-
公开(公告)号：US5389686A
公开(公告)日：1995-02-14
申请号：US91691
申请日：1993-07-13
IPC分类号： C07C217/48 , A61K31/135
CPC分类号： C07C217/48
摘要： Process for the treatment of painful syndromes, especially local and/or visceral, consisting in the parenteral or topical administration of a therapeutically effective quantity of the (-) tartrate of (+)-(R)-1-[(3,4,5-trimethoxy)benzyloxymethyl]-1-phenyl-N,N-dimethyl-n-propylamine.
摘要翻译： 用于治疗疼痛综合征，特别是局部和/或内脏的方法，其组合在肠胃外或局部施用治疗有效量的（+） - （R）-1 - [（3,4,5-三甲基 - 5-三甲氧基）苄氧基甲基] -1-苯基-N，N-二甲基 - 正丙胺。
-
2.发明授权Propanamines, their pharmacological properties and their application as an antidiarrheal 失效丙胺，其药理特性及其作为止泻药的应用
公开(公告)号：US5236947A
公开(公告)日：1993-08-17
申请号：US899712
申请日：1992-06-17
IPC分类号： C07C205/04 , C07C205/09 , C07C205/32 , C07C205/45 , C07C217/72 , C07C225/16 , C07D317/28
CPC分类号： C07C225/16 , C07C205/04 , C07C205/09 , C07C205/32 , C07C205/45 , C07C217/72 , C07D317/28
摘要： The present invention relates to propanamines of general formula (I) ##STR1## in which: R1 is a phenyl radical optionally mono-, di- or trisubstituted in an identical or different manner with halogen atoms, or lower alkyl, lower haloalkyl or lower alkoxy radicals;R2 is a lower alkyl radical,R3 and R4 are a hydrogen atom or a lower alkyl, lower alkenyl or lower cycloalkyalkyl radical,R5 is a 5-to 7-membered cycloalkyl radical or a phenyl radical, andW represents a heterocycle .dbd.C[Q--(CH.sub.2).sub.n --Q] in which Q is an oxygen or sulfur atom and n is 2 or 3,and their acid addition salts with pharmaceutically acceptable acids. The invention also relates to antidiarrheal pharmaceutical compositions comprising the claimed propanamines.
摘要翻译： 本发明涉及通式（I）的丙胺，其中：R 1是任选地以与卤素原子相同或不同的方式单，二或三取代的苯基，或低级烷基低级卤代烷基 或低级烷氧基; R2是低级烷基，R3和R4是氢原子或低级烷基，低级烯基或低级环烷基，R5是5-至7-元环烷基或苯基，W表示杂环= C [ Q-（CH2）nQ]其中Q是氧或硫原子，n是2或3，以及它们与药学上可接受的酸的酸加成盐。 本发明还涉及包含所要求保护的丙胺的止泻药物组合物。
-
3.发明授权Propanamines, their pharmacological properties and their application for therapeutic in particular antidiarrheal, purposes 失效丙氨酸，其药理学特性及其在特异性抗病毒治疗中的应用，目的
公开(公告)号：US5143938A
公开(公告)日：1992-09-01
申请号：US660873
申请日：1991-02-26
IPC分类号： A61K31/135 , A61K31/335 , A61K31/357 , A61K31/385 , C07C205/04 , C07C205/09 , C07C205/32 , C07C205/45 , C07C215/30 , C07C217/72 , C07C225/16 , C07C225/18 , C07C323/29 , C07D317/28 , C07D339/06
CPC分类号： C07C225/16 , C07C205/04 , C07C205/09 , C07C205/32 , C07C205/45 , C07C217/72 , C07D317/28
摘要： A compound which is a propanamine of general formula (I) ##STR1## in which: R1 is a phenyl radical optionally mono-, di- or trisubstituted,or is a 5- or 6-membered monocyclic heteroaryl radical in which the single heteroatom is nitrogen, oxygen or sulfur,R2 is a lower alkyl radical,R3 and R4 are a hydrogen atom or a lower alkyl, lower alkenyl or lower cycloalkylalkyl radical,or, together with the nitrogen atom to which they are attached, form a saturated 5- to 6-membered heterocycle comprising only one heteroatom,R5 is a 5- to 7-membered cycloalkyl radical, a phenyl radical or a 5- or 6-membered monocyclic heteroaryl radical,and W representsa group .dbd.CH--QH,or a heterocycle .dbd.C[Q--(CH2)n--Q],or a group .dbd.C.dbd.Q, in which groupsQ is an oxygen or sulfur atom,n has the value 2 or 3,W being .dbd.C.dbd.Q only when R3 and R4 are not both hydrogen, and their additions salts with pharmaceutically acceptable acids.A pharmaceutical composition comprising a compound of general formula (I) with the above definitions for the treatment of diarrheal states.
