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1. 发明授权

US5998462A 5-alkyl indole compounds 失效
标题翻译： 5-烷基吲哚化合物
公开(公告)号：US5998462A
公开(公告)日：1999-12-07
申请号：US767323
申请日：1996-12-16
申请人： Abdelmalik Slassi , Louise Edwards , Qingchang Meng , Sumanas Rakhit
发明人： Abdelmalik Slassi , Louise Edwards , Qingchang Meng , Sumanas Rakhit
IPC分类号： C07D209/16 , C07D403/06 , A61K31/40
CPC分类号： C07D403/06 , C07D209/16
摘要： Described herein are compounds selective for the 5-HT.sub.1D -like receptor, which have the general formula: ##STR1## wherein: R.sup.1 is linear or branched loweralkyl;R.sup.2 is selected from a group of Formula II, III, IV and V: ##STR2## R.sup.3 is selected from H and loweralkyl; R.sup.4 is selected from H and loweralkyl;One of R.sup.5 and R.sup.6 is H and the other is independently selected from H, loweralkoxy, loweralkyl and hydroxy; andn is 1-3;or a salt, solvate or hydrate thereof.Also described is the use of these compounds as pharmaceuticals to treat indications where stimulation of the 5-HT.sub.1D -like receptor is implicated, such as migraine.
摘要翻译：本文描述的是对具有以下通式的5-HT1D样受体有选择性的化合物：其中：R1是直链或支链的低级烷基; R2选自式II，III，IV和V的基团：R3选自H和低级烷基; R4选自H和低级烷基; R5和R6之一是H，另一个独立地选自H，低级烷氧基，低级烷基和羟基; n为1-3; 或其盐，溶剂合物或水合物。还描述了这些化合物作为药物用于治疗涉及5-HT1D样受体的刺激的指征，例如偏头痛。

2. 发明授权

US5998438A 5-cyclo indole compounds 失效
标题翻译： 5-环吲哚化合物
公开(公告)号：US5998438A
公开(公告)日：1999-12-07
申请号：US976103
申请日：1997-11-21
申请人： Abdelmalik Slassi , Louise Edwards , Qingchang Meng , Sumanas Rakhit
发明人： Abdelmalik Slassi , Louise Edwards , Qingchang Meng , Sumanas Rakhit
IPC分类号： C07D209/14 , C07D209/18 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/14 , A61K31/40
CPC分类号： C07D401/04 , C07D209/14 , C07D209/18 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/14
摘要： Described herein are compounds selective for a 5-HT.sub.1D -like receptor, which have the general formula: ##STR1## wherein A is selected from a six-membered, non-aromatic, optionally substituted carbocycle and a six-membered, non-aromatic, optionally substituted heterocycle having one or two heteroatoms selected from O, S, SO, SO.sub.2 and N.sup.4 ;R.sup.1 is selected from H and OH;n is 0 or 1 as permited by chemical structure;R.sup.2 is selected from CR.sup.5 CR.sup.6 CH.sub.2 NR.sup.7 R.sup.8 or a group of formula II, III or IV: ##STR2## R.sup.3 is selected from H and benzoyl; R.sup.4 is selected from H, loweralkyl, benzyl, loweralkylcarbonyl, loweralkylaminocarbonyl, loweralkylaminothiocarbonyl, loweralkanoyl, loweralkylaminoimide and loweralkoxy-substituted loweralkylene;R.sup.5 and R.sup.6 are independently selected from H, loweralkoxy and hydroxy;R.sup.7 and R.sup.8 are independently selected from H and loweralkyl or R.sup.7 and R.sup.8 form an alkylene bridge which, together with the nitrogen atom to which they are attached, creates an optionally substituted 3- to 6-membered ring;denotes a single or double bond; andR.sup.9, R.sup.10 and R.sup.11 are independently selected from H and loweralkyl.Also described is the use of these compounds as pharmaceuticals to treat indications where stimulation of a 5-HT.sub.1D -like receptor is implicated, such as migraine.
摘要翻译：本文描述了对具有以下通式的5-HT1D样受体选择性的化合物：其中A选自六元非芳族任选取代的碳环和六元非芳族任选取代的杂环具有一个或两个选自O，S，SO，SO 2和N 4的杂原子; R1选自H和OH; n为化学结构允许的0或1; R2选自CR5CR6CH2NR7R8或式II，III或IV的基团：R3选自H和苯甲酰基; R4选自H，低级烷基，苄基，低级烷基羰基，低级烷基氨基羰基，低级烷基氨基硫代羰基，低级烷酰基，低级烷基氨基酰亚胺和低级烷氧基取代的低级亚烷基; R5和R6独立地选自H，低级烷氧基和羟基; R 7和R 8独立地选自H和低级烷基或R 7和R 8形成亚烷基桥，其与它们所连接的氮原子一起产生任选取代的3至6元环; 表示单键或双键; 并且R 9，R 10和R 11独立地选自H和低级烷基。还描述了这些化合物作为药物用于治疗涉及5-HT1D样受体的刺激的指征，例如偏头痛。

