专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明授权

US6150539A Triptolide prodrugs having high aqueous solubility 失效
标题翻译：具有高溶解度的雷公藤内酯前药
公开(公告)号：US6150539A
公开(公告)日：2000-11-21
申请号：US389769
申请日：1999-09-02
申请人： John H. Musser
发明人： John H. Musser
IPC分类号： A61K31/343 , A61K31/5377 , A61K31/661 , A61P29/00 , A61P37/06 , C07D303/17 , C07D303/31 , C07D493/14 , C07D493/22 , C07F9/655 , C07D307/77
CPC分类号： C07D493/14
摘要： Compounds useful in immunosuppressive and anti-inflammatory treatment are described. The compounds are hydrolyzable triptolide analogs with improved water solubility and generally lower toxicity than the parent compound.
摘要翻译：描述了可用于免疫抑制和抗炎治疗的化合物。该化合物是具有改善的水溶性的水解性雷公藤内酯类似物，并且通常比母体化合物的毒性低。

42. 发明授权

US5892112A Process for preparing synthetic matrix metalloprotease inhibitors 失效
标题翻译：制备合成基质金属蛋白酶抑制剂的方法
公开(公告)号：US5892112A
公开(公告)日：1999-04-06
申请号：US184727
申请日：1994-01-21
申请人： Daniel E. Levy , Damian Grobelny , Cho Tang , Kevin R. Holme , Richard E. Galardy , Gregory S. Schultz , Asaad Nematalia , John H. Musser
发明人： Daniel E. Levy , Damian Grobelny , Cho Tang , Kevin R. Holme , Richard E. Galardy , Gregory S. Schultz , Asaad Nematalia , John H. Musser
IPC分类号： A61K45/00 , A61K31/00 , A61K31/165 , A61K31/17 , A61K31/195 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/44 , A61K31/445 , A61K31/454 , A61K31/535 , A61K38/00 , A61K38/04 , A61K38/55 , A61P29/00 , A61P35/00 , C07C259/06 , C07C271/02 , C07D209/20 , C07D209/26 , C07D401/12 , C07K5/072 , C07K5/078 , C07B57/00 , C07C227/18 , C07C235/16
CPC分类号： C07D401/12 , A61K31/00 , A61K31/165 , A61K31/17 , A61K31/195 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/445 , A61K31/454 , A61K31/535 , A61K38/005 , A61K38/04 , A61K38/55 , C07C259/06 , C07C271/02 , C07D209/20 , C07D209/26 , C07K5/06104 , C07K5/06113 , C07K5/06156 , C07C2101/16
摘要： Synthetic mammalian matrix metalloprotease inhibitors are disclosed that are useful for treating or preventing diseases wherein said diseases are caused by unwanted mammalian matrix metalloprotease activity and include skin disorders, keratoconus, restenosis, rheumatoid arthritis, wounds, cancer, angiogenesis and shock.
摘要翻译：合成的哺乳动物基质金属蛋白酶抑制剂可用于治疗或预防所述疾病由不想要的哺乳动物基质金属蛋白酶活性引起的疾病，并且包括皮肤病，圆锥角膜，再狭窄，类风湿性关节炎，伤口，癌症，血管生成和休克。

