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1. 发明授权

US06479531B1 Gastrin and cholecystokinin receptor ligands 失效
标题翻译：胃泌素和胆囊收缩素受体配体
公开(公告)号：US06479531B1
公开(公告)日：2002-11-12
申请号：US09831385
申请日：2001-08-02
申请人： Sarkis Barret Kalindjian , Ildiko Maria Buck , Ian Duncan Linney , Paul Trevor Wright , Iain Mair McDonald , Katherine Isobel Mary Steel , Robert Antony David Hull , Sonia Patricia Roberts , John David Gaffen , Jeremy Gilbert Vinter , Martin Keith Walker , James Whyte Black , Gillian Fairfull Watt , Elaine Anne Harper , Nigel Paul Shankley , Matthew John Tozer , David John Dunstone , Michael John Pether , Elliot James Lilley , David Andrew Sykes , Caroline Minli Rachel Low , Eric Peter Griffin , Laurence Wright
发明人： Sarkis Barret Kalindjian , Ildiko Maria Buck , Ian Duncan Linney , Paul Trevor Wright , Iain Mair McDonald , Katherine Isobel Mary Steel , Robert Antony David Hull , Sonia Patricia Roberts , John David Gaffen , Jeremy Gilbert Vinter , Martin Keith Walker , James Whyte Black , Gillian Fairfull Watt , Elaine Anne Harper , Nigel Paul Shankley , Matthew John Tozer , David John Dunstone , Michael John Pether , Elliot James Lilley , David Andrew Sykes , Caroline Minli Rachel Low , Eric Peter Griffin , Laurence Wright
IPC分类号： C07D40306
CPC分类号： C07D233/64 , C07D207/34 , C07D233/88 , C07D233/90 , C07D263/34 , C07D277/56 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04
摘要： Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently ═N—, —N(R5)—═CH—, —S— or —O—. n is from 1 to 4; R1 is H or C1 to C15 hydrocarbyl R2 is selected from H, Me, Et, Pr and OH, R3 is selected from H, Me, Et and Pr; or (when n is greater than 1) each R3 is independently selected from H, Me, Et and Pr, or two R3 groups on neighbouring carbon atoms are linked to form a C3 to C6 carbocylic ring, or R2 and R3 on the same carbon atom together represent an ═O group; R4 is C1 to C15 hydrocarbyl Z is —(NR7)a—CO—(NR8)b— (wherein a is 0 or 1, b is 0 or 1, —CO—NR7—CH2—CO—NR8—, —CO—O—, —CH2—CH2—, —CH═CH—, —CH2—NR8— or a bond; Q is —R9V, or (II), (wherein R9 is —CH2—; —CH2—CH2—; or (III), R9 and R8, together with the nitrogen atom to which R8 is attached, form a piperidine or pyrrolidine ring which is substituted by V; V is —CO—NH—SO2—Ph, —SO2—NH—CO—Ph, —CH2OH, or a group of the formula —R10U, (wherein U is —COOH, tetrazolyl, —CONHOH— or —SO3H; and R10 is a bond; C1 to C6 hydrocarbylene, —O—(C1 to C3 alkylene)—; —SO2NR11—CHR12—; —CO—NR11—CHR12—, or —NH—(CO)c—CH2—, c being 0 or 1).
摘要翻译：式（I）化合物及其药学上可接受的盐是胃泌素和/或胆囊收缩素受体的配体。 X和Y独立地为= N-，-N（R 5） - = CH - ， - S-或-O-。 n为1至4; R1为H或C1至C15烃基R2选自H，Me，Et，Pr和OH，R3选自H，Me，Et和Pr; 或（当n大于1时），每个R 3独立地选自H，Me，Et和Pr，或相邻碳原子上的两个R 3基团连接形成C 3至C 6碳环，或在相同碳上的R 2和R 3 原子一起代表a = O组; R4为C1〜C15烃基Z为 - （NR7）a-CO-（NR8）b-（其中a为0或1，b为0或1，-CO-NR7-CH2-CO-NR8-，-CO- O，-CH 2 -CH 2 - ， - CH = CH - ， - CH 2 -NR 8 - 或键; Q为-R 9 V或（II）（其中R 9为-CH 2 - ; -CH 2 -CH 2 - III），R9和R8与R8所连接的氮原子一起形成被V取代的哌啶或吡咯烷环; V是-CO-NH-SO 2-Ph，-SO 2 -NH-CO-Ph， -CH 2 OH或式-R 10 U的基团（其中U为-COOH，四唑基，-CONHOH-或-SO 3 H; R 10为键; C 1至C 6亚烃基，-O-（C 1至C 3亚烷基） - ; -SO2NR11-CHR12-; -CO-NR11-CHR12-或-NH-（CO）c-CH2-，c为0或1）。

