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11. 发明申请

US20060241154A1 Benzotropolone derivatives and modulation of inflammatory response 失效
公开(公告)号：US20060241154A1
公开(公告)日：2006-10-26
申请号：US11473821
申请日：2006-06-23
申请人： Chi-Tang Ho , Geetha Ghai , Shengmin Sang , Jin-Woo Jhoo , Mou-Tuan Huang , Robert Rosen , Slavik Dushenkov
发明人： Chi-Tang Ho , Geetha Ghai , Shengmin Sang , Jin-Woo Jhoo , Mou-Tuan Huang , Robert Rosen , Slavik Dushenkov
IPC分类号： A61K31/44 , A61K31/40 , A61K31/381 , C07D333/24 , C07C69/76 , C07C69/88
CPC分类号： C07C69/017 , C07C49/747 , C07C49/753 , C07C59/90 , C07C62/38 , C07C69/738 , C07C69/757 , C07C2601/14 , C07C2602/12 , C07D311/58 , C07D311/62
摘要： The present invention provides novel benzotropolone derivatives represented by the general formula: including neotheaflavate B and EGCGCa. The benzotropolone derivatives of the present invention are effective antioxidant and anti-inflammatory agents. The present invention also provides novel method of synthesizing benzotropolone compounds in high yields and method of treating inflammatory conditions using benzotropolone containing compounds.

12. 发明授权

US07105471B2 Arylphenyl-substituted cyclic ketoenols 失效
标题翻译：芳基苯基取代的环酮酮
公开(公告)号：US07105471B2
公开(公告)日：2006-09-12
申请号：US10777528
申请日：2004-02-12
申请人： Folker Lieb , Reiner Fischer , Alan Graff , Udo Schneider , Thomas Bretschneider , Christoph Erdelen , Wolfram Andersch , Mark-Wilhelm Drewes , Markus Dollinger , Ingo Wetcholowsky , Randy Allen Myers
发明人： Folker Lieb , Reiner Fischer , Alan Graff , Udo Schneider , Thomas Bretschneider , Christoph Erdelen , Wolfram Andersch , Mark-Wilhelm Drewes , Markus Dollinger , Ingo Wetcholowsky , Randy Allen Myers
IPC分类号： C07D401/04 , A01N43/56
CPC分类号： A01N43/36 , C07C45/673 , C07C45/68 , C07C49/747 , C07C57/58 , C07C57/72 , C07C57/76 , C07C59/88 , C07C62/38 , C07C69/013 , C07C69/24 , C07C69/65 , C07C69/67 , C07C69/738 , C07C69/757 , C07C69/96 , C07C211/47 , C07C233/51 , C07C233/52 , C07C255/29 , C07C323/61 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/50 , C07D207/38 , C07D209/96 , C07D307/60 , C07D307/94 , C07D311/74 , C07D333/50 , C07D401/12 , C07D405/04 , C07D491/10 , C07D493/10
摘要： The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.
摘要翻译：本发明涉及式（I）的新型芳基苯基取代的环酮酮，其中X表示卤素，烷基，烷氧基，烯氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，卤代烷基，卤代烷氧基，卤代烯基氧基，硝基，氰基或在各种情况下任选取代苯基，苯氧基，苯硫基，苯基烷氧基或苯基烷硫基，Y代表各自为任选取代的环烷基，芳基或杂芳基，Z表示氢，卤素，烷基，烷氧基，烯氧基，卤代烷基，卤代烷氧基，卤代烯氧基，硝基或氰基，CKE代表其中A，B，D，G和Q 1至Q 6的基团各自如说明书中所定义，涉及多种制备方法及其用途作为农药和除草剂。

