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1. 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）

2. 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##

3. 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）。

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

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.

6. 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。

7. 发明授权

US07034048B2 Gastrin and cholecystokinin receptor ligands (III) 失效
公开(公告)号：US07034048B2
公开(公告)日：2006-04-25
申请号：US10275613
申请日：2001-05-04
申请人： Sarkis Barret Kalindjian , Ildiko Maria Buck , Caroline Minli Rachel Low , Matthew John Tozer
发明人： Sarkis Barret Kalindjian , Ildiko Maria Buck , Caroline Minli Rachel Low , Matthew John Tozer
IPC分类号： A61K31/4164 , A61K31/404 , C07D403/04
CPC分类号： C07D403/04 , A61K31/415 , A61K31/42 , A61K45/06 , C07D413/04 , A61K2300/00
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)—(R5 being selected from H, Me, Et, Pr, Bn, OH and —CH2COOR6, wherein R6 represents H, Me, Et, Pr or Bn), ═CH—, —O— or —S—; n is from 1 to 4; A is an optionally substituted 5- or 6-membered carbocyclic ring wherein (a) 1 or 2 C atoms may optionally be replaced by N, O and/or S atoms, (b) A is fused with the aromatic group in formula (I) to form a fused bicycle, and (c) the ring containing X and Y is linked to a C atom of A; R1 is H or C1 to C15 hydrocarbyl wherein up to three 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; 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 (when n is 1) 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 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 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; V is —CO—NH—SO2—Ph, —SO2—NH—CO—PH, —CH2OH, or a group of the formula —R7U, (wherein U is —COOH, tetrazolyl, —CONHOH or —SO3H; and R7 is a bond; C1 to C6 hydrocarbylene optionally substituted by hydroxy, amino or acetamido; —O—(C1 to C3 alkylene)—; —SO2NR8—CHR9—; —CO—NR8—CHR9—, R8 and R9 being independently selected from H and methyl; or —NH—(CO)c—CH2, c being 0 or 1); or a pharmaceutically acceptable salt thereof. Compositions comprising a compound a formula (I) are also described

8. 发明授权

US06407132B1 Substituted imidazole derivatives and their use as histamine H3 receptor ligands 失效
标题翻译：取代的咪唑衍生物及其作为组胺H3受体配体的用途
公开(公告)号：US06407132B1
公开(公告)日：2002-06-18
申请号：US09463445
申请日：2000-03-13
申请人： Sarkis Barret Kalindjian , Ildiko Maria Buck
发明人： Sarkis Barret Kalindjian , Ildiko Maria Buck
IPC分类号： A61K314164
CPC分类号： C07D233/64 , Y10S435/968 , Y10S435/975
摘要： Compounds of formula (I) and their pharmaceutically acceptable salts are useful as histamine H3 receptor ligands. R1 and R3 are optional substituents such as C1 to C6 alkyl. R2 represents a bond or C1 to C5 (preferably C1 to C3) hydrocarbylene; R4 represents a bond or C1 to C5 (preferably C1 to C3) hydrocarbylene; R5 is hydrogen, C1 to C3 alkyl, R8—O—(C1 to C3)alkyl (wherein R8 is hydrogen or C1 to C3 alkyl), aryl, aryl(C1 to C3)alkyl; R6 represents a bond or —NR9—, wherein R9 is any of the groups mentioned above for R5; R7 is H or C1 to C15 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen, and up to three carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms); a is from 0 to 2; and b is from 0 to 3.
摘要翻译：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和R 3是任选的取代基，例如C 1至C 6烷基。 R2表示键或C1至C5（优选C1至C3）亚烃基; R4表示键或C1至C5（优选C1至C3）亚烃基; R 5为氢，C 1至C 3烷基，R 8 -O-（C 1至C 3）烷基（其中R 8为氢或C 1至C 3烷基），芳基，芳基（C 1至C 3） R 6表示键或-NR 9 - ，其中R 9是上述对R 5的任何基团; R 7是H或C 1至C 15烃基（其中一个或多个氢原子可以被卤素取代，并且最多三个碳原子可被氧，氮或硫原子替代）; a为0〜2; b为0〜3。

9. 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

10. 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）

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