公开(公告)号：US06288094B1

公开(公告)日：2001-09-11

申请号：US09774053

申请日：2001-01-31

申请人： Gerhard Jähne ,  Karl Geisen ,  Hans-Jochen Lang ,  Martin Bickel

发明人： Gerhard Jähne ,  Karl Geisen ,  Hans-Jochen Lang ,  Martin Bickel

IPC分类号： A61K31429

摘要： The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example as anorectics and in the treatment or prophylaxis of type II diabetes.

公开(公告)号：US06222040B1

公开(公告)日：2001-04-24

申请号：US09343993

申请日：1999-06-30

申请人： Mohammad R. Marzabadi ,  Peter Bühlmayer ,  Heinrich Rüeger ,  Wai C. Wong ,  Yasuchika Yamaguchi ,  Stewart A. Noble

发明人： Mohammad R. Marzabadi ,  Peter Bühlmayer ,  Heinrich Rüeger ,  Wai C. Wong ,  Yasuchika Yamaguchi ,  Stewart A. Noble

IPC分类号： A61K31429

CPC分类号： C07D277/60 ,  C07D277/42 ,  C07D417/12 ,  C07D513/04

摘要： This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.

摘要翻译： 本发明涉及作为NPY（Y5）受体的选择性拮抗剂的三环化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明提供通过将治疗有效量的本发明化合物与药学上可接受的载体组合而成的药物组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。

公开(公告)号：US06310056B1

公开(公告)日：2001-10-30

申请号：US09355272

申请日：1999-07-28

申请人： Yuko Kano ,  Kazuhiro Aihara ,  Yumiko Toyooka ,  Toshiro Sasaki ,  Hiromasa Takizawa ,  Kenichi Fushihara ,  Kazuko Kobayashi ,  Kunio Atsumi ,  Katsuyoshi Iwamatsu ,  Takashi Ida

发明人： Yuko Kano ,  Kazuhiro Aihara ,  Yumiko Toyooka ,  Toshiro Sasaki ,  Hiromasa Takizawa ,  Kenichi Fushihara ,  Kazuko Kobayashi ,  Kunio Atsumi ,  Katsuyoshi Iwamatsu ,  Takashi Ida

IPC分类号： A61K31429

CPC分类号： C07D519/00

摘要： The carbapenem derivatives represented by the following formula (I) is disclosed. These compounds have strong anti-bacterial activities against bacteria including methicillin resistant Staphylococcus aureus, penicillin resistant Streptococcus pneumoniae, Enterococci, influenza, and &bgr;-lactamase producing bacteria, and have high stabilities to DHP-1 wherein R1 represents hydrogen or methyl, either one of R2, R3, R4, or R5 represents the bond to the 2-position on the carbapenem ring, and the remaining three respectively represent hydrogen, halogen, nitro, cyano, alkyl, cycloalkyl, alkylthio, alkenyl, formyl, alkylcarbonyl, alkoxycarbonyl, aminosulfonyl, aryl carbonyl, aryl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylaminocarbonyl, lower alkoxyiminomethyl, or hydroxyiminomethyl, R6 is not present or represents alkyl, cycloalkyl, or alkenyl, and R is not present, or represents hydrogen or a group which may be metabolically hydrolyzed in the body, provided that when R6 is not present, R represents hydrogen or a group which may be metabolically hydrolyzed in the body, and when R6 is present, R is not present, and the compound forms an inner salt.

摘要翻译： 公开了由下式（I）表示的碳青霉烯衍生物。 这些化合物对包括耐甲氧西林金黄色葡萄球菌，青霉素耐药性肺炎链球菌，肠球菌，流感和β-内酰胺酶生产细菌在内的细菌具有很强的抗细菌活性，并且对于DHP-1具有高稳定性，其中R 1表示氢或甲基，R 2 ，R 3，R 4或R 5表示碳青霉烯环上2-位的键，其余3个分别表示氢，卤素，硝基，氰基，烷基，环烷基，烷硫基，烯基，甲酰基，烷基羰基，烷氧基羰基，氨基磺酰基， 芳基羰基，芳基，氨基甲酰基，N-低级烷基氨基甲酰基，N，N-二低级烷基氨基羰基，低级烷氧基亚氨基甲基或羟基亚氨基甲基，R6不存在或表示烷基，环烷基或烯基，R不存在，或表示氢或 可以在体内代谢水解的基团，条件是当R 6不存在时，R代表氢或可以代谢地水解的基团 e体，当R 6存在时，R不存在，且该化合物形成内盐。

