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1. 发明授权

US06992101B2 N-(indole-2-carbonyl) and H-thieno[2,3-b]pyrrole-5-carboxamide anti-diabetic agents 失效
标题翻译： N-（吲哚-2-羰基）和H-噻吩并[2,3-b]吡咯-5-甲酰胺抗糖尿病药
公开(公告)号：US06992101B2
公开(公告)日：2006-01-31
申请号：US10703035
申请日：2003-11-06
申请人： Donald L. Bussolotti , Ronald B. Gammill , Jana Polivkova
发明人： Donald L. Bussolotti , Ronald B. Gammill , Jana Polivkova
IPC分类号： C07D209/04 , C07D495/02 , A61K31/407 , A61K31/381
CPC分类号： C07D409/12 , C07D209/42 , C07D495/04
摘要： The present invention provides compounds of formula (I) the prodrugs thereof, and the pharmaceutically acceptable salts of the compounds and prodrugs, wherein R′, R″, R′″, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof in treating diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, and tissue ischemia.
摘要翻译：本发明提供式（I）化合物及其药物前体药物及其药学上可接受的盐，其中R'，R“，R”'和Z如本文所定义; 其药物组合物; 及其用于治疗糖尿病，胰岛素抵抗，糖尿病性神经病，糖尿病性肾病，糖尿病性视网膜病变，白内障，高血糖症，高胆固醇血症，高血压，高胰岛素血症，高脂血症，动脉粥样硬化和组织缺血的用途。

2. 发明授权

US06992092B2 Anti-diabetic agents 失效
标题翻译：抗糖尿病药
公开(公告)号：US06992092B2
公开(公告)日：2006-01-31
申请号：US10825279
申请日：2004-04-15
申请人： Donald L. Bussolotti , Ronald B. Gammill
发明人： Donald L. Bussolotti , Ronald B. Gammill
IPC分类号： A61K31/4439 , C07D401/401 , C07D401/14
CPC分类号： C07D401/12 , C07D495/04
摘要： The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1, R2, Ra, Rb, X, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.
摘要翻译：本发明提供式（I）化合物，其立体异构体和前药，以及化合物，立体异构体和前药的药学上可接受的盐; 其中R 1，R 2，R b，R b，X和Z如本文所定义; 其药物组合物; 及其用途。

3. 发明授权

US5703075A Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones 失效
标题翻译：抗动脉粥样硬化和抗血栓形成的1-苯并吡喃-4-酮和2-氨基-1,3-苯并恶嗪-4-酮
公开(公告)号：US5703075A
公开(公告)日：1997-12-30
申请号：US484584
申请日：1995-06-07
申请人： Ronald B. Gammill , Thomas M. Judge , Joel Morris
发明人： Ronald B. Gammill , Thomas M. Judge , Joel Morris
IPC分类号： C07D265/22 , C07D311/22 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , A61K31/535 , A61K31/54 , C07D413/04 , C07D413/14
CPC分类号： C07D265/22 , C07D311/22 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of Formula I ##STR1## which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I are useful inhibitors of cell proliferation.
摘要翻译：本发明涉及与作为抗动脉粥样硬化剂的药物载体相关的式I化合物。此外，式I的各种化合物是细胞增殖的有用抑制剂。

4. 发明授权

US5385906A Antibacterial quinolone compounds 失效
标题翻译：抗菌喹诺酮化合物
公开(公告)号：US5385906A
公开(公告)日：1995-01-31
申请号：US94829
申请日：1993-07-20
申请人： Ronald B. Gammill , Sharon N. Bisaha , Joseph M. Timko , Thomas M. Judge , Michael R. Barbachyn , Kyoung S. Kim
发明人： Ronald B. Gammill , Sharon N. Bisaha , Joseph M. Timko , Thomas M. Judge , Michael R. Barbachyn , Kyoung S. Kim
IPC分类号： C07D215/56 , C07D401/04 , C07D471/04 , A61K31/47
CPC分类号： C07D215/56 , C07D401/04 , C07D471/04
摘要： A quinolone compound of Formula (I) ##STR1## as defined herein having antibacteria properties, pharmaceutical compositions containing the quinoline compound and method for treating bacterial infections in animals including humans.
摘要翻译：本文定义的具有抗菌特性的式（I）的喹诺酮化合物，含有喹啉化合物的药物组合物和用于治疗包括人在内的动物的细菌感染的方法。

