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31. 发明申请

US20060240097A1 TRPV1 agonist compounds and methods for making and using the same 有权
标题翻译： TRPV1激动剂化合物及其制备和使用方法
公开(公告)号：US20060240097A1
公开(公告)日：2006-10-26
申请号：US11411328
申请日：2006-04-25
申请人： Gene Jamieson , Naweed Muhammad , Keith Bley
发明人： Gene Jamieson , Naweed Muhammad , Keith Bley
IPC分类号： A61K31/24 , A61K9/48 , C07C235/72
CPC分类号： C07C233/20 , A61K47/55 , A61K47/60 , C07C233/18 , C07C2601/14
摘要： Described here are TRPV1 agonist compounds and their methods of synthesis and use. In addition to specifically identified compounds, capsaicin prodrugs, gemini dimers, and mutual prodrugs are also described. Formulations of the TRPV1 agonist compounds may be in the form of a liquid, tablets, capsules, gel, cream, emulsion, a patch, or the like. Methods for treating medical conditions using the compounds, compositions, or prodrugs described, are also provided.
摘要翻译：这里描述的是TRPV1激动剂化合物及其合成和使用方法。除了具体鉴定的化合物之外，还描述了辣椒素前药，双子二聚体和共同前药。 TRPV1激动剂化合物的制剂可以是液体，片剂，胶囊，凝胶，霜剂，乳剂，贴剂等的形式。还提供了使用所述化合物，组合物或前药治疗医学病症的方法。

32. 发明授权

US5633268A Substituted ortho-ethenylphenylacetic acid derivatives 失效
标题翻译：取代邻乙烯基苯乙酸衍生物
公开(公告)号：US5633268A
公开(公告)日：1997-05-27
申请号：US433515
申请日：1995-05-12
申请人： Reinhard Kirstgen , Hans Theobald , Klaus Oberdorf , Reinhard Doetzer , Ralf Klintz , Bernd Schaefer , Volker Harries , Uwe Kardorff , Gisela Lorenz , Eberhard Ammermann
发明人： Reinhard Kirstgen , Hans Theobald , Klaus Oberdorf , Reinhard Doetzer , Ralf Klintz , Bernd Schaefer , Volker Harries , Uwe Kardorff , Gisela Lorenz , Eberhard Ammermann
IPC分类号： A01N37/06 , A01N37/10 , A01N37/30 , A01N37/34 , A01N37/36 , A01N37/50 , A01N43/40 , A01N43/72 , A01N43/80 , A01N43/824 , C07C69/65 , C07C69/734 , C07C69/738 , C07C205/42 , C07C205/53 , C07C205/56 , C07C235/34 , C07C235/36 , C07C235/38 , C07C235/72 , C07C239/20 , C07C239/22 , C07C243/32 , C07C243/38 , C07C251/40 , C07C251/48 , C07C251/52 , C07C251/64 , C07C251/66 , C07C255/14 , C07C255/38 , C07C255/41 , C07C255/62 , C07C255/64 , C07C255/66 , C07C259/06 , C07C271/60 , C07C291/02 , C07C323/10 , C07C323/62 , C07C327/20 , C07C327/38 , C07C331/02 , C07D295/32 , C07D285/08 , A61K31/41
CPC分类号： C07D295/32 , A01N37/36 , A01N37/50 , A01N43/80 , C07C205/42 , C07C205/53 , C07C205/56 , C07C235/34 , C07C235/36 , C07C235/38 , C07C239/22 , C07C243/32 , C07C243/38 , C07C251/40 , C07C251/48 , C07C251/52 , C07C251/66 , C07C255/14 , C07C255/38 , C07C255/41 , C07C255/62 , C07C255/64 , C07C255/66 , C07C259/06 , C07C271/60 , C07C69/65 , C07C69/734 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2103/74
摘要： Compounds of the formula I ##STR1## where the index and the substituents have the following meanings as defined in the specification.
摘要翻译： PCT No.PCT / EP93 / 03067 Sec。 371日期：1995年5月12日 102（e）日期1995年5月12日PCT提交1993年11月12日PCT公布。公开号WO94 / 11334 日期1994年5月26日化学式I 其中指数和取代基具有如说明书中定义的以下含义。