摘要翻译： 作为通式（I）的丙胺的化合物，其中：R 1是任选被一个，二或三取代的苯基，或是5或6元单环杂芳基，其中 单个杂原子是氮，氧或硫，R2是低级烷基，R3和R4是氢原子或低级烷基，低级烯基或低级环烷基烷基，或者与它们相连的氮原子一起形成 饱和的5至6元杂环，仅包含一个杂原子，R 5为5-至7-元环烷基，苯基或5-或6-元单环杂芳基，W表示基团= CH-QH， 或杂环= C [Q-（CH 2）nQ]或基团= C = Q，其中基团Q是氧或硫原子，n具有值2或3，W仅当R 3为 和R4不同时为氢，并且它们与药学上可接受的酸相加。 一种药物组合物，其包含具有上述定义用于治疗腹泻状态的通式（I）的化合物。
-
4.发明授权Use of (+)-1-[(3,4,5-trimethoxy)-benzyloxymethyl]-1-phenyl-N,N-dimethyl-n-propy lamine to increase gastric discharge in a subject 失效（+） - 1 - [（3,4,5-三甲氧基） - 苄氧基甲基] -1-苯基-N，N-二甲基正丙胺用于增加受试者胃排出量
公开(公告)号：US5266599A
公开(公告)日：1993-11-30
申请号：US931994
申请日：1992-08-19
申请人： Gilbert G. Aubard , Alain P. Calvet , Agnes Grouhel , Henri Jacobelli , Jean-Louis Junien , Xavier B. Pascaud , Francois J. Roman
发明人： Gilbert G. Aubard , Alain P. Calvet , Agnes Grouhel , Henri Jacobelli , Jean-Louis Junien , Xavier B. Pascaud , Francois J. Roman
IPC分类号： C07C217/48 , A61K31/135
CPC分类号： C07C217/48 , Y10S514/928
摘要： (+)-1-[(3,4,5-trimethoxy)-benzyloxymethyl]-1-phenyl-N,N-dimethyl-n-propylamine of formula ##STR1## is a medicament of use in gastroenterology.
摘要翻译： 式（IMA）的（+） - [（3,4,5-三甲氧基） - 苄氧基甲基] -1-苯基-N，N-二甲基正丙胺是用于胃肠病学的药物。
-
5.发明授权Enantiomers derived from (S)-2-amino-2-(3,4-dichlorobenzyl)-1-propanol, their use and method of preparation 失效衍生自（S）-2-氨基-2-（3,4-二氯苄基）-1-丙醇的对映异构体，其用途和制备方法
公开(公告)号：US5348980A
公开(公告)日：1994-09-20
申请号：US58698
申请日：1993-05-03
申请人： Gilbert Aubard , Jacques Bure , Alain Calvet , Claude J. Gouret , Agnes Grouhel , Jean-Louis Junien
发明人： Gilbert Aubard , Jacques Bure , Alain Calvet , Claude J. Gouret , Agnes Grouhel , Jean-Louis Junien
IPC分类号： C07C219/22 , C07C233/54 , C07D213/80 , C07D295/084 , A61K31/135 , C07C215/00
CPC分类号： C07D213/80 , C07C219/22 , C07C233/54 , C07D295/092 , C07C2101/08 , C07C2101/14
摘要： Enantiomers of (S) configuration of formula (I) ##STR1## in which R is H or methyl, with antiallergic and in particular antihistaminic activity, useful as medicinal products.
