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51. 发明申请

US20040171881A1 N,N'-substituted-1,3-diamino-2-hydroxypropane derivatives 失效
标题翻译： N，N'-取代-1,3-二氨基-2-羟基丙烷衍生物
公开(公告)号：US20040171881A1
公开(公告)日：2004-09-02
申请号：US10291318
申请日：2002-11-08
发明人： Varghese John , Michel Maillard , Barbara Jagodzinska , James Beck , Andrea Gailunas , John Freskos , John Mickelson , Lakshman Samala , Jennifer Sealy , Ruth TenBrink , Lawrence Fang , Roy Hom
IPC分类号： C07C255/53 , C07C215/46
CPC分类号： C07D263/32 , C07C233/36 , C07C233/40 , C07C233/58 , C07C233/78 , C07C235/20 , C07C235/50 , C07C235/74 , C07C237/04 , C07C237/06 , C07C237/08 , C07C237/22 , C07C237/42 , C07C251/38 , C07C255/58 , C07C271/28 , C07C271/44 , C07C311/08 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/37 , C07C317/46 , C07C317/50 , C07C323/60 , C07C323/62 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/267 , C07D207/27 , C07D209/42 , C07D211/58 , C07D211/60 , C07D211/96 , C07D213/71 , C07D213/80 , C07D213/82 , C07D213/85 , C07D215/36 , C07D215/42 , C07D215/48 , C07D215/56 , C07D217/22 , C07D231/14 , C07D231/38 , C07D233/84 , C07D233/90 , C07D237/14 , C07D239/28 , C07D239/42 , C07D239/48 , C07D241/20 , C07D241/24 , C07D241/44 , C07D243/08 , C07D249/06 , C07D249/10 , C07D251/46 , C07D251/54 , C07D257/04 , C07D257/06 , C07D261/08 , C07D261/14 , C07D261/18 , C07D263/34 , C07D263/48 , C07D263/54 , C07D263/58 , C07D265/36 , C07D271/08 , C07D271/12 , C07D275/06 , C07D277/30 , C07D277/36 , C07D277/56 , C07D277/68 , C07D277/82 , C07D279/16 , C07D285/06 , C07D285/10 , C07D285/135 , C07D295/155 , C07D295/185 , C07D295/192 , C07D295/26 , C07D307/20 , C07D307/46 , C07D307/68 , C07D307/84 , C07D307/86 , C07D307/91 , C07D311/04 , C07D333/22 , C07D333/32 , C07D333/34 , C07D333/38 , C07D333/62 , C07D333/68 , C07D335/06 , C07D401/04 , C07D405/12 , C07D409/04 , C07D411/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D473/06 , C07D473/08 , C07D473/16 , C07D487/04 , C07D495/04
摘要： Disclosed are compounds of the formula 1 wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of beta-secretase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.
摘要翻译：公开了下式的化合物，其中变量RN，RC，R1，R25，R2和R3如本文所定义。这些化合物具有作为β-分泌酶抑制剂的活性，因此可用于治疗诸如阿尔茨海默氏病之类的各种紊乱。

52. 发明申请

US20040077698A1 Tricyclic lactam and sultam derivatives and their use as histone deacetylase inhibitors 失效
标题翻译：三环内酰胺和苏丹衍生物及其作为组蛋白脱乙酰酶抑制剂的用途
公开(公告)号：US20040077698A1
公开(公告)日：2004-04-22
申请号：US10470121
申请日：2003-07-24
发明人： Guy Georges , Adelbert Grossmann , Olaf Mundigl , Wolfgang von der Saal , Tim Sattelkau
IPC分类号： A61K031/425 , A61K031/403 , C07D209/90 , C07D275/06
CPC分类号： C07D275/06 , C07D209/92
摘要： A compound of formula (I) wherein A and B are optionally substituted cyclohexenyl or phenyl groups, X is carbonyl or sulfonyl, and Y is 5-7 atoms-linker, is useful as histone deacetylase inhibitors, particularly for inhibiting cell proliferation. 1
摘要翻译：式（I）的化合物，其中A和B为任选取代的环己烯基或苯基，X为羰基或磺酰基，Y为5-7个原子的连接体，可用作组蛋白脱乙酰酶抑制剂，尤其用于抑制细胞增殖。

53. 发明授权

US06703368B2 Peptide-containing &agr;-ketoamide cysteine and serine protease inhibitors 失效
公开(公告)号：US06703368B2
公开(公告)日：2004-03-09
申请号：US09879336
申请日：2001-06-12
申请人： Sankar Chatterjee , John P. Mallamo , Ron Bihovsky , Gregory J. Wells
发明人： Sankar Chatterjee , John P. Mallamo , Ron Bihovsky , Gregory J. Wells
IPC分类号： A61K3805
CPC分类号： C07D207/08 , C07C311/06 , C07C311/46 , C07C311/48 , C07D207/20 , C07D207/48 , C07D211/76 , C07D211/96 , C07D213/70 , C07D213/74 , C07D235/06 , C07D239/42 , C07D275/06 , C07D277/40 , C07D277/54 , C07D333/34 , C07D333/62 , C07D409/04 , C07D409/14 , C07D413/04 , C07K5/0202 , C07K5/06069
摘要： This invention relates to peptide-containing &agr;-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.