13. 发明申请

US20020188136A1 Arylphenyl-substituted cyclic ketoenols 有权
标题翻译：芳基苯基取代的环酮酮
公开(公告)号：US20020188136A1
公开(公告)日：2002-12-12
申请号：US10137763
申请日：2002-05-02
发明人： Folker Lieb , Reiner Fischer , Alan Graff , Udo Schneider , Thomas Bretschneider , Christoph Erdelen , Wolfram Andersch , Mark-Wilhelm Drewes , Markus Dollinger , Ingo Wetcholowsky , Randy Allen Myers
IPC分类号： C07D333/34 , C07D307/56 , C07D231/50 , C07D207/273
CPC分类号： A01N43/36 , C07C45/673 , C07C45/68 , C07C49/747 , C07C57/58 , C07C57/72 , C07C57/76 , C07C59/88 , C07C62/38 , C07C69/013 , C07C69/24 , C07C69/65 , C07C69/67 , C07C69/738 , C07C69/757 , C07C69/96 , C07C211/47 , C07C233/51 , C07C233/52 , C07C255/29 , C07C323/61 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/50 , C07D207/38 , C07D209/96 , C07D307/60 , C07D307/94 , C07D311/74 , C07D333/50 , C07D401/12 , C07D405/04 , C07D491/10 , C07D493/10
摘要： The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) 1 in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups 2 nullin which A, B. D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.
摘要翻译：本发明涉及式（I）的新型芳基苯基取代的环酮酮，其中X表示卤素，烷基，烷氧基，烯氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，卤代烷基，卤代烷氧基，卤代烯基氧基，硝基，氰基或在各种情况下任选取代苯基，苯氧基，苯硫基，苯基烷氧基或苯基烷硫基，Y代表各自为任选取代的环烷基，芳基或杂芳基，Z表示氢，卤素，烷基，烷氧基，烯氧基，卤代烷基，卤代烷氧基，卤代烯氧基，硝基或氰基，CKE代表其中A，B，D，G和Q1至Q6各自如本说明书所定义，其多个制备方法及其作为农药和除草剂的用途。

14. 发明授权

US06465221B1 Method of producing a taxane-type diterpene 有权
标题翻译：紫杉烷类双萜的制备方法
公开(公告)号：US06465221B1
公开(公告)日：2002-10-15
申请号：US08562517
申请日：2001-03-19
申请人： Yukihito Yukimune , Yasuhiro Hara , Hiroaki Tan , Ikuo Tomino
发明人： Yukihito Yukimune , Yasuhiro Hara , Hiroaki Tan , Ikuo Tomino
IPC分类号： C12P1702
CPC分类号： C07C261/04 , C07C62/38 , C07C233/63 , C07C239/18 , C07C251/44 , C07C251/84 , C07C281/12 , C07C2601/08 , C12N5/0025 , C12P17/02
摘要： The present invention relates to a method of producing a taxane-type diterpene wherein a cell and/or a tissue of a plant which produces the taxane-type diterpene is cultured in the presence of at least one substance selected from the group consisting of coronatines, a bacterium which produces the coronatines, a culture solution or a culture extract of such bacterium, cyclic polysaccharides, fatty acids, and an imino or amino derivative of jasmonic acids, then the taxane-type diterpene is recovered from the resulting cultures.
摘要翻译：本发明涉及生产紫杉烷类双萜的方法，其中在选自下组的至少一种物质的存在下培养产生紫杉烷类双萜的植物的细胞和/或组织：冠状病毒，产生该冠状病毒的细菌，这种细菌的培养液或培养物提取物，环状多糖，脂肪酸和茉莉酸的亚氨基或氨基衍生物，然后从得到的培养物中回收紫杉烷型二萜。

15. 发明授权

US5925680A Synthetic excitatory amino acids 失效
标题翻译：合成兴奋性氨基酸
公开(公告)号：US5925680A
公开(公告)日：1999-07-20
申请号：US935737
申请日：1997-09-23
申请人： David R. Helton , James A. Monn , Darryle D. Schoepp , Joseph P. Tizzano
发明人： David R. Helton , James A. Monn , Darryle D. Schoepp , Joseph P. Tizzano
IPC分类号： C07C229/46 , A61K31/00 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/415 , A61P25/00 , A61P25/18 , C07C62/38 , C07C69/74 , C07C69/757 , C07C229/50 , C07D233/78 , C07D235/02 , A61K31/19
CPC分类号： C07D235/02 , A61K31/00 , A61K31/198 , A61K31/215 , C07C229/50 , C07C62/38 , C07C69/757 , C07C2102/18 , Y10S514/81 , Y10S514/811 , Y10S514/812 , Y10S514/813
摘要： The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.
摘要翻译：本发明提供影响某些兴奋性氨基酸受体的新化合物，并且可用于治疗神经障碍和精神障碍。

16. 发明授权

US5750566A Synthetic excitatory amino acids 失效
公开(公告)号：US5750566A
公开(公告)日：1998-05-12
申请号：US496643
申请日：1995-06-29
申请人： James A. Monn , Darryle D. Schoepp
发明人： James A. Monn , Darryle D. Schoepp
IPC分类号： A61K31/00 , A61K31/198 , A61K31/215 , C07C62/38 , C07C229/50 , C07D235/02 , A61K31/21
CPC分类号： C07D235/02 , A61K31/00 , A61K31/198 , A61K31/215 , C07C229/50 , C07C62/38 , C07C2102/18 , Y10S514/81 , Y10S514/811 , Y10S514/812 , Y10S514/813
摘要： The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.

