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1. 发明授权

US5955492A Carboxylic acid indole inhibitors of chemokines 失效
标题翻译：趋化因子的羧酸吲哚抑制剂
公开(公告)号：US5955492A
公开(公告)日：1999-09-21
申请号：US155220
申请日：1998-09-24
申请人： Scott K. Thompson , Stacie M. Halbert , Katherine L. Widdowson
发明人： Scott K. Thompson , Stacie M. Halbert , Katherine L. Widdowson
IPC分类号： A61K31/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61P1/00 , A61P7/00 , A61P7/02 , A61P9/00 , A61P11/00 , A61P13/00 , A61P13/12 , A61P17/00 , A61P19/00 , A61P19/02 , A61P33/00 , A61P33/06 , A61P37/00 , A61P43/00 , C07D209/42 , C07D405/06 , C07D405/14 , A61K31/405 , C07C62/36 , C07D209/18
CPC分类号： C07D405/06 , C07D209/42 , C07D405/14 , Y10S514/826 , Y10S514/863
摘要： This invention relates to novel carboxylic acid indole compounds and compositions for use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
摘要翻译： PCT No.PCT / US97 / 04938 Sec。 371日期：1998年9月24日 102（e）1998年9月24日PCT 1997年3月27日PCT公布。公开号WO97 / 35572 日期1997年10月2日本发明涉及用于治疗由趋化因子介导的疾病状态白细胞介素-8（IL-8）的新型羧酸吲哚化合物和组合物。

3. 发明授权

US4642372A Novel process for preparation of 1-furenyl-2,2-dimethyl-cyclopropane carboxylic acid derivatives 失效
标题翻译：制备1-呋喃基-2,2-二甲基 - 环丙烷羧酸衍生物的新方法
公开(公告)号：US4642372A
公开(公告)日：1987-02-10
申请号：US760313
申请日：1985-07-29
申请人： Jacques Martel , Jean Tessier , Jean-Pierre Demoute
发明人： Jacques Martel , Jean Tessier , Jean-Pierre Demoute
IPC分类号： C07C62/16 , A01N53/00 , C07C51/00 , C07C51/373 , C07C62/36 , C07C67/00 , C07C69/757 , C07C253/00 , C07C255/45 , C07C255/46 , C07C255/48 , C07C317/46
CPC分类号： C07C255/00 , A01N53/00 , C07C317/46 , C07C51/373
摘要： A process for the preparation of cyclopropane carboxylic acid derivatives of the formula ##STR1## wherein Z is selected from the group consisting of --CN, --COOH and --COOR.sub.1, R.sub.1 is alkyl of 1 to 6 carbon atoms and R.sub.2 and R.sub.3 are alkyl of 1 to 4 carbon atoms or taken together with the carbon atom to which they are attached form a carbon homocycle of 3 to 6 carbon atoms comprising reacting at low temperatures in a solvent in the presence of a strong base a compound of the formula ##STR2## wherein Z has the above definitions and R is alkyl of 1 to 6 carbon atoms or together form a polymethylene of 2 to 3 carbon atoms with a sulfone of the formula ##STR3## wherein R.sub.2 and R.sub.3 have the above definitions and Y is an aromatic group followed by aqueous treatment to obtain a compound of the formula ##STR4## wherein Y, R, R.sub.2, R.sub.3 and Z have the above definitions, reacting the latter at a low temperature in a solvent with a strong base while letting the temperature rise to obtain a compound of the formula ##STR5## wherein R, R.sub.2, R.sub.3 and Z have the above definitions of the cis/trans configuration richer in the trans isomer and either reacting the latter when Z is --CN or --COOR.sub.1 with a strong base in an aqueous media followed by acidification to obtain a compound of the formula ##STR6## wherein R, R.sub.2 and R.sub.3 have the above definitions having the same configuration as the compound of formula V or reacting the compound of formula V or Va with an acid agent in an aqueous media to obtain the corresponding compound of formula I with the same configuration as the compound of formula V or Va and optionally treating the latter with a weak base at room temperature to obtain the compound of formula I with a trans configuration which are valuable intermediates for the preparation of esters of cyclopropane carboxylic acid having elevated insecticidal activity.
摘要翻译：一种制备下式的环丙烷羧酸衍生物的方法，其中Z选自-CN，-COOH和-COOR 1，R 1是1至6个碳原子的烷基，R 2和R 3是烷基 1至4个碳原子或与它们所连接的碳原子一起形成3至6个碳原子的碳原子碳原子，包括在弱碱存在下在低温下在溶剂中使下式化合物 >其中Z具有上述定义，R是1至6个碳原子的烷基或一起形成2至3个碳原子的聚亚甲基与下式的砜其中R2和R3具有上述定义，Y是芳族基团，然后进行水处理，得到式IV的化合物，其中Y，R，R 2，R 3和Z具有上述定义，后者在低温下在溶剂中与强碱反应，同时使升温得到t的化合物其中R，R2，R3和Z具有上述反式异构体中更稠的顺式/反式构型的定义，并且当Z是-CN或-COOR1时在后者中与强碱在水性介质中反应然后酸化以得到下式的化合物其中R，R 2和R 3具有与式V化合物相同构型的上述定义，或使式V或Va的化合物与酸剂在水溶液培养基以获得与式V或Va化合物相同构型的相应的式I化合物，并任选地在室温下用弱碱处理后者，得到具有反式构型的式I化合物，其为具有提高的杀虫活性的环丙烷羧酸的酯的制备。