5. 发明授权

US5132400A Peptides containing a (1-amino-2-hydroxy-2-heterocyclic)ethyl moiety 失效
标题翻译：含有（1-氨基-2-羟基-2-环己基）乙酸酯的肽
公开(公告)号：US5132400A
公开(公告)日：1992-07-21
申请号：US511273
申请日：1990-04-20
申请人： Ronald B. Gammill , Tomi K. Sawyer
发明人： Ronald B. Gammill , Tomi K. Sawyer
IPC分类号： C07D295/12 , A61K38/55 , A61P5/38 , A61P9/00 , A61P9/12 , C07D263/06 , C07D265/06 , C07D277/28 , C07D279/06 , C07D403/12 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/10 , C07K5/117 , C07K14/81
CPC分类号： C07K5/0227 , C07K5/1024
摘要： The present invention provides novel peptides of the formula X-A.sub.6 -B.sub.7 -C.sub.8 -D.sub.9 -E.sub.10 -F.sub.11 containing a novel (1-amino-2-hydroxy-2-heterocyclic) ethyl moiety of the formula XL.sub.2c at the E.sub.10 -F.sub.11 -position, X is a terminal group, and the remaining variables are amino acid residues. The present invention also provides novel intermediate compounds. These peptides are useful as renin inhibitors and as inhibitors of retroviral proteases. Renin inhibitors are useful for the diagnosis and control of renin-dependent hyperaldosterism, other renin-dependent cardiovascular disorders and ocular disorders. Inhibitors of retroviral proteases, such as the HIV-I protease, are useful for treating diseases caused by retroviruses, such as human acquired immunodificiency disease syndrome (AIDS). ##STR1##
摘要翻译：本发明提供了在E10-F11-F11中含有式XL2c的新的（1-氨基-2-羟基-2-杂环）乙基部分的式X-A6-B7-C8-D9-E10-F11的新型肽，位置，X是末端基团，剩余的变量是氨基酸残基。本发明还提供了新的中间体化合物。这些肽可用作肾素抑制剂和作为逆转录病毒蛋白酶的抑制剂。肾素抑制剂可用于诊断和控制肾素依赖性醛固酮增多症，其他肾素依赖性心血管疾病和眼部疾病。逆转录病毒蛋白酶如HIV-1蛋白酶的抑制剂可用于治疗由逆转录病毒引起的疾病，例如人类获得性免疫疾病疾病综合征（AIDS）。 XL2c

6. 发明授权

US4459420A Pyrogallol synthesis of anti-atherogenic furochromones 失效
标题翻译：邻苯三酚合成抗动脉粥样硬化的呋喃色酮
公开(公告)号：US4459420A
公开(公告)日：1984-07-10
申请号：US378686
申请日：1982-05-17
申请人： Ronald B. Gammill
发明人： Ronald B. Gammill
IPC分类号： A61K31/34 , A61K31/343 , A61K31/35 , A61P9/10 , C07D307/86 , C07D493/04 , C07D307/79
CPC分类号： C07D493/04 , C07D307/86
摘要： The present invention provides a total synthesis of known intermediates useful in the synthesis of khellin and antiatherosclerotic analogs thereof from pyrogallol. Pyrogallol is converted to 3,6,7-benzofurantriol triacetate using zinc chloride and chloracetanitrile, then catalytically reduced and deactoxylated at the 3 position to yield the corresponding 2,3-dihydrofuran. This substance is subjected to a Fries rearrangement to the corresponding diol, the phenolic hydroxyl group of which is then selectively alkylated. This yields 6-hydroxy-7-alkoxy-5-benzofuranyl methyl ketone, a known intermediate for the production of 4-desmethoxy khellin and analogs thereof. This compound is then selectively alkoxylated at the 4 position using lead tetraacetate or thallium (III) nitrate in an alkanol solvent to yield known chemical intermediates in the preparation of khellin and analogs thereof.
摘要翻译：本发明提供了可用于合成来自邻苯三酚的凯辛及其抗动脉粥样硬化类似物的已知中间体的全合成。使用氯化锌和氯乙腈将邻苯三酚转化为3,6,7-苯并呋喃三醇酯，然后在3位催化还原和脱氧化，得到相应的2,3-二氢呋喃。将该物质进行Fries重排，然后将其酚羟基选择性烷基化成相应的二醇。这得到6-羟基-7-烷氧基-5-苯并呋喃基甲基酮，其是生产4-脱甲氧基壳聚糖的公知中间体及其类似物。然后使用四乙酸铅或硝酸铊在链烷醇溶剂中将该化合物在4位选择性烷氧基化，得到其制备凯辛及其类似物的已知化学中间体。

