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1. 发明授权

US06211223B1 Indole derivatives useful in therapy 失效
标题翻译：吲哚衍生物用于治疗
公开(公告)号：US06211223B1
公开(公告)日：2001-04-03
申请号：US09551779
申请日：2000-04-18
申请人： Stephen Challenger , Kevin Neil Dack , Andrew Michael Derrick , Roger Peter Dickinson , David Ellis , Yousef Hajikarimian , Kim James , David James Rawson
发明人： Stephen Challenger , Kevin Neil Dack , Andrew Michael Derrick , Roger Peter Dickinson , David Ellis , Yousef Hajikarimian , Kim James , David James Rawson
IPC分类号： A61K31404
CPC分类号： C07D405/06
摘要： The invention provides S-(+)-3-{1-(1,3-benzodioxol-5-yl)-2-[(2-methoxy-4-methylphenyl)sulfonylamino]-2-oxoethyl}-1-methyl-1H-indole-6-carboxylic acid, which is substantially free from its (R)-(−)-enantiomer, and pharmaceutically acceptable derivatives thereof. The compounds are useful in the treatment of inter alia acute renal failure, restenosis and pulmonary hypertension.
摘要翻译：本发明提供了S - （+） - 3- {1-（1,3-苯并间二氧杂环戊烯-5-基）-2 - [（2-甲氧基-4-甲基苯基）磺酰基氨基] -2-氧代乙基} -1-甲基基本上不含其（R） - （ - ） - 对映异构体的-1H-吲哚-6-羧酸及其药学上可接受的衍生物。该化合物可用于治疗尤其是急性肾衰竭，再狭窄和肺动脉高压

2. 再颁专利

USRE35865E Preparation of glutaric acid derivatives 失效
标题翻译：戊二酸衍生物的制备
公开(公告)号：USRE35865E
公开(公告)日：1998-07-28
申请号：US856612
申请日：1997-05-15
申请人： Stephen Challenger
发明人： Stephen Challenger
IPC分类号： C07C67/313 , C07C51/285 , C07C67/333 , C07C67/475 , C07C69/34 , C07C69/347 , C07C69/42 , C07C69/608 , C07C69/74 , C07C69/757 , C07C205/42
CPC分类号： C07C67/30 , C07C201/12 , C07C67/313 , C07C2101/08
摘要： The Invention provides a process for preparing a compound of the formula: ##STR1## or a base salt thereof, wherein R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl optionally substituted by up to 3 substituents each independently selected from the group consisting of C.sub.1 -C.sub.6 alkoxy and C.sub.1 -C.sub.6 alkoxy(C.sub.1 -C.sub.6 alkoxy)-; and R.sup.3 is C.sub.1 -C.sub.6 alkyl or benzyl, said benzyl group being optionally ring-substituted by up to 2 nitro or C.sub.1 -C.sub.4 alkoxy substituents comprising reacting a compound of the formula: ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl, phenyl or benzyl or C.sub.1 -C.sub.4 alkoxy; and R.sup.2 and R.sup.3 are as previously defined for a compound of the formula (I), with hydrogen peroxide or a source of peroxide ions: said process being optionally followed by conversion of the compound of the formula (I) to a base salt thereof. The present invention also relates to novel compounds of the formula (II).
摘要翻译：本发明提供一种制备下式化合物或其碱盐的方法，其中R 2为氢或任选被至多3个取代基取代的C 1 -C 6烷基，所述取代基各自独立地选自C1 -C 1-6烷氧基和C 1 -C 6烷氧基（C 1 -C 6烷氧基） - ; 并且R 3是C 1 -C 6烷基或苄基，所述苄基任选被至多2个硝基或C 1 -C 4烷氧基取代基环取代，包括使下式化合物：其中R 1是C 1 -C 4烷基，苯基或苄基或C 1 -C 4烷氧基; 并且R2和R3如先前对于式（I）化合物所定义，与过氧化氢或过氧化物离子的来源：所述方法任选地随后将式（I）化合物转化为其碱式盐。本发明还涉及新的式（II）化合物。

