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1. 发明授权

US5354767A Renin inhibiting polyhydroxy-monoamides 失效
标题翻译：肾素抑制多羟基 - 单酰胺
公开(公告)号：US5354767A
公开(公告)日：1994-10-11
申请号：US990779
申请日：1992-12-10
申请人： Paul C. Anderson , Gary W. Bantle , Grace L. Jung , Pierre Lavallee , Bruno Simoneau
发明人： Paul C. Anderson , Gary W. Bantle , Grace L. Jung , Pierre Lavallee , Bruno Simoneau
IPC分类号： C07C235/08 , C07C235/26 , C07C235/34 , C07D233/54 , C07D233/88 , C07D277/36 , C07D307/58 , A61K31/16
CPC分类号： C07D233/64 , C07C235/08 , C07C235/26 , C07C235/34 , C07D233/88 , C07D277/36 , C07D307/58 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要： Disclosed herein are compounds of the formula:R.sup.1 CH.sub.2 CH(X)CH(Y)CH(Z)CHR.sup.2 C(O)NHCHR.sup.3 CH(OH)CH(OH)R.sup.4wherein R.sup.1 is a terminal unit, for example lower cycloalkyl or phenyl; R.sup.2 is, for example, an optionally substituted alkyl, cycloalkylmethyl, benzyl, 4-imidazolylmethyl, 2-thienylmethyl or 4-thiazolylmethyl; R.sup.3 is alkyl, cycloalkylmethyl or an optionally substituted benzyl; R.sup.4 is alkyl or cycloalkyl; and X and Y each is hydroxy and Z is hydrogen, or X and Z each is hydroxy and Y is hydrogen; with the provisos that (a) the carbon atom bearing R.sup.2 has the "R" configuration except when R.sup.2 is 2-thienylmethyl or 2-thiazolylmethyl, X and Y each is hydroxy and Z is hydrogen, then the carbon atom bearing R.sup.2 has the "S" configuration; (b) the carbon atoms bearing R.sup.3 and R.sup.4 each has the "S" configuration; and (c) the carbon atom located between the last-said two carbon atoms has the "R" configuration. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.
摘要翻译：本文公开的是下式的化合物：R1CH2CH（X）CH（Y）CH（Z）CHR2C（O）NHCHR3CH（OH）CH（OH）R4其中R1是末端单元，例如低级环烷基或苯基; R2是例如任选取代的烷基，环烷基甲基，苄基，4-咪唑基甲基，2-噻吩基甲基或4-噻唑基甲基; R3是烷基，环烷基甲基或任选取代的苄基; R4是烷基或环烷基; X和Y各自为羟基，Z为氢，或X和Z各自为羟基，Y为氢; 条件是（a）带有R2的碳原子具有“R”构型，除非R2是2-噻吩基甲基或2-噻唑基甲基，X和Y各自为羟基，Z为氢，则带有R2的碳原子具有“ S“配置; （b）含有R 3和R 4的碳原子各自具有“S”构型; 和（c）位于最后所述两个碳原子之间的碳原子具有“R”构型。该化合物抑制肾素活性，并被指示用于治疗高血压和充血性心力衰竭。

2. 发明授权

US5554634A N-(hydroxyethyl)butanediamide derivatives 失效
标题翻译： N-（羟乙基）丁二酰胺衍生物
公开(公告)号：US5554634A
公开(公告)日：1996-09-10
申请号：US432503
申请日：1995-05-01
申请人： Paul C. Anderson , Teddy Halmos , Grace L. Jung , Marc-Andr e Poupart , Bruno Simoneau
发明人： Paul C. Anderson , Teddy Halmos , Grace L. Jung , Marc-Andr e Poupart , Bruno Simoneau
IPC分类号： A61K31/16 , A61K31/165 , A61K31/40 , A61K31/4015 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61P9/12 , A61P43/00 , C07C233/18 , C07C233/19 , C07C237/22 , C07D207/26 , C07D207/27 , C07D213/40 , C07D233/54 , C07D233/64 , C07D277/28 , C07D277/30 , C07D277/40 , C07D317/58 , C07D417/12 , A61K31/425 , C07D277/38
CPC分类号： C07D207/27 , C07C233/18 , C07C233/19 , C07D213/40 , C07D233/64 , C07D277/30 , C07D277/40 , C07D317/58 , C07C2101/02 , C07C2101/14
摘要： Disclosed herein are compounds of the formula:A'--N(R.sup.1')c(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A' is HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1' is R.sup.7 R.sup.8 NC(O)CH.sub.2 wherein R.sup.7 hydrogen or lower alkyl and R.sup.8 is lower alkyl; R.sup.2 is, for example, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.
摘要翻译：本文公开的是下式的化合物：A'-N（R 1'）c（O）CH 2 CHR 2 C（O）-B，其中A'是HO-CR 5（R 6）CH 2，其中R 5和R 6与它们所连接的碳原子一起形成1,1-（低级环烷二基）; R 1'为R 7 R 8 NC（O）CH 2，其中R 7为氢或低级烷基，且R 8为低级烷基; R2是例如4-噻唑基甲基或（2-氨基-4-噻唑基）甲基; B是肾素底物过渡态模拟物，例如[1（S） - （环己基甲基）-2（R），3（S） - 二羟基-5-甲基己基]氨基。该化合物抑制肾素活性，并被指示用于治疗高血压和充血性心力衰竭。