33. 发明授权

US5548078A Process for the preparation of alkoxyiminoacetamide derivatives and their use as fungicides 失效
标题翻译：制备烷氧基亚氨基乙酰胺衍生物的方法及其作为杀真菌剂的用途
公开(公告)号：US5548078A
公开(公告)日：1996-08-20
申请号：US359639
申请日：1994-12-20
申请人： Yoshio Hayase , Takahiro Kataoka , Hideyuki Takenaka , Mitsuhiro Ichinari , Michio Masuko , Toshio Takahashi , Norihiko Tanimoto
发明人： Yoshio Hayase , Takahiro Kataoka , Hideyuki Takenaka , Mitsuhiro Ichinari , Michio Masuko , Toshio Takahashi , Norihiko Tanimoto
IPC分类号： C07C251/50 , A01N37/18 , A01N37/50 , A01N41/04 , A01N41/10 , A01N43/08 , A01N43/16 , A01N43/20 , A01N43/40 , A01N43/42 , A01N43/44 , A01N43/54 , A01N43/78 , A01N55/00 , C07C235/72 , C07C235/78 , C07C249/12 , C07C251/48 , C07C317/44 , C07C317/48 , C07C323/47 , C07C323/60 , C07C323/62 , C07C323/63 , C07D213/64 , C07D215/22 , C07D215/227 , C07D239/34 , C07D277/20 , C07D277/34 , C07D277/68 , C07D303/46 , C07D307/36 , C07D307/40 , C07D307/42 , C07D309/12 , C07D333/24 , C07D521/00 , C07F7/08 , C07F7/10 , C07D213/63
CPC分类号： C07C249/12 , A01N37/50 , C07C251/48 , C07C317/44 , C07C323/60 , C07D213/64 , C07D215/227 , C07D239/34 , C07D277/68 , C07D303/46 , C07D307/36 , C07D307/40 , C07D307/42 , C07D309/12 , C07F7/10
摘要： A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.
摘要翻译：一种用于农业用途的杀真菌组合物，其包含下式的化合物：其中R 1和R 2各自为氢，低级烷基或环（低级）烷基; R3是低级烷基或环（低级）烷基; R4和R5各自为氢，低级烷基，低级烷氧基，卤素取代的低级烷基，低级烷基取代的甲硅烷基，卤素或硝基; A表示不饱和烃基，卤素取代的不饱和烃基，苯基或杂环基，其中苯基和杂环基可以任选被不多于三个取代基取代; Z为-CH 2 - ， - CH（OH） - ， - CO - ， - O - ， - S - ， - NR-（R为氢或低级烷基），-CH 2 CH 2 - ， - CH = CH-， -CH 2 - ， - CH 2 S - ， - CH 2 SO - ， - OCH 2 - ， - CH 2 - 或-SOCH 2 - 。

34. 发明授权

US5502252A Process of producing intermediates for use in production of alkoxyiminoacetamides and intermediates to be used therein 失效
公开(公告)号：US5502252A
公开(公告)日：1996-03-26
申请号：US339254
申请日：1994-11-10
申请人： Akira Takase , Hiroyuki Kai , Kuniyoshi Nishida , Moriyasu Masui
发明人： Akira Takase , Hiroyuki Kai , Kuniyoshi Nishida , Moriyasu Masui
IPC分类号： C07D215/12 , C07C51/58 , C07C59/84 , C07C59/88 , C07C59/90 , C07C227/02 , C07C229/42 , C07C231/02 , C07C233/56 , C07C235/72 , C07C235/78 , C07C237/20 , C07C249/08 , C07C319/12 , C07C319/20 , C07C323/62 , C07D215/20 , C07D215/36 , C07D239/26 , C07D239/34 , C07D239/38 , C07D239/42 , C07D261/08 , C07D261/10 , C07D261/12 , C07D261/14 , C07D263/32 , C07D263/36 , C07D263/46 , C07D263/48 , C07D263/56 , C07D263/58 , C07D277/62 , C07D303/38 , C07D413/04 , C07C233/05
CPC分类号： C07C59/84 , C07C231/02 , C07C249/08
摘要： There is disclosed a process of producing an .alpha.-ketamide as an intermediate for use in the production of various alkoxyiminoacetamide compounds which are useful as fungicides. Also disclosed is an intermediate to be used in this process.

