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1. 发明授权

US08329745B2 Small molecule inhibitors of ghrelin O-acyltransferase 有权
标题翻译：生长素释放肽O-酰基转移酶的小分子抑制剂
公开(公告)号：US08329745B2
公开(公告)日：2012-12-11
申请号：US13226471
申请日：2011-09-06
申请人： Patrcik G. Harran , Michael S. Brown , Joseph L. Goldstein , Jing Yang , Tong-Jin Zhao
发明人： Patrcik G. Harran , Michael S. Brown , Joseph L. Goldstein , Jing Yang , Tong-Jin Zhao
IPC分类号： A61K31/4164 , A61K31/505 , A61K31/27 , A61K31/216 , A61K31/165 , C07D233/60 , C07D239/26 , C07C275/18 , C07C271/22 , C07C235/32
CPC分类号： C07D233/60 , A61K9/146 , A61K31/4166 , A61K31/4172 , A61K31/54 , C07D207/273 , C07D235/16 , C07D239/26 , C07D263/14 , C07D263/32 , C07D291/06 , G01N2333/91188
摘要： Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules of the general formula: Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.
摘要翻译： Ghrelin O-酰基转移酶（GOAT）被设计为通式的小分子抑制：方法包括使GOAT与抑制剂接触并检测所得的抑制作用。

2. 发明授权

US07919613B2 RNAi modulation of SCAP and therapeutic uses thereof 有权
标题翻译： SCAP的RNAi调节及其治疗用途
公开(公告)号：US07919613B2
公开(公告)日：2011-04-05
申请号：US12749159
申请日：2010-03-29
申请人： Juergen Soutschek , Pamela Tan , Jay D. Horton , Michael S. Brown , Joseph L. Goldstein , Young-Ah Moon
发明人： Juergen Soutschek , Pamela Tan , Jay D. Horton , Michael S. Brown , Joseph L. Goldstein , Young-Ah Moon
IPC分类号： C07H21/04 , C07H21/02 , A61K48/00 , C12N15/63 , C12N15/85
CPC分类号： C12N15/113 , C12N2310/14 , C12N2310/314 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/346 , C12N2310/3515 , C12N2310/3521
摘要： The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a SCAP gene (Human SCAP gene), comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of a SCAP gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by Human SCAP expression and the expression of a SCAP gene using the pharmaceutical composition; and methods for inhibiting the expression of a SCAP gene in a cell.
摘要翻译：本发明涉及用于抑制SCAP基因（人SCAP基因）表达的双链核糖核酸（dsRNA），其包含具有长度小于30个核苷酸的核苷酸序列的反义链，通常为19-25个核苷酸长度，并且其与SCAP基因的至少一部分基本上互补。本发明还涉及包含dsRNA与药学上可接受的载体的药物组合物; 用于治疗由人SCAP表达引起的疾病和使用该药物组合物表达SCAP基因的方法; 以及抑制细胞中SCAP基因表达的方法。

3. 发明授权

US5962243A Methods for the identification of farnesyltransferase inhibitors 失效
标题翻译：鉴定法呢基转移酶抑制剂的方法
公开(公告)号：US5962243A
公开(公告)日：1999-10-05
申请号：US429964
申请日：1995-04-27
申请人： Michael S. Brown , Joseph L. Goldstein , Guy L. James
发明人： Michael S. Brown , Joseph L. Goldstein , Guy L. James
IPC分类号： A61K38/00 , C07K5/103 , C07K7/06 , C07K14/82 , C12N9/10 , C12Q1/48 , C07H21/04
CPC分类号： C07K5/1013 , C07K14/82 , C07K7/06 , C12N9/1085 , C12Q1/48 , A61K38/00
摘要： Disclosed are methods and compositions for the identification of inhibitors of farnesyltransferase enzymes involved in the prenylation of various cellular proteins, including cancer related ras proteins, such as p21.sup.ras, particularly, K-rasB. Enclosed are procedures for using purified farnesyltransferase enzymes and K-rasB proteins in screening protocols for the identification of possible anticancer agents that inhibit the enzyme and thereby prevent prenylation of proteins such as K-RasB.
摘要翻译：公开了用于鉴定参与各种细胞蛋白（包括癌症相关的ras蛋白，例如p21ras，特别是K-rasB）的异戊烯基化的法呢基转移酶的抑制剂的方法和组合物。包括在筛选方案中使用纯化的法呢基转移酶和K-rasB蛋白的程序，用于鉴定抑制酶的可能的抗癌剂，从而防止诸如K-RasB的蛋白质的异戊二酰化。

