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1. 发明授权

US5266599A 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
标题翻译：（+） - 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。

2. 发明授权

US5245080A (+)-1-[(3 ,4,5-trimethoxy)-benzyloxymethyl]-1-phenyl-N,N-dimethyl-N-propylamine, process for preparing it and its therapeutical use 失效
标题翻译：（+） - 1 - [（3,4,5-三甲氧基） - 苄氧基甲基] -1-苯基-N，N-二甲基-N-丙胺，其制备方法及其治疗用途
公开(公告)号：US5245080A
公开(公告)日：1993-09-14
申请号：US931957
申请日：1992-08-19
申请人： Gilbert G. Aubard , Alain A. Calvet , Henri Jacobelli , Jean-Louis Junien , Xavier B. Pascaud
发明人： Gilbert G. Aubard , Alain A. Calvet , Henri Jacobelli , Jean-Louis Junien , Xavier B. Pascaud
IPC分类号： C07C217/48
CPC分类号： C07C217/48
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。

3. 发明授权

US5236947A Propanamines, their pharmacological properties and their application as an antidiarrheal 失效
标题翻译：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
申请人： Alain Calvet , Agnes Grouhel , Henri Jacobelli , Jean-Louis Junien , Xavier Pascaud
发明人： Alain Calvet , Agnes Grouhel , Henri Jacobelli , Jean-Louis Junien , Xavier Pascaud
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。

4. 发明授权

US5143938A Propanamines, their pharmacological properties and their application for therapeutic in particular antidiarrheal, purposes 失效
标题翻译：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
申请人： Alain Calvet , Agnes Grouhel , Henri Jacobelli , Jean-Louis Junien , Xavier Pascaud
发明人： Alain Calvet , Agnes Grouhel , Henri Jacobelli , Jean-Louis Junien , Xavier Pascaud
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。

5. 发明授权

US5326784A Cycloalkylalkylamines which are sigma-receptor ligands and their application in therapy 失效
标题翻译：作为σ-受体配体的环烷基烷基胺及其在治疗中的应用
公开(公告)号：US5326784A
公开(公告)日：1994-07-05
申请号：US99299
申请日：1993-07-29
申请人： Jean-Louis Junien , Alain Calvet , Henri Jacobelli , Francois Roman
发明人： Jean-Louis Junien , Alain Calvet , Henri Jacobelli , Francois Roman
IPC分类号： A61K31/13 , A61K31/15 , A61K31/275 , A61K31/35 , A61K31/352 , A61K31/357 , A61P1/04 , A61P25/00 , A61P25/02 , A61P25/18 , C07C211/38 , C07C215/42 , C07C225/18 , C07C251/44 , C07D311/22 , C07D311/32 , C07D311/68 , C07D317/72 , C07D493/10 , A61K31/135 , C07C211/19 , C07D311/74
CPC分类号： C07D317/72 , C07C215/42 , C07C225/18 , C07C251/44 , C07D311/22 , C07D493/10 , C07C2101/02 , C07C2101/04 , C07C2101/14 , C07C2102/08 , C07C2102/10 , C07C2102/12
摘要： New cycloalkylalkylamines which are sigma-receptor ligands of formule (I) ##STR1## in which: R.sub.1 is H or lower alkyl; X and Y are H, OH, lower alkyl, lower alkoxy, halogen or nitrile; V.sub.1 and V.sub.2 together form a double bond attached to an oxygen atom or to a hydroxyimino radical, or are linked as an ethylenedioxy chain; A represents a valency bond, an oxygen atom, a methylene or an ethylene group; m is equal to 0, 1 or 2; n has the value of an integer from 1 to 5. Psychotropic drug which is also useful in gastroenterology.
摘要翻译：新的环烷基烷基胺，其是式（I）的σ-受体配体。其中：R 1是H或低级烷基; X和Y是H，OH，低级烷基，低级烷氧基，卤素或腈; V1和V2一起形成连接到氧原子或羟基亚氨基的双键，或者作为亚乙二氧基链连接; A表示价键，氧原子，亚甲基或亚乙基; m等于0,1或2; n具有从1到5的整数的值。精神药物也可用于胃肠病学。