3. 发明授权

US5770742A Thiophene-tryptamine derivatives 失效
标题翻译：噻吩 - 色胺衍生物
公开(公告)号：US5770742A
公开(公告)日：1998-06-23
申请号：US648842
申请日：1996-05-16
申请人： Qingchang Meng , Abdelmalik Slassi , Sumanas Rakhit
发明人： Qingchang Meng , Abdelmalik Slassi , Sumanas Rakhit
IPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D403/06
CPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： 5-Thiophene-substituted tryptamine analogs are provided, which exhibit selectivity towards 5-HT.sub.D1 receptors and consequently show potential in alleviation of the symptoms of migraine. The analogs are represented by the following general chemical formula: ##STR1## in which X represents H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 hydroxyalkyl or halogen, at the 4- or 5-position of the thiophene nucleus; Y represents a direct bond or a C.sub.1 -C.sub.3 alkylene group optionally substituted with hydroxyl: and Z represents amino, mono- or di-N-lower alkyl-substituted amino, or optionally N-lower alkyl-substituted pyrrolidine.
摘要翻译：提供了5-噻吩取代的色胺类似物，其显示出对5-HTD1受体的选择性，因此显示缓解偏头痛症状的潜力。类似物由以下通用化学式表示：其中X表示噻吩核的4-或5-位上的X表示H，C 1 -C 4烷基，C 1 -C 4羟基烷基或卤素的 Y表示直接键或任选被羟基取代的C 1 -C 3亚烷基：Z表示氨基，单或二-N-低级烷基取代的氨基或任选的N-低级烷基取代的吡咯烷。

4. 发明授权

US5654431A 5-alkoxy tryptamine derivatives 失效
标题翻译： 5-烷氧基色胺衍生物
公开(公告)号：US5654431A
公开(公告)日：1997-08-05
申请号：US655588
申请日：1996-05-30
申请人： Qingchang Meng , Abdelmalik Slassi , Sumanas Rakhit
发明人： Qingchang Meng , Abdelmalik Slassi , Sumanas Rakhit
IPC分类号： C07D209/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D417/12 , C07D417/14 , C07D209/08 , C07D221/06
CPC分类号： C07D403/06 , C07D209/14 , C07D403/12 , C07D403/14 , C07D417/12 , C07D417/14
摘要： Novel 5-alkoxy tryptamine derivatives are provided, corresponding to the general formula: ##STR1## in which R may be alkaline, X may be amino, and Y is various N-heterocyclic or N-branched chain moieties. The compounds show selective binding to 5-HT.sub.1D receptor subtypes, and have potential pharmaceutical utility in manufacture of migraine-treating drugs.
摘要翻译：提供了新的5-烷氧基色胺衍生物，其对应于通式：其中R可以是碱性的，X可以是氨基，Y是各种N-杂环或N-支链部分。这些化合物显示出与5-HT1D受体亚型的选择性结合，并且在制造偏头痛药物方面具有潜在的药用效用。