4. 发明授权

US3309383A Process and intermediates for manufacture of 16-oxa steroids 失效
标题翻译：用于制造16-oxa类固醇的方法和中间体
公开(公告)号：US3309383A
公开(公告)日：1967-03-14
申请号：US52810466
申请日：1966-02-17
申请人： SEARLE & CO
发明人： RAPHAEL PAPPO
IPC分类号： C07C62/34 , C07C62/36 , C07D307/60
CPC分类号： C07C62/34 , C07C62/36 , C07C2603/26 , C07D307/60

5. 发明授权

US08541618B2 Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation 有权
公开(公告)号：US08541618B2
公开(公告)日：2013-09-24
申请号：US13035625
申请日：2011-02-25
申请人： Derek B. Lowe , Philip L. Wickens , Xin Ma , Mingbao Zhang , William H. Bullock , Philip D. G. Coish , Ingo A. Mugge , Andreas Stolle , Ming Wang , Yamin Wang , Chengzhi Zhang , Hai-Jun Zhang , Lei Zhu , Manami Tsutsumi , James N. Livingston
发明人： Derek B. Lowe , Philip L. Wickens , Xin Ma , Mingbao Zhang , William H. Bullock , Philip D. G. Coish , Ingo A. Mugge , Andreas Stolle , Ming Wang , Yamin Wang , Chengzhi Zhang , Hai-Jun Zhang , Lei Zhu , Manami Tsutsumi , James N. Livingston
IPC分类号： C07C59/00 , C07C62/36 , C07C62/38 , C07C65/30 , C07C65/34 , A01N43/76 , A61K31/42
CPC分类号： C07D277/32 , C07B2200/07 , C07C51/412 , C07C51/44 , C07C59/72 , C07C69/732 , C07C69/734 , C07C69/738 , C07C2602/08 , C07D263/32 , C07D277/24 , C07D277/40 , C07D413/04 , C07D413/10 , C07D413/12
摘要： This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.

6. 发明授权

US5344845A Compound and use of the same as medicine 失效
标题翻译：复合和使用与药物相同
公开(公告)号：US5344845A
公开(公告)日：1994-09-06
申请号：US938170
申请日：1992-12-04
申请人： Akihide Koda , Koji Waragai , Yutaka Ono , Hideyuki Ozawa , Hideki Kawamura , Masao Maruno , Takeshi Wakamatsu
发明人： Akihide Koda , Koji Waragai , Yutaka Ono , Hideyuki Ozawa , Hideki Kawamura , Masao Maruno , Takeshi Wakamatsu
IPC分类号： A61K31/12 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/357 , A61K31/36 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4468 , A61K31/454 , A61P37/08 , C07C62/04 , C07C62/20 , C07C62/24 , C07C62/30 , C07C62/34 , C07C62/36 , C07C62/38 , C07C69/734 , C07C233/09 , C07C233/40 , C07C233/78 , C07C235/34 , C07C235/36 , C07C235/54 , C07C237/20 , C07C237/22 , C07C271/22 , C07C323/25 , C07D211/16 , C07D211/58 , C07D211/62 , C07D233/54 , C07D233/60 , C07D233/70 , C07D233/88 , C07D235/06 , C07D295/092 , C07D295/185 , C07D295/22 , C07D309/12 , C07D317/60 , C07D401/12 , C07D405/12 , C07D407/12 , C07D493/08 , C07D521/00 , A61K31/495 , C07D213/75 , C07C103/82
CPC分类号： C07D233/56 , C07C233/40 , C07C233/78 , C07C235/34 , C07C235/36 , C07C235/54 , C07C237/20 , C07C237/22 , C07C271/22 , C07C323/25 , C07C62/04 , C07C62/20 , C07C62/24 , C07C62/30 , C07C62/34 , C07C62/36 , C07C62/38 , C07C69/734 , C07D211/58 , C07D211/62 , C07D231/12 , C07D249/08 , C07D295/088 , C07D295/185 , C07D309/12 , C07D317/60 , C07D493/08 , C07C2101/08 , C07C2101/14 , C07C2102/22
摘要： Disclosed herein is a specific cinnamic acid derivative such as methyl 4-(4-acetoxy-3-methoxycinnamanide)-1-cyclohexanecarboxylate, or a pharmaceutically acceptable salt thereof. These compounds are useful as IV-type allergic reaction-suppressive drugs.
摘要翻译： PCT No.PCT / JP92 / 00451 Sec。 371日期1992年12月4日第 102（e）日期1992年12月4日PCT提交1992年4月10日PCT公布。 WO92 / 18463 PCT出版物 1992年10月29日的日期。本文公开了特定的肉桂酸衍生物，例如4-（4-乙酰氧基-3-甲氧基肉桂酸）-1-环己烷羧酸甲酯或其药学上可接受的盐。这些化合物可用作IV型过敏反应抑制药物。