43. 发明授权

US5789385A Sialyl Lewis.sup.x mimetics containing phenyl backbones 失效
标题翻译：含有苯基主链的唾液酸Lewisx模拟物
公开(公告)号：US5789385A
公开(公告)日：1998-08-04
申请号：US604162
申请日：1996-02-21
申请人： Mark B. Anderson , Daniel E. Levy , Peng Cho Tang , John H. Musser , Narasinga Rao , Jing Rong Cui
发明人： Mark B. Anderson , Daniel E. Levy , Peng Cho Tang , John H. Musser , Narasinga Rao , Jing Rong Cui
IPC分类号： C07D309/10 , C07D405/12 , C07D407/12 , C07D493/04 , C07D499/00 , C07H3/06 , C07H11/00 , C07H15/04 , C07H15/18 , A61K31/70 , C07H15/00
CPC分类号： C07D493/04 , A61K31/7012 , C07D309/10 , C07D405/12 , C07D407/12 , C07D499/00 , C07H11/00 , C07H15/04 , C07H15/18 , C07H3/06
摘要： Compounds that possess selectin binding activity are described that have a three-dimensionally stable configuration for sialic acid and fucose, or analogs, derivatives, or mimics of these groups, such that sialic acid and fucose or their mimics are separated by a linker that permits binding between those groups and the selecting, such compounds being represented by the following general structural formula I: ##STR1##
摘要翻译：描述了具有选择蛋白结合活性的化合物，其具有唾液酸和岩藻糖的三维稳定构型，或这些基团的类似物，衍生物或模拟物，使得唾液酸和岩藻糖或其模拟物通过允许结合的接头分离在这些基团和选择之间，这些化合物由以下通式结构式I表示：（I）

44. 发明授权

US5728685A Methods of treating inflammation using cell adhesion inhibitors 失效
标题翻译：使用细胞粘附抑制剂治疗炎症的方法
公开(公告)号：US5728685A
公开(公告)日：1998-03-17
申请号：US466667
申请日：1995-06-06
申请人： Saeed A. Abbas , Falguni Dasgupta , Darwin Asa , John H. Musser , Mina A. Nashed
发明人： Saeed A. Abbas , Falguni Dasgupta , Darwin Asa , John H. Musser , Mina A. Nashed
IPC分类号： C07H15/04 , A61K31/70 , A61K31/7028 , A61K31/7042 , A61K31/7048 , A61P9/08 , A61P9/10 , A61P29/00 , A61P35/00 , A61P37/06 , C07H3/04 , C07H3/06 , C07H11/00 , C07H15/18 , C07H17/04 , C07H23/00 , A61K31/715
CPC分类号： C07H11/00 , C07H15/18 , C07H23/00 , C07H3/04 , C07H3/06 , Y10S514/825 , Y10S514/885 , Y10S514/886 , Y10S514/921
摘要： Compounds and methods of making them having the following formula are described which bind to selectin receptors and thus modulate the course of inflammation, cancer and related diseases by modulating cell-cell adhesion events: ##STR1## wherein each R.sup.1 is independently H or lower alkyl (1-4C); R.sup.2 is H, OH or lower alkyl (1-4C), or a lipophilic group such as a higher alkyl group (5-15C), alkylaryl or one or more additional saccharide residues; R.sup.3 is a negatively charged moiety including SO.sub.4.sup.2-, PO.sub.4.sup.2-, or related group; Y is H or lower alkyl (1-4C); and X is H or --CHR.sup.4 (CHOR.sup.1).sub.2 CHR.sup.5 OR.sup.1 wherein R.sup.4 and R.sup.5 are each independently H, lower alkyl (1-4C), or taken together result in a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ; said five- or six-membered ring optionally substituted with one substituent selected from the group consisting of R.sup.1, CH.sub.2 OR.sup.1, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NHCOR.sup.1, and SR.sup.1 with the proviso that if X represents a hexose substituent R.sup.3 and R.sup.4, taken together, cannot provide a hexose substituent.
摘要翻译：描述了使其具有下式的化合物和方法，它们结合选择素受体，从而通过调节细胞粘附事件来调节炎症，癌症和相关疾病的过程：其中每个R1独立地是H或低级烷基（ 1-4C）; R2是H，OH或低级烷基（1-4C），或亲脂基团如高级烷基（5-15C），烷基芳基或一个或多个另外的糖残基; R3是包含SO42-，PO42-或相关基团的带负电荷的部分; Y为H或低级烷基（1-4C）; 并且X是H或-CHR 4（CHOR 1）2 CHR 5 OR 1，其中R 4和R 5各自独立地为H，低级烷基（1-4C）或一起形成任选含有选自以下的杂原子的五元或六元环：的O，S和NR1; 所述五元或六元环任选被一个选自R 1，CH 2 OR 1，OR 1，OOCR 1，NR 12，NHCOR 1和SR 1的取代基取代，条件是如果X表示己糖取代基R 3和R 4，不能提供己糖取代基。