摘要翻译： 式（I）的（S）构型的对映异构体（I）其中R为H或甲基，具有抗过敏能力，特别是抗组胺活性，可用作药用产品。
-
6.发明授权N-cycloalkylalkylamines, process for their preparation, their use as medicament and their synthesis intermediates 失效N-环烷基烷基胺，其制备方法，它们作为药物及其合成中间体的用途
公开(公告)号：US5034419A
公开(公告)日：1991-07-23
申请号：US484403
申请日：1990-02-26
申请人： Gilbert G. Aubard , Alain P. Calvet , Jean-Pierre DeFaux , Claude J. Gouret , Agnes M. Grouhel , Henry L. Jacobelli , Jean-Louis Junien , Xavier Pascaud , Francois F. Roman , James P. Hudspeth , Yuan Lin
发明人： Gilbert G. Aubard , Alain P. Calvet , Jean-Pierre DeFaux , Claude J. Gouret , Agnes M. Grouhel , Henry L. Jacobelli , Jean-Louis Junien , Xavier Pascaud , Francois F. Roman , James P. Hudspeth , Yuan Lin
IPC分类号： A61K31/135 , A61P1/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , C07C57/42 , C07C57/58 , C07C67/00 , C07C209/00 , C07C211/27 , C07C211/28 , C07C211/29 , C07C217/58 , C07C217/62 , C07C217/64 , C07C233/03 , C07C233/05 , C07C233/08 , C07C233/12 , C07C233/13 , C07C233/21 , C07C241/00 , C07C255/24 , C07C255/30 , C07C255/42 , C07C265/06 , C07C265/08
CPC分类号： C07C265/08 , C07C211/28 , C07C211/29 , C07C217/58 , C07C217/62 , C07C233/03 , C07C233/05 , C07C233/12 , C07C233/13 , C07C233/21 , C07C255/42 , C07C2101/02 , C07C2101/04 , C07C2101/08 , Y10S514/925 , Y10S514/926 , Y10S514/927
摘要： N-Cycloalkylalkylamines of formula I: ##STR1## in which: R1 is phenyl which is optionally mono-, di- or trisubstituted by halogens or lower alkyl, haloalkyl or lower alkoxy radicals, or is an aromatic heterocyclic radical having 5 to 7 chain members, in which the hetero atom is nitrogen, oxygen or sulphur,R2 is lower alkyl,R3 is hydrogen or lower alkyl,m has the value of 1 or 2,R4 is cycloalkyl --CH(CH2)n, in which a carbon atom may carry a radical Rx, which is lower alkyl or phenyl; and in which n has the values from 2 to 5,R5 is phenyl, which can be mono-, di- or trisubstituted by halogens or by lower alkoxy radicals, andQ represents an ethylene-1,2-diyl group --CH.dbd.CH-- or a cyclopropane-1,2-diyl group ##STR2##
摘要翻译： 式I的N-环烷基烷基胺：其中：R 1是任选被卤素或低级烷基，卤代烷基或低级烷氧基单取代，二取代或三取代的苯基，或是具有5-7个链的芳族杂环基 成员，其中杂原子是氮，氧或硫，R2是低级烷基，R3是氢或低级烷基，m的值是1或2，R4是环烷基-CH（CH2）n，其中碳原子 可以携带基团Rx，它是低级烷基或苯基; 并且其中n具有2至5的值，R 5是苯基，其可以被卤素或低级烷氧基单取代，二取代或三取代，并且Q表示乙烯-1,2-二基-CH = CH - 或环丙烷-1,2-二基
-
公开(公告)号：US08030335B2
公开(公告)日：2011-10-04
申请号：US11920141
申请日：2006-05-10
CPC分类号： A61K31/00 , A61K31/18 , A61K31/195 , Y10S514/866
摘要： The present invention generally relates to a novel therapeutical use of liver X receptor (LXR) agonsits. More specifically, the present invention relates to the use of LXR agonist for the preparation of a medicament useful for the treatment and/or the prevention of a disease associated with beta cells degeneration, such as diabetes, and a method for increasing ex vivo viability of pancreatic islet cells, comprising contacting said islet cells with a LXR agonist.
