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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

US5795907A Gastin and CCK receptor ligands 失效
标题翻译：加斯汀和CCK受体配体
公开(公告)号：US5795907A
公开(公告)日：1998-08-18
申请号：US583008
申请日：1996-03-18
申请人： Sarkis Barret Kalindjian , Katherine Isobel Mary Steel , Michael John Pether , Jonathan Michael Richard Davies , Caroline Minli Rachel Low , Martin Lyn Hudson , Ildiko Maria Buck , Iain Mair McDonald , David John Dunstone , Matthew John Tozer
发明人： Sarkis Barret Kalindjian , Katherine Isobel Mary Steel , Michael John Pether , Jonathan Michael Richard Davies , Caroline Minli Rachel Low , Martin Lyn Hudson , Ildiko Maria Buck , Iain Mair McDonald , David John Dunstone , Matthew John Tozer
IPC分类号： C07C233/65 , C07C233/82 , C07C237/22 , C07C237/48 , C07D207/16 , C07D209/08 , C07D209/42 , C07D209/88 , C07D217/26 , C07D235/06 , C07D235/24 , C07D307/84 , C07D333/70 , C07D401/06 , C07D403/06 , C07D403/12 , C07D403/14 , C07D453/02 , C07D471/04 , A61K31/40 , A61K31/415 , C07D415/54
CPC分类号： C07D235/06 , C07C233/65 , C07C233/82 , C07C237/22 , C07C237/48 , C07D207/16 , C07D209/08 , C07D209/42 , C07D209/88 , C07D217/26 , C07D235/24 , C07D307/84 , C07D333/70 , C07D401/06 , C07D403/06 , C07D403/12 , C07D403/14 , C07D453/02 , C07D471/04 , C07C2103/74
摘要： Compounds of formula (Ia), (Ib), or (Ic), wherein A represents a group having two fused rings, or a group of formula (Id), R.sup.1.sub.(m) represents up to 6 substituents, K represents --O--, --S--, --CH.sub.2 --, --N(R.sup.2)-- or --N(COR.sup.2)--, in which R.sup.2 is H or C.sub.1 to C.sub.3 alkyl, W is a carbonyl, sulfonyl or sulfinyl group, provided that at least one of W and X contains carbonyl, Y and Z are as given in the description, and their pharmaceutically acceptable salts are ligands at CCK and/or gastrin receptors. ##STR1##
摘要翻译： PCT No.PCT / GB94 / 01741 Sec。 371日期：1996年3月18日 102（e）1996年3月18日PCT 1994年8月9日PCT PCT。公开号WO95 / 04720 日期：1995年2月16日，式（Ia），（Ib）或（Ic）的化合物，其中A表示具有两个稠合环的基团或式（Id）的基团，R 1（m） K表示-O - ， - S - ， - CH 2 - ， - N（R 2） - 或-N（COR 2） - ，其中R 2是H或C 1至C 3烷基，W是羰基，磺酰基或亚磺酰基， W和X中的至少一个含有羰基，Y和Z如说明书中给出，并且其药学上可接受的盐是CCK和/或胃泌素受体的配体。（Ia）（Ib）（Ic）（Id）

