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1.
公开(公告)号:US6077854A
公开(公告)日:2000-06-20
申请号:US48592
申请日:1998-03-26
IPC分类号: A61K31/44 , A61P11/06 , A61P43/00 , C07C1/26 , C07C1/32 , C07C15/02 , C07C15/12 , C07C17/263 , C07C25/02 , C07C25/18 , C07C43/20 , C07C57/30 , C07C59/64 , C07C237/04 , C07C307/04 , C07C311/00 , C07C323/00 , C07C327/00 , C07C327/48 , C07C335/04 , C07D213/30 , C07D521/00 , C07D213/02
CPC分类号: C07D213/30
摘要: Tri-substituted phenyl derivatives and processes for their preparation. In a preferred embodiment, the compounds have the general formula (1) ##STR1## wherein L may be --OR; Z may be --C(R.sup.3)(R.sup.4)--C(R.sup.5)(R.sup.6)(R.sup.7); R may be an optionally substituted cycloalkyl group; R.sup.3, R.sup.6 and R.sup.7 may be hydrogen; R.sup.4 may be --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar'; R.sup.5 may be --(CH.sub.2).sub.t Ar; Ar may be a monocyclic or bicyclic aryl or heteroaryl group; L.sup.1 may be a divalent linking group; and Ar' is Ar or an Ar containing group. Compounds of the invention may be potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.
摘要翻译: 三取代苯基衍生物及其制备方法。 在优选的实施方案中,化合物具有通式(1),其中L可以是-OR; Z可以是-C(R 3)(R 4)-C(R 5)(R 6)(R 7); R可以是任选取代的环烷基; R3,R6和R7可以是氢; R4可以是 - (CH2)t-Ar-(L1)n-Ar'; R5可以是 - (CH2)tAr; Ar可以是单环或双环芳基或杂芳基; L1可以是二价连接基团; Ar'为Ar或含Ar基团。 本发明的化合物可以是有效的选择性磷酸二酯酶IV型抑制剂,并且可用于预防和治疗与不想要的炎性反应或肌肉痉挛相关的各种疾病,例如哮喘。
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2.
公开(公告)号:US5786354A
公开(公告)日:1998-07-28
申请号:US492639
申请日:1995-06-20
IPC分类号: A61K31/44 , A61P11/06 , A61P43/00 , C07C1/26 , C07C1/32 , C07C15/02 , C07C15/12 , C07C17/263 , C07C25/02 , C07C25/18 , C07C43/20 , C07C57/30 , C07C59/64 , C07C237/04 , C07C307/04 , C07C311/00 , C07C323/00 , C07C327/00 , C07C327/48 , C07C335/04 , C07D213/30 , C07D521/00 , A61K31/435
CPC分类号: C07D213/30
摘要: Tri-substituted phenyl derivatives and processes for their preparation. In a preferred embodiment, the compounds have the general formula (2) ##STR1## wherein L is preferably --OR; Z is preferably --C(R.sup.3)(R.sup.4)--C(R.sup.5)(R.sup.6)(R.sup.7); R is preferably an optionally substituted cycloalkyl group: R.sup.3 is preferably hydrogen; R.sup.4 is hydrogen, --(CH.sub.2).sub.t Ar or --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar'; R.sup.5 is --(CH.sub.2).sub.t Ar or --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar'; R.sup.6 and R.sup.7 are preferably hydrogen or methyl; Ar is a monocyclic or bicyclic aryl or heteroaryl group; L.sup.1 is a divalent linking group; and Ar' is Ar or an Ar containing group. Compounds of the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.
