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31. 发明授权

US06770671B2 7,8-dihydro-xanthenone-8-carboxylic acid derivative and novel microbe producing the same 失效
标题翻译： 7,8-二氢呫吨酮-8-羧酸衍生物及其生产新颖的微生物
公开(公告)号：US06770671B2
公开(公告)日：2004-08-03
申请号：US10220724
申请日：2002-09-04
申请人： Jung Joon Lee , Jeong-Hyung Lee , Hang Sub Kim , Young-Soo Hong , Yun Joo Park
发明人： Jung Joon Lee , Jeong-Hyung Lee , Hang Sub Kim , Young-Soo Hong , Yun Joo Park
IPC分类号： A61K3135
CPC分类号： C12R1/66 , C07D311/86 , C12P17/06
摘要： Disclosed are a novel compound represented by the following chemical formula (1), useful for the prophylaxis and treatment of angiogenic diseases, its production, and a novel microorganism producing the same. Aspergillus sp. Y80118 isolated from soil was found to produce 7,8-dihydro-1,7-dihydroxy-3-hydroxymethyl-xanthenone-8-carboxylic acid methylester which inhibits VEGF-induced proliferation of HUVEC, angiogenesis in CAM assay, and tumor growth. The novel compound can be effectively used for the medical treatment of anigiogenic diseases, including cancers, rheumatoid arthritis, and diabetic retinopathy.
摘要翻译：公开了由以下化学式（1）表示的新型化合物，其用于预防和治疗血管生成疾病及其生产，以及生产该新化合物的新型微生物。曲霉菌发现从土壤中分离的Y80118产生抑制VEGF诱导的HUVEC增殖，CAM测定中的血管发生和肿瘤生长的7,8-二氢-1,7-二羟基-3-羟甲基 - 呫吨酮-8-羧酸甲酯。该新型化合物可有效地用于治疗致病性疾病，包括癌症，类风湿性关节炎和糖尿病性视网膜病变。

32. 发明授权

US06765016B1 Bicyclic ketolide derivatives 失效
标题翻译：双环酮内酯衍生物
公开(公告)号：US06765016B1
公开(公告)日：2004-07-20
申请号：US10455648
申请日：2003-06-05
申请人： Yao-Ling Qiu , Ly Tam Phan , Zhigang Chen , Tongzhu Liu , Yat Sun Or
发明人： Yao-Ling Qiu , Ly Tam Phan , Zhigang Chen , Tongzhu Liu , Yat Sun Or
IPC分类号： A61K3135
CPC分类号： A61K31/35 , C07H17/08
摘要： The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
摘要翻译：本发明公开了式I化合物或其药学上可接受的盐，酯或前药：其表现出抗菌性质。本发明还涉及包含上述化合物的药物组合物，用于给予需要抗生素治疗的受试者。本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。本发明还包括制备本发明化合物的方法。

33. 发明授权

US06756403B2 Methods for producing chiral chromones, chromanes, amino substituted chromanes and intermediates therefor 有权
公开(公告)号：US06756403B2
公开(公告)日：2004-06-29
申请号：US10297096
申请日：2003-07-11
申请人： Barbara Briggs , James Kanter , John J. G. Mullins , Gerd Ruhter , Uko Udodong , Milton Zmijewski, Jr. , Daniel Verral, II
发明人： Barbara Briggs , James Kanter , John J. G. Mullins , Gerd Ruhter , Uko Udodong , Milton Zmijewski, Jr. , Daniel Verral, II
IPC分类号： A61K3135
CPC分类号： C07D311/74 , A61K31/353 , C07D311/22 , C07D311/24 , C07D311/58
摘要： Disclosed are process steps and novel processes for producing chromane compositions enriched in at least one (2R or 2S) enantiomer, preferably chroman-2-yl carboxylic acid compounds and chroman-2-yl carboxylic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors. Further disclosed are enzymatic processes for resolving chiral intermediates or final products to provide desired enantiomers.