45. 发明授权

US5591835A Substituted lactose derivatives 失效
标题翻译：取代的乳糖衍生物
公开(公告)号：US5591835A
公开(公告)日：1997-01-07
申请号：US189630
申请日：1994-02-01
申请人： Saeed A. Abbas , Falguni Dasgupta , Darwin Asa , John H. Musser , Mina A. Nashed
发明人： Saeed A. Abbas , Falguni Dasgupta , Darwin Asa , John H. Musser , Mina A. Nashed
IPC分类号： C07H15/04 , A61K31/70 , A61K31/7028 , A61K31/7042 , A61K31/7048 , A61P9/08 , A61P9/10 , A61P29/00 , A61P35/00 , A61P37/06 , C07H3/04 , C07H3/06 , C07H11/00 , C07H15/18 , C07H17/04 , C07H23/00
CPC分类号： C07H11/00 , C07H15/18 , C07H23/00 , C07H3/04 , C07H3/06 , Y10S514/825 , Y10S514/885 , Y10S514/886 , Y10S514/921
摘要： Compounds and methods of making them having the following formula are described which bind to selectin receptors and thus modulate the course of inflammation, cancer and related diseases by modulating cell-cell adhesion events: ##STR1## wherein each R.sup.1 is independently H or lower alkyl (1-4C); R.sup.2 is H, OH or lower alkyl (1-4C), or a lipophilic group such as a higher alkyl group (5-15C), alkylaryl or one or more additional saccharide residues;R.sup.3 is a negatively charged moiety including SO.sub.4.sup.2-, PO.sub.4.sup.2-, or related group;Y is H or lower alkyl (1-4C); andX is H or --CHR.sub.4 (CHOR.sup.1).sub.2 CHR.sup.5 OR.sup.1 wherein R.sup.4 and R.sup.5 are each independently H, lower alkyl (1-4C), or taken together result in a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ;the five- or six-membered ring optionally substituted with one substituent selected from the group consisting of R.sup.1, CH.sub.2 OR.sup.1, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NHCOR.sup.1, and SR.sup.1 with the proviso that if X represents a hexose substituent R.sup.3 and R.sup.4, taken together, cannot provide a hexose substituent.
摘要翻译：描述了使其具有下式的化合物和方法，它们结合选择素受体，从而通过调节细胞粘附事件来调节炎症，癌症和相关疾病的过程：其中每个R1独立地是H或低级烷基（ 1-4C）; R2是H，OH或低级烷基（1-4C），或亲脂基团如高级烷基（5-15C），烷基芳基或一个或多个另外的糖残基; R3是包含SO42-，PO42-或相关基团的带负电荷的部分; Y为H或低级烷基（1-4C）; 并且X是H或-CHR 4（CHOR 1）2 CHR 5 OR 1，其中R 4和R 5各自独立地为H，低级烷基（1-4C）或一起形成任选含有选自以下的杂原子的五元或六元环：的O，S和NR1; 任选被一个选自R1，CH2OR1，OR1，OOCR1，NR12，NHCOR1和SR1的取代基取代的五元或六元环，条件是如果X表示己糖取代基R 3和R 4，不能提供己糖取代基。

