专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明授权

US5026882A Phosphinic acid substituted steroids as inhibitors of steroid 5.alpha.-reductase 失效
标题翻译：次膦酸取代的类固醇作为类固醇5α-还原酶的抑制剂
公开(公告)号：US5026882A
公开(公告)日：1991-06-25
申请号：US290212
申请日：1988-12-23
申请人： Dennis A. Holt , Mark A. Levy , Brian W. Metcalf
发明人： Dennis A. Holt , Mark A. Levy , Brian W. Metcalf
IPC分类号： A61K31/56 , A61K31/565 , A61P3/06 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07J51/00 , C07J61/00 , C07J63/00
CPC分类号： C07J63/002 , C07J51/00 , C07J61/00
摘要： The invention relates to 3-phosphinic acid steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase.

42. 发明授权

US4954446A Aromatic steroid 5-.alpha.-reductase inhibitors 失效
标题翻译：芳香类固醇5-抗原酶抑制剂
公开(公告)号：US4954446A
公开(公告)日：1990-09-04
申请号：US380226
申请日：1989-07-14
申请人： Dennis A. Holt , Mark A. Levy , Brian W. Metcalf
发明人： Dennis A. Holt , Mark A. Levy , Brian W. Metcalf
IPC分类号： C07J1/00 , C07J3/00 , C07J7/00 , C07J9/00 , C07J13/00 , C07J21/00 , C07J31/00 , C07J41/00
CPC分类号： C07J1/0059 , C07J13/005 , C07J13/007 , C07J21/00 , C07J3/00 , C07J3/005 , C07J31/006 , C07J41/0033 , C07J41/0094 , C07J7/0095 , C07J9/00
摘要： Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.
摘要翻译：发明的是甾体合成化合物的取代的丙烯酸酯类似物，含有这些化合物的药物组合物，以及使用这些化合物抑制类固醇5-α-还原酶的方法，包括使用这些化合物来减少前列腺的大小。还发明了用于制备这些化合物的中间体。

43. 发明授权

US4910226A Steroid 5-alpha-reductase inhibitors 失效
标题翻译：类固醇5-α-还原酶抑制剂
公开(公告)号：US4910226A
公开(公告)日：1990-03-20
申请号：US127147
申请日：1987-12-01
申请人： Dennis A. Holt , Mark A. Levy , Brian W. Metcalf
发明人： Dennis A. Holt , Mark A. Levy , Brian W. Metcalf
IPC分类号： A61K31/57 , A61K31/575 , A61K31/58 , A61P43/00 , C07J1/00 , C07J3/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J51/00 , C07J61/00 , C07J63/00 , C07J71/00 , C12N9/99
CPC分类号： C07J71/001 , C07J1/0011 , C07J1/0022 , C07J1/007 , C07J21/00 , C07J3/00 , C07J3/005 , C07J31/006 , C07J41/0066 , C07J41/0094 , C07J51/00 , C07J61/00 , C07J63/002 , C07J7/0095 , C07J9/00 , C07J9/005
摘要： Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates used in preparing these compounds.