3. 发明授权

US5919829A Gastrin and cck receptor ligands 失效
标题翻译：胃泌素和cck受体配体
公开(公告)号：US5919829A
公开(公告)日：1999-07-06
申请号：US64849
申请日：1998-04-23
申请人： Sarkis Barret Kalindjian , Katherine Isobel Mary Steel , Michael John Pether , Jonathan Michael Richard Davies , Caroline Minli Rachel Low , Martin Lyn Hudson , Ildiko Maria Buck , Iain Mair McDonald , David John Dunstone , Matthew John Tozer
发明人： Sarkis Barret Kalindjian , Katherine Isobel Mary Steel , Michael John Pether , Jonathan Michael Richard Davies , Caroline Minli Rachel Low , Martin Lyn Hudson , Ildiko Maria Buck , Iain Mair McDonald , David John Dunstone , Matthew John Tozer
IPC分类号： A61K31/38 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/47 , A61K31/472 , A61P1/00 , A61P1/16 , A61P3/04 , A61P25/20 , A61P29/00 , A61P35/00 , A61P43/00 , C07C233/65 , C07C233/81 , C07C233/82 , C07C233/83 , C07C237/22 , C07C237/48 , C07D207/09 , C07D207/16 , C07D209/08 , C07D209/42 , C07D209/88 , C07D217/26 , C07D235/04 , C07D235/06 , C07D235/22 , C07D235/24 , C07D307/79 , C07D307/84 , C07D333/70 , C07D401/06 , C07D403/06 , C07D403/12 , C07D403/14 , C07D453/02 , C07D471/04 , C07D415/54
CPC分类号： C07D235/06 , C07C233/65 , C07C233/82 , C07C237/22 , C07C237/48 , C07D207/16 , C07D209/08 , C07D209/42 , C07D209/88 , C07D217/26 , C07D235/24 , C07D307/84 , C07D333/70 , C07D401/06 , C07D403/06 , C07D403/12 , C07D403/14 , C07D453/02 , C07D471/04 , C07C2103/74
摘要： Compounds of formula (Ia), (Ib), or (Ic), wherein A represents a group having two fused rings, or a group of formula (Id), R.sup.1.sub.(m) represents up to 6 substituents, K represents --O--, --S--, --CH.sub.2 --, --N(R.sup.2)-- or --N(COR.sup.2)--, in which R.sup.2 is H or C.sub.1 to C.sub.3 alkyl, W is a carbonyl, sulfonyl or sulfinyl group, provided that at least one of W and X contains carbonyl, Y and Z are as given in the description, and their pharmaceutically acceptable salts are ligands at CCK and/or gastrin receptors. ##STR1##
摘要翻译：式（Ia），（Ib）或（Ic）的化合物，其中A表示具有两个稠环的基团或式（Id）的基团，R 1（m）表示至多6个取代基，K表示-O- ，-S-，-CH 2 - ， - N（R 2） - 或-N（COR 2） - ，其中R 2是H或C 1至C 3烷基，W是羰基，磺酰基或亚磺酰基，条件是至少一个 W和X含有羰基，Y和Z如说明书中所给出，其药学上可接受的盐是CCK和/或胃泌素受体的配体。

4. 发明授权

US5674905A Bicyclooctane and bicycloheptane derivatives 失效
标题翻译：双环辛烷和双环庚烷衍生物
公开(公告)号：US5674905A
公开(公告)日：1997-10-07
申请号：US351320
申请日：1994-12-19
申请人： Sarkis Barret Kalindjian , Caroline Minli Rachel Low , Michael John Pether , Jonathan Michael Richard Davies , David John Dunstone , Iain Mair McDonald
发明人： Sarkis Barret Kalindjian , Caroline Minli Rachel Low , Michael John Pether , Jonathan Michael Richard Davies , David John Dunstone , Iain Mair McDonald
IPC分类号： A61K38/00 , C07C233/58 , C07C233/63 , C07C237/22 , C07D207/16 , C07D209/20 , C07K5/078 , C07C69/76 , C07C235/40 , C07C237/26
CPC分类号： C07K5/06165 , C07C233/58 , C07C233/63 , C07C237/22 , C07D207/16 , C07D209/20 , A61K38/00 , C07C2103/66 , C07C2103/72 , C07C2103/74 , C07C2103/88
摘要： Compounds of formula (I), wherein A is selected from (a), (b), (c), (d), (e), (f) and B is selected from (g), (h), and (i), wherein W is a carbonyl, sulphonyl or sulphinyl group, and X is a carbonyl, sulphonyl or sulphinyl group or --C(O)--CH.sub.2 -- (in which the carbonyl group is bonded to Y), provided that at least one of W and X contains carbonyl, Y is R.sub.9 --O-- or R.sub.9 --N(R.sub.10)--, Z is selected from (i), (ii), (iii), (iv) or Z is absent and W is H, with a number of provisions and phamaceutically acceptable salts thereof are ligands at CCK and/or gastrin receptors. ##STR1##
摘要翻译： PCT No.PCT / GB93 / 01301 Sec。 371日期1994年12月19日第 102（e）1994年12月19日PCT PCT 1993年6月18日PCT公布。第WO94 / 00421号公报日期1994年1月6日其中A选自（a），（b），（c），（d），（e），（f）和B的式（I）化合物选自（g） h）和（i）其中W是羰基，磺酰基或亚磺酰基，X是羰基，磺酰基或亚磺酰基或-C（O）-CH 2 - （其中羰基与Y键合）条件是W和X中的至少一个含有羰基，Y是R9-O-或R9-N（R10） - ，Z选自（i），（ii），（iii），（iv）或Z不存在并且W是H，其中许多规定和其药学上可接受的盐是CCK和/或胃泌素受体的配体。（a）（a）（b）（c）（d）>（iii）（iv）