3. 发明授权

US06660756B2 N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase 失效
标题翻译： N-苯丙基环戊基取代的戊二酰胺衍生物作为中性内肽酶的抑制剂
公开(公告)号：US06660756B2
公开(公告)日：2003-12-09
申请号：US10096218
申请日：2002-03-12
申请人： Stephen Challenger , Andrew Simon Cook , Adam Thomas Gillmore , Donald Stuart Middleton , David Cameron Pryde , Alan Stobie
发明人： Stephen Challenger , Andrew Simon Cook , Adam Thomas Gillmore , Donald Stuart Middleton , David Cameron Pryde , Alan Stobie
IPC分类号： A61K3144
CPC分类号： C07D319/18 , C07C235/82 , C07C255/60 , C07C323/40 , C07C2601/08 , C07C2602/08 , C07D213/40 , C07D215/12 , C07D231/56 , C07D307/81 , C07D311/74 , C07D317/62
摘要： The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.
摘要翻译：本发明涉及用于治疗例如性功能障碍的式（I）化合物，其中R 1是任选取代的C 1-6烷基，任选取代的碳环基，任选取代的杂环基，氢，C 1-6烷氧基，-NR 2 R 3或-NR 4 SO 2 R 5; X是连接 - （CH 2）n - 或 - （CH 2）q -O-（其中Y连接到氧上）; 其中连接X中的一个或多个氢原子可以被C 1-4烷氧基独立地取代; 羟基; 羟基（C 1-3烷基）; C 3-7环烷基; 碳环基杂环基或被任选被一个或多个氟或苯基取代的C 1-4烷基; n为3,4,5,6或7; q为2,3,4,5或6; Y为苯基或吡啶基，各自可以被取代; 或相邻碳原子上的两个R 8基团与互连碳原子一起可以形成稠合的任选取代的5或6元碳环或杂环基。

4. 发明授权

US5166406A Preparation of glutaric acid derivatives 失效
标题翻译：戊二酸衍生物的制备
公开(公告)号：US5166406A
公开(公告)日：1992-11-24
申请号：US504493
申请日：1990-04-04
申请人： Stephen Challenger
发明人： Stephen Challenger
IPC分类号： C07C67/313 , C07C51/285 , C07C67/333 , C07C67/475 , C07C69/34 , C07C69/347 , C07C69/42 , C07C69/608 , C07C69/74 , C07C69/757 , C07C205/42
CPC分类号： C07C67/30 , C07C201/12 , C07C67/313 , C07C2101/08
摘要： The invention provides a process for preparing a compound of the formula: ##STR1## or a base salt thereof, wherein R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl optionally substituted by up to 3 substituents each independently selected from the group consisting of C.sub.1 -C.sub.6 alkoxy and C.sub.1 -C.sub.6 alkoxy(C.sub.1 -C.sub.6 alkoxy)-; and R.sup.3 is C.sub.1 -C.sub.6 alkyl or benzyl, said benzyl group being optionally ring-substituted by up to 2 nitro or C.sub.1 -C.sub.4 alkoxy substituents comprising reacting a compound of the formula: ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl, phenyl or benzyl or C.sub.1 -C.sub.4 alkoxy; and R.sup.2 and R.sup.3 are as previously defined for a compound of the formula (I), with hydrogen peroxide or a source of peroxide ions: said process being optionally followed by conversion of the compound of the formula (I) to a base salt thereof. The present invention also relates to novel compounds of the formula (II).
摘要翻译：本发明提供了制备下式化合物或其碱盐的方法：其中R 2为氢或任选被至多3个取代基取代的C 1 -C 6烷基，所述取代基各自独立地选自C1 -C 1-6烷氧基和C 1 -C 6烷氧基（C 1 -C 6烷氧基） - ; 并且R 3是C 1 -C 6烷基或苄基，所述苄基任选被至多2个硝基或C 1 -C 4烷氧基取代基环取代，包括使下式化合物：其中R 1是C 1 -C 4烷基，苯基或苄基或C 1 -C 4烷氧基; 并且R2和R3如先前对于式（I）化合物所定义，与过氧化氢或过氧化物离子的来源：所述方法任选地随后将式（I）化合物转化为其碱式盐。本发明还涉及新的式（II）化合物。