4. 发明授权

US5843941A Ras farnesyl transferase inhibitors 失效
标题翻译： Ras法呢基转移酶抑制剂
公开(公告)号：US5843941A
公开(公告)日：1998-12-01
申请号：US313068
申请日：1994-09-26
申请人： James C. Marsters, Jr. , Michael S. Brown , Craig W. Crowley , Joseph L. Goldstein , Guy L. James , Robert S. McDowell , David Oare , Thomas E. Rawson , Mark Reynolds , Todd C. Somers
发明人： James C. Marsters, Jr. , Michael S. Brown , Craig W. Crowley , Joseph L. Goldstein , Guy L. James , Robert S. McDowell , David Oare , Thomas E. Rawson , Mark Reynolds , Todd C. Somers
IPC分类号： A61K31/55 , A61K31/551 , A61K38/00 , A61P31/04 , A61P35/00 , C07D223/16 , C07D243/10 , C07D243/14 , C07D243/24 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D498/04 , C07D513/04 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/083 , C07K5/097 , C07K5/10 , C07K5/103 , C07K5/117
CPC分类号： C07D223/16 , C07D243/10 , C07D243/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D409/14 , C07D487/04 , C07D513/04 , C07K5/0207 , C07K5/0606 , C07K5/06139 , C07K5/06191 , C07K5/081 , C07K5/0821 , C07K5/0827 , C07K5/1013 , C07K5/1024 , C07K5/1027 , A61K38/00
摘要： Benzodiazepine derivatives represented by the structure below are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases foe which inhibition of the ras farnesyl:protein transferase as indicated. ##STR1##
摘要翻译： PCT No.PCT / US94 / 05157 Sec。 371日期：1994年9月26日 102（e）1994年9月26日PCT PCT 1994年5月10日PCT公布。第WO94 / 26723号公报 1994年11月24日公开了由以下结构表示的苯并二氮杂衍生物，其作为法西诺酯：蛋白转移酶的有效抑制剂。提供含有这些苯并二氮杂的药物组合物，用于治疗如所指出的对法拉西蛋白转移酶的抑制作用的疾病。

5. 发明授权

US5532359A Ras farnesyl transferase inhibitors 失效
标题翻译： Ras法呢基转移酶抑制剂
公开(公告)号：US5532359A
公开(公告)日：1996-07-02
申请号：US328595
申请日：1994-10-25
申请人： James C. Marsters, Jr. , Michael S. Brown , Craig W. Crowley , Joseph L. Goldstein , Guy L. James , Robert S. McDowell , David Oare , Thomas E. Rawson , Mark Reynolds , Todd C. Somers
发明人： James C. Marsters, Jr. , Michael S. Brown , Craig W. Crowley , Joseph L. Goldstein , Guy L. James , Robert S. McDowell , David Oare , Thomas E. Rawson , Mark Reynolds , Todd C. Somers
IPC分类号： A61K31/55 , A61K31/551 , A61K38/00 , A61P31/04 , A61P35/00 , C07D223/16 , C07D243/10 , C07D243/14 , C07D243/24 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D498/04 , C07D513/04 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/083 , C07K5/097 , C07K5/10 , C07K5/103 , C07K5/117 , C07D223/18
CPC分类号： C07D223/16 , C07D243/10 , C07D243/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D409/14 , C07D487/04 , C07D513/04 , C07K5/0207 , C07K5/0606 , C07K5/06139 , C07K5/06191 , C07K5/081 , C07K5/0821 , C07K5/0827 , C07K5/1013 , C07K5/1024 , C07K5/1027 , A61K38/00
摘要： Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated. Also disclosed are benzazepines of the following general formula (II) having similar utility as the aforementioned benzodiazepines: ##STR1##
摘要翻译：公开了苯并二氮杂衍生物，其作为法拉第鞭毛蛋白的有效抑制剂：蛋白质转移酶。提供含有这些苯二氮卓类药物的药物组合物，用于治疗对法拉第法：蛋白转移酶的抑制作用的疾病的治疗。还公开了具有与上述苯并二氮杂类似的效用的以下通式（II）的苯并吖庚因：