54. 发明授权

US06410485B1 Saccharin-5-carbonyl derivatives with herbicidal effect 失效
标题翻译：具有除草效果的糖精-5-羰基衍生物
公开(公告)号：US06410485B1
公开(公告)日：2002-06-25
申请号：US09914797
申请日：2001-09-05
申请人： Ulf Misslitz , Ernst Baumann , Wolfgang von Deyn , Steffen Kudis , Klaus Langemann , Guido Mayer , Ulf Neidlein , Matthias Witschel , Roland Götz , Michael Rack , Peter Plath , Martina Otten , Karl-Otto Westphalen , Helmut Walter
发明人： Ulf Misslitz , Ernst Baumann , Wolfgang von Deyn , Steffen Kudis , Klaus Langemann , Guido Mayer , Ulf Neidlein , Matthias Witschel , Roland Götz , Michael Rack , Peter Plath , Martina Otten , Karl-Otto Westphalen , Helmut Walter
IPC分类号： A01N4380
CPC分类号： C07D275/06 , A01N43/80
摘要： The present application relates to saccharin-5-carbonyl derivatives of the formula I in which the substituents have the following meanings: L is C1-C6-alkyl, C1-C6-alkoxy; Z is C1-C6-alkyl, C3-C8-cycloalkyl, C3-C6-alkenyl, C3-C5-alkynyl, phenyl-C1-C6-alkyl or phenyl, where the phenyl rings are in each case optionally mono- or polysubstituted by C1-C6-alkyl, C1-C6-alkoxy or halogen; M is hydrogen, C1-C6-alkyl, C1-C6-alkoxy, halogen, cyano, nitro or halo-C1-C6-alkyl; R1, R2, R3, R4, R5, R6, R7, R8 are hydrogen, C1-C6-alkyl; and agriculturally utilizable salts of the compound I.
摘要翻译：本申请涉及式Iin的糖精-5-羰基衍生物，其取代基具有以下含义：L是C1-C6-烷基，C1-C6-烷氧基; Z是C1-C6-烷基，C3-C8-环烷基，C 3 -C 6 - 烯基，C 3 -C 5炔基，苯基-C 1 -C 6 - 烷基或苯基，其中苯环在每种情况下任选被C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基或卤素单取代或多取代 ; M是氢，C 1 -C 6烷基，C 1 -C 6烷氧基，卤素，氰基，硝基或卤代-C 1 -C 6烷基; R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8是氢， -C 1-6 - 烷基;以及化合物I的农业上可利用的盐。

