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1. 发明申请

WO2007110782A1 MUSCARINIC RECEPTOR ANTAGONISTS 审中-公开
标题翻译：肌肉受体拮抗剂
公开(公告)号：WO2007110782A1
公开(公告)日：2007-10-04
申请号：PCT/IB2007/050003
申请日：2007-01-02
申请人： RANBAXY LABORATORIES LIMITED , KUMAR, Naresh , CLIFFE, Ian, Anthony , SALMAN, Mohammad , PALLE, Venkata, P. , KAUR, Kirandeep , SHEJUL, Yogesh, D. , CHUGH, Anita , GUPTA, Suman , RAY, Abhijit , MALHOTRA, Shivani , SHIRUMALLA, Raj, Kumar
发明人： KUMAR, Naresh , CLIFFE, Ian, Anthony , SALMAN, Mohammad , PALLE, Venkata, P. , KAUR, Kirandeep , SHEJUL, Yogesh, D. , CHUGH, Anita , GUPTA, Suman , RAY, Abhijit , MALHOTRA, Shivani , SHIRUMALLA, Raj, Kumar
IPC分类号： C07D487/08 , A61K31/403
CPC分类号： C07D209/52
摘要： This present invention generally relates to muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.
摘要翻译：本发明一般涉及毒蕈碱受体拮抗剂，其可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病，以及其它用途。本发明还涉及制备所公开的化合物的方法，含有所公开的化合物的药物组合物，以及用于治疗通过毒蕈碱受体介导的疾病的方法。

2. 发明申请

WO0013682A3 4-QUINOLINEMETHANOL DERIVATIVES AS PURINE RECEPTOR ANTAGONISTS.(II) 审中-公开
标题翻译：（II）作为嘌呤受体拮抗剂的4-喹啉甲醇衍生物
公开(公告)号：WO0013682A3
公开(公告)日：2000-06-02
申请号：PCT/GB9902924
申请日：1999-09-03
申请人： CEREBRUS PHARM LTD , GILLESPIE ROGER JOHN , LERPINIERE JOANNE , GILES PAUL RICHARD , ADAMS DAVID REGINALD , KNUTSEN LARS JACOB STRAY , CLIFFE IAN ANTHONY
发明人： GILLESPIE ROGER JOHN , LERPINIERE JOANNE , GILES PAUL RICHARD , ADAMS DAVID REGINALD , KNUTSEN LARS JACOB STRAY , CLIFFE IAN ANTHONY
IPC分类号： A61K31/47 , A61P25/16 , A61P25/24
CPC分类号： A61K31/47
摘要： Wherein: R1 is hydrogen or alkyl; R2 is selected from hydrogen, alkyl, aryl and 4,5,6,7 or 8 membered satured and partially unsaturated heterocyclic rings containing one or more heteroatoms selected from O, S and N; R3 and R4 are independently selected from hydrogen, alkyl, aryl, COR13, CO2R13, CONR13R14, CONR13NR14R15, SO2R13, SO2NR13R14, SO2NR13NR14R15 or may form a ring. Or R1 and R4 together may form a heterocyclic ring or R2 and R3 together may form a heterocyclic ring. R5 and R6 are independently selected from hydrogen, alkyl, aryl and heterocyclic with the proviso that where R3 and R5 together form a ring, then R3, and R4 do not also form a ring; or a pharmaceutically acceptable salt or prodrug thereof, in the manufacture of a medicament for the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, such as a movement disorder, for example, Parkinson's Disease or progressive supernuclear palsy, Huntingtons disease, multiple system atrophy, corticobasal degeneration, Wilsons disease, Hallerrorder-Spatz disease, progressive pallidal atrophy, Dopa-responsive dystonia-Parkinsonism, spasticity, Alzheimer's disease or other disorders of the basal ganglia which result in dyskinesias.
摘要翻译：其中：R1为氢或烷基; R2选自氢，含有一个或多个选自O，S和N的杂原子的烷基，芳基和4,5,6,7或8元饱和和部分不饱和的杂环; R3和R4独立地选自氢，烷基，芳基，COR13，CO2R13，CONR13R14，CONR13NR14R15，SO2R13，SO2NR13R14，SO2NR13NR14R15或可以形成环。或者R1和R4一起可以形成杂环，或者R2和R3可以一起形成杂环。 R5和R6独立地选自氢，烷基，芳基和杂环，条件是当R3和R5一起形成环时，则R3和R4也不形成环; 或其药学上可接受的盐或前药在制备用于治疗或预防其中阻断嘌呤受体，特别是腺苷受体，更特别是A 2A受体可能是有益的病症例如运动障碍的药物中的用途，例如帕金森氏病或进行性超核麻痹，亨廷顿病，多系统萎缩，皮质基底节变性，Wilsons病，Hallerrorder-Spatz病，进行性苍白球性萎缩，多巴反应性肌张力障碍 - 帕金森综合征，痉挛状态，阿尔茨海默病或其他基底节病导致运动障碍。