34. 发明授权

US06734210B2 Therapeutically improved salts of azelaic acid 失效
标题翻译：治疗改善的壬二酸盐
公开(公告)号：US06734210B2
公开(公告)日：2004-05-11
申请号：US09791358
申请日：2001-02-23
申请人： Rolland F. Hebert
发明人： Rolland F. Hebert
IPC分类号： A61K3135
CPC分类号： A61K31/74 , A61K31/722 , A61K38/00 , Y10S514/859
摘要： Stable salts of azelaic acid with polycations such as chitosan are described. The salts according to the invention are water-soluble, therapeutically more efficacious and are valuable for use as active constituents in pharmaceutical as well as cosmeceutical compositions.
摘要翻译：描述了壬二酸与聚阳离子如壳聚糖的稳定盐。根据本发明的盐是水溶性的，治疗上更有效，并且对于用作药物和药妆组合物中的活性成分是有价值的。

35. 发明授权

US06727277B1 Compounds affecting cholesterol absorption 失效
标题翻译：影响胆固醇吸收的化合物
公开(公告)号：US06727277B1
公开(公告)日：2004-04-27
申请号：US10292720
申请日：2002-11-12
申请人： Duy H. Hua , Sung I. Koo , Sang K. Noh
发明人： Duy H. Hua , Sung I. Koo , Sang K. Noh
IPC分类号： A61K3135
CPC分类号： G01N33/92 , C07C43/23 , C07C2602/28 , C07D311/78 , G01N33/5088 , G01N2800/044
摘要： A class of novel compounds is described for use in affecting lymphatic absorption of cholesterol. Compounds of particular interest are defined by Formula I: or a pharmaceutically acceptable salt thereof.
摘要翻译：一类新型化合物被用于影响胆固醇的淋巴吸收。特别感兴趣的化合物由式I定义：或其药学上可接受的盐。

36. 发明授权

US06720352B1 Compositions and process for nematode control 有权
标题翻译：线虫控制的组成和过程
公开(公告)号：US06720352B1
公开(公告)日：2004-04-13
申请号：US09980500
申请日：2002-03-11
申请人： Rodrigo Rodriguez-Kabana
发明人： Rodrigo Rodriguez-Kabana
IPC分类号： A61K3135
CPC分类号： A01N43/08 , A01N65/08 , A01N43/16 , A01N47/48 , A01N47/12 , A01N43/88 , A01N35/04 , A01N47/46 , A01N47/14 , A01N43/40 , A01N2300/00 , A01N25/04
摘要： Chemical compositions having superior nematicidal properties are formulated. The compositions contain one or more selected aldehydes as the major component and one or more aliphatic or cyclic isothiocyanates as a minor component. Preferred mixtures contain furfural and one or both of methyl isothiocyanate and allyl isothiocyanate. Plant-parasitic nematodes are controlled by contacting the nematodes with the nematicidal compositions, by, for example, applying the compositions to soil or other plant growth media containing the nematodes.
摘要翻译：配制具有优异杀线虫性的化学成分。组合物含有一种或多种选择的醛作为主要组分和一种或多种脂族或环状异硫氰酸酯作为次要组分。优选的混合物包含糠醛和异硫氰酸甲酯和异硫氰酸烯丙酯中的一种或两种。通过将线虫与杀线虫组合物接触来控制植物寄生线虫，例如通过将组合物施用于含有线虫的土壤或其他植物生长培养基。

37. 发明授权

US06706756B1 Vasodilating compound and method of use 有权
标题翻译：血管舒张化合物及其使用方法
公开(公告)号：US06706756B1
公开(公告)日：2004-03-16
申请号：US10065770
申请日：2002-11-18
申请人： David F. Fitzpatrick
发明人： David F. Fitzpatrick
IPC分类号： A61K3135
CPC分类号： A61K31/35
摘要： The present invention is an isolated compound and method of inducing endothelium-dependent relaxation in blood vessels including the step of introducing isolated procyanidins having a preponderance of (−)-epicatechins to a patient wherein the procyanidins are preferably galloylated. To achieve both bioavailability and potency, it is also preferred that the number of epicatechins monomers forming each procyanidin is between two and five. More specifically, isolated epicatechin-(4-8)-epicatechin-(4-8)-epicatechin-gallate (C1-gallate) is administered to the patient.
摘要翻译：本发明是分离的化合物和诱导血管内皮依赖性松弛的方法，包括将具有优势（ - ） - 表儿茶素的分离的原花青素引入到其中原花青素优选被加成半乳糖化的步骤的步骤。为了实现生物利用度和效力，还优选形成每种原花青素的表儿茶素单体数目在2-5之间。更具体地，向患者施用分离的表儿茶素 - （4-8） - 表儿茶素 - （4-8） - 表儿茶素 - 没食子酸酯（没食子酸偏高糖酸盐）。