6. 发明授权

US5498696A Sterol regulatory element binding proteins and their use in screening assays 失效
标题翻译：甾醇调节元件结合蛋白及其在筛选试验中的应用
公开(公告)号：US5498696A
公开(公告)日：1996-03-12
申请号：US61697
申请日：1993-05-13
申请人： Michael R. Briggs , Michael S. Brown , Joseph L. Goldstein , Xiaodong Wang
发明人： Michael R. Briggs , Michael S. Brown , Joseph L. Goldstein , Xiaodong Wang
IPC分类号： C07K14/47 , C12N15/67
CPC分类号： C12N15/67 , C07K14/4702
摘要： A nuclear protein which binds sterol regulatory elements (SREs), such as SRE-1 of the low density lipoprotein (LDL) receptor gene, and mediates sterol-regulated transcription of the LDL receptor gene is disclosed. Also described are screening assay and methods for the identification of agents capable of promoting LDL receptor gene transcription for use in reducing plasma cholesterol and treating the various medical problems associated therewith.
摘要翻译：公开了结合固醇调节元件（SREs）的核蛋白，例如低密度脂蛋白（LDL）受体基因的SRE-1，并介导LDL受体基因的固醇调节的转录。还描述了用于鉴定能够促进LDL受体基因转录用于降低血浆胆固醇并治疗与其相关的各种医学问题的试剂的筛选测定和方法。

7. 发明授权

US5420245A Tetrapeptide-based inhibitors of farnesyl transferase 失效
标题翻译：法呢基转移酶的四肽类抑制剂
公开(公告)号：US5420245A
公开(公告)日：1995-05-30
申请号：US863169
申请日：1992-04-03
申请人： Michael S. Brown , Joseph L. Goldstein , Yuval Reiss
发明人： Michael S. Brown , Joseph L. Goldstein , Yuval Reiss
IPC分类号： A61K38/00 , C07K5/103 , C07K7/06 , C07K14/82 , C12N9/10 , C07K5/00 , C07K7/00
CPC分类号： C07K7/06 , C07K14/82 , C07K5/1013 , C12N9/1085 , A61K38/00
摘要： Disclosed are methods and compositions for the identification, characterization and inhibition of mammalian farnesyl protein transferases, enzymes involved in the farnesylation of various cellular proteins, including cancer related ras proteins such as p21.sup.ras. One farnesyl protein transferase which is disclosed herein exhibits a molecular weight of between about 70,000 and about 100,000 upon gel exclusion chromatography. Also disclosed are methods and compositions for the preparation of farnesyl transferase by recombinant means, following the molecular cloning and co-expression of its two subunits, for assay and purification of the enzyme, as well as procedures for using the purified enzyme in screening protocols for the identification of possible anticancer agents which inhibit the enzyme and thereby prevent expression of proteins such as p21.sup.ras. Also disclosed is a families of compounds which act either as false substrates for the enzyme or as pure inhibitors and can therefore be employed for inhibition of the enzyme. The most potent inhibitors are ones in which phenylalanine occurs at the third position of a tetrapeptide whose amino terminus is cysteine.
摘要翻译：公开了用于鉴定，表征和抑制哺乳动物法尼糖蛋白转移酶的方法和组合物，涉及各种细胞蛋白的法呢基化的酶，包括与癌相关的ras蛋白如p21ras。本文公开的一种法呢基蛋白转移酶在凝胶排阻色谱上显示约70,000至约100,000的分子量。还公开了通过重组方法制备法呢基转移酶的方法和组合物，其分子克隆和其两个亚基的共表达用于酶的测定和纯化，以及在筛选方案中使用纯化酶的程序识别抑制酶的可能的抗癌剂，从而防止蛋白质如p21ras的表达。还公开了作为酶的假底物或纯抑制剂的化合物家族，因此可用于抑制酶。最有效的抑制剂是其氨基末端是半胱氨酸的四肽的第三位发生苯丙氨酸的抑制剂。