3. 发明授权

US5523315A N-(hydroxyethyl)butanediamide derivatives 失效
标题翻译： N-（羟乙基）丁二酰胺衍生物
公开(公告)号：US5523315A
公开(公告)日：1996-06-04
申请号：US123954
申请日：1993-09-20
申请人： Paul C. Anderson , Teddy Halmos , Grace L. Jung , Marc-Andre Poupart , Bruno Simoneau
发明人： Paul C. Anderson , Teddy Halmos , Grace L. Jung , Marc-Andre Poupart , Bruno Simoneau
IPC分类号： A61K31/16 , A61K31/165 , A61K31/40 , A61K31/4015 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61P9/12 , A61P43/00 , C07C233/18 , C07C233/19 , C07C237/22 , C07D207/26 , C07D207/27 , C07D213/40 , C07D233/54 , C07D233/64 , C07D277/28 , C07D277/30 , C07D277/40 , C07D317/58 , C07D417/12 , A61K31/425 , C07D277/38
CPC分类号： C07D207/27 , C07C233/18 , C07C233/19 , C07D213/40 , C07D233/64 , C07D277/30 , C07D277/40 , C07D317/58 , C07C2101/02 , C07C2101/14
摘要： Disclosed herein are compounds of the formula:A--N(R.sup.1)C(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A is various oxygen-bearing radicals; for example, HO--CH(R.sup.3)CH.sub.2 wherein R.sup.3 is, inter alia, hydrogen, lower alkyl, lower cycloalkyl or phenyl; or HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein each of R.sup.5 and R.sup.6 is lower alkyl, or R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R.sup.2 is, for example, cyclo-alkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.
摘要翻译：本文公开的是下式的化合物：A-N（R 1）C（O）CH 2 CHR 2 C（O）-B，其中A是各种含氧基团; 例如，HO-CH（R3）CH2，其中R3尤其是氢，低级烷基，低级环烷基或苯基; 或HO-CR 5（R 6）CH 2，其中R 5和R 6各自为低级烷基，或者R 5和R 6与它们所连接的碳原子一起形成1,1-（低级环烷二基）; R1是例如苄基，烷基或取代的烷基，例如环己基甲基; R2是例如环烷基甲基，1H-咪唑-4-基甲基，4-噻唑基甲基或（2-氨基-4-噻唑基）甲基; B是肾素底物过渡态模拟物，例如[1（S） - （环己基甲基）-2（R），3（S） - 二羟基-5-甲基己基]氨基。该化合物抑制肾素活性，并被指示用于治疗高血压和充血性心力衰竭。

4. 发明授权

US5565476A N-(hydroxyethyl)butanediamide derivatives 失效
标题翻译： N-（羟乙基）丁二酰胺衍生物
公开(公告)号：US5565476A
公开(公告)日：1996-10-15
申请号：US432409
申请日：1995-05-01
申请人： Paul C. Anderson , Teddy Halmos , Grace L. Jung , Marc-Andr e Poupart , Bruno Simoneau
发明人： Paul C. Anderson , Teddy Halmos , Grace L. Jung , Marc-Andr e Poupart , Bruno Simoneau
IPC分类号： A61K31/16 , A61K31/165 , A61K31/40 , A61K31/4015 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61P9/12 , A61P43/00 , C07C233/18 , C07C233/19 , C07C237/22 , C07D207/26 , C07D207/27 , C07D213/40 , C07D233/54 , C07D233/64 , C07D277/28 , C07D277/30 , C07D277/40 , C07D317/58 , C07D417/12
CPC分类号： C07D207/27 , C07C233/18 , C07C233/19 , C07D213/40 , C07D233/64 , C07D277/30 , C07D277/40 , C07D317/58 , C07C2101/02 , C07C2101/14
摘要： Disclosed herein are compounds of the formula:A'--N(R.sup.1')C(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A' is, for example, HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1' is R.sup.7 R.sup.8 NC(O)CH.sub.2 wherein R.sup.7 is lower alkyl and R.sup.8 is pyridinyl-(CH.sub.2).sub.n wherein n is the integer one or two; R.sup.2 is, for example, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R), 3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.
摘要翻译：本文公开的是下式的化合物：A'-N（R 1'）C（O）CH 2 CHR 2 C（O）-B，其中A'是例如HO-CR 5（R 6）CH 2，其中R 5和R 6与碳原子它们连接形成1,1-（低级环烷二基）; R 1'是R 7 R 8 NC（O）CH 2，其中R 7是低级烷基，R 8是吡啶基 - （CH 2）n，其中n是整数1或2; R2是例如4-噻唑基甲基或（2-氨基-4-噻唑基）甲基; B是肾素底物过渡态模拟物，例如[1（S） - （环己基甲基）-2（R），3（S） - 二羟基-5-甲基己基]氨基。该化合物抑制肾素活性，并被指示用于治疗高血压和充血性心力衰竭。