7. 发明授权

US4438274A Antiatherosclerotic furochromones 失效
标题翻译：抗动脉粥样硬化红细胞
公开(公告)号：US4438274A
公开(公告)日：1984-03-20
申请号：US378700
申请日：1982-05-17
申请人： Ronald B. Gammill
发明人： Ronald B. Gammill
IPC分类号： A61K31/35 , A61P9/10 , C07D493/04 , C07D311/78
CPC分类号： C07D493/04
摘要： The present specification provides novel analogs of khellin, a natural product, which are useful in the treatment and prevention of atherosclerosis. Particularly, the present disclosure provides novel 5H-furo[3,2-g]-benzopyran-5-one substituted at the four and nine positions by methoxy or optionally substituted at the four position by hydroxy or alkoxy groups other than methoxy, certain 7-(N,N-dialkylaminoethen-2-yl substituted compounds. Also provided are certain novel antiatherosclerotic 7H-furo[3,2-g][1]benzopyrans.
摘要翻译：本说明书提供了一种可用于治疗和预防动脉粥样硬化的天然产物凯辛的新型类似物。特别地，本公开提供了在四位和九位被甲氧基取代的新颖的5H-呋喃并[3,2-g] - 苯并吡喃-5-酮，或者在四位被羟基或除甲氧基以外的烷氧基取代， - （N，N-二烷基氨基乙烯-2-基取代的化合物。还提供某些新的抗动脉粥样硬化的7H-呋喃并[3,2-g] [1]苯并吡喃。

8. 发明授权

US5700799A Oxazolidinone antimicrobials containing substituted diazine moieties 失效
标题翻译：含有取代的二嗪部分的恶唑烷酮抗微生物剂
公开(公告)号：US5700799A
公开(公告)日：1997-12-23
申请号：US610031
申请日：1996-03-04
申请人： Douglas K. Hutchinson , Michael R. Barbachyn , Steven J. Brickner , Ronald B. Gammill , Mahesh V. Patel
发明人： Douglas K. Hutchinson , Michael R. Barbachyn , Steven J. Brickner , Ronald B. Gammill , Mahesh V. Patel
IPC分类号： A61K31/395 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/495 , A61K31/496 , A61K31/551 , A61P31/00 , A61P31/04 , C07D263/20 , C07D263/24 , C07D413/10 , C07D413/12 , C07D413/14 , C07D245/02
CPC分类号： C07D263/20 , C07D413/10 , C07D413/12
摘要： A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is choosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.
摘要翻译：结构式I的化合物或其药学上可接受的盐，其中：每个n独立地为1至3; 从本文定义的a-n中选择Y; 其中所述C 1-6烷基的每次出现可以被一个或多个F，Cl，Br，I，OR1，CO 2 R 1，CN，SR 1或R 1（其中R 1是氢或C 1-4烷基）取代; X和Z独立地是C 1-6烷基，C 3-12环烷基或氢，或X和Z形成C0-3桥连基，优选X和Z是氢; U，V和W独立地是C 1-6烷基，F，Cl，Br，氢或被F，Cl，Br或I中的一个或多个取代的C 1-6烷基，优选U和V是F，W是氢; R是氢，C 1-12烷基，C 3-12环烷基，C 1-6烷氧基，被一个或多个F，Cl，Br，I或OH取代的C 1-6烷基; q为0〜4。具有与N-芳基环结合的取代的二嗪部分的恶唑烷酮衍生物是有效的抗微生物剂，其对许多人类和兽医病原体有效，包括多重耐药性葡萄球菌和链球菌，以及厌氧生物体如杀菌剂和梭菌属物种，以及耐酸生物如结核分枝杆菌和鸟分枝杆菌。

9. 发明授权

US4614809A Antiatherosclerotic furochromones and intermediates therefor 失效
标题翻译：抗动脉粥样硬化的呋喃色酮及其中间体
公开(公告)号：US4614809A
公开(公告)日：1986-09-30
申请号：US603533
申请日：1984-04-25
申请人： Ronald B. Gammill
发明人： Ronald B. Gammill
IPC分类号： C07D307/86 , C07D493/04 , C07D311/78
CPC分类号： C07D493/04 , C07D307/86
摘要： The present invention particularly provides novel furochromones and intermediates for their preparation.
摘要翻译：本发明特别提供新的呋喃色酮及其制备中间体。

10. 发明授权

US4532340A Furochromone intermediates 失效
标题翻译：呋喃色酮中间体
公开(公告)号：US4532340A
公开(公告)日：1985-07-30
申请号：US545988
申请日：1983-10-27
申请人： Ronald B. Gammill
发明人： Ronald B. Gammill
IPC分类号： C07D307/68 , C07D307/86 , C07D493/04 , C07D307/54
CPC分类号： C07D493/04 , C07D307/68 , C07D307/86
摘要： The present invention provides novel intermediates used for preparation of anti-atherosclerotic furochromones.
摘要翻译：本发明提供了用于制备抗动脉粥样硬化的呋喃色酮的新型中间体。

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