6. 发明申请

US20050245548A1 Alkynylated fused ring pyrimidine compounds 审中-公开
标题翻译：炔烃基稠环嘧啶化合物
公开(公告)号：US20050245548A1
公开(公告)日：2005-11-03
申请号：US11148880
申请日：2005-06-09
申请人： Bernard Gaudilliere , Henri Jacobelli , Joseph Picard , Michael Wilson
发明人： Bernard Gaudilliere , Henri Jacobelli , Joseph Picard , Michael Wilson
IPC分类号： A61K31/517 , A61K31/519 , A61P1/02 , A61P1/04 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P19/10 , A61P27/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D239/96 , C07D403/06 , C07D471/04 , C07D487/04 , C07D521/00 , C07F7/18
CPC分类号： C07D231/12 , A61K31/517 , C07D233/56 , C07D239/96 , C07D249/08 , C07D403/06 , C07D471/04 , C07D487/04 , C07F7/1804
摘要： A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N═X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.
摘要翻译：选自式（I）的化合物的化合物：其中W 1代表O，S或-NR 3，其中R 3表示氢，烷基，OH或CN; W 2表示选自氢，CF 3，NH 2，单烷基氨基，二烷基氨基，烷基，烯基，炔基，芳基，芳基烷基，环烷基烷基，杂环，这些基团任选被取代，或者W 1和W 2 2一起形成式-NX 4 -W _{3 < - >如描述中所定义，X 1，X 2和X 3表示N或C任选取代的n 是0至8，Z表示-CR 12 R 13，其中R 12和R 13定义同上在描述中，A表示环系，基团R 2表示氢或如说明书中定义的各种化学基团，q为0至7; R 1表示氢，烷基，烯基，炔基或环系，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐和药物产品含有它们的特异性抑制剂可用作13型基质金属蛋白酶的特异性抑制剂。}

7. 发明授权

US06962922B2 Alkynylated quinazoline compounds 失效
标题翻译：炔烃基喹唑啉化合物
公开(公告)号：US06962922B2
公开(公告)日：2005-11-08
申请号：US10269197
申请日：2002-10-11
申请人： Bernard Gaudilliere , Henri Jacobelli , Joseph Armand Picard , Michael William Wilson
发明人： Bernard Gaudilliere , Henri Jacobelli , Joseph Armand Picard , Michael William Wilson
IPC分类号： C07D239/96 , C07D403/06 , C07D471/04 , A61K31/517 , A61P19/02 , C07D401/10
CPC分类号： C07D403/06 , C07D239/96 , C07D471/04
摘要： A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N═X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.
摘要翻译：选自式（I）的化合物的化合物：其中W 1代表O，S或-NR 3，其中R 3表示氢，烷基，OH或CN; W 2表示选自氢，CF 3，NH 2，单烷基氨基，二烷基氨基，烷基，烯基，炔基，芳基，芳基烷基，环烷基烷基，杂环，这些基团任选被取代，或者W 1和W 2 2一起形成式-NX 4 -W _{3 < - >如描述中所定义，X 1，X 2和X 3表示N或C任选取代的n 是0至8，Z表示-CR 12 R 13，其中R 12和R 13定义同上在描述中，A表示环系，基团R 2表示氢或如说明书中定义的各种化学基团，q为0至7; R 1表示氢，烷基，烯基，炔基或环系，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐和药物产品含有它们的特异性抑制剂可用作13型基质金属蛋白酶的特异性抑制剂。}

8. 发明授权

US06849637B2 Triazolo compounds as MMP inhibitors 失效
标题翻译：三唑酚化合物作为MMP抑制剂
公开(公告)号：US06849637B2
公开(公告)日：2005-02-01
申请号：US10075654
申请日：2002-02-14
申请人： Charles Andrianjara , Francine Breuzard , Bernard Gaudilliere , Henri Jacobelli
发明人： Charles Andrianjara , Francine Breuzard , Bernard Gaudilliere , Henri Jacobelli
IPC分类号： A61K31/519 , A61P1/02 , A61P1/04 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04
摘要： A compound selected from those of formula (I): in which: W represents N or C—R1; in which R1 is as defined in the description, X represents N or C—R2 in which R2 is as defined in the description, Y represents a group selected from oxygen, sulfur, —NH, and —Nalkyl, Z represents a group selected from oxygen, sulphur, —NR8 in which R8 is as defined in the description, and optionally carbon depending the definition of Y, n is an integer from 0 to 8 inclusive, Z1 represents a group —CR9R10 wherein R9 and R10, are as defined in the description, which group contains optionally multiple bonds or heteroatomes, A represents a cyclic group, m is an integer from 0 to 7 inclusive, the group(s) R4 is (are) as defined in the description, R3 represents a group selected from hydrogen, alkyl, alkenyl, alkynyl, and the group of formula: in which p, Z2, B, q, and R13 are as defined in the description, optionally, its racemic forms, isomers thereof, N-oxydes thereof, and its the pharmaceutically acceptable salts thereof, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix mettaloprotease.
摘要翻译：选自式（I）的化合物：其中：W表示N或C-R 1; 其中R1如说明书中所定义，X表示N或C-R2，其中R2如说明书中所定义，Y表示选自氧，硫，-NH和-N烷基的基团，Z表示选自氧，硫，-NR 8，其中R8如说明书中所定义，可选地取决于Y的定义，n为0至8的整数，其中Z 1为基团-CR 9 R 10，其中R 9和R 10如描述，该组包含任选的多个键或杂原子，A表示环状基团，m是0至7的整数，包括端值，其中R 4是如在说明书中所定义的（是），R 3表示选自氢，烷基，烯基，炔基和下式的基团：其中p，Z2，B，q和R13如说明书中所定义，任选地，其外消旋形式，异构体，其N-氧化物及其其药学上可接受的盐和含有它们的药物可用作特异性抑制剂的13型基质金属蛋白酶。

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