8. 发明授权

US5141851A Isolated farnesyl protein transferase enzyme 失效
标题翻译：分离的FARNESYL蛋白转移酶
公开(公告)号：US5141851A
公开(公告)日：1992-08-25
申请号：US615715
申请日：1990-11-20
申请人： Michael S. Brown , Joseph L. Goldstein , Yuval Reiss
发明人： Michael S. Brown , Joseph L. Goldstein , Yuval Reiss
IPC分类号： A61K38/45 , A61K38/00 , A61K38/55 , A61P35/00 , C07K1/107 , C07K1/22 , C07K5/10 , C07K5/103 , C07K5/107 , C07K5/11 , C07K5/117 , C07K7/02 , C07K7/06 , C07K14/00 , C07K14/435 , C07K14/82 , C12N9/10 , C12N9/99 , C12N15/09 , C12N15/54 , C12Q1/48
CPC分类号： C07K7/06 , C07K1/1077 , C07K14/82 , C07K5/1013 , C07K5/1016 , C07K5/1019 , C07K5/1024 , C07K7/02 , C12N9/1085 , A61K38/00 , Y10S435/815
摘要： Disclosed are methods and compositions for the identification, characterization and inhibition of farnesyl protein transferases, enzymes involved in the farnesylation of various cellular proteins, including cancer related ras proteins such as p21.sup.ras. One farnesyl protein transferase which is disclosed herein exhibits a molecular weight of between about 70,000 and about 100,000 upon gel exclusion chromatography. The enzyme appears to comprise one or two subunits of approximately 50 kDa each. Methods are disclosed for assay and purification of the enzyme, as well as procedures for using the purified enzyme in screening protocols for the identification of possible anticancer agents which inhibit the enzyme and thereby prevent expression of proteins such as p21.sup.ras. Also disclosed is a families of compounds which act either as false substrates for the enzyme or as pure inhibitors and can therefore be employed for inhibition of the enzyme. The most potent inhibitors are ones in which phenylalanine occurs at the third position of a tetrapeptide whose amino terminus is cysteine.
摘要翻译：公开了用于鉴定，表征和抑制法呢基蛋白转移酶的方法和组合物，涉及各种细胞蛋白的法呢基化的酶，包括癌相关的ras蛋白如p21ras。本文公开的一种法呢基蛋白转移酶在凝胶排阻色谱上显示约70,000至约100,000的分子量。该酶似乎包含一个或两个约50kDa的亚单位。公开了用于酶的测定和纯化的方法，以及在筛选方案中使用纯化酶鉴定可能的抗癌剂的方法，所述抗癌剂抑制酶，从而阻止诸如p21ras的蛋白质的表达。还公开了作为酶的假底物或纯抑制剂的化合物家族，因此可用于抑制酶。最有效的抑制剂是其氨基末端是半胱氨酸的四肽的第三位发生苯丙氨酸的抑制剂。

9. 发明授权

US4745060A Methods and compositions for the detection of Familial Hypercholesterolemia 失效
标题翻译：用于检测家族性高胆固醇血症的方法和组合物
公开(公告)号：US4745060A
公开(公告)日：1988-05-17
申请号：US687087
申请日：1984-12-28
申请人： Michael S. Brown , Joseph L. Goldstein , David W. Russell
发明人： Michael S. Brown , Joseph L. Goldstein , David W. Russell
IPC分类号： G01N33/50 , C07K14/705 , C12N1/20 , C12N15/00 , C12N15/09 , C12Q1/68 , C12R1/19 , G01N33/566 , G01N33/92 , C07H21/00
CPC分类号： C07K14/705 , C12Q1/6827 , C12Q1/6883 , G01N33/566 , G01N33/92 , C12Q2600/156 , G01N2800/044 , Y10S435/803 , Y10S436/811 , Y10S530/808 , Y10S530/825
摘要： Recombinant DNA transfer vectors containing DNA inserts which are complementary to either the human LDL receptor gene, or its mRNA transcript, are disclosed. Also disclosed are methods which utilize these genetic probes for diagnosing Familial Hypercholesterolemia (FH) in a suspected individual. A case study of one such individual, FH 274, is disclosed wherein the genetic deletion mutation is detailed with great precision through the practice of this invention.
摘要翻译：公开了含有与人LDL受体基因或其mRNA转录物互补的DNA插入片段的重组DNA转移载体。还公开了利用这些遗传探针在怀疑个体中诊断家族性高胆固醇血症（FH）的方法。公开了一种这样的个体FH 274的病例研究，其中遗传缺失突变通过本发明的实践以极高的精度被详细描述。

10. 发明申请

US20100086955A1 Small Molecule Inhibitors of Ghrelin O-Acyltransferase 有权
标题翻译： Ghrelin O-Acyltransferase的小分子抑制剂
公开(公告)号：US20100086955A1
公开(公告)日：2010-04-08
申请号：US12571538
申请日：2009-10-01
申请人： Patrcik G. Harran , Michael S. Brown , Joseph L. Goldstein , Jing Yang , Tong-Jin Zhao
发明人： Patrcik G. Harran , Michael S. Brown , Joseph L. Goldstein , Jing Yang , Tong-Jin Zhao
IPC分类号： C12Q1/48 , C07C69/76 , C07D291/00 , C07D239/02 , C07D235/12
CPC分类号： C07D233/60 , A61K9/146 , A61K31/4166 , A61K31/4172 , A61K31/54 , C07D207/273 , C07D235/16 , C07D239/26 , C07D263/14 , C07D263/32 , C07D291/06 , G01N2333/91188
摘要： Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.
摘要翻译：生长素释放肽O-酰基转移酶（GOAT）被设计的小分子抑制。方法包括使GOAT与抑制剂接触并检测所得抑制。

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