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1. 发明授权

US06878734B2 Gastrin and cholecystokinin receptor ligands(II) 失效
公开(公告)号：US06878734B2
公开(公告)日：2005-04-12
申请号：US10275741
申请日：2001-05-04
申请人： Sarkis Barret Kalindjian , Ildiko Maria Buck , Katherine Isobel Mary Steel , Paul Trevor Wright , Matthew John Tozer , Michael John Pether , Caroline Minli Rachel Low
发明人： Sarkis Barret Kalindjian , Ildiko Maria Buck , Katherine Isobel Mary Steel , Paul Trevor Wright , Matthew John Tozer , Michael John Pether , Caroline Minli Rachel Low
IPC分类号： A61K31/42 , A61K45/06 , A61P1/04 , C07D233/54 , C07D403/04 , C07D413/04 , C07D417/04 , A61K31/415 , C07D233/06 , C07D237/08 , C07D247/02 , C07D405/04 , C07D413/02
CPC分类号： C07D233/64 , A61K31/42 , A61K45/06 , C07D403/04 , C07D413/04 , C07D417/04 , A61K2300/00
摘要： Ligands for the gastrin and cholecystokinin (CCK) receptors are provided, together with methods for preparing such ligands, and compounds which are useful intermediates in such methods. Pharmaceutical compositions comprising such ligands, methods for preparing such pharmaceutical compositions, and methods of treatment using these compositions also are provided. The ligands have the formula (I): where n is from 1 to 3; X and Y are independently ═N— or —N(R5)— where R5 is selected from the group consisting of H, Me, Et, Pr, Bn, —OH and —CH2COOR6, where R6 represents H, Me, Et, Pr or Bn; R1 is H or a C1-C15 saturated carbocylic ring optionally substituted with OMe, NMe2, CF3, Me, F, Cl, Br or I where up to three H atoms may optionally be replaced by halogen atoms; R2 is selected from H, Me, Et, Pr and OH, each R2 being independently selected from H, Me, Et, Pr and OH when n is greater than 1; R3 is selected from the group consisting of H, Me, Et and Pr when n is 1; or, when n is greater than 1, each R3 is independently selected from the group consisting of H, Me, Et and Pr, or two R3 groups on neighbouring carbon atoms are linked to form a C3 to C6 carbocylic ring, or two R3 groups are absent from neighbouring carbon atoms which are linked by a double bond; or R2 and R3 on the same carbon atom together represent an ═O group; R4 is H or a C3 to C10 alicyclic ring where up to three H atoms may optionally be replaced by halogen atoms; Z is selected from the group consisting of: Q is a 6-membered aromatic carbocycle substituted with 1 or 2 V groups and optionally substituted with 1, 2 or 3 T groups; V is selected from the group consisting of —CO—NH—SO2—Ph, —SO2—NH—CO—Ph, —CH2OH, or a group of the formula —R7U, where U is selected from the group consisting of —COOH, tetrazolyl, —CONHOH and —SO3H; and R7 is selected from the group consisting of a bond; C1 to C6 hydrocarbylene, optionally substituted by hydroxy, amino or acetamido; —O—(C1 to C3 alkylene)-; —SO2NR8—CHR9—; —CO—NR8—CHR9—, where R8 and R9 are independently selected from H and methyl; and —NH—(CO)c—CH2—, where c is 0 or 1.

2. 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）。

3. 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）

4. 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。

5. 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。

6. 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##

7. 发明授权

US06956053B2 Pyrazole derivatives and their use as gastrin and cholecystokin receptor ligands 失效
标题翻译：吡唑衍生物及其作为胃泌素和胆囊收缩素受体配体的用途
公开(公告)号：US06956053B2
公开(公告)日：2005-10-18
申请号：US10275614
申请日：2001-05-04
申请人： Iain Mair McDonald , Caroline Minli Rachel Low , Katherine Isobel Mary Steel , John Spencer
发明人： Iain Mair McDonald , Caroline Minli Rachel Low , Katherine Isobel Mary Steel , John Spencer
IPC分类号： A61K31/415 , A61K31/4439 , A61P1/04 , C07D231/14 , C07D231/20 , C07D231/22 , C07D231/10
CPC分类号： C07D231/22 , A61K31/415 , A61K31/4439 , C07D231/14 , C07D231/20 , A61K2300/00
摘要： Compounds of formula (I), (IIa) or (IIb) wherein R1-R6, Z, Q and n are as defined in claim 1 and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. Compositions comprising a compound of formula (I), (IIa) or (IIb) are also described.
摘要翻译：式（I），（IIa）或（IIb）其中R 1，R 6，Z，Q和n如权利要求1中所定义的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。还描述了包含式（I），（IIa）或（IIb）化合物的组合物。

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