5. 发明授权

US5856510A 5-alkenyl and 5-alkynyl indole compounds 失效
标题翻译： 5-链烯基和5-炔基吲哚化合物
公开(公告)号：US5856510A
公开(公告)日：1999-01-05
申请号：US767322
申请日：1996-12-16
申请人： Oingchang Meng , Abdelmalik Slassi , Louise Edwards , Sumanas Rakhit
发明人： Oingchang Meng , Abdelmalik Slassi , Louise Edwards , Sumanas Rakhit
IPC分类号： C07D209/16 , C07D403/04 , C07D403/14 , C07D409/14 , C07D403/02 , A61K31/405 , A61K31/415 , C07D209/02 , C07D209/04
CPC分类号： C07D403/04 , C07D209/16 , C07D403/14 , C07D409/14
摘要： Described herein are compounds selective for 5-HT.sub.1D -like receptors, which have the general formula: ##STR1## wherein: R.sup.1 is selected from H, aryl and aryl substituted with 1, 2 or 3 substituents independently selected from loweralkyl, loweralkoxy, loweralkylcarbonyl, loweralkyl-S--, loweralkyl-S(O)--, loweralkyl-SO.sub.2 -, S.dbd.C.dbd.N--, O.dbd.C.dbd.N--, halo, loweralkoxycarbonyl, nitro, amino, loweralkyl-NH--, (loweralkyl).sub.2 --N--, loweralkyl-SO.sub.2 -loweralkyl-;A is a double or triple bond;R.sup.2 is selected from a group of Formula II, III, IV and V: ##STR2## R.sup.3 is selected from H and loweralkyl; R.sup.4 is selected from H and loweralkyl;One of R.sup.5 and R.sup.6 is H and the other is independently selected from H, loweralkoxy, loweralkyl and hydroxy; andR.sup.7 and R.sup.8 are independently selected from H and loweralkyl or R.sup.7 and R.sup.8, together with the nitrogen atom to which they are attached, form an optionally substituted 3- to 6-membered ring;or a salt, solvate or hydrate thereof.Also described is the use of these compounds as pharmaceuticals to treat indications where stimulation of the 5-HT.sub.1D -like receptor is implicated, such as migraine.
摘要翻译：本文描述了对具有以下通式的5-HT1D样受体选择性的化合物：1和被1,2或3个独立地选自低级烷基，低级烷氧基，低级烷基羰基，低级烷基-S-，低级烷基-S（O） - ， - 低级烷基-SO 2 - ，S = C = N-，O = C = N-，卤素，低级烷氧基羰基，硝基，氨基，低级烷基-NH-，（低级烷基）2-N-，低级烷基-SO 2 - 低级烷基 - A是双重或三重键; R 2选自式II，III，IV和V的组：V 3选自H和低级烷基; R4选自H和低级烷基; R5和R6之一是H，另一个独立地选自H，低级烷氧基，低级烷基和羟基; 并且R 7和R 8独立地选自H和低级烷基，或者R 7和R 8与它们所连接的氮原子一起形成任选取代的3至6元环; 或其盐，溶剂合物或水合物。还描述了这些化合物作为药物用于治疗涉及5-HT1D样受体的刺激的指征，例如偏头痛。