5. 发明授权

US5939437A CCK and gastrin receptor ligands 失效
公开(公告)号：US5939437A
公开(公告)日：1999-08-17
申请号：US737317
申请日：1996-12-20
申请人： Sarkis Barret Kalindjian , Katherine Isobel Mary Steel , David John Dunstone , Ildiko Maria Buck
发明人： Sarkis Barret Kalindjian , Katherine Isobel Mary Steel , David John Dunstone , Ildiko Maria Buck
IPC分类号： C07C237/22 , C07C237/36 , C07C237/42 , C07D207/34 , C07D209/08 , C07D213/82 , C07D307/68 , A61K31/165
CPC分类号： C07D213/82 , C07C237/22 , C07C237/36 , C07C237/42 , C07D207/34 , C07D209/08 , C07D307/68 , C07C2101/18 , C07C2103/74
摘要： Compounds of formula (I) and their pharmaceutically active salts are gastrin and CCK receptor ligands, where Ar is a monocyclic aromatic group, R.sup.1 is halo, amino, nitro, cyano, sulphamoyl, sulphonyl, trifluoromethyl, C.sub.1 to C.sub.3 alkyl, C.sub.1 to C.sub.3 alkylamino, C.sub.1 to C.sub.3 dialkylamino, phenyl, substituted phenyl, C.sub.1 to C.sub.3 alkoxy, hydroxy, esterified hydroxy, C.sub.1 to C.sub.3 hydroxyalkyl, C.sub.1 to C.sub.3 alkylcarboxyamino, carboxy, esterified carboxy and amidated carboxy, m is 0, 1, 2, 3, or 4, provided that m is not more than 2 unless R.sup.1 is exclusively halo, x+y=0 or 1, R.sup.2 and R.sup.4 independently are II, or C.sub.1 to C.sub.3 alkyl, R.sup.3 is H or C.sub.1 to C.sub.15 hydrocarbyl, where one or more hydrogen atoms of die hydrocarbyl group may be replaced by a halogen atom, and where up to two of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom, provided that R.sup.3 does not contain a --O--O-- group, R.sup.5 is H or C.sub.1 to C.sub.3 alkyl, U is a cyclic moiety, selected from the group consisting of aryl, aromatic heterocyclic, non-aromatic heterocyclic, and cycloalkyl groups, where the aryl or aromatic group contains up to 3 substituents selected from the group consisting of halo, amino, nitro, cyano, sulphamoyl, sulphonyl, trifluoromethyl, C.sub.1 to C.sub.3 alkyl, C.sub.1 to C.sub.3 alkylamino, C.sub.1 to C.sub.3 dialkylamino, phenyl, C.sub.1 to C.sub.3 alkoxy, hydroxy, esterified hydroxy, C.sub.1 to C.sub.3 hydroxyalkyl, C.sub.1 to C.sub.3 alkylcarboxyamino, carboxy, esterified carboxy and amidated carboxy, Z is a group of the formula (IIa) or (IIb) where R.sup.6 is H or C.sub.1 to C.sub.3 alkyl, X is --CO.sub.2 H, esterified carboxy, amidated carboxy, tetrazolyl, hydroxy, cyano, amidino, --CH.sub.2 OH, --SO.sub.2 NHCOR.sup.7, --SONHCOR.sup.7, --COR.sup.7, --NHSO.sub.2 R.sup.7, --CONHSO.sub.2 R.sup.7,--NHCOR.sup.7 or --SO.sub.2 NHR.sup.8, where R.sup.7 is C.sub.1 to C.sub.6, alkyl, C.sub.1 to C.sub.6 aryl or substituted aryl, and R.sup.8 is --OH, --CN, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 haloalkyl, aryl or substituted aryl, Y is H or a group selected from those recited above for X, and a is 0, 1, or 2. ##STR1##