3. 发明申请

WO1994021610A1 PIPERAZINE DERIVATIVES AS 5-HT1A LIGANDS 审中-公开
标题翻译：哌嗪衍生物作为5-HT1A配体
公开(公告)号：WO1994021610A1
公开(公告)日：1994-09-29
申请号：PCT/GB1994000539
申请日：1994-03-17
申请人： JOHN WYETH & BROTHER LIMITED , ASHWELL, Mark, Antony , CLIFFE, Ian, Anthony , WARD, Terence, James , WHITE, Alan, Chapman , WARRELLOW, Graham, John
发明人： JOHN WYETH & BROTHER LIMITED
IPC分类号： C07D213/38
CPC分类号： C07D213/50 , C07D213/38
摘要： Piperazine derivatives of formula (I) and their salts are 5-HT1A binding agents and may be used, for example, as anxiolytics. In the formula, R, R and R are hydrogen or lower alkyl, R is mono- or bicyclic aryl or heteroaryl, R is lower alkyl or cycloalkyl, A is an alkylene chain and X is -CO-, -CR OH- (where R is hydrogen, lower alkyl or cycloalkyl), -S-, -SO- or -SO2- or X can also be -(CH2)n- (where n is 0, 1 or 2) when R is cycloalkyl.
摘要翻译：式（I）的哌嗪衍生物及其盐是5-HT1A结合剂，可用作抗焦虑剂。在式中，R 1，R 2和R 4为氢或低级烷基，R 1为单环或双环芳基或杂芳基，R 3为低级烷基或环烷基，A为亚烷基链， X是-CO-，-CR 5 OH-（其中R 5是氢，低级烷基或环烷基），-S-，-SO-或-SO 2 - 或X也可以是 - （CH 2）n - （其中n为0,1或2）当R 3为环烷基时。

4. 发明申请

WO1994003444A1 AMIDE DERIVATIVES 审中-公开
标题翻译：酰胺衍生物
公开(公告)号：WO1994003444A1
公开(公告)日：1994-02-17
申请号：PCT/GB1993001542
申请日：1993-07-22
申请人： JOHN WYETH & BROTHER LIMITED , CLIFFE, Ian, Anthony , WHITE, Alan, Chapman
发明人： JOHN WYETH & BROTHER LIMITED
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D211/70
摘要： Amide derivatives of formula (1) and their pharmaceutically acceptable salts (where a and b each represent 0, 1, 2 or 3 such that a + b = 0, 1, 2 or 3, the dotted line represents an optional double bond, A is an optionally substituted C1-2-alkylene chain, R is mono or bicyclic aryl or heteroaryl radical, R1 is hydrogen or lower alkyl, R2 is an aryl, aralkyl, heteroaryl or heteroarylalkyl and -CONR3R4 represents a specified amide group) are 5-HT1A binding agents and may be used, for example, as anxiolytics.
摘要翻译：式（1）的酰胺衍生物及其药学上可接受的盐（其中a和b各自表示0,2,2或3，使得a + b = 0,1,2或3，虚线表示任选的双键，A 是任选取代的C 1-2 - 亚烷基链，R是单或双环芳基或杂芳基，R 1是氢或低级烷基，R 2是芳基，芳烷基，杂芳基或杂芳基烷基，-CONR 3 R 4代表指定的酰胺基） HT1A结合剂，可用作抗焦虑剂。