摘要翻译: 三取代苯基衍生物及其制备方法。 在优选的实施方案中,化合物具有通式(2)其中L优选为-OR; Z优选为-C(R 3)(R 4)-C(R 5)(R 6)(R 7); R优选为任选取代的环烷基:R 3优选为氢; R4是氢, - (CH2)tAr或 - (CH2)t-Ar-(L1)n-Ar'; R5是 - (CH2)tAr或 - (CH2)t-Ar-(L1)n-Ar'; R6和R7优选为氢或甲基; Ar是单环或双环芳基或杂芳基; L1是二价连接基团; Ar'是Ar或含Ar的基团。 本发明的化合物是有效和选择性的磷酸二酯酶IV型抑制剂,并且可用于预防和治疗与不想要的炎症反应或肌肉痉挛相关的各种疾病,例如哮喘。
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公开(公告)号:US5254715A
公开(公告)日:1993-10-19
申请号:US747031
申请日:1991-08-19
IPC分类号: A61K31/27 , A61K31/34 , A61K31/341 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/4453 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61P3/06 , A61P9/10 , A61P43/00 , C07C307/04 , C07C307/06 , C07C307/08 , C07C307/10 , C07D209/08 , C07D213/42 , C07D235/28 , C07D235/30 , C07D295/22 , C07D295/26 , C07D307/14
CPC分类号: C07D213/42 , C07C307/06 , C07C307/08 , C07C307/10 , C07D235/30 , C07D295/26 , C07D307/14 , C07C2101/14
摘要: A compound of the following general formula which is useful in treating hypocholesterolemia and atherosclerosis: ##STR1## wherein X is oxygen or sulfur; R is hydrogen, alkyl having from 1 to 8 carbon atoms, or benzyl; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, a heterocyclic group, or a hydrocarbon chain of from 1 to 20 carbon atoms which is saturated or contains 1 to 3 double bonds and each of R.sub.2 and R.sub.3 is selected from hydrogen, provided both are not hydrogen, an aralkyl group, a hydrocarbon chain of from 1 to 20 carbon atoms which is saturated or contains 1 to 3 double bonds, an w-substituted alkylC.sub.1-6, a heterocyclic group, phenyl, substituted phenyl or NR.sub.2 R.sub.3 taken together form a monocyclic heterocyclic group.
摘要翻译: 用于治疗低血胆固醇血症和动脉粥样硬化的以下通式的化合物:其中X是氧或硫; R为氢,具有1至8个碳原子的烷基或苄基; R1是饱和或含1〜3个双键的苯基,取代的苯基,萘基,取代的萘基,芳烷基,杂环基或烃链,R2和R3各自选自 氢,其既不是氢,芳烷基,具有1-20个碳原子的饱和或含有1〜3个双键的烃链,w取代的烷基C 1-6,杂环基,苯基,取代的苯基或 NR2R3一起形成单环杂环基。
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公开(公告)号:US5214206A
公开(公告)日:1993-05-25
申请号:US747040
申请日:1991-08-19
IPC分类号: A61K31/445 , A61K31/64 , A61P3/06 , A61P9/10 , A61P43/00 , C07C307/04 , C07C307/06 , C07C307/08 , C07C307/10 , C07D211/96 , C07D211/98 , C07D261/08 , C07D261/14 , C07D263/32 , C07D263/48 , C07D295/22 , C07D307/14 , C07D333/20
CPC分类号: C07D211/96 , C07C307/06 , C07C307/08 , C07C307/10 , C07D307/14 , C07C2101/14
摘要: The present invention provides pharmaceutically useful compounds which are aminosulfonyl urea compounds which are ACAT inhibitors rendering them useful in controlling blood cholesterol levels, pharmaceutical compositions and methods of using the ACAT inhibitors and closely related compounds which are also aminosulfonyl urea compounds.
摘要翻译: 本发明提供药学上有用的化合物,其是作为ACAT抑制剂的氨基磺酰脲化合物,其可用于控制血液胆固醇水平,药物组合物和使用也是氨基磺酰脲化合物的ACAT抑制剂和紧密相关化合物的方法。
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公开(公告)号:US20220177418A1
公开(公告)日:2022-06-09
申请号:US17599083
申请日:2020-03-27
申请人: The Regents of the University of California , The United States Government represented by the Department of Veterans Affairs
IPC分类号: C07C233/13 , C07C233/40 , C07C233/91 , C07C235/76 , C07C255/46 , C07C307/04 , C07C49/537 , C07C49/697 , C07C69/618 , C07D207/273 , C07D207/38 , C07D211/70 , C07D213/46 , C07D307/46 , C07D303/32 , C07D263/32
摘要: The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.
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公开(公告)号:US5886044A
公开(公告)日:1999-03-23
申请号:US641990
申请日:1996-03-20
申请人: Katherine Louisa Widdowson , Daniel Frank Veber , Anthony Joseph Jurewicz , Robert Phillip Hertzberg , Melvin Clarence Rutledge, Jr.
发明人: Katherine Louisa Widdowson , Daniel Frank Veber , Anthony Joseph Jurewicz , Robert Phillip Hertzberg , Melvin Clarence Rutledge, Jr.
