36 , A61K31/135 , C07C91/42
CPC分类号： C07C45/46 , C07C49/753 , C07C51/36
摘要： A method of producing .alpha..sub.2 -adrenergic receptor agonist activity by contacting an .alpha..sub.2 -adrenergic receptor with an effective amount of a compound of the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen or loweralkyl of 1 or 2 carbon atoms, or a pharmaceutically acceptable salt thereof.
摘要翻译：通过使α2-肾上腺素能受体与有效量的下式化合物接触来产生α2-肾上腺素能受体激动剂活性的方法：其中R 1，R 2，R 3和R 4独立地选自氢或1或1的低级烷基或2个碳原子，或其药学上可接受的盐。

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