35. 发明授权

US5472980A Parental administration of pyruyate precursors 失效
标题翻译：亲本管理丙酮酸前体
公开(公告)号：US5472980A
公开(公告)日：1995-12-05
申请号：US285683
申请日：1994-08-04
申请人： Robert H. Miller
发明人： Robert H. Miller
IPC分类号： A61K31/19 , A61K31/195 , A61K31/40 , A61P3/04 , C07C231/02 , C07C235/72
CPC分类号： A61K31/40 , A61K31/195 , Y10S514/866 , Y10S514/909
摘要： A method for administering pyruvate is disclosed which comprises administering a therapeutically effective amount of a pyruvate precursor to a mammal in the form of pyruvamide or a pyruvyl-amino acid. The pyruvyl-amino acid is preferably selected from the group comprising pyruvyl-glycine, pyruvyl-alanine, pyruvyl-leucine, pyruvyl-valine, pyruvyl-isoleucine, pyruvyl-phenylalanine, pyruvyl-proline and pyruvyl-sarcosine, and their amides and esters as well as their salts. Associated with the administration of a pyruvate precursor to a mammal in accordance with this invention are improved insulin resistance, lower fasting insulin levels, and reduced fat gain. Novel methods of synthesizing several pyruvate precursors are also disclosed.
摘要翻译：公开了一种给予丙酮酸盐的方法，其包括给予哺乳动物治疗有效量的丙酮酸前体以丙酮酰胺或丙酮酸 - 氨基酸的形式。丙酮酸氨基酸优选选自丙酮酸 - 甘氨酸，丙酮酸 - 丙氨酸，丙酮酸 - 亮氨酸，丙酮酸 - 缬氨酸，丙酮酸 - 异亮氨酸，丙酮酸 - 苯丙氨酸，丙酮酸 - 脯氨酸和丙酮酸 - 肌氨酸，其酰胺和酯为以及它们的盐。与根据本发明的哺乳动物的丙酮酸前体的施用相关联的是改善的胰岛素抵抗，降低的空腹胰岛素水平和降低的脂肪增加。还公开了合成若干丙酮酸前体的新方法。

36. 发明授权

US5401772A Heteroacetic acid derivatives 失效
标题翻译：异丁酸衍生物
公开(公告)号：US5401772A
公开(公告)日：1995-03-28
申请号：US154203
申请日：1993-11-18
申请人： Naokata Yokoyama, deceased , Gordon N. Walker , Alan J. Main
发明人： Naokata Yokoyama, deceased , Gordon N. Walker , Alan J. Main
IPC分类号： A61K31/165 , A61P3/06 , C07C41/00 , C07C229/18 , C07C229/36 , C07C233/56 , C07C235/72 , C07C323/37 , C07C323/52 , C07J41/00 , A61K31/24
CPC分类号： C07C323/52 , C07C229/18 , C07C229/36 , C07C233/56 , C07J41/0055
摘要： Disclosed are compounds of formula ##STR1## wherein R is hydroxy, esterified hydroxy or etherified hydroxy;R.sub.1 is halogen, trifluoromethyl or lower alkyl;R.sub.2 is halogen, trifluoromethyl or lower alkyl;R.sub.3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; orR.sub.3 is the radical ##STR2## wherein R.sub.8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R.sub.9 is hydroxy or acyloxy; R.sub.10 represents hydrogen or lower alkyl; or R.sub.9 and R.sub.10 together represent oxo;R.sub.4 is hydrogen, halogen, trifluoromethyl or lower alkyl;X is --NR.sub.7, S or O;W is O or S;R.sub.5 represents hydrogen, lower alkyl or aryl-lower alkyl;andR.sub.6 represents hydrogen; orR.sub.5 and R.sub.6 together represent oxo provided that X represents --NR.sub.7;R.sub.7 represents hydrogen or lower alkyl;Z represents carboxyl, carboxyl derivatized as a pharmaceutically acceptable ester or as a pharmaceutically acceptable amide; and pharmaceutically acceptable salts thereof; which are useful as hypocholesteremic agents.
摘要翻译：公开了式（I）的化合物，其中R是羟基，酯化的羟基或醚化的羟基; R1是卤素，三氟甲基或低级烷基; R2是卤素，三氟甲基或低级烷基; R3是卤素，三氟甲基，低级烷基，芳基，芳基 - 低级烷基，环烷基或环烷基 - 低级烷基; 或R3是基团，其中R8是氢，低级烷基，芳基，环烷基，芳基 - 低级烷基或环烷基 - 低级烷基; R9是羟基或酰氧基; R 10表示氢或低级烷基; 或R 9和R 10一起代表氧代; R4是氢，卤素，三氟甲基或低级烷基; X是-NR 7，S或O; W为O或S; R5代表氢，低级烷基或芳基 - 低级烷基; R6代表氢; 或者R 5和R 6一起代表氧代，条件是X代表-NR7; R7代表氢或低级烷基; Z表示羧基，羧基衍生化为药学上可接受的酯或作为药学上可接受的酰胺; 及其药学上可接受的盐; 其可用作低胆固醇剂。