44. 发明授权

US4325877A Production of intermediates for enzyme inhibitors 失效
标题翻译：生产酶抑制剂的中间体
公开(公告)号：US4325877A
公开(公告)日：1982-04-20
申请号：US160057
申请日：1980-06-16
申请人： Brian W. Metcalf , Jerry L. Adams
发明人： Brian W. Metcalf , Jerry L. Adams
IPC分类号： C07C69/66 , C07C69/716 , C07C69/74 , C07C117/08
CPC分类号： C07C247/00 , C07C323/00
摘要： 5-Amino-4-oxo-pentanoic acids of the formula ##STR1## wherein R is CF.sub.3, CHF.sub.2 or CH.sub.2 F; R.sub.1 is H or akyl of 1-4 carbon atoms; and R.sub.2 is H or alkyl or 1-4 carbon atoms or benzyl, which are intermediates to ACE inhibitors or elastase inhibitors, are produced by reacting a 1-(methylthio)-1-methylsulfinyl)-2-R.sub.1 -ethylmetal with an ester of a 3-R-acrylic acid; optionally R.sub.2 -alkylating the thus-produced ester enolate anion of 4-(methylsulfinyl)-4-(methylthio)-5-R.sub.1 R-pentanoic acid followed by splitting off of methylsulfinic acid; reacting the thus-produced 2-R.sub.2 -5-R.sub.1 -4-(methylthio)-3-R-4-pentenoic acid ester with a source of Br.sup.+ to produce a 5-bromo-substituted acid or ester thereof otherwise corresponding to the desired 5-amino-4-oxo-pentanoic acid; and replacing the bromine atom with an amino group, e.g., via the corresponding 5-azido- and 5-N-acylamino- compounds, with hydrolysis of the ester group, if still remaining.
摘要翻译：其中R是CF 3，CHF 2或CH 2 F的5-氨基-4-氧代 - 戊酸; R1是H或1-4个碳原子的烷基; R2是H或烷基或1-4个碳原子，或作为ACE抑制剂或弹性蛋白酶抑制剂的中间体的苄基是通过使1-（甲硫基）-1-甲基亚磺酰基）-2-R 1 - 乙基金属与 3-R-丙烯酸; 任选地将4-（甲基亚磺酰基）-4-（甲硫基）-5-R1R-戊酸由此产生的酯烯醇化物阴离子R2-烷基化，随后分解出甲基亚磺酸; 使由此产生的2-R2-5-R1-4-（甲硫基）-3-R-4-戊烯酸酯与Br +源反应，产生5-溴取代的酸或酯，否则对应于所需的 5-氨基-4-氧代 - 戊酸; 并且如果仍然存在，则通过相应的5-叠氮基 - 和5-N-酰基氨基化合物用氨基取代溴原子，同时酯基的水解。

45. 发明授权

US4323704A .alpha.Acetylene and .alpha.-vinyl derivatives of amino acids 失效
标题翻译： α乙炔和氨基酸的α-乙烯基衍生物
公开(公告)号：US4323704A
公开(公告)日：1982-04-06
申请号：US225503
申请日：1981-01-16
申请人： Brian W. Metcalf , Michel Jung , Charles Danzin
发明人： Brian W. Metcalf , Michel Jung , Charles Danzin
IPC分类号： C07C103/52 , C07C101/28 , C07C103/68 , C07C125/065 , C07C125/073 , C07C129/12
摘要： Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.b can be the same or different; with the provisos that when R.sub.2 is hydrogen, R.sub.1 is --C.tbd.CH; when A is ethylidene, R.sub.2 is hydrogen; and when R.sub.a is ##STR6## A is methylene; and pharmaceutically acceptable salts and individual optical isomers thereof.
摘要翻译：新颖的式（Ⅰ）化合物，其中A是亚甲基，亚乙基或亚乙基; R1是-C3BCH或-CH = CH2; R2是氢或COR，其中R是羟基，1至8个碳原子的直链或支链烷氧基，-NR4R5，其中R4和R5分别是氢或1-4个碳原子的直链或支链低级烷基或其中R 6是氢，1至4个碳原子的直链或支链低级烷基，苄基或对羟基苄基; R a是氢，其中烷基部分具有1至4个碳原子并且是直链或支链的烷氧基羰基，其中烷氧基部分具有1至4个碳原子并且是直链或支链或其中R7被选定由氢，1至4个碳原子的直链或支链低级烷基，苄基和对羟基苄基; 并且Rb具有与Ra所定义的相同的含义，不同之处在于Rb不是＆lt; IMAGE＆gt;并且Ra和Rb可以相同或不同; 条件是当R2是氢时，R1是-C3BCH; 当A为亚乙基时，R 2为氢; 而当Ra为亚甲基时，及其药学上可接受的盐和单独的光学异构体。