摘要翻译： 本发明一般涉及肝X受体（LXR）治疗的新型治疗用途。 更具体地说，本发明涉及LXR激动剂在制备可用于治疗和/或预防与β细胞变性相关的疾病（例如糖尿病）的药物中的用途，以及增加体内存活力的方法 胰岛细胞，包括使所述胰岛细胞与LXR激动剂接触。
-
公开(公告)号：US20100297761A1
公开(公告)日：2010-11-25
申请号：US12787881
申请日：2010-05-26
IPC分类号： C12N5/02
CPC分类号： A61K31/00 , A61K31/18 , A61K31/195 , Y10S514/866
摘要： A method of increasing the ex vivo viability of pancreatic islet cells comprising contacting the islet cells with a liver X receptor (LXR) agonist, particularly an LXRalpha agonist. Examples of especially useful LXR agonists include GW3965 and T0901317.
摘要翻译： 包括增加胰岛细胞的离体活力的方法，包括使胰岛细胞与肝X受体（LXR）激动剂，特别是LXRα激动剂接触。 特别有用的LXR激动剂的实例包括GW3965和T0901317。
-
公开(公告)号：US20100029575A1
公开(公告)日：2010-02-04
申请号：US12300610
申请日：2007-05-25
申请人： Jean-Louis Junien , Pierre J.M. Riviere , Claudio D. Schteingart , Javier Sueiras Diaz , Jerzy A. Trojnar , Todd W. Vanderah , Michael E. Lewis
发明人： Jean-Louis Junien , Pierre J.M. Riviere , Claudio D. Schteingart , Javier Sueiras Diaz , Jerzy A. Trojnar , Todd W. Vanderah , Michael E. Lewis
CPC分类号： C07K5/1016 , A61K38/00
摘要： Certain peptides which exhibit high selectivity for the kappa opioid receptor (KOR) versus the mu opioid receptor and little or no CYP3A4 inhibitory activity including tetrapeptides of four D-isomer amino acid residues having a C-terminus which is an N-oxide-substituted amide such, as H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl-N-oxide. A preferred compound, which has an affinity for the KOR at least 1,000 times its affinity for the mu opioid receptor and an IC50 for CYP3 A4 of greater than about 10 micromolar, is H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl-N-oxide
摘要翻译： 对于κ阿片样物质受体（KOR）与μ-阿片样物质受体显示出高选择性的某些肽，并且很少或没有CYP3A4抑制活性，包括具有C-末端的四个D-异构体氨基酸残基的四肽，其是N-氧化物取代的酰胺 如HD-Phe-D-Phe-D-Nle-D-Arg-NH-4-吡啶甲酰基-N-氧化物。 HD-Phe-D-Phe-D-Nle-D-D对于KOR具有对μ-阿片样物质受体的亲和力至少1000倍的亲和力以及大于约10微摩尔的CYP3A4的IC 50的优选化合物， Arg-NH-4-吡啶甲酰基-N-氧化物
-
10.发明授权Polypeptide derivatives of dog gastric lipase and pharmaceutical compositions containing same 失效狗胃脂肪酶的多肽衍生物和含有其的药物组合物
公开(公告)号：US05998189A
公开(公告)日：1999-12-07
申请号：US73674
申请日：1998-05-06
摘要： The present invention relates to polypeptide derivatives of dog gastric lipase as obtained by genetic engineering as well as to the nucleotide sequence encoding this recombinant DGL. It also relates to the use of this recombinant DGL for the production of pharmaceutical compositions intended especially for the treatment of pathologies linked to the insufficiency, or even the absence, of secretion of lipases in the body of an individual.
摘要翻译： 本发明涉及通过遗传工程获得的狗胃脂肪酶的多肽衍生物以及编码该重组DGL的核苷酸序列。 它还涉及这种重组DGL用于制备药物组合物的用途，该药物组合物特别用于治疗与个体身体中脂肪酶分泌不足或甚至不存在相关的病理学。
-
-
-
-
-
-
-
-
-
搜索结果
38 条记录 (耗时 0.022 秒)