37. 发明授权

US5393788A Phenylalkyl oxamides 失效
标题翻译：苯基烷基酰胺
公开(公告)号：US5393788A
公开(公告)日：1995-02-28
申请号：US961716
申请日：1993-03-02
申请人： Paul E. Bender , Siegfried B. Christensen, IV , Klaus M. Esser , Cornelia J. Forster , Michael D. Ryan , Philip L. Simon
发明人： Paul E. Bender , Siegfried B. Christensen, IV , Klaus M. Esser , Cornelia J. Forster , Michael D. Ryan , Philip L. Simon
IPC分类号： A61K31/195 , A61K31/16 , A61K31/22 , A61K31/34 , A61K31/341 , A61K31/415 , A61K31/495 , A61K31/505 , A61P17/00 , A61P27/02 , A61P29/00 , A61P37/00 , C07C20060101 , C07C233/18 , C07C233/31 , C07C233/36 , C07C233/43 , C07C233/47 , C07C233/56 , C07C235/72 , C07C237/22 , C07C255/44 , C07C259/06 , C07C271/20 , C07C317/32 , C07C323/41 , C07D213/36 , C07D213/40 , C07D213/56 , C07D213/75 , C07D233/64 , C07D233/88 , C07D237/08 , C07D237/20 , C07D239/26 , C07D239/42 , C07D307/12 , A61K31/165 , C07C233/00
CPC分类号： C07D213/40 , C07C233/18 , C07C233/31 , C07C233/36 , C07C233/43 , C07C233/47 , C07C237/22 , C07C255/44 , C07C259/06 , C07C271/20 , C07C317/32 , C07C323/41 , C07D213/75 , C07C2101/08
摘要： Novel oxamide derivatives are described which inhibit the production of TNF and are useful in the treatment of disease states mediated or exacerbated by TNF production. The compounds of the present invention are also useful as inhibitors of PDE IV and are therefor useful in the treatment of disease states mediated or exacerbated thereby.
摘要翻译： PCT No.PCT / US91 / 04795 371日期1993年3月2日 102（e）1993年3月2日PCT PCT 1991年7月8日PCT公布。出版物WO92 / 00968 1992年1月23日的日期。描述了抑制TNF产生的新型草酰胺衍生物，可用于治疗由TNF产生介导或加重的疾病状态。本发明的化合物还可用作PDE IV的抑制剂，因此可用于治疗由此介导或加剧的疾病状态。

38. 发明授权

US5371222A Alkoxyiminoacetamide derivatives and their use as fungicides 失效
公开(公告)号：US5371222A
公开(公告)日：1994-12-06
申请号：US962345
申请日：1992-10-16
申请人： Yoshio Hayase , Takahiro Kataoka , Hideyuki Takenaka , Mitsuhiro Ichinari , Michio Masuko , Toshio Takahashi , Norihiko Tanimoto
发明人： Yoshio Hayase , Takahiro Kataoka , Hideyuki Takenaka , Mitsuhiro Ichinari , Michio Masuko , Toshio Takahashi , Norihiko Tanimoto
IPC分类号： C07C251/50 , A01N37/18 , A01N37/50 , A01N41/04 , A01N41/10 , A01N43/08 , A01N43/16 , A01N43/20 , A01N43/40 , A01N43/42 , A01N43/44 , A01N43/54 , A01N43/78 , A01N55/00 , C07C235/72 , C07C235/78 , C07C249/12 , C07C251/48 , C07C317/44 , C07C317/48 , C07C323/47 , C07C323/60 , C07C323/62 , C07C323/63 , C07D213/64 , C07D215/22 , C07D215/227 , C07D239/34 , C07D277/20 , C07D277/34 , C07D277/68 , C07D303/46 , C07D307/36 , C07D307/40 , C07D307/42 , C07D309/12 , C07D333/24 , C07D521/00 , C07F7/08 , C07F7/10 , C07D239/02 , C07D277/02 , C07D321/00 , C07D401/02
CPC分类号： C07C249/12 , A01N37/50 , C07C251/48 , C07C317/44 , C07C323/60 , C07D213/64 , C07D215/227 , C07D239/34 , C07D277/68 , C07D303/46 , C07D307/36 , C07D307/40 , C07D307/42 , C07D309/12 , C07F7/10
摘要： A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.