7. 发明授权

US5077309A Prostaglandins 失效
公开(公告)号：US5077309A
公开(公告)日：1991-12-31
申请号：US501358
申请日：1990-03-28
申请人： Robert L. Jones , Norman H. Wilson
发明人： Robert L. Jones , Norman H. Wilson
IPC分类号： C07C59/80 , C07C62/34 , C07C62/36 , C07C405/00 , C07D493/08
CPC分类号： C07D493/08 , C07C405/0041 , C07C405/0091 , C07C59/80 , C07C62/34 , C07C62/36
摘要： Novel compounds have the formula (I) ##STR1## where ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)-NV'R, respectively; R.sup.1 is a group --(CH.sub.2).sub.b --(A).sub.a --(CH.sub.2).sub.c --B--CH.sub.2 --CO.sub.2 R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO.sub.2 R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --OR.sup.3, --OR.sup.4, --D--R.sup.3, --N.dbd. R.sup.5 or --NW.G.W' in which D is --NH, --NH,CS--, --NH.CO--, --NH.CO.CH.sub.2 N(R.sup.6)--, --NH.SO.sub.2 --, --NH.CO.NH--, --NH.CS.NH--, --NH.CO.O-- or --NH.CS.O--, G is --CO-- or --CS-- and W and W' together are a group --(CH.sub.2).sub.d -- in which d is 3, 4, or 5, R.sup.3 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by one or more aromatic groups directly or through an oxygen or sulphur atom, R.sup.4 is an aliphatic hydrocarbon group which is substituted through an oxygen atom by an aliphatic hydrocarbon group which is itself substituted directly by one or more aromatic groups, R.sup.5 is an aliphatic hydrocarbon group, and aromatic group in which the .pi.-electron system is not fully delocalized over the entire ring system, or aliphatic hydrocarbon group substituted by one or more aromatic groups directly or through an oxygen or sulphur atom, and R.sup.6 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by one or more aromatic groups directly or through an oxygen or sulphur atom. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

8. 发明授权

US4596823A Prostaglandins 失效
公开(公告)号：US4596823A
公开(公告)日：1986-06-24
申请号：US349084
申请日：1982-02-12
申请人： Robert L. Jones , Norman H. Wilson
发明人： Robert L. Jones , Norman H. Wilson
IPC分类号： A61K31/16 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/27 , A61K31/34 , A61K31/343 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/4406 , A61K31/557 , A61P7/02 , A61P9/08 , A61P11/08 , A61P29/00 , A61P37/08 , A61P43/00 , C07C33/05 , C07C45/30 , C07C45/44 , C07C47/225 , C07C47/47 , C07C57/26 , C07C59/11 , C07C59/147 , C07C59/205 , C07C59/46 , C07C59/74 , C07C59/80 , C07C62/16 , C07C62/22 , C07C62/36 , C07C62/38 , C07C67/00 , C07C69/66 , C07C69/73 , C07C69/732 , C07C231/00 , C07C235/40 , C07C235/82 , C07C251/18 , C07C251/42 , C07C251/54 , C07C251/82 , C07C251/88 , C07C281/06 , C07C281/10 , C07C313/00 , C07C323/47 , C07C323/48 , C07C323/53 , C07C323/55 , C07C335/04 , C07C401/00 , C07C403/00 , C07C405/00 , C07D213/75 , C07D263/58 , C07D277/82 , C07D307/935 , C07D493/08 , C07C177/00
CPC分类号： C07D493/08 , C07C251/72 , C07C403/20 , C07C405/0041 , C07C405/0066 , C07C405/0091 , C07C45/305 , C07C45/44 , C07C47/225 , C07C47/47 , C07C57/26 , C07C2101/16
摘要： Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo[2,2,1]hept-2Z-ene, bicyclo[2,2,1]heptane, 7-oxabicyclo[2,2,1]hept-2Z-ene, 7-oxabicyclo[2,2,1]heptane, bicyclo[2,2,2]oct-2Z-ene or bicyclo[2,2,2]octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group C(R.sup.2).dbd.NR, a 6,6-dimethyl-bicyclo[3,1,1]heptane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group C(R.sup.2).dbd.NR or at the 5-position by the group C(R.sup.2).dbd.NR and at the 6-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group C(R.sup.2).dbd.NR, or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group C(R.sup.2).dbd.NR, R.sup.1 is a 6-caboxyhex-2-enyl group or a modification thereof as defined herein, R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R is a group --OR.sup.3, --OR.sup.4, --A--R.sup.3 or -- N.dbd.R.sup.5 in which A is --NH--, --NH.CO--, --NH.CO.CH.sub.2 N(R.sup.6)--, --NH.SO.sub.2 --, --NH.CO.NH or --NH.CS.NH-- and wherein R.sup.3 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, R.sup.4 is an aliphatic hydrocarbon group which is substituted through an oxygen atom ay an aliphatic hydrocarbon group which is itself substituted by an aromatic group, R.sup.5 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R.sup.6 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, with the proviso that when R is a group --OR.sup.3, --NH.COR.sup.3 or --NH.CO.NHR.sup.3 then ##STR3## excludes bicyclo[2,2,1]hept-2Z-enes and bicyclo[2,2,1]heptanes. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