6. 发明授权

US5627194A Anti-viral guanidino-substituted compounds 失效
标题翻译：抗病毒胍基取代的化合物
公开(公告)号：US5627194A
公开(公告)日：1997-05-06
申请号：US322492
申请日：1994-10-14
申请人： Sumanas Rakhit , Abdelmalik Slassi
发明人： Sumanas Rakhit , Abdelmalik Slassi
IPC分类号： C07C279/16 , C07D211/06 , C07H15/04 , C07H15/08 , A61K31/35 , A61K31/17 , A61K31/38 , A61K31/445
CPC分类号： C07H15/04 , C07C279/16 , C07D211/06 , C07H15/08
摘要： Novel guanidino-substituted compounds are described having the following general formula (I): ##STR1## in which X may be carbon, oxygen, nitrogen or sulfur; R.sub.1 may be H, OH, linear or branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine, lower alkyl-thio, hydroxy substituted lower alkoxy, lower alkoxy-alkoxy substituted lower alkoxy, hydroxy substituted lower alkyl-amine, alkoxy substituted lower alkyl-amine and terminally guanidino-substituted linear of branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine or lower alkyl-thio; and R.sub.2 and R.sub.3 are independently one of linear or branched lower alkyl, alkoxy, alkyl-substituted alkoxy and alkylamine.These compounds have been found to inhibit effectively herpesvirus replication. Particularly preferred compounds in accordance with formula (I) for this purpose are guanidino-substituted sugar derivatives.
摘要翻译：描述了新的胍基取代的化合物，其具有以下通式（I）：其中X可以是碳，氧，氮或硫; R 1可以是H，OH，直链或支链的低级烷基，低级烷氧基，低级（烷基取代的烷氧基），低级烷基 - 胺，低级烷基 - 硫代，羟基取代的低级烷氧基，低级烷氧基 - 烷氧基取代的低级烷氧基，烷基胺，烷氧基取代的低级烷基胺和末端胍基取代的直链的支链低级烷基，低级烷氧基，低级（烷基取代的烷氧基），低级烷基 - 胺或低级烷基 - 硫代; R2和R3独立地为直链或支链的低级烷基，烷氧基，烷基取代的烷氧基和烷基胺之一。已经发现这些化合物有效地抑制疱疹病毒复制。特别优选的根据式（I）的化合物是胍基取代的糖衍生物。

7. 发明授权

US5198425A Inhibitors of bacterial ribonucleotide reductase 失效
标题翻译：细菌核糖核苷酸还原酶抑制剂
公开(公告)号：US5198425A
公开(公告)日：1993-03-30
申请号：US900366
申请日：1992-06-18
申请人： Sumanas Rakhit , Raymond Plante , Gregory P. Cosentino
发明人： Sumanas Rakhit , Raymond Plante , Gregory P. Cosentino
IPC分类号： A61K38/00 , C07K7/06
CPC分类号： C07K7/06 , A61K38/00
摘要： Disclosed herein are peptides of the formulaY--R.sup.1 --R.sup.2 --R.sup.3 --R.sup.4 --R.sup.5 --R.sup.6 --R.sup.7 --R.sup.8 --R.sup.9 --Zwherein R.sup.1 to R.sup.9 are designated amino acid residues; Y is hydrogen or lower alkanoyl, or Y is the hexapeptide radical W-lle-R.sup.10 -Ser-R.sup.11 -Val-R.sup.12 wherein W is hydrogen or lower alkanoyl and R.sup.10, R.sup.11 and R.sup.12 are designated amino acid residues, or Y is a fragment of the hexapeptide radical wherein from one to five of the amino acid residues (i.e. Ile to Val) may be deleted serially from the amino terminus of the hexapeptide radical; and Z is hydroxy, amino, lower alkylamino or di(lower alkyl)amino. The peptides inhibit bacterial ribonucleotide reductase and are indicated for preventing or ameliorating bacterial infections.
摘要翻译：本文公开的是式Y-R1-R2-R3-R4-R5-R6-R7-R8-R9-Z的肽，其中R1至R9被指定为氨基酸残基; Y为氢或低级烷酰基，或Y为六肽基团W-Lle-R10-Ser-R11-Val-R12，其中W为氢或低级烷酰基，R10，R11和R12为氨基酸残基，或Y为片段的六肽基团，其中一至五个氨基酸残基（即Ile至Val）可以从六肽基团的氨基末端连续缺失; 和Z是羟基，氨基，低级烷基氨基或二（低级烷基）氨基。肽抑制细菌核糖核苷酸还原酶，并且用于预防或改善细菌感染。