46. 发明授权

US5527890A Derivatives of triterpenoid acids and uses thereof 失效
标题翻译：三萜酸的衍生物及其用途
公开(公告)号：US5527890A
公开(公告)日：1996-06-18
申请号：US49018
申请日：1993-04-16
申请人： Narasinga Rao , Mark B. Anderson , John H. Musser
发明人： Narasinga Rao , Mark B. Anderson , John H. Musser
IPC分类号： C07D335/02 , A61K31/35 , A61K31/351 , A61K31/38 , A61K31/382 , A61K31/44 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61K47/48 , A61K51/04 , A61P29/00 , A61P35/00 , A61P37/06 , C07D211/06 , C07D211/68 , C07D211/80 , C07D309/10 , C07H17/00 , C07H17/02 , C07H17/04 , C07J63/00 , C07J17/00 , A61K31/705
CPC分类号： A61K51/0491 , A61K47/48023 , A61K47/48123 , C07D309/10 , C07J63/008 , A61K2121/00 , A61K2123/00 , Y10S514/885 , Y10S514/889
摘要： Triterpenoid acid derivatives are described that exhibit dual pharmacophobic activities, specifically selectin ligand and leukotriene biosynthetic inhibitory activities, and that thus have significant applications for the treatment or prevention of certain diseases including cancer and diseases associated with the inflammatory process as well as applications for the diagnosis of disease.
摘要翻译：描述了三萜酸衍生物，其表现出双重排斥性活性，特别是选择蛋白配体和白细胞三烯生物合成抑制活性，因此具有治疗或预防某些疾病（包括癌症和与炎症过程相关的疾病）以及诊断应用的显着应用的疾病

47. 发明授权

US5286730A Method of treating immunoinflammatory disease 失效
标题翻译：免疫炎症治疗方法
公开(公告)号：US5286730A
公开(公告)日：1994-02-15
申请号：US931242
申请日：1992-08-17
申请人： Craig E. Caufield , John H. Musser , Surendra N. Sehgal
发明人： Craig E. Caufield , John H. Musser , Surendra N. Sehgal
IPC分类号： A61K31/435 , A61K20060101 , A61K31/436 , A61K38/13 , A61P1/00 , A61P17/00 , A61P17/06 , A61P37/00 , C07D498/18 , C07K7/64 , A61K35/00 , A61K31/395
CPC分类号： A61K31/70 , A61K38/13
摘要： This invention provides a method of treating immunionflammatory skin disease in a mammal in need thereof which comprises administering an antiimmunoinflammatory amount of rapamycin, alone or in combination with cyclosporin A, orally, parenterally, intranasally, intrabronchially, topically, transdermally, or rectally. As such, rapamycin, alone or in combination with cyclosporin A, is useful in treating skin diseases such as psoriasis, atopic dermatitis, contact dermatitis, eczematous dermatitis, seborrheic dermatitis, Lichen planus, Pemphigus, bulus pemphigoid, Epidermolysis bullosa, urticaria, angioedemas, vasculitides, erythemas, cutaneous eosinphilias, and the like.
摘要翻译：本发明提供了一种在有需要的哺乳动物中治疗免疫炎症性皮肤病的方法，其包括单独或与环孢菌素A组合施用抗免免炎的量的雷帕霉素，口服，肠胃外，鼻内，子宫内，局部，经皮或直肠。因此，单独或与环孢菌素A组合的雷帕霉素可用于治疗皮肤疾病如牛皮癣，特应性皮炎，接触性皮炎，湿疹性皮炎，脂溢性皮炎，扁平苔藓，天疱疮，鳞状上皮性天疱疮，大疱性表皮松解症，荨麻疹，血管瘤，血管炎，红斑，皮肤嗜酸性粒细胞等。