55. 发明授权

US06277987B1 Sulfonylamino acid and sulfonylamino hydroxamic acid derivatives 失效
标题翻译：磺酰氨基酸和磺酰氨基异羟肟酸衍生物
公开(公告)号：US06277987B1
公开(公告)日：2001-08-21
申请号：US09243854
申请日：1999-02-03
申请人： Paivi Jaana Kukkola , Leslie Anne Robinson , Motowo Nakajima , Junichi Sakaki
发明人： Paivi Jaana Kukkola , Leslie Anne Robinson , Motowo Nakajima , Junichi Sakaki
IPC分类号： C07D23972
CPC分类号： C07D417/12 , C07C311/19 , C07D233/74 , C07D239/96 , C07D275/06 , C07D417/14 , C07D471/04
摘要： Compounds of formula wherein W is —OH or —NHOH; X is a heterocycle with the proviso that when X is a nitrogen containing heterocycle, the heterocycle is attached to the (CH2)m moiety by a ring nitrogen, —CONR2R3, —NR1COR2, —NR1SO2R2, —NR1CONR2R3, —NR1COOR4, heteroarylthio, alkylthio, arylalkylthio, heteroarylalkylthio, heterocycloalkylalkylthio, heterocycloalkylthio or arylthio; Y is carbon, nitrogen, oxygen or sulfur, provided that when Y is carbon, n is 2; Z is alkyl, aryl, alkoxy, aryloxy, aralkoxyaryl, aralkoxyheteroaryl, heteroaryl, heterocycloalkyl, heteroaryloxy, —CONR2R3, —NR1COR2, —NR1CONR2R3, —OCONR2R3, —NR1COOR4, or —SO2R2; R1 is hydrogen, alkyl, heterocycloalkylalkyl, aralkyl or heteroarylalkyl; R2 and R3 are independently R1, aryl or heteroaryl; or R2 and R3 taken together with the nitrogen atom to which they are attached form a 5- to 7-membered ring, which may optionally contain another heteroatom selected from oxygen, nitrogen and sulfur; R4 is alkyl, heterocycloalkylalkyl, aralkyl, aryl or heteroaryl; m represents an integer from one to six; n represents the integer one or two; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinases in mammals using such compounds. Compounds of formula I are inhibitors of matrix-degrading metalloproteinases and are useful for the treatment of conditions related thereto.
摘要翻译：肟基的化合物W是-OH或-NHOH; X是杂环，条件是当X是含氮杂环时，杂环通过环氮-CONR2R3，-NR1COR2，-NR1SO2R2与（CH2）m部分连接，-NR 1 CONR 2 R 3，-NR 1 COOR 4，杂芳硫基，烷硫基，芳烷硫基，杂芳基烷硫基，杂环烷基烷硫基，杂环烷硫基或芳硫基; Y为碳，氮，氧或硫，条件是当Y为碳时，n为2; Z为烷基，芳基，烷氧基，芳氧基，芳烷氧基芳基，芳烷氧基杂芳基，杂芳基，杂环烷基，杂芳氧基，-CONR2R3，-NR1COR2，-NR1CONR2R3，-OCONR2R3，-NR1COOR4或-SO2R2; R1是氢，烷基，杂环烷基烷基，芳烷基或杂芳基烷基; R2和R3独立地是R1，芳基或杂芳基; 或者R 2和R 3与它们所连接的氮原子一起形成5-至7-元环，其可任选地含有选自氧，氮和硫的其它杂原子; R 4是烷基，杂环烷基烷基，芳烷基，芳基或杂芳基 ; m表示1至6的整数; n表示整数1或2; 及其药学上可接受的盐; 包含所述化合物的药物组合物; 以及使用这些化合物抑制哺乳动物中的基质降解金属蛋白酶的方法。式I化合物是基质降解金属蛋白酶的抑制剂，可用于治疗与之相关的病症。

56. 发明授权

US06221889B1 IL-8 receptor antagonists 失效
标题翻译： IL-8受体拮抗剂
公开(公告)号：US06221889B1
公开(公告)日：2001-04-24
申请号：US09600380
申请日：2000-07-14
申请人： Melvin C. Rutledge, Jr. , Katherine L. Widdowson
发明人： Melvin C. Rutledge, Jr. , Katherine L. Widdowson
IPC分类号： A61K31428
CPC分类号： C07D275/06
摘要： This invention provides for a method of treating a chemokine mediated disease, wherein the chemokine is one which binds to an IL-8 &agr; or &bgr; receptor and which method comprises administering an effective amount of a compound of Formular (I) or a pharmaceuticlly acceptable salt thereof. In particular the chemokine is IL-8.
摘要翻译：本发明提供了治疗趋化因子介导的疾病的方法，其中趋化因子是与IL-8α或β受体结合的趋化因子，该方法包括给予有效量的式（I）化合物或药学上可接受的盐其中。特别是趋化因子是IL-8。

57. 发明授权

US06207680B1 Heteroarylpiperidines and their use as antipsychotics and analgesics 失效
标题翻译：杂芳基哌啶及其作为抗精神病药和镇痛药的用途
公开(公告)号：US06207680B1
公开(公告)日：2001-03-27
申请号：US08468993
申请日：1995-06-06
申请人： Edward J. Glamkowski , Yulin Chiang , Joseph T. Strupczewski , Kenneth J. Bordeau , Peter A. Nemoto , John J. Tegeler
发明人： Edward J. Glamkowski , Yulin Chiang , Joseph T. Strupczewski , Kenneth J. Bordeau , Peter A. Nemoto , John J. Tegeler
IPC分类号： A61K31535
CPC分类号： C07D231/56 , C07C45/45 , C07C45/673 , C07C45/71 , C07C233/25 , C07C233/33 , C07C255/54 , C07C323/22 , C07D207/08 , C07D261/20 , C07D275/04 , C07D275/06 , C07D277/82 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07F7/1804 , C07C49/84 , C07C49/755 , C07C47/575
摘要： Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
摘要翻译：杂芳基哌啶，吡咯烷酮和哌嗪可用作抗精神病药和镇痛药。通过向哺乳动物施用精神病治疗有效量的一种化合物，该化合物特别可用于治疗精神病。化合物的储备衍生物可用于提供化合物的长效作用。通过向哺乳动物施用减轻疼痛的有效量的一种化合物，化合物也可用作镇痛药。