5. 发明授权

US5384253A Genetic transformation of maize cells by electroporation of cells pretreated with pectin degrading enzymes 失效
标题翻译：通过用果胶降解酶预处理的细胞的电穿孔来玉米细胞的遗传转化
公开(公告)号：US5384253A
公开(公告)日：1995-01-24
申请号：US635279
申请日：1990-12-28
申请人： Richard A. Krzyzek , Cheryl R. M. Laursen , Paul C. Anderson
发明人： Richard A. Krzyzek , Cheryl R. M. Laursen , Paul C. Anderson
IPC分类号： A01H5/00 , A01H5/10 , C12N5/10 , C12N15/09 , C12N15/82 , C12N15/00 , C12N15/05
CPC分类号： A01H5/10 , C12N15/8206
摘要： The present invention provides a method to increase the susceptibility of cultured Zea mays cells to stable transformation with recombinant DNA via electroporation, by pretreating the Zea mays cells with certain pectin-degrading enzymes, so that the cells retain their ability to regenerate fertile, transgenic Zea mays plants containing the DNA which is also heritable.
摘要翻译：本发明提供了一种通过电穿孔增加培养的玉米鳞状细胞与重组DNA稳定转化的敏感性的方法，通过用某些果胶降解酶预处理玉米鳞状细胞，使得细胞保持其再生可育转基因玉米的能力含有也是可遗传的DNA的植物的植物。

6. 发明授权

US07705215B1 Methods and compositions for the production of stably transformed, fertile monocot plants and cells thereof 失效
标题翻译：用于生产稳定转化的肥沃单子叶植物及其细胞的方法和组合物
公开(公告)号：US07705215B1
公开(公告)日：2010-04-27
申请号：US08113561
申请日：1993-08-25
申请人： Thomas R. Adams , Paul C. Anderson , Sheryl A. Chambers , Paul S. Chomet , Richard J. Daines , Christopher E. Flick , Kimberly Glassman , William J. Gordon-Kamm , Albert P. Kausch , Lucille B. Laccetti , Peggy G. Lemaux , Catherine J. Mackey , Mary Lou Mangano , Michael T. Mann , James V. O'Brien , Emil M. Orozco , Peter Orr , Thomas B. Rice , T. Michael Spencer , William G. Start , Michael A. Stephens , Clayton S. Vetsch , David A. Walters , Donald S. Walters , Nancy G. Willetts , Susan J. Zachwieja
发明人： Thomas R. Adams , Paul C. Anderson , Sheryl A. Chambers , Paul S. Chomet , Richard J. Daines , Christopher E. Flick , Kimberly Glassman , William J. Gordon-Kamm , Albert P. Kausch , Lucille B. Laccetti , Peggy G. Lemaux , Catherine J. Mackey , Mary Lou Mangano , Michael T. Mann , James V. O'Brien , Emil M. Orozco , Peter Orr , Thomas B. Rice , T. Michael Spencer , William G. Start , Michael A. Stephens , Clayton S. Vetsch , David A. Walters , Donald S. Walters , Nancy G. Willetts , Susan J. Zachwieja
IPC分类号： C12N15/82 , C12N5/04 , A01H5/00 , A01H5/10 , C12N15/53 , C12P7/64
CPC分类号： C12N15/8241 , A01H4/00 , A01H4/001 , C07K14/415 , C12N5/0025 , C12N5/04 , C12N9/0006 , C12N9/88 , C12N15/8207 , C12N15/8209 , C12N15/87
摘要： This invention relates to a reproducible system for the production of stable, genetically transformed maize cells, and to methods of selecting cells that have been transformed. One method of selection disclosed employs the Streptomyces bar gene introduced by microprojectile bombardment into embryogenic maize cells which were grown in suspension cultures, followed by exposure to the herbicide bialaphos. The methods of achieving stable transformation disclosed herein include tissue culture methods and media, methods for the bombardment of recipient cells with the desired transforming DNA, and methods of growing fertile plants from the transformed cells. This invention also relates to the transformed cells and seeds and to the fertile plants grown from the transformed cells and to their pollen.
摘要翻译：本发明涉及用于生产稳定的遗传转化的玉米细胞的可再现系统，以及选择已经转化的细胞的方法。公开的一种选择方法使用通过微粒轰击引入的链霉菌棒基因，其在悬浮培养物中生长，然后暴露于除草剂双乙二胺磷的胚发生玉米细胞中。实现本文公开的稳定转化的方法包括组织培养方法和培养基，用所需转化DNA轰击受体细胞的方法，以及从转化细胞生长可育植物的方法。本发明还涉及转化的细胞和种子以及从转化细胞和其花粉生长的可育植物。