IPC分类号: A61K31/17 , A61K31/18 , A61K31/223 , A61K31/275 , A61K31/277 , A61K31/36 , A61K31/381 , A61K31/426 , A61K31/47 , A61P29/00 , A61P37/00 , C07C253/14 , C07C255/53 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/40 , C07C275/42 , C07C307/04 , C07C307/10 , C07C309/15 , C07C311/10 , C07C311/13 , C07C311/15 , C07C311/21 , C07C311/29 , C07C311/46 , C07C317/42 , C07C323/44 , C07C335/16 , C07C335/18 , C07D213/30 , C07D213/71 , C07D215/36 , C07D217/02 , C07D277/36 , C07D277/46 , C07D317/66 , C07D333/28 , C07D333/34 , C07D333/36 , C07D409/04
CPC分类号: C07D213/30 , A61K31/17 , A61K31/18 , A61K31/223 , A61K31/275 , A61K31/277 , A61K31/36 , A61K31/381 , A61K31/426 , A61K31/47 , C07C275/34 , C07C275/38 , C07C275/40 , C07C275/42 , C07C307/10 , C07C309/15 , C07C311/10 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/46 , C07C317/42 , C07C323/44 , C07C335/18 , C07D213/71 , C07D215/36 , C07D217/02 , C07D277/36 , C07D277/46 , C07D317/66 , C07D333/28 , C07D333/34 , C07D333/36 , C07D409/04 , C07C2102/08 , C07C2103/18
摘要: This invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
摘要翻译: 本发明涉及苯脲类治疗由趋化因子介导的疾病状态,白细胞介素-8(IL-8)的新用途。
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公开(公告)号:US5480720A
公开(公告)日:1996-01-02
申请号:US204929
申请日:1994-03-01
IPC分类号: C07C307/04 , C07D207/26 , C07D207/273 , C07D477/02 , C07D477/14 , C07D477/20 , C07D501/00 , C08L63/00 , C09J133/06 , B32B27/38
CPC分类号: C07D207/273 , C07C307/04 , C07D477/02 , C07D477/14 , C07D477/20 , C07D501/00 , C09J133/064 , C08L63/00 , Y10T428/31515 , Y10T428/31895 , Y10T428/31928
摘要: An adhesive composition includes from about 30 weight percent to about 70 weight percent solids dispersed in an aqueous medium. The solids include from about 60 weight percent to about 97.9 weight percent of a polymer having a glass transition temperature of about -40.degree. C. to about 10.degree. C. and including first repeating units derived from an alkyl (meth)acrylate monomer, a vinyl ester monomer, a styrenic monomer or a mixture thereof and second repeating units derived from a hydroxyalkyl (meth)acrylate monomer, a monoethylenically unsaturated nitrogenous monomer or a mixture thereof; from about 2 weight percent to about 30 weight percent of a polyfunctional epoxy resin including two or more epoxide groups per molecule; from about 0.1 weight percent to about 10 weight percent of a polyfunctional curing agent including two or more amino groups or amido groups per molecule; and from about 0.01 weight percent to about 30 weight percent of a metal salt. A method for making a laminate includes applying a layer of the aqueous adhesive composition to a first substrate layer and covering the layer of adhesive composition with a second substrate layer to form the laminated article. A laminate includes two substrate layers bonded together by an interposed layer of the solids of the adhesive composition.
摘要翻译: 粘合剂组合物包含分散在水性介质中的约30重量%至约70重量%的固体。 固体包括约60重量%至约97.9重量%的玻璃化转变温度为约-40℃至约10℃的聚合物,并且包括衍生自(甲基)丙烯酸烷基酯单体的第一重复单元, 乙烯基酯单体,苯乙烯单体或其混合物,以及衍生自(甲基)丙烯酸羟烷基酯单体,单烯属不饱和含氮单体或其混合物的第二重复单元; 约2重量%至约30重量%的每分子包含两个或更多个环氧基团的多官能环氧树脂; 约0.1重量%至约10重量%的每分子含有两个或多个氨基或酰氨基的多官能固化剂; 和约0.01重量%至约30重量%的金属盐。 制造层压体的方法包括将水性粘合剂组合物层施加到第一基材层并用第二基材层覆盖粘合剂组合物层以形成层压制品。 层压体包括通过粘合剂组合物的固体的插入层粘合在一起的两个基底层。
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公开(公告)号:US09156783B2
公开(公告)日:2015-10-13
申请号:US14108162
申请日:2013-12-16
申请人: Shoujun Chen , Keizo Koya , Zachary Demko , Lijun Sun
发明人: Shoujun Chen , Keizo Koya , Zachary Demko , Lijun Sun