48. 发明授权

US5023262A Hydrogenated rapamycin derivatives 失效
标题翻译：氢化雷帕霉素衍生物
公开(公告)号：US5023262A
公开(公告)日：1991-06-11
申请号：US567858
申请日：1990-08-14
申请人： Craig E. Caufield , John H. Musser , James M. Rinker
发明人： Craig E. Caufield , John H. Musser , James M. Rinker
IPC分类号： A61K31/435 , A61K31/395 , A61P31/04 , A61P31/10 , C07D311/00 , C07D498/18 , C07H19/01
CPC分类号： C07D498/18 , C07H19/01
摘要： A derivative of rapamycin where one, two, or three of the double bonds at the 1-,3-, or 5-positions of rapamycin have been reduced to the corresponding alkane, or a pharmaceutically acceptable salt thereof, which by virtue of its antifungal activity is useful in treating fungal infections. ##STR1##
摘要翻译：雷帕霉素的衍生物，其中雷帕霉素的1-，3-或5-位上的一个，两个或三个双键已被还原成相应的烷烃或其药学上可接受的盐，由于其抗真菌活性可用于治疗真菌感染。

49. 发明授权

US4698346A Thiazolo[5,4-h]quinoline compounds useful as anti-allergy agents 失效
标题翻译：噻唑并[5,4-h]喹啉化合物可用作抗过敏剂
公开(公告)号：US4698346A
公开(公告)日：1987-10-06
申请号：US889021
申请日：1986-07-24
申请人： John H. Musser , Richard E. Brown
发明人： John H. Musser , Richard E. Brown
IPC分类号： C07D215/28 , C07D498/04 , A61K31/425 , C07D513/04
CPC分类号： C07D215/28
摘要： New quinoline compound, and the corresponding 1,2-; 1,3-; and 1,4-benzodiazines, the quinoline compounds being of the formula: ##STR1## and salts thereof, wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, halo, trifluoromethyl, amino, lower alkyl amino, lower acylamino, cyano, aryl, aryl/lower alkylene, nitro, lower alkynyl, lower alkenyl, lower alkyl sulfinyl, lower alkyl sulfonyl, lower alkoxycarbonyl, carboxyl, lower alkoxy, lower alkanoyl, or lower alkenoyl,Y is oxygen, sulfur, nitrogen or R.sub.3 N wherein R.sub.3 is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, aralkyl, acyl, aminoalkyl, or carboxyalkyl,Z is oxygen, sulfur or nitrogen,X is cyano, carbalkoxyl, carboxyl, formyloximino, tetrazolyl, carbalkoxyalkyl or carboxyalkyl, andm is 0 or 1, are useful as medicinals, especially for treatment of asthma, and/or as intermediates in the preparation of compounds useful for treating asthma.
摘要翻译：新喹啉化合物及相应的1,2-; 1,3- 和1,4-苯并二嗪，喹啉化合物具有下式：其中R1和R2独立地是氢，低级烷基，卤素，三氟甲基，氨基，低级烷基氨基，低级酰氨基，氰基，芳基，芳基/低级亚烷基，硝基，低级炔基，低级烯基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷酰基，羧基，低级烷氧基，低级烷酰基或低级烯酰基，Y为氧，硫，氮或R 3 N，其中R 3为氢低级烷基，烯基，炔基，芳基，芳烷基，酰基，氨基烷基或羧基烷基，Z是氧，硫或氮，X是氰基，烷氧羰基，羧基，甲酰肟基，四唑基，烷氧基烷基或羧基烷基，m是0或1，可用作药物，特别是用于治疗哮喘，和/或作为制备用于治疗哮喘的化合物的中间体。

50. 发明授权

US08088741B2 Compounds for enzyme inhibition 有权
标题翻译：用于酶抑制的化合物
公开(公告)号：US08088741B2
公开(公告)日：2012-01-03
申请号：US11596028
申请日：2005-05-09
申请人： Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , Kevin D. Shenk , Peggy A. Radel
发明人： Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , Kevin D. Shenk , Peggy A. Radel
IPC分类号： A61K38/06 , C12Q1/34
CPC分类号： C07K5/0812 , C07K5/06034 , C07K5/0827 , Y02A50/412
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
摘要翻译：包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。肽类化合物包括环氧化物或氮丙啶，并且在N-末端官能化。除了其他治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式