7. 发明授权

US07288403B2 Anthranilate synthase gene and method for increasing tryptophan production 失效
标题翻译：邻氨基苯甲酸合酶基因和增加色氨酸生产的方法
公开(公告)号：US07288403B2
公开(公告)日：2007-10-30
申请号：US11196176
申请日：2005-08-03
申请人： Paul C. Anderson , Paul S. Chomet , Matthew C. Griffor , Alan L. Kriz
发明人： Paul C. Anderson , Paul S. Chomet , Matthew C. Griffor , Alan L. Kriz
IPC分类号： C12N1/20 , C12N15/05 , C07H21/04 , A01H1/00 , C12P13/22
CPC分类号： C12N15/8241 , C12N9/0006 , C12N9/88 , C12N15/8207 , C12N15/8209 , C12N15/8216 , C12N15/8251 , C12N15/8254
摘要： The present invention provides a method for conferring tolerance to an amino acid analog of tryptophan to a plant and/or altering the tryptophan content of a plant by introducing and expressing an isolated DNA segment encoding an anthranilate synthase in the cells of the plant. Transgenic plants transformed with an isolated DNA segment encoding an anthranilate synthase, as well as seeds and progeny derived from these plants, are also provided. The present invention also provides a cDNA sequence of an alpha and a beta subunit of a maize anthranilate synthase.
摘要翻译：本发明提供了通过在植物细胞中引入和表达编码邻氨基苯甲酸合酶的分离的DNA区段来赋予植物对色氨酸的氨基酸类似物的耐受性和/或改变植物的色氨酸含量的方法。还提供了用编码邻氨基苯甲酸合酶的分离的DNA区转化的转基因植物，以及源自这些植物的种子和后代。本发明还提供了玉米邻氨基苯甲酸合酶的α和β亚基的cDNA序列。

8. 发明授权

US06399861B1 Methods and compositions for the production of stably transformed, fertile monocot plants and cells thereof 失效
标题翻译：用于生产稳定转化的肥沃单子叶植物及其细胞的方法和组合物
公开(公告)号：US06399861B1
公开(公告)日：2002-06-04
申请号：US08447985
申请日：1995-05-23
申请人： Paul C. Anderson , Christopher E. Flick , William J. Gordon-Kamm , Albert P. Kausch , Catherine J. Mackey , Emil M. Orozco , Peter Orr , Michael A. Stephens , David A. Walters , Donald S. Walters
发明人： Paul C. Anderson , Christopher E. Flick , William J. Gordon-Kamm , Albert P. Kausch , Catherine J. Mackey , Emil M. Orozco , Peter Orr , Michael A. Stephens , David A. Walters , Donald S. Walters
IPC分类号： A01H500
CPC分类号： C12N15/8241 , A01H4/00 , A01H4/001 , C07K14/415 , C12N5/0025 , C12N5/04 , C12N9/0006 , C12N9/88 , C12N15/8207 , C12N15/8209 , C12N15/87
摘要： This invention relates to a reproducible system for the production of stable, genetically transformed maize cells, and to methods of selecting cells that have been transformed. One method of selection disclosed employs the Streptomyces bar gene introduced by microprojectile bombardment into embryogenic maize cells which were grown in suspension cultures, followed by exposure to the herbicide bialaphos. The methods of achieving stable transformation disclosed herein include tissue culture methods and media, methods for the bombardment of recipient cells with the desired transforming DNA, and methods of growing fertile plants from the transformed cells. This invention also relates to the transformed cells and seeds and to the fertile plants grown from the transformed cells and to their pollen.
摘要翻译：本发明涉及用于生产稳定的遗传转化的玉米细胞的可再现系统，以及选择已经转化的细胞的方法。公开的一种选择方法使用通过微粒轰击引入的链霉菌棒基因，其在悬浮培养物中生长，然后暴露于除草剂双乙二胺磷的胚发生玉米细胞中。实现本文公开的稳定转化的方法包括组织培养方法和培养基，用所需转化DNA轰击受体细胞的方法，以及从转化细胞生长可育植物的方法。本发明还涉及转化的细胞和种子以及从转化细胞和其花粉生长的可育植物。