2. 发明授权

US6057311A Benzodiazonine derivatives binding to cholecystokinin or gastrin receptors 失效
标题翻译：苯并噻嗪衍生物与胆囊收缩素或胃泌素受体结合
公开(公告)号：US6057311A
公开(公告)日：2000-05-02
申请号：US142533
申请日：1998-10-26
申请人： Sarkis Barret Kalindjian , Iain Mair McDonald , Michael John Pether , Caroline Minli Rachel Low , Katherine Isobel Mary Steel , Ian Duncan Linney
发明人： Sarkis Barret Kalindjian , Iain Mair McDonald , Michael John Pether , Caroline Minli Rachel Low , Katherine Isobel Mary Steel , Ian Duncan Linney
IPC分类号： A61K38/00 , C07D225/06 , C07D245/06 , C07D403/12 , C07K5/06 , C07K5/078 , A61K31/395 , C07D255/04
CPC分类号： C07D403/12 , C07D225/06 , C07D245/06 , C07K5/06139 , C07K5/06191 , A61K38/00
摘要： Compounds of the formula whereinone of U and V is --CHR.sup.2 --, and the other of U and V is selected from --N(COR.sup.4)--, --CH(COR.sup.4)--, --N(SO.sub.2 R.sup.4)-- and --CH(SO.sub.2 R.sup.4)--,and pharmaceutically acceptable salts thereof are ligands at gastrin and/or cholecystokinin receptors.
摘要翻译： PCT No.PCT / GB97 / 00632 Sec。 371日期：1998年10月26日 102（e）日期1998年10月26日PCT 1997年3月7日PCT公布。公开号WO97 / 32860 PCT 日期：1997年9月12日下式的化合物其中U和V之一为-CHR2-，U和V中的另一个选自-N（COR 4） - ， - CH（COR 4） - ， - N（SO 2 R 4） - 和-CH（SO 2 R 4） - 及其药学上可接受的盐是胃泌素和/或胆囊收缩素受体的配体。

