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1. 发明授权

US5648337A Antiherpes pentapeptides 失效
标题翻译：反相五肽
公开(公告)号：US5648337A
公开(公告)日：1997-07-15
申请号：US90681
申请日：1993-07-13
申请人： Julian Adams , Pierre Louis Beaulieu , Pierre Lavallee , Raymond Plante , Sumanas Rakhit
发明人： Julian Adams , Pierre Louis Beaulieu , Pierre Lavallee , Raymond Plante , Sumanas Rakhit
IPC分类号： A61K38/00 , C07K5/103 , C07K14/035 , C07K5/00 , C07K7/00
CPC分类号： C07K5/101 , C07K14/005 , A61K38/00 , C12N2710/16622
摘要： Disclosed herein are pentapeptide derivatives of the formula (SEQ ID NO: 24) XNR.sup.1 --CH(R.sup.2)--C(O)--NH--CH(R.sup.3 --C(O)--NR.sup.4 --CH(CH.sub.2 Y)--CO--NH--CH[CR.sup.5 (R.sup.6)--COOH]--C(W)--NH--CH(R.sup.7)--Z wherein X is a terminal group, for example, alkanoyl or phenylalkanoyl radicals, R.sup.1 is alkyl or phenylalkyl, R.sup.2, R.sup.3 and R.sup.7 are selected from the side chains of amino acid or derived amino acid residues, R.sup.4, R.sup.5, and R.sup.6 are hydrogen or lower alkyl, W is oxo or thioxo, Y is carboxy, carbamyl or 5-1H-tetrazolyl and Z is carboxy or 5-1H-tetrazolyl. The derivatives are useful for treating herpes infections.
摘要翻译：本文公开了式（SEQ ID NO：24）的五肽衍生物XNR1-CH（R2）-C（O）-NH-CH（R3-C（O）-NR4-CH（CH2Y）-CO-NH-CH [CR5（R6）-COOH] -C（W）-NH-CH（R7）-Z其中X是端基，例如烷酰基或苯基烷酰基，R1是烷基或苯基烷基，R2，R3和R7被选择由氨基酸或衍生氨基酸残基的侧链，R4，R5和R6是氢或低级烷基，W是氧代或硫代，Y是羧基，氨基甲酰基或5-1H-四唑基，Z是羧基或5-1H 四唑基，衍生物可用于治疗疱疹感染。

2. 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。

3. 发明授权

US5071835A Ribonucleotide reductase inhibitors 失效
标题翻译： RIBONUCLEOTIDE还原抑制剂
公开(公告)号：US5071835A
公开(公告)日：1991-12-10
申请号：US474589
申请日：1990-02-01
申请人： Yvan Guindon , Pierre Lavallee , Sumanas Rakhit , Gregory P. Cosentino
发明人： Yvan Guindon , Pierre Lavallee , Sumanas Rakhit , Gregory P. Cosentino
IPC分类号： C12N9/99 , A61K38/00 , A61K38/55 , A61P35/00 , C07K1/04 , C07K1/06 , C07K7/06 , C07K7/08 , C12Q1/26
CPC分类号： C07K7/06 , C07K7/08 , C12Q1/26 , 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 --Zwherein R.sup.1 to R.sup.5 are designated amino acid residues; R.sup.6 is Phe, homoPhe or an amino acid residue derived from 2-amino-3-cyclohexylpropionic acid, 2-amino-3-(4-(lower alkoxy)phenyl) propionic acid or 2-amino-3-(4-halophenyl)propionic acid; Y is Phe, desamino-Phe, (lower alkanoyl)-Phe, p-haloPhe, Tyr, desamino-Tyr or (lower alkanoyl)-Tyr, or Y is the decapeptide radical W--Val--R.sup.7 --Ser--R.sup.8 --R.sup.9 --Thr--Glu--R.sup.10 --Ser--Phe wherein W is hydrogen or lower alkanoyl and R.sup.7 to R.sup.10 are designated amino acids residues, or Y is a fragment of the decapeptide radical wherein from one to nine of the amino acid residues (i.e. Val to Ser) may be deleted serially from the amino terminus of the decapeptide radical; and Z is hydroxy, amino, lower alkylamino or di(lower alkyl)amino. The peptides inhibit mammalian ribonucleotide reductase and are indicated for preventing or ameliorating abnormal cell proliferation.

4. 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。

5. 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。

6. 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。

7. 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。

8. 发明授权

US5561127A Muscarinic receptor ligands 失效
标题翻译：毒蕈碱受体配体
公开(公告)号：US5561127A
公开(公告)日：1996-10-01
申请号：US358471
申请日：1994-12-19
申请人： Ashok Tehim , Sumanas Rakhit
发明人： Ashok Tehim , Sumanas Rakhit
IPC分类号： C07D487/08 , A61K31/55 , C07D403/04 , C07D413/04 , C07D417/00
CPC分类号： C07D487/08
摘要： Described herein are D4 receptor-selective compounds of the general formula I: ##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--NEt.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--;n is 1 or 2; andZ is selected from C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;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 M1/M2 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是通式I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-元的同或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-NEt 2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，SO 2和SO; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; n为1或2; Z选自任选被选自OH，卤素，C 1-4烷基和C 1-4烷氧基的取代基取代的C 1-6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M1 / M2受体涉及的指征的药物，例如精神分裂症。

9. 发明授权

US06103715A Dopamine receptor ligands 失效
标题翻译：多巴胺受体配体
公开(公告)号：US06103715A
公开(公告)日：2000-08-15
申请号：US139715
申请日：1998-08-25
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
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; andE 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独立地选择，任选取代的饱和或不饱和的5-或6-元，均 - 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

US5968478A N- methyl piperazine compounds having dopamine receptor affinity 失效
标题翻译：具有多巴胺受体亲和力的N-甲基哌嗪化合物
公开(公告)号：US5968478A
公开(公告)日：1999-10-19
申请号：US948051
申请日：1997-10-09
申请人： Jian-Min Fu , Sumanas Rakhit
发明人： Jian-Min Fu , Sumanas Rakhit
IPC分类号： C07D243/38 , C07D267/18 , C07D337/14 , A61K51/00 , A61M36/14
CPC分类号： C07D267/18 , C07D243/38 , C07D337/14
摘要： Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein X.sub.1 is selected from CH.sub.2, NH, O and S;X.sub.2 -- is selected from CH=, CH.sub.2 --, and N=;R.sub.1 to R.sub.8 are each independently selected from H, C.sub.1-4 alkyl, halo, cyano, nitro and halo-substituted C.sub.1-4 alkyland 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X 1选自CH 2，NH，O和S; X2-选自CH =，CH 2 - 和N =; R 1至R 8各自独立地选自H，C 1-4烷基，卤素，氰基，硝基和卤素取代的C 1-4烷基及其酸加成盐，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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