17. 发明授权

US5192817A Phenanthrene derivatives 失效
标题翻译：衍生物衍生物
公开(公告)号：US5192817A
公开(公告)日：1993-03-09
申请号：US775973
申请日：1991-11-05
申请人： Yoshihisa Takaishi , Kiyoto Goto , Takuji Uesako , Toshiko Kuwahara , Masaaki Takai , Yukihisa Ono , Yoshihiro Taniguchi , Sachiko Manabe , Takahiro Asakuni
发明人： Yoshihisa Takaishi , Kiyoto Goto , Takuji Uesako , Toshiko Kuwahara , Masaaki Takai , Yukihisa Ono , Yoshihiro Taniguchi , Sachiko Manabe , Takahiro Asakuni
IPC分类号： C07C49/747 , C07C50/34 , C07C50/38 , C07C62/32 , C07C62/34 , C07C62/38 , C07C69/00 , C07C69/007 , C07C69/013 , C07C69/757 , C07D307/77
CPC分类号： C07D307/77 , C07C49/747 , C07C50/34 , C07C50/38 , C07C62/32 , C07C62/34 , C07C62/38 , C07C69/007 , C07C69/013 , C07C69/757 , C07C2103/26
摘要： Novel phenanthrene derivatives represented by the general formula (1), ##STR1## wherein the group of the formula ##STR2## is a group of the formula ##STR3## (wherein R.sup.1 is a hydrogen atom or a lower alkyl group), a group of the formula ##STR4## (wherein R.sup.2 is a hydrogen atom or a lower alkanoyl group) or a group of the formula ##STR5## (wherein R.sup.2 is the same as defined above), and salts thereof, and other compounds derived therefrom and salts thereof; processes for preparing the same; and interleukin-1 (IL-1) inhibitors containing the abovementioned novel phenanthrene derivatives as to the active ingredient(s).
摘要翻译： PCT No.PCT / JP91 / 00289 Sec。 371日期1991年11月5日 102（e）日期1991年11月5日PCT 1991年3月5日PCT公布。公开号WO91 / 13855 1991年9月19日，由通式（1）表示的新颖的菲衍生物，其中式（IMAGE）的基团是式（IMAGE）的基团（其中R1是氢原子或低级烷基），式（IMAGE）（其中R 2是氢原子或低级烷酰基）或下式的基团（其中R 2与上述定义相同）的基团，以及盐和其衍生的其它化合物及其盐; 制备方法和含有上述新型菲衍生物的白细胞介素-1（IL-1）抑制剂的活性成分。

18. 发明授权

US5177257A Benzocycloalkenecarboxylic acid and process for its preparation 失效
标题翻译：苯并二恶唑酸及其制备方法
公开(公告)号：US5177257A
公开(公告)日：1993-01-05
申请号：US776385
申请日：1991-11-20
申请人： Andreas von Sprecher , Hansjurg Wetter
发明人： Andreas von Sprecher , Hansjurg Wetter
IPC分类号： A61K31/19 , A61P29/00 , A61P43/00 , C07B57/00 , C07C51/487 , C07C62/38
CPC分类号： C07C62/38 , C07C51/487
摘要： The novel (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic i.e. the compound of the formula ##STR1## in free form or in salt form, can be used as active ingredient in pharmaceutical preparations and can be prepared by a novel process, which is characterized in that racemic 4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid is reacted at elevated temperature with at least the equimolar amount of quinine in an alcoholic solvent for from approximately 6 to approximately 48 hours, the quinine salt of the (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid, precipitated in crystalline form as the direct reaction product, is separated from the reaction mixture, and the (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid is set free from this salt by acid treatment in a customary manner, and, if desired, this free acid is converted into a salt.
摘要翻译： PCT No.PCT / CH91 / 00064 Sec。 371日期1991年11月20日 102（e）1991年11月20日日期PCT 1991年3月19日PCT公布。 WO91 / 14671 PCT出版物日期为1991年10月3日。新型（S）-4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸，即游离形式或盐形式的式（I）化合物，可以用作药物制剂中的活性成分，并且可以通过一种新的方法制备，其特征在于外消旋的4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸在升高的温度下至少与在酒精溶剂中等摩尔量的奎宁约6至约48小时，（S）-4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸的奎宁盐以晶体形式沉淀作为直接反应产物，与反应混合物分离，并以常规方式通过酸处理使（S）-4-（2-溴苯甲酰基）-5-羟基 - 苯并环丁烯-1-羧酸不含该盐，如果需要，将该游离酸转化成盐。