46. 发明授权

US4317817A Novel steroid 5.alpha.-reductase inhibitors 失效
标题翻译：新型类固醇5α-还原酶抑制剂
公开(公告)号：US4317817A
公开(公告)日：1982-03-02
申请号：US216112
申请日：1980-12-15
申请人： Thomas R. Blohm , Brian W. Metcalf
发明人： Thomas R. Blohm , Brian W. Metcalf
IPC分类号： C07J1/00 , C07J3/00 , C07J9/00 , C07J17/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J51/00 , A01N47/08 , A61K31/655
CPC分类号： C07J9/005 , C07J1/0011 , C07J17/00 , C07J21/00 , C07J3/00 , C07J3/005 , C07J31/006 , C07J41/0005 , C07J51/00 , C07J9/00
摘要： Compounds of the following general formula are testosterone 5.alpha.-reductase inhibitors rendering the compounds useful in the treatment of acne and oily skin and benign prostatic hypertrophy: ##STR1## wherein R is: .dbd.O, --OH, --OCO--alkyl C.sub.1-5, --COOH, --CH.sub.2 OH, --COO--alkyl C.sub.1-6, --COCH.sub.3, ##STR2##
摘要翻译：以下通式的化合物是睾酮5α-还原酶抑制剂，其使得化合物可用于治疗痤疮和油性皮肤和良性前列腺肥大：其中R为：= O，-OH，-OCO-烷基C1-5 ，-COOH，-CH 2 OH，-COO-烷基C 1-6，-COCH 3，＆lt; IMAGE＆gt; + TR＆lt; IMAGE＆gt;

47. 发明授权

US4180509A .alpha.-Ethynyl tryptophanes 失效
标题翻译： α-乙炔基色氨酸
公开(公告)号：US4180509A
公开(公告)日：1979-12-25
申请号：US812052
申请日：1977-07-01
申请人： Brian W. Metcalf , Michel Jung
发明人： Brian W. Metcalf , Michel Jung
IPC分类号： C07D209/20 , C07D317/30 , C07D501/20 , A61K31/405
CPC分类号： C07C243/00 , C07D209/20 , C07D317/30 , Y10S514/922
摘要： Novel compounds of the following general formula ##STR1## and pharmaceutically acceptable salts and individual optical isomers thereof. The compounds are useful as aromatic amine decarboxylase inhibitors.
摘要翻译：下列通式的新颖化合物及其药学上可接受的盐和单独的光学异构体。该化合物可用作芳族胺脱羧酶抑制剂。

48. 发明授权

US08993582B2 Processes for preparing JAK inhibitors and related intermediate compounds 有权
公开(公告)号：US08993582B2
公开(公告)日：2015-03-31
申请号：US13761830
申请日：2013-02-07
申请人： Jiacheng Zhou , David Meloni , Pingli Liu , Brian W. Metcalf , Tai-Yuen Yue
发明人： Jiacheng Zhou , David Meloni , Pingli Liu , Brian W. Metcalf , Tai-Yuen Yue
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00 , C07D487/04 , C07F7/18 , C07F7/10
CPC分类号： C07D487/04 , C07F5/025 , C07F7/083 , C07F7/10 , C07F7/1892 , Y02P20/55
摘要： The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.

49. 发明授权

US08940752B2 Pyrimidinones as PI3K inhibitors 有权
标题翻译：嘧啶酮作为PI3K抑制剂
公开(公告)号：US08940752B2
公开(公告)日：2015-01-27
申请号：US12824924
申请日：2010-06-28
申请人： Yun-Long Li , Brian W. Metcalf
发明人： Yun-Long Li , Brian W. Metcalf
IPC分类号： A01N43/54 , C07D239/72 , C07D401/00
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
摘要翻译：本发明提供调节磷酸肌醇3-激酶（PI3K）的活性的嘧啶酮，并且可用于治疗与PI3Ks的活性相关的疾病，包括例如炎症性疾病，基于免疫的疾病，癌症和其它疾病。

50. 发明授权

US08410265B2 Processes for preparing JAK inhibitors and related intermediate compounds 有权
公开(公告)号：US08410265B2
公开(公告)日：2013-04-02
申请号：US12687623
申请日：2010-01-14
申请人： Jiacheng Zhou , Pingli Liu , Qiyan Lin , Brian W. Metcalf , David Meloni , Yongchun Pan , Michael Xia , Mei Li , Tai-Yuen Yue , James D. Rodgers , Haisheng Wang
发明人： Jiacheng Zhou , Pingli Liu , Qiyan Lin , Brian W. Metcalf , David Meloni , Yongchun Pan , Michael Xia , Mei Li , Tai-Yuen Yue , James D. Rodgers , Haisheng Wang
IPC分类号： C07D487/00
CPC分类号： C07D487/04 , C07F5/025 , C07F7/083 , C07F7/10 , C07F7/1892 , Y02P20/55
摘要： The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式