5. 发明授权

US5714628A Preparation of glutaric acid derivatives 失效
标题翻译：戊二酸衍生物的制备
公开(公告)号：US5714628A
公开(公告)日：1998-02-03
申请号：US672682
申请日：1996-06-28
申请人： Stephen Challenger
发明人： Stephen Challenger
IPC分类号： C07C67/42 , C07C69/757 , C07C205/42 , C07C69/74
CPC分类号： C07C67/42 , C07C201/12 , C07C69/757
摘要： The invention provides a process for preparing a compound of the formula: ##STR1## or a base salt thereof, wherein R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl optionally substituted by up to 3 substituents each independently selected from the group consisting of C.sub.1 -C.sub.6 alkoxy and C.sub.1 -C.sub.6 alkoxy(C.sub.1 -C.sub.6 alkoxy)-; and R.sup.3 is C.sub.1 -C.sub.6 alkyl or benzyl, said benzyl group being optionally ring-substituted by up to 2 nitro or C.sub.1 -C.sub.4 alkoxy substituents. comprising reacting a compound of the formula: ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl, phenyl or benzyl or C.sub.1 -C.sub.4 alkoxy; and R.sup.2 and R.sup.3 are as previously defined for a compound of the formula (I), with hydrogen peroxide or a source of peroxide ions: said process being optionally followed by conversion of the compound of the formula (I) to a base salt thereof. The present invention also relates to novel compounds of the formula (II).
摘要翻译：本发明提供了制备下式化合物或其碱盐的方法：其中R 2为氢或任选被至多3个取代基取代的C 1 -C 6烷基，所述取代基各自独立地选自C1 -C 1-6烷氧基和C 1 -C 6烷氧基（C 1 -C 6烷氧基） - ; 并且R 3是C 1 -C 6烷基或苄基，所述苄基任选被至多2个硝基或C 1 -C 4烷氧基取代基环取代。包括使下式化合物：其中R 1是C 1 -C 4烷基，苯基或苄基或C 1 -C 4烷氧基; 并且R2和R3如先前对于式（I）化合物所定义，与过氧化氢或过氧化物离子的来源：所述方法任选地随后将式（I）化合物转化为其碱式盐。本发明还涉及新的式（II）化合物。

6. 发明授权

US5618970A Hydrogenation 失效
标题翻译：氢化
公开(公告)号：US5618970A
公开(公告)日：1997-04-08
申请号：US612940
申请日：1996-03-07
申请人： Stephen Challenger
发明人： Stephen Challenger
IPC分类号： B01J31/24 , C07B61/00 , C07C67/303 , C07C69/708 , C07C69/757 , C07C231/12 , C07C235/40 , C07C69/74
CPC分类号： C07C69/757 , Y02P20/55
摘要： Compounds of formula ##STR1## where R is 5-indanyl or a carboxylic acid protecting group, or an amine salt thereof, are prepared by hydrogenating an (E)-allylic ether of formula ##STR2## in the presence of a stereoselective rhodium or ruthenium biphosphine catalyst and a protic solvent.
摘要翻译： PCT No.PCT / EP94 / 03036 Sec。 371日期：1996年3月7日 102（e）1996年3月7日PCT PCT 1994年9月9日PCT公布。第WO95 / 08526号公报日期：1995年3月30日通过氢化（E） - 烯丙基胺（I）制备其中R为5-二氢化茚基或羧酸保护基或其胺盐的式（I）或（Ia）化合物或其在立体选择性铑或钌二膦催化剂和质子溶剂的存在下，通式为“IMAGE”或“IMAGE”（IIa）的醚。

7. 发明授权

US06849649B2 N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase 失效
标题翻译：的N- phenpropylcyclopentyl取代的戊二酰胺衍生物作为中性内肽酶抑制剂
公开(公告)号：US06849649B2
公开(公告)日：2005-02-01
申请号：US10696021
申请日：2003-10-28
申请人： Stephen Challenger , Andrew Simon Cook , Adam Thomas Gillmore , Donald Stuart Middleton , David Cameron Pryde , Alan Stobie
发明人： Stephen Challenger , Andrew Simon Cook , Adam Thomas Gillmore , Donald Stuart Middleton , David Cameron Pryde , Alan Stobie
IPC分类号： C07C235/82 , C07C255/60 , C07C323/40 , C07D213/40 , C07D215/12 , C07D231/56 , C07D307/81 , C07D311/74 , C07D317/62 , C07D319/18 , A61K31/44 , A01N43/32 , A01N43/56 , A61K31/335 , A61K31/415
CPC分类号： C07D319/18 , C07C235/82 , C07C255/60 , C07C323/40 , C07C2601/08 , C07C2602/08 , C07D213/40 , C07D215/12 , C07D231/56 , C07D307/81 , C07D311/74 , C07D317/62
摘要： The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.
摘要翻译：本发明涉及用于治疗例如性功能障碍的式（I）化合物，其中R 1是任选取代的C 1-6烷基，任选取代的碳环基，任选取代的杂环基，氢，C 1-6烷氧基，-NR 2 R 3或-NR 4 SO 2 R 5; X是键 - （CH 2）n - 或 - （CH 2）Q-O-（其中Y连接至氧）; 其中连接X中的一个或多个氢原子可以被C 1-4烷氧基独立地取代; 羟基; 羟基（C 1-3烷基）; C 3-7环烷基; 碳环基杂环基或被任选被一个或多个氟或苯基取代的C 1-4烷基; n为3,4,5,6或7; q为2,3,4,5或6; Y为苯基或吡啶基，各自可以被取代; 或相邻碳原子上的两个R 8基团与互连碳原子一起可以形成稠合的任选取代的5或6元碳环或杂环基。

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