9. 发明授权

US4349481A Tritiated gibberellin aldehydes 失效
标题翻译：氚化赤霉素醛
公开(公告)号：US4349481A
公开(公告)日：1982-09-14
申请号：US24780
申请日：1979-10-15
申请人： Manfred Lischewski , Habil G. Adam , Edward P. Serebryakov
发明人： Manfred Lischewski , Habil G. Adam , Edward P. Serebryakov
IPC分类号： C07C62/32 , C07C62/36 , C07D307/93 , G01N33/60 , C07D307/00
CPC分类号： C07C62/36 , C07C62/32 , C07D307/93
摘要： Is the objective of the invention to develop a process for the production of tagged gibberellin-(7)-aldehydes which is of general applicability. As per the invention a gibberellin-(7)-aldehyde is converted into the gibberellin-(7)-aldehyde tagged at the C-15 position of the basic gibberellin skeleton under the influences of ultraviolet radiation, in given cases after the isolation of a developing 7-Hydroxy-7,15-cyclo butane derivative, and in the presence of compounds with tritium or deuterium donor properties respectively. The process is of particular suitability for the tagging of alkali-sensitive gibberellin-(7)-aldehydes. The tagged gibberellin-(7)-aldehydes produced by the process as per invention, are of importance for instance as primary materials for the obtaining of tagged natural gibberellins and their derivatives.
摘要翻译：本发明的目的是开发生产具有一般适用性的标记的赤霉素 - （7） - 醛的方法。根据本发明，在紫外线辐射的影响下，将赤霉素 - （7） - 醛转变成在碱性赤霉素骨架的C-15位置标记的赤霉素 - （7）显影7-羟基-7,15-环丁烷衍生物，并分别在具有氚或氘供体性质的化合物存在下进行。该方法特别适用于标记碱敏感的赤霉素 - （7） - 醛。通过本发明方法生产的标记的赤霉素 - （7） - 醛是例如作为获得标记天然赤霉素及其衍生物的主要材料的重要手段。

10. 发明申请

US20190382330A1 NOVEL ESTER COMPOUND AND PIN1 INHIBITOR, INFLAMMATORY DISEASE THERAPEUTIC, AND COLON CANCER THERAPEUTIC IN WHICH SAID ESTER COMPOUND IS USED 审中-公开
公开(公告)号：US20190382330A1
公开(公告)日：2019-12-19
申请号：US16464034
申请日：2017-11-29
申请人： Hiroshima University , Tokyo University of Pharmacy & Life Sciences , The University of Tokyo
发明人： Tomoichiro Asano , Yusuke Nakatsu , Hisanaka Ito , Takayoshi Okabe
IPC分类号： C07C65/30 , A61P35/00 , A61P1/16 , A61P1/04 , A61K9/00 , C07C65/40 , C07C62/36 , C07D307/68 , C07C59/74 , C07D265/38 , C07D209/86 , C07D209/08 , C07C229/56 , C07C229/16
摘要： An object of the present invention is to develop a therapeutic agent for an inflammatory disease such as an inflammatory bowel disease or NASH, which therapeutic agent shows less side effects and high effectiveness. The present invention provides a compound represented by Formula (I) or a salt thereof; and a Pin1 inhibitor, a pharmaceutical composition, a therapeutic agent or a prophylactic agent for an inflammatory disease, and a therapeutic agent or a prophylactic agent for colon cancer, containing the compound.

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