9. 发明授权

US5614533A Substituted pipecolinic acid derivatives as HIV protease inhibitors 失效
标题翻译：取代的哌可酸衍生物作为HIV蛋白酶抑制剂
公开(公告)号：US5614533A
公开(公告)日：1997-03-25
申请号：US336637
申请日：1994-11-09
申请人： Paul C. Anderson , Fran.cedilla.ois Soucy , Christiane Yoakim , Pierre Lavall ee , Pierre L. Beaulieu
发明人： Paul C. Anderson , Fran.cedilla.ois Soucy , Christiane Yoakim , Pierre Lavall ee , Pierre L. Beaulieu
IPC分类号： C07D211/60 , C07D401/12 , C07D401/14 , A61K31/47 , A61K31/505 , A61K31/535 , C07D413/14
CPC分类号： C07D401/12 , C07D211/60 , C07D401/14
摘要： Disclosed herein are compounds of formula 1 ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an optionally mono- or disubstituted carbamoyl; B is absent or an amino acid residue, for example, Val or Ash; R.sup.1 is hydrogen or a ring substituent, for example, fluoro or methyl; R.sup.2 is alkyl; and Y is a ring substituent, for example, phenoxy, 2-pyridinylmethoxy, phenylthio or 2-pyridinylthio. The compounds inhibit the activity of human immunodeficiency virus (HIV) protease and interfere with HIV induced cytopathogenic effects in human cells. These properties render the compounds useful for combating HIV infections.
摘要翻译：本文公开了式1的化合物其中X是末端基团，例如芳氧基羰基，烷酰基或任选的单或二取代的氨基甲酰基; B不存在或氨基酸残基，例如Val或Ash; R1是氢或环取代基，例如氟或甲基; R2是烷基; Y为环取代基，例如苯氧基，2-吡啶基甲氧基，苯硫基或2-吡啶硫基。这些化合物抑制人类免疫缺陷病毒（HIV）蛋白酶的活性，并干扰人体细胞中HIV诱导的致细胞致病作用。这些性质使化合物可用于抗艾滋病毒感染。

10. 发明授权

US5331107A Herbicide resistance in plants 失效
标题翻译：植物除草剂抗性
公开(公告)号：US5331107A
公开(公告)日：1994-07-19
申请号：US169094
申请日：1988-03-08
申请人： Paul C. Anderson , Kenneth A. Hibberd
发明人： Paul C. Anderson , Kenneth A. Hibberd
IPC分类号： A01H1/00 , A01H1/04 , A01H1/06 , A01H5/10 , C12N5/04 , C12N15/01 , C12N15/52 , C12N15/82 , A01H1/02 , C12N15/00
CPC分类号： A01H1/00 , A01H1/04 , A01H1/06 , A01H5/10 , C12N15/01 , C12N15/52 , C12N15/8278 , C12N5/04
摘要： This invention is directed to the production of plants, plant tissues and plant seeds which are resistant to inhibition by an herbicide which normally inhibits the growth and development of those plants, plant tissues and plant seeds. In particular this invention is directed to altered acetohydroxyacid synthase enzymes which are resistant to inhibition by herbicides which normally inhibit the activity of the synthase before such alteration. This invention further relates to genes encoding such enzymes, and to processes for utilizing these novel genes and enzymes. Further products of the invention include plants, plant tissues and seeds which exhibit resistance to such herbicides resulting from expression of genes encoding herbicide resistant acetohydroxyacid synthase enzyme.
摘要翻译：本发明涉及对通常抑制这些植物，植物组织和植物种子的生长和发育的除草剂有抑制作用的植物，植物组织和植物种子的生产。特别地，本发明涉及对通常在这种改变之前抑制合酶的活性的除草剂的抑制作用的改变的乙酰羟酸合酶。本发明还涉及编码这些酶的基因，以及利用这些新基因和酶的方法。本发明的其它产品包括对编码除草剂抗性乙酰羟酸合成酶的基因的表达产生的对这种除草剂具有抗性的植物，植物组织和种子。

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