3. 发明授权

US06878736B1 Histamine H3 receptor ligands 失效
标题翻译：组胺H3受体配体
公开(公告)号：US06878736B1
公开(公告)日：2005-04-12
申请号：US09622544
申请日：1999-02-15
申请人： Sarkis Barret Kalindjian , Ildiko Maria Buck , Ian Duncan Linney , Gillian Fairfull Watt , Elaine Anne Harper , Nigel Paul Shankley
发明人： Sarkis Barret Kalindjian , Ildiko Maria Buck , Ian Duncan Linney , Gillian Fairfull Watt , Elaine Anne Harper , Nigel Paul Shankley
IPC分类号： C07D295/12 , A61K31/395 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/445 , A61K31/4453 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/5375 , A61P1/04 , A61P25/00 , A61P25/20 , A61P25/24 , A61P43/00 , C07D207/08 , C07D207/09 , C07D211/24 , C07D211/28 , C07D215/48 , C07D295/088 , C07D295/092 , C07D295/13 , C07D309/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12
CPC分类号： C07D207/08 , C07D211/24 , C07D295/088 , C07D295/13 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12
摘要： Compounds of formula (I) (and pharmaceutically acceptable salts thereof) are histamine H3 receptor ligands. A in the formula represents (CH2)m, m being from 1 to 3; B is (CH2)n, n being from 1 to 3; x is from 0 to 2; R1 is C1 to C10 hydrocarbyl, in which up to 2 carbon atoms may be replaced by O, S or N; and up to 2 hydrogen atoms may be replaced by halogen; R2 is H or C1 to C15 hydrocarbyl, in which up to 3 carbon atoms may be replaced by O, S or N, and up to 3 hydrogen atoms may be replaced by halogen; R3 is absent when —Y—Z—R2 is attached to W, or is H or C1 to C7 hydrocarbyl when —Y—Z—R2 is not attached to W; W is nitrogen; X is —CH2—, —O— or —NR4—, R4 being H or C1 to C3 alkyl; Y replaces a hydrogen atom on any of A, B, W and X, and is C2 to C10 alkylene, in which one non-terminal carbon atom may be replaced by O; and Z is (II), (III), (IV), (V), (VI), or (VII) wherein R5, R6 and R7 are independently H or C1 to C15 hydrocarbyl, in which up to 3 carbon atoms may be replaced by O or N, and up to 3 hydrogen atoms may be replaced by halogen, and Q is H or methyl, or Q is linked to R5 or R7 to form a five-membered ring or Q is linked to R2 to form a six-membered ring
摘要翻译：式（I）化合物（及其药学上可接受的盐）是组胺H3受体配体。式中的A表示（CH 2）m，m为1〜3; B为（CH 2）n，n为1至3; x为0〜2; R 1是C 1至C 10烃基，其中最多2个碳原子可以被O，S或N代替; 并且多达2个氢原子可被卤素取代; R 2是H或C 1至C 15烃基，其中最多3个碳原子可以被O，S或N代替，并且多达3个氢原子可以被卤素取代; 当-Y-Z-R2连接到W时，R 3不存在，或者当-Y-Z-R 2不连接到W时为H或C 1至C 7的烃基; W是氮; X是-CH 2 - ， - O-或-NR 4 - ，R 4是H或C 1至C 3烷基; Y代替A，B，W和X中的任一个上的氢原子，并且是C2-C10亚烷基，其中一个非末端碳原子可以被O取代; 并且Z为（II），（III），（IV），（V），（VI）或（VII）其中R 5，R 6和R 7独立地为H或C 1至C 15烃基，其中最多3个碳原子可以被O或N替代，并且多达3个氢原子可被卤素取代，Q是H或甲基，或Q连接到R 5或R 7至形成五元环或Q与R 2连接形成六元环