19. 发明授权

US5049562A 17.beta.-acyl-4-aza-5.alpha.-androst-1-ene-3-ones as 5.alpha.-reductase inhibitors 失效
标题翻译： 17β-酰基-4-氮杂-5α-雄甾-1-烯-3-酮作为5α-还原酶抑制剂
公开(公告)号：US5049562A
公开(公告)日：1991-09-17
申请号：US396184
申请日：1989-08-21
申请人： Gary H. Rasmusson , Glenn F. Reynolds
发明人： Gary H. Rasmusson , Glenn F. Reynolds
IPC分类号： A61K31/56 , C07C62/38 , C07J73/00
CPC分类号： C07C62/38 , C07J73/005 , C07C2103/16
摘要： 17.beta.-Acyl-4-aza-5.alpha.-androst-1-ene-3-ones of the formula ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR.sup.2 is monocyclic aryl optionally containing 1 or more lower alkyl substituents of from 1-2 carbon atoms and/or 1 or more halo (Cl or Br) substituents;and R', R" and R'" are each selected from hydrogen and methyl and pharmaceutical formulation of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful for treatment of acne, seborrhea, female hirsutism, androgenic alopecia, prostatic carcinoma and benign prostatic hypertrophy.
摘要翻译： 17β-丙基-4-氮杂-5α-雄甾-1-烯-3-酮其中R选自氢，甲基和乙基，R 2是任选含有一个或多个低级烷基的单环芳基 1-2个碳原子和/或1个或更多个卤素（Cl或Br）取代基的取代基; 和R'，R“和R”'分别选自氢和甲基，并且上述化合物的药物制剂作为睾酮5α-还原酶抑制剂是有活性的，因此可用于治疗痤疮，皮脂溢，雌性多毛症，雄激素脱发，前列腺癌和良性前列腺肥大。

20. 发明授权

US4916147A 3-[(4-Aroyl) phenoxy (or phenylthio)]-cyclopentanecarboxylic acid analogues and treatment of cerebral edema therewith 失效
标题翻译： 3 - [（4-芳酰基）苯氧基（或苯硫基）] - 环戊烷羧酸类似物，并用其治疗脑水肿
公开(公告)号：US4916147A
公开(公告)日：1990-04-10
申请号：US887772
申请日：1986-06-21
申请人： Katsuhiro Imaki , Tadao Okegawa , Yoshinobu Arai
发明人： Katsuhiro Imaki , Tadao Okegawa , Yoshinobu Arai
IPC分类号： C07C62/08 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/41 , A61P3/00 , A61P7/10 , A61P43/00 , C07C45/29 , C07C45/46 , C07C45/67 , C07C49/84 , C07C51/00 , C07C51/09 , C07C62/38 , C07C67/00 , C07C69/757 , C07C201/00 , C07C205/45 , C07C231/00 , C07C231/12 , C07C235/46 , C07C235/66 , C07C313/00 , C07C323/61 , C07D257/04 , C07D307/46 , C07D333/16 , C07D333/22 , C07D333/56
CPC分类号： C07D257/04 , C07C205/45 , C07C45/292 , C07C45/46 , C07C45/673 , C07C49/84 , C07C62/38 , C07D307/46 , C07D333/22 , C07D333/56
摘要： Novel compounds of the general formula: ##STR1## [wherein X represents an oxygen atom or sulfur atom, R.sup.1, R.sup.2 and R.sup.3 represent a hydrogen atom, a halogen atom or an alkyl group of from 1 to 4 carbon atom(s) independently or a formula: R.sup.3' ##STR2## (wherein R.sup.3' represents a hydrogen atom or an alkyl group of from 1 to 4 carbon(s))in place of a formula: ##STR3## R.sup.4 represents a general formula: ##STR4## or --N(R.sup.9).sub.2 (in which W represents an oxygen atom or sulfur atom, R.sup.6, R.sup.7 and R.sup.8 represent a hydrogen atom, a halogen atom, a nitro group, an alkyl group of from 1 to 4 carbon atom(s), a hydroxy group or an alkoxy group of from 1 to 4 carbon atom(s) independently, each of R.sup.9 represents a hydrogen atom, an alkyl group of from 1 to 4 carbon atom(s) or a phenyl group and Y represents a single bond or an alkylene group or an alkenylene group of from 1 to 4 carbon atom(s).), and R.sup.5 represents a 5-tetrazolyl group or a general formula: --COOR.sup.10 (in which R.sup.10 represents a hydrogen atom or an alkyl group of from 1 to 4 carbon atom(s))]and non-toxic salts possess inhibitory effect on cerebral edema.
摘要翻译：新颖的通式化合物：其中X表示氧原子或硫原子，R1，R2和R3表示氢原子，卤素原子或1-4个碳原子的烷基（s ）或其分子式：R 3'（其中R 3'表示氢原子或1至4个碳的烷基）代替下式：R 4表示以下通式：

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