39. 发明授权

US5312985A Method of synthesizing the precursor pyruvamide 失效
标题翻译：合成丙酮酸前体丙酮酰胺的方法
公开(公告)号：US5312985A
公开(公告)日：1994-05-17
申请号：US43699
申请日：1993-04-08
申请人： Madhup K. Dhaon , John A. Houbion
发明人： Madhup K. Dhaon , John A. Houbion
IPC分类号： A61K31/19 , A61K31/195 , A61K31/40 , A61P3/04 , C07C231/02 , C07C235/72
CPC分类号： A61K31/40 , A61K31/195 , Y10S514/866 , Y10S514/909
摘要： A method for administering pyruvate is disclosed which comprises administering a therapeutically effective amount of a pyruvate precursor to a mammal in the form of pyruvamide or a pyruvyl-amino acid. The pyruvyl-amino acid is preferably selected from the group comprising pyruvyl-glycine, pyruvyl-alanine, pyruvyl-leucine, pyruvyl-valine, pyruvyl-isoleucine, pyruvyl-phenylalanine, pyruvyl-proline and pyruvyl-sarcosine, and their amides and esters as well as their salts. Associated with the administration of a pyruvate precursor to a mammal in accordance with this invention are improved insulin resistance, lower fasting insulin levels, and reduced fat gain. Novel methods of synthesizing several pyruvate precursors are also disclosed.
摘要翻译：公开了一种给予丙酮酸盐的方法，其包括给予哺乳动物治疗有效量的丙酮酸前体以丙酮酰胺或丙酮酸 - 氨基酸的形式。丙酮酸氨基酸优选选自丙酮酸 - 甘氨酸，丙酮酸 - 丙氨酸，丙酮酸 - 亮氨酸，丙酮酸 - 缬氨酸，丙酮酸 - 异亮氨酸，丙酮酸 - 苯丙氨酸，丙酮酸 - 脯氨酸和丙酮酸 - 肌氨酸，其酰胺和酯为以及它们的盐。与根据本发明的哺乳动物的丙酮酸前体的施用相关联的是改善的胰岛素抵抗，降低的空腹胰岛素水平和降低的脂肪增加。还公开了合成若干丙酮酸前体的新方法。

40. 发明授权

US5283260A Method for reducing insulin resistance in mammals 失效
标题翻译：减少哺乳动物胰岛素抵抗的方法
公开(公告)号：US5283260A
公开(公告)日：1994-02-01
申请号：US43720
申请日：1993-04-08
申请人： Robert H. Miller , Nickki L. Parlet , Kent L. Cipollo , Madhup K. Dhaon , John A. Houbion , Edwin O. Lundell
发明人： Robert H. Miller , Nickki L. Parlet , Kent L. Cipollo , Madhup K. Dhaon , John A. Houbion , Edwin O. Lundell
IPC分类号： A61K31/19 , A61K31/195 , A61K31/40 , A61P3/04 , C07C231/02 , C07C235/72
CPC分类号： A61K31/40 , A61K31/195 , Y10S514/866 , Y10S514/909
摘要： A method for administering pyruvate is disclosed which comprises administering a therapeutically effective amount of a pyruvate precursor to a mammal in the form of pyruvamide or a pyruvyl-amino acid. The pyruvyl-amino acid is preferably selected from the group comprising pyruvyl-glycine, pyruvyl-alanine, pyruvyl-leucine, pyruvyl-valine, pyruvyl-isoleucine, pyruvylphenyl al anine, pyruvyl-proline and pyruvyl-sarcosine, and their amides and esters as well as their salts. Associated with the administration of a pyruvate precursor to a mammal in accordance with this invention are improved insulin resistance, lower fasting insulin levels, and reduced fat gain. Novel methods of synthesizing several pyruvate precursors are also disclosed.
摘要翻译：公开了一种给予丙酮酸盐的方法，其包括给予哺乳动物治疗有效量的丙酮酸前体以丙酮酰胺或丙酮酸 - 氨基酸的形式。丙酮酸氨基酸优选选自丙酮酸 - 甘氨酸，丙酮酸 - 丙氨酸，丙酮酸 - 亮氨酸，丙酮酸 - 缬氨酸，丙酮酸 - 异亮氨酸，丙酮酰基苯胺，丙酮酸 - 脯氨酸和丙酮酸 - 肌氨酸，其酰胺和酯为以及它们的盐。与根据本发明的哺乳动物的丙酮酸前体的施用相关联的是改善的胰岛素抵抗，降低的空腹胰岛素水平和降低的脂肪增加。还公开了合成若干丙酮酸前体的新方法。

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