4. 发明授权

US06355665B1 1H-4(5)-substituted imidazole derivatives, their preparation and their use as histamine H3 receptor ligands 失效
标题翻译： 1H-4（5） - 取代咪唑衍生物，其制备及其作为组胺H3受体配体的用途
公开(公告)号：US06355665B1
公开(公告)日：2002-03-12
申请号：US09463012
申请日：2000-03-14
申请人： Matthew John Tozer , Sarkis Barret Kalindjian , Ian Duncan Linney , Katherine Isabel Mary Steel , Michael John Pether , Tracey Cooke
发明人： Matthew John Tozer , Sarkis Barret Kalindjian , Ian Duncan Linney , Katherine Isabel Mary Steel , Michael John Pether , Tracey Cooke
IPC分类号： C07D23354
CPC分类号： C07D233/64 , C07D417/04
摘要： A compound of the formula wherein R2 is an optionally substituted Cz to Cg alkylene or alkylene chain; R3 is C2 to C15 optionally substituted hydrocarbyl; X is a bond or —NR4—, wherein R4 is hydrogen or non-aromatic C1 to C5 optionally substituted hydrocarbyl, or aryl(C1 to C3)alkyl, or a pharmaceutically acceptable salt thereof. A method of modifing histamine activity in a patient comprising administering to said patient a pharmaceutical composition containing an effective amount of a compound of formula wherein R1 is selected from C1 to C6 alkyl, C1 to C6 alkoxy, C1 to C6 alkylthio, carboxy, carboxy(C1 to C6)alkyl, formyl, C1 to C6 alkylcarbonyl, C1 to C6 alkylcarbonylalkoxy, nitro, trihalomethyl, hydroxy, amino, C1 to C6 alkylcarbonylalkoxy, nitro, trihalomethyl, hydroxy, amino, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, aryl, C1 to C6 alkylaryl, halo, sulfamoyl and cyano; R2 is optionally substituted C2 to C20 hydrocarbylene, in which one or more hydrogen atoms may be replaced by halogen atoms and up to 6 carbon atoms may be replaced by oxygen or nitrogen atoms, R2 being in the form of an optionally substituted C2 to C8 alkylene or alkenylene chain; R3 is hydrogen or C1 to C15 optionally substituted hydrocarbyl; X is a bond or —NR4—; and a is from 0 to 2, or a pharmaceutically acceptable salt thereof.
摘要翻译：化学式R 2的化合物是任选取代的C 1至C 8亚烷基或亚烷基链; R3是C2至C15任选取代的烃基; X是键或-NR 4 - ，其中R 4是氢或非芳族C 1至C 5任选取代的烃基或芳基（C 1至C 3）烷基或其药学上可接受的盐。1，一种修饰患者组胺活性的方法，向所述患者施用含有有效量的蛔虫素R1化合物的药物组合物选自C1至C6烷基，C1至C6烷氧基，C1至C6烷硫基，羧基，羧基（C1至C6）烷基，甲酰基，C1至C6 烷基羰基，C 1至C 6烷基羰基烷氧基，硝基，三卤代甲基，羟基，氨基，C 1至C 6烷基羰基烷氧基，硝基，三卤甲基，羟基，氨基，C 1至C 6烷基氨基，二（C 1至C 6烷基）氨基，芳基，C 1至C 6烷基芳基，，氨磺酰基和氰基; R2是任选取代的C 2至C 20亚烃基，其中一个或多个氢原子可以被卤素原子取代，并且最多6个碳原子可被氧或氮原子取代，R 2为任选取代的C 2至C 8亚烷基或亚烯基链; R 3是氢或C 1至C 15任选取代的烃基; X是键或-NR4-; 和a为0至2，或其药学上可接受的盐。

5. 发明授权

US07105558B2 Gastrin and cholecystokinin receptor lignads (iv) 失效
公开(公告)号：US07105558B2
公开(公告)日：2006-09-12
申请号：US10275615
申请日：2001-05-04
申请人： Ian Duncan Linney , Iain Mair McDonald
发明人： Ian Duncan Linney , Iain Mair McDonald
IPC分类号： A61K31/4192 , C07D249/06 , A61P1/04
CPC分类号： C07D249/04 , A61K31/4192 , A61K45/06 , A61K2300/00
摘要： Compounds of the formula (I) or (II) and their pharmaceutically acceptable salts are ligands at gastrin and/or chole-cystokinin receptors n is from 1 to 4; R4 is C1 to C15 hydrocarbyl wherein up to two C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; Z is —(NR5)a—CO—(NR6)b-(wherein a is 0 or 1, b is 0 or 1, and R5 and R6 are independently selected from H, Me, Et, Pr, Bn), —CO—NR5—CH2—CO—NR6—, —CO—O—, —CH2—CH2—, —CH═CH—, CH2—NR6— or a bond; Q is R7V, or(a) wherein R7 is —CH2—; —CH2—; or(b) R7 and R6, together with the nitrogen atom to which R6 is attached, form a piperidine or pyrrolidine ring which is substituted by V; V is —CO—NH—SO2-Ph, —SO2—NH—CO-Ph, CH2OH, or a group of the formula —R8U, (wherein U is —COOH, tetrazolyl, —CONHOH— or —SO3H; and R8 is a bond; C1 to C6 hydrocarbylene, optionally substituted by hydroxy, amino or acetamino; —O—(C1 to C3 alkylene)-; —SO2NR9—CHR10—; —CO—NR9—CHR10—, R9 and R10 being independently selected from H and methyl; or —NH—(CO)c—CH2—, c being 0 or 1); m is 1 or 2; q is from 0 to 2, with the proviso that q is 1 or 2 when Z is a bond); Compositions comprising a compound of formula (I) or (II) are also described.

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