公开(公告)号：US06566363B2

公开(公告)日：2003-05-20

申请号：US09923432

申请日：2001-08-08

申请人： Wesley Kwan Mung Chong ,  Rohit Kumar Duvadie

发明人： Wesley Kwan Mung Chong ,  Rohit Kumar Duvadie

IPC分类号： A61K31429

CPC分类号： C07D513/04 ,  C07D277/42

摘要： Pyrazole-thiazole compounds that modulate and/or inhibit the activity of cyclin-dependent kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating cyclin-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

摘要翻译： 描述了调节和/或抑制细胞周期蛋白依赖性激酶活性的吡唑 - 噻唑化合物。 这些化合物和含有它们的药物组合物能够介导细胞周期蛋白依赖性疾病调节和/或抑制不期望的细胞增殖。 本发明还涉及含有这些化合物的药物组合物的治疗或预防用途，以及治疗癌症以及与不想要的血管生成和/或细胞增殖相关的其它疾病状态的方法，例如糖尿病性视网膜病，青光眼，类风湿性关节炎， 和银屑病，通过施用有效量的这种化合物。

公开(公告)号：US06380228B1

公开(公告)日：2002-04-30

申请号：US09828061

申请日：2001-04-06

申请人： Craig A. Stump ,  Theresa M. Williams

发明人： Craig A. Stump ,  Theresa M. Williams

IPC分类号： A61K31429

CPC分类号： C07D487/04 ,  A61K31/335 ,  A61K41/00 ,  A61K41/0038 ,  A61K45/06 ,  C07D513/04 ,  A61K31/00 ,  A61K2300/00

摘要： The present invention is directed to peptidomimetic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

摘要翻译： 本发明涉及抑制异戊烯基 - 蛋白质转移酶和致癌基因蛋白Ras的异戊烯化的拟肽化合物。 本发明还涉及含有本发明化合物的化疗组合物和抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的方法。

公开(公告)号：US06541503B2

公开(公告)日：2003-04-01

申请号：US09924431

申请日：2001-08-08

申请人： Stephen Thomas Davis ,  Scott Howard Dickerson ,  Stephen Vernon Frye ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael Joseph Luzzio ,  James Marvin Veal ,  Duncan Herrick Walker

发明人： Stephen Thomas Davis ,  Scott Howard Dickerson ,  Stephen Vernon Frye ,  Philip Anthony Harris ,  Robert Neil Hunter, III ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael Joseph Luzzio ,  James Marvin Veal ,  Duncan Herrick Walker

IPC分类号： A61K31429

CPC分类号： C07D231/12 ,  C07D209/34 ,  C07D209/40 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D513/04

摘要： Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by cancer chemotherapy or radiotherapy.

公开(公告)号：US06403624B1

公开(公告)日：2002-06-11

申请号：US09790911

申请日：2001-02-23

申请人： Gerhard Jaehne ,  Matthias Gossel ,  Martin Bickel

发明人： Gerhard Jaehne ,  Matthias Gossel ,  Martin Bickel

IPC分类号： A61K31429

CPC分类号： C07D277/60

摘要： The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.

摘要翻译： 本发明涉及多环二氢噻唑及其生理上可接受的盐和生理功能衍生物。描述了其中基团如上所定义的式I化合物及其生理上可接受的盐及其制备方法。 所述化合物例如适合作为抗精神病药。

公开(公告)号：US06288093B1

公开(公告)日：2001-09-11

申请号：US09697151

申请日：2000-10-27

申请人： Gerhard Jähne ,  Karl Geisen ,  Hans-Jochen Lang ,  Martin Bickel

发明人： Gerhard Jähne ,  Karl Geisen ,  Hans-Jochen Lang ,  Martin Bickel

IPC分类号： A61K31429

CPC分类号： C07D277/60 ,  C07D513/04

摘要： The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example as anorectics and in the treatment or prophylaxis of type II diabetes.

摘要翻译： 本发明涉及多环噻唑烷-2-亚基胺及其生理上耐受的盐和生理功能衍生物。式I的多环噻唑烷-2-亚基胺，其中基团具有所述含义，以及它们的生理学耐受的盐和方法 描述了它们的准备。 这些化合物是适合的，例如作为抗精神病药和治疗或预防II型糖尿病。