58. 再颁专利

USRE37029E1 N-[(3-heteroaryl-1-pyrrolidinyl)-alkyl]phthalimides and related compounds and their therapeutic utility 失效
标题翻译： N - [（3-杂芳基-1-吡咯烷基） - 烷基]苯二酰亚胺和相关化合物及其治疗用途
公开(公告)号：USRE37029E1
公开(公告)日：2001-01-23
申请号：US09185968
申请日：1998-11-05
申请人： Joseph T. Strupczewski , Edward J. Glamkowski , Yulin Chiang , Kenneth J. Bordeau , Peter A. Nemoto , John J. Tegler
发明人： Joseph T. Strupczewski , Edward J. Glamkowski , Yulin Chiang , Kenneth J. Bordeau , Peter A. Nemoto , John J. Tegler
IPC分类号： A61K31495
CPC分类号： C07D231/56 , C07C45/45 , C07C45/673 , C07C45/71 , C07C233/25 , C07C233/33 , C07C255/54 , C07C323/22 , C07D207/08 , C07D261/20 , C07D275/04 , C07D275/06 , C07D277/82 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07F7/1804 , C07C49/84 , C07C49/755 , C07C47/575
摘要： Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
摘要翻译：杂芳基哌啶，吡咯烷酮和哌嗪可用作抗精神病药和镇痛药。该化合物特别可用于通过向哺乳动物施用精神病治疗有效量的一种化合物来治疗精神病。化合物的储备衍生物可用于提供化合物的长效作用。通过向哺乳动物施用减轻疼痛的有效量的一种化合物，化合物也可用作镇痛药。

59. 发明授权

US6166055A Benzoisothiazole compounds useful as IL-8 receptor antagonists 失效
标题翻译：可用作IL-8受体拮抗剂的苯并噻唑化合物
公开(公告)号：US6166055A
公开(公告)日：2000-12-26
申请号：US341382
申请日：1999-07-09
申请人： Katherine L. Widdowson , Hong Nie , Melvin Clarence Rutledge, Jr.
发明人： Katherine L. Widdowson , Hong Nie , Melvin Clarence Rutledge, Jr.
IPC分类号： A61K31/404 , A61K31/416 , A61K31/423 , A61K31/428 , A61P1/00 , A61P1/04 , A61P7/02 , A61P9/00 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P25/28 , A61P43/00 , C07D209/08 , C07D209/34 , C07D231/56 , C07D261/20 , C07D275/04 , C07D275/06
CPC分类号： C07D275/06 , C07D231/56 , C07D261/20
摘要： This invention relates to compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). ##STR1##
摘要翻译： PCT No.PCT / US98 / 01292 Sec。 371日期1999年7月9日 102（e）日期1999年7月9日PCT提交1998年1月23日PCT公布。公开号WO98 / 32438 日期：1998年7月30日本发明涉及式（I）化合物及其组合物，其可用于治疗由趋化因子介导的疾病状态，白细胞介素-8（IL-8）。

60. 发明授权

US6150378A Peptidyl-containing .alpha.-ketoamide cysteine and serine protease inhibitors 失效
标题翻译：含肽基的α-酮酰胺半胱氨酸和丝氨酸蛋白酶抑制剂
公开(公告)号：US6150378A
公开(公告)日：2000-11-21
申请号：US166808
申请日：1998-10-06
申请人： Sankar Chatterjee , John P. Mallamo , Ron Bihovsky , Gregory J. Wells
发明人： Sankar Chatterjee , John P. Mallamo , Ron Bihovsky , Gregory J. Wells
IPC分类号： C07D295/18 , A61K31/422 , A61K31/4406 , A61K31/4433 , A61K31/4436 , A61K31/497 , A61K31/5375 , A61K31/5377 , A61K38/00 , A61P1/18 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P19/02 , A61P25/08 , A61P25/16 , A61P25/28 , A61P43/00 , C07C311/06 , C07C311/46 , C07C311/48 , C07D207/08 , C07D207/20 , C07D207/48 , C07D211/76 , C07D211/96 , C07D213/70 , C07D213/71 , C07D213/74 , C07D233/54 , C07D235/06 , C07D239/42 , C07D275/06 , C07D277/40 , C07D277/54 , C07D333/34 , C07D333/62 , C07D409/04 , C07D409/14 , C07D413/04 , C07K5/062 , C07K5/065 , C07K5/078 , A61K31/44 , C07D333/02
CPC分类号： C07D207/08 , C07C311/06 , C07C311/46 , C07C311/48 , C07D207/20 , C07D207/48 , C07D211/76 , C07D211/96 , C07D213/70 , C07D213/74 , C07D235/06 , C07D239/42 , C07D275/06 , C07D277/40 , C07D277/54 , C07D333/34 , C07D333/62 , C07D409/04 , C07D409/14 , C07D413/04 , C07K5/0202 , C07K5/06069
摘要： This invention relates to peptide-containing .alpha.-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.
摘要翻译：本发明涉及半胱氨酸和丝氨酸蛋白酶的含肽α-酮酰胺抑制剂，制备这些化合物的方法及其使用方法。

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