IPC分类号: A61K31/15 , C07C243/14 , C07C243/42 , C07C327/56 , C07C243/28 , C07C255/66 , C07C257/22 , C07C261/04 , C07C281/06 , C07C307/04 , C07C311/49 , C07C311/51 , C07C337/06 , C07D207/34 , C07D207/36 , C07D233/74 , C07D263/48 , C07D271/10 , C07D271/113 , C07D307/66 , C07F9/44 , A61K31/16 , A61K31/166 , A61K31/18 , A61K31/277 , A61K31/341 , A61K31/40 , A61K31/4245 , A61K31/664 , C07C243/34 , C07C311/55 , C07F9/22 , C07F9/46
CPC分类号: C07C327/56 , A61K31/16 , A61K31/166 , A61K31/18 , A61K31/277 , A61K31/341 , A61K31/40 , A61K31/4245 , A61K31/664 , C07C243/28 , C07C243/34 , C07C255/66 , C07C257/22 , C07C261/04 , C07C281/06 , C07C307/04 , C07C311/49 , C07C311/51 , C07C311/55 , C07C337/06 , C07C2601/02 , C07D207/34 , C07D207/36 , C07D233/74 , C07D263/48 , C07D271/10 , C07D271/113 , C07D307/66 , C07F9/228 , C07F9/4423 , C07F9/4496 , C07F9/46
摘要: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
摘要翻译: 公开了式(I),(III),(IV),(VII),(X),(XI),(XII),(XIII)和(XIV)的化合物,其中变量如权利要求 以及使用本发明化合物治疗患有增殖性疾病(例如癌症)的受试者的方法,以及用于治疗对Hsp70诱导和/或自然杀伤诱导反应的病症的方法。 还公开了包含本发明化合物和药学上可接受的载体的药物组合物。
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公开(公告)号:US20080039654A1
公开(公告)日:2008-02-14
申请号:US11781557
申请日:2007-07-23
申请人: Patricia Savu , William Lamanna , Thomas Klun
发明人: Patricia Savu , William Lamanna , Thomas Klun
IPC分类号: C07C307/04 , C07C307/02
CPC分类号: G03C1/895 , C09K3/16 , Y10T428/31507 , Y10T428/3154 , Y10T428/31551
摘要: The present invention provides polyoxyalkylene ammonium imide or methide salts and their use as antistatic agents. Another embodiment provides articles comprising these salts, and processes for making and using these salts.
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公开(公告)号:US20050234106A1
公开(公告)日:2005-10-20
申请号:US10997734
申请日:2004-11-24
申请人: John Lloyd , Yoon Jeon , Heather Finlay , Lin Yan , Michael Gross , Serge Beaudoin
发明人: John Lloyd , Yoon Jeon , Heather Finlay , Lin Yan , Michael Gross , Serge Beaudoin
IPC分类号: A61K20060101 , A61K45/06 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/65 , C07C235/06 , C07C235/34 , C07C235/46 , C07C235/60 , C07C279/16 , C07C279/24 , C07C279/28 , C07C307/02 , C07C307/04 , C07C307/08 , C07C307/10 , C07C311/16 , C07C311/29 , C07C311/55 , C07C311/59 , C07C311/64 , C07C323/62 , C07D213/40 , C07D213/69 , C07D213/82 , C07D217/22 , C07D233/48 , C07D233/54 , C07D233/76 , C07D235/10 , C07D235/14 , C07D239/42 , C07D239/94 , C07D239/95 , C07D241/06 , C07D249/04 , C07D251/44 , C07D251/46 , C07D261/08 , C07D261/14 , C07D271/06 , C07D295/13 , C07D295/185 , C07D295/215 , C07D295/26 , C07D307/68 , C07D309/04 , C07D309/08 , C07D333/20 , C07D333/28 , C07D333/38 , C07D333/58 , C07D333/62 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D521/00 , C07D43/02 , A61K31/4164 , A61K31/4172 , A61K31/4439
CPC分类号: C07D213/40 , A61K45/06 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/65 , C07C235/06 , C07C235/34 , C07C235/46 , C07C235/60 , C07C279/16 , C07C279/24 , C07C279/28 , C07C307/02 , C07C307/04 , C07C307/08 , C07C307/10 , C07C311/16 , C07C311/29 , C07C311/55 , C07C311/59 , C07C311/64 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/10 , C07C2601/14 , C07C2602/08 , C07C2603/66 , C07D213/69 , C07D213/82 , C07D217/22 , C07D231/12 , C07D233/48 , C07D233/56 , C07D233/64 , C07D233/76 , C07D235/14 , C07D239/42 , C07D239/94 , C07D239/95 , C07D241/06 , C07D249/04 , C07D249/08 , C07D251/44 , C07D251/46 , C07D261/08 , C07D261/14 , C07D271/06 , C07D295/13 , C07D295/185 , C07D295/215 , C07D295/26 , C07D307/68 , C07D309/04 , C07D309/08 , C07D333/20 , C07D333/28 , C07D333/38 , C07D333/58 , C07D333/62 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04
摘要: Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.
摘要翻译: 可用作钾通道功能抑制剂的新型环烷基化合物(特别是电压门控K +通道抑制剂,尤其是抑制剂K + > 1.5,其与超快速活化延迟整流器K +电流I K连接),使用这些化合物在预防和治疗心律失常中的方法, 相关条件和含有这些化合物的药物组合物。
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