6. 发明授权

US6159994A Histamine H.sub.3 receptor ligands 失效
标题翻译：组胺H3受体配体
公开(公告)号：US6159994A
公开(公告)日：2000-12-12
申请号：US462910
申请日：2000-03-13
申请人： Iain Mair McDonald , David John Dunstone , Matthew John Tozer
发明人： Iain Mair McDonald , David John Dunstone , Matthew John Tozer
IPC分类号： C07D417/06 , C07D417/12 , A01K31/433
CPC分类号： C07D417/06 , C07D417/12
摘要： Compounds of formula (I) and pharmaceutically acceptable salt thereof are useful as histamine H.sub.3 receptor ligands. R.sup.1 is an optional substituent such as C.sub.1 to C.sub.6 alkyl. The moiety (1) replaces any available hydrogen atom on a carbon or nitrogen atom in the ring which includes X. R.sup.2 is C.sub.1 to C.sub.8 hydrocarbylene (in which one or more hydrogen atoms may be replaced by halogen atoms, and up to 2 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms); R.sup.3 replaces any available hydrogen atom on a carbon or nitrogen atom in the ring which includes X, and is hydrogen or C.sub.1 to C.sub.15 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen atoms, and up to 3 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms); the (or each) R.sup.4 group is independently selected from H, non-aromatic C.sub.1 to C.sub.6 hydrocarbyl, and aryl (C.sub.1 to C.sub.3 alkyl); X is --SO-- or --SO.sub.2 --; Y and Z are each hydrogen, or together represent .dbd.O or --N--R.sup.5, wherein R.sup.5 is H, non-aromatic C.sub.1 to C.sub.6 hydrocarbyl, or aryl (C.sub.1 to C.sub.3 alkyl), or one of Y and Z is non-aromatic C.sub.1 to C.sub.6 hydrocarbyl, or aryl (C.sub.1 to C.sub.3 alkyl) and the other is H; a is from 0 to 2; and n is 1 or 2.
摘要翻译： PCT No.PCT / GB98 / 02062 Sec。 371日期2000年3月13日 102（e）日期2000年3月13日PCT提交1998年7月14日PCT公布。出版物WO99 / 05141 日期1999年2月4日式（I）化合物及其药学上可接受的盐可用作组胺H3受体配体。 R 1是任选的取代基，例如C 1至C 6烷基。部分（1）取代了包含X的环中的碳或氮原子上的任何可用的氢原子。R2是C1-C8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2个碳原子）可以被氧，氮或硫原子取代）; R3代替包含X的环中的碳原子或氮原子上的任何可用的氢原子，并且是氢或C 1至C 15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3个碳原子可以是用氧，氮或硫原子代替）; （或每个）R 4基团独立地选自H，非芳族C1至C6烃基和芳基（C1至C3烷基）; X是-SO-或-SO 2 - ; Y和Z各自为氢，或一起代表= O或-N-R5，其中R5为H，非芳族C1至C6烃基或芳基（C1至C3烷基），或Y和Z之一为非芳族 C1至C6烃基或芳基（C1至C3烷基），另一个为H; a为0〜2; n为1或2。

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