8. 发明授权

US4316885A Acyl derivatives of rapamycin 失效
标题翻译：雷帕霉素的酰基衍生物
公开(公告)号：US4316885A
公开(公告)日：1982-02-23
申请号：US181252
申请日：1980-08-25
申请人： Sumanas Rakhit
发明人： Sumanas Rakhit
IPC分类号： A61K31/435 , A61P31/04 , A61P31/10 , C07D498/18 , A61K35/74 , C07D491/14
CPC分类号： C07D498/18
摘要： Disclosed are monoacyl and diacyl derivatives of rapamycin, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are useful, inter alia, as antifungal antibiotics.
摘要翻译：公开了雷帕霉素的单酰基和二酰基衍生物，其制备方法，使用衍生物的衍生物的方法和衍生物的药物组合物。该衍生物尤其用作抗真菌抗生素。

9. 发明授权

US5798350A Dopamine receptor ligands 失效
标题翻译：多巴胺受体配体
公开(公告)号：US5798350A
公开(公告)日：1998-08-25
申请号：US642264
申请日：1996-05-03
申请人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
发明人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
IPC分类号： A61K31/00 , A61K31/55 , A61P25/18 , A61P25/20 , C07D243/10 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/12 , C07D491/00 , A61K31/495 , A61K31/435 , C07D401/14 , C07D403/14
CPC分类号： C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO; X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--; R.sub.1 represents C.sub.1-4 alkyl; Y is selected from CH and N; n is 0, 1 or 2; q is 1 or 2; R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S; D is cyclohexane or benzene; and E is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元，杂环或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; R 1表示C 1-4烷基; Y选自CH和N; n为0,1或2; q为1或2; R2是任选地加入选自N，O和S的杂原子的C 1-6烷基; D是环己烷或苯; 并且E是掺杂有1,2或3个选自O，N和S的杂原子的饱和或不饱和的5-或6-元杂环，其中E任选被1或2个选自卤素，C 1-4烷基和卤素 - 取代的C 1-4烷基; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。

10. 发明授权

US5703072A Bicyclic nonane and decane compounds having dopamine receptor affinity 失效
标题翻译：具有多巴胺受体亲和力的双环壬烷和癸烷化合物
公开(公告)号：US5703072A
公开(公告)日：1997-12-30
申请号：US625358
申请日：1996-04-01
申请人： Patricia L. Power , Sumanas Rakhit
发明人： Patricia L. Power , Sumanas Rakhit
IPC分类号： C07D471/04 , C07D487/04 , A61K31/55
CPC分类号： C07D471/04 , C07D487/04
摘要： Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, substituted or unsubstituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings; X.sub.1 is selected from O, S, SO, SO.sub.2, CH.sub.2, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, and C.dbd.CHCN; X.sub.2 --- is selected from N.dbd., CH.sub.2 --, CH.dbd. and C(O)--; n is 1 or 2; R.sub.1 is selected from H and the .alpha.-carbon side chain of an amino acid; R.sub.2 and R.sub.3 are selected independently from H, OH, --NH.sub.2, --C(O)NH.sub.2 .dbd.O, .dbd.S,halo,cyano, C.sub.1-9 alkyl, C.sub.1-9 alkoxy, C.sub.1-4 alkylS--, C.sub.1-4 alkylSO--, C.sub.1-4 alkylSO.sub.2 --, phenoxy, benzyloxy and piperonyloxy; and H* is in either the R- or the S-configuration, and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立选择，取代或未取代的不饱和5-或6-元，均 - 或杂环; X选自O，S，SO，SO 2，CH 2，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl和C = CHCN; X2 ---选自N =，CH 2 - ，CH =和C（O） - ; n为1或2; R1选自H和氨基酸的α-碳侧链; R2和R3独立地选自H，OH，-NH2，-C（O）NH2 = O，= S，卤素，氰基，C1-9烷基，C1-9烷氧基，C1-4烷基，C1-4烷基， 4-烷基SO2-，苯氧基，苄氧基和哌嗪氧基; 和H *为R-或S-构型，以及其酸加成盐，溶剂合物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。

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