38. 发明授权

US06677371B1 4-oxybenzopyran derivative 失效
标题翻译： 4-羟基苯并吡喃衍生物
公开(公告)号：US06677371B1
公开(公告)日：2004-01-13
申请号：US10069002
申请日：2002-03-29
申请人： Keizo Tanikawa , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
发明人： Keizo Tanikawa , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
IPC分类号： A61K3135
CPC分类号： C07D311/22
摘要： This invention relates to a 4-oxybenzopyran derivative of formula (I) wherein, R1 and R2 represent each independently a hydrogen atom, a C1-6 alkyl group or a phenyl group; R3 represents a hydroxyl group or C1-6 alkylcarbonyloxy group; R4 represents a hydrogen atom, a C3-6 cycloalkyl group, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C1-6 alkylaminocarbonyl group, a di-C1-6 alkylaminocarbonyl group, an aryl group or a heteroaryl group; R5 represents a hydrogen atom or a C1-6 alkyl group; X is absent or represents C═O or SO2; R6 represents a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group; R7 represents a hydrogen atom, a halogen atom, a nitro group or a cyano group; or a pharmaceutically acceptable salt thereof. And this invention also relates to a drug for treating arrhytmia having the prolongation effect on the functional refractory period comprising said compound or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译：本发明涉及式（I）的4-氧代苯并吡喃衍生物，其中R 1和R 2各自独立地表示氢原子，C 1-6烷基或苯基; R 3表示羟基或C 1-6烷基羰基氧基; R 4表示氢原子，C 3-6环烷基，C 1-6烷基，C 1-6烷基羰基，C 1-6烷基氨基羰基，二-C 1-6烷基氨基羰基，芳基或杂芳基; R 5表示氢原子或C 1-6烷基; X不存在或表示C = O或SO 2; R 6表示氢原子，C 1-6烷基或C 3-6环烷基; R 7表示氢原子，卤素原子，硝基或氰基; 或其药学上可接受的盐。本发明还涉及一种用于治疗对包含所述化合物或其药学上可接受的盐作为活性成分的具有对功能不应期的延长作用的心律的药物。

39. 发明授权

US06589980B2 Substituted 10,11-benzo[b]fluoren-10-ones as estrogenic agents 失效
标题翻译：取代的10,11-苯并[b]芴-10-酮作为雌激素
公开(公告)号：US06589980B2
公开(公告)日：2003-07-08
申请号：US10146562
申请日：2002-05-15
申请人： Christopher P. Miller , Michael D. Collini , Heather A. Harris , James C. Keith, Jr.
发明人： Christopher P. Miller , Michael D. Collini , Heather A. Harris , James C. Keith, Jr.
IPC分类号： A61K3135
CPC分类号： C07D493/04
摘要： This invention provides estrogen receptor modulators of formula I, having the structure wherein X, Y1, Y2, Y3, Y4, Z1, Z2, Z3, and Z4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供式I的雌激素受体调节剂，其具有其中X，Y 1，Y 2，Y 3，Y 4，Z 1，Z 2，Z 3和Z 4如本说明书中所定义的结构或其药学上可接受的盐。

40. 发明授权

US06583174B1 Composition and method for stabilizing the same 有权
标题翻译：用于稳定其组合物和方法
公开(公告)号：US06583174B1
公开(公告)日：2003-06-24
申请号：US09688351
申请日：2000-10-16
申请人： Ryuji Ueno , Tsuyoshi Habe
发明人： Ryuji Ueno , Tsuyoshi Habe
IPC分类号： A61K3135
CPC分类号： A61K9/4858 , A61K9/0048 , C07C69/738 , C07D311/94 , C07D333/78 , C07D335/04
摘要： Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.
摘要翻译：公开了包含预期是药学活性的新型双环化合物和甘油酯的新型组合物。通过将它们溶解在甘油酯中可以显着提高双环化合物的稳定性。

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