5. 发明申请

WO1995002592A1 N-(PIPERIDINYL-1-ALKYL)-SUBSTITUTED CYCLOHEXANE CARBOXYLIC ACID AMIDES AS 5-HT1A RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为5-HT1A受体拮抗剂的N-（哌啶-1-基 - 烷基）-SUBSTITUTED CYCLOHEXANC CARBOXYLIC ACID AMIDES
公开(公告)号：WO1995002592A1
公开(公告)日：1995-01-26
申请号：PCT/GB1994001507
申请日：1994-07-12
申请人： JOHN WYETH & BROTHER LTD. , AMERICAN HOME PRODUCTS CORPORATION , CLIFFE, Ian, Anthony , ASHWELL, Mark, Antony , WARD, Terence, James , WHITE, Alan, Chapman , BAUDY, Reinhardt, Bernhard
发明人： JOHN WYETH & BROTHER LTD. , AMERICAN HOME PRODUCTS CORPORATION
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
摘要： Compounds of formula (I) and the pharmaceutically acceptable acid addition salts thereof are 5-HT1Abinding agents and may be used, for example, as anxiolytics. In the formula a and b each represents 0, 1, 2 or 3 such that the sum of a + b is 0, 1, 2 or 3, the dotted line represents an optional double bond which may be present in the ring, provided that a is at least 1, A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, R is a mono or bicyclic aryl or heteroaryl radical with the proviso that R is not an unsubstituted phenyl group, R is a mono or bicyclic heteroaryl radical, and R is cycloalkyl or cycloalkenyl.
摘要翻译：式（I）化合物及其药学上可接受的酸加成盐是5-HT1结合剂，可用作抗焦虑剂。式a和b各自表示0,2,2或3，使得a + b的和为0,1,2或3，虚线表示可存在于环中的任选双键，条件是 a是至少1，A是任选被一个或多个低级烷基取代的1或2个碳原子的亚烷基链，R是单或双环芳基或杂芳基，条件是R不是未取代的苯基，R 1是单环或双环杂芳基，R 2是环烷基或环烯基。

6. 发明申请

WO1994020481A1 4-AMINO-2-(HETERO)ARYL-BUTANAMIDES USEFUL AS 5-HT1A-ANTAGONISTS 审中-公开
标题翻译：作为5-HT1A拮抗剂有用的4-氨基-2-（异噻唑）亚苄基氨基甲酸
公开(公告)号：WO1994020481A1
公开(公告)日：1994-09-15
申请号：PCT/GB1994000372
申请日：1994-02-25
申请人： JOHN WYETH & BROTHER LIMITED , CLIFFE, Ian, Anthony , IFILL, Anderson, Decourtney
发明人： JOHN WYETH & BROTHER LIMITED
IPC分类号： C07D295/185
CPC分类号： C07D295/185 , C07C2602/10 , C07D209/14 , C07D215/38 , C07D311/58 , C07D319/20
摘要： Amide derivatives of the formula (I): R NR (CR2)2CHR CONR R and their pharmaceutically acceptable salts are 5-HTA1A binding agents and may be used, for example, as anxiolytics. The radicals, R, R , R , R , R and R have specified meanings.
摘要翻译：式（I）的酰胺衍生物：R 5 NR 4（CR 2）2 CHR 3 CONR 1 R 2及其药学上可接受的盐是5-HTA1A结合剂，可以用于例如，作为抗焦虑药。基团R 1，R 2，R 2，R 3，R 4和R 5具有特定含义。

7. 发明申请

WO1994015919A1 PIPERAZINE DERIVATIVES 审中-公开
标题翻译：哌嗪衍生物
公开(公告)号：WO1994015919A1
公开(公告)日：1994-07-21
申请号：PCT/GB1993002660
申请日：1993-12-24
申请人： JOHN WYETH & BROTHER LIMITED , CLIFFE, Ian, Anthony , BRIGHTWELL, Christopher, Ian , MANSELL, Howard, Langham , WHITE, Alan, Chapman
发明人： JOHN WYETH & BROTHER LIMITED
IPC分类号： C07D209/42
CPC分类号： C07D215/40 , C07D209/08 , C07D209/42 , C07D215/38
摘要： Piperazine derivatives of formula (I) and their pharmaceutically acceptable salts are 5-HT1A binding agents and may be used, for example, as anxiolytics. In the formula, A is an optionally substituted alkylene chain, Z is a specified bicyclic nitrogen containing heteroaromatic radical, R is hydrogen or lower alkyl, R is aryl or aryl(lower)alkyl and R and R are hydrogen or specified organic radicals or -NR R represents a heterocyclic ring.
摘要翻译：式（I）的哌嗪衍生物及其药学上可接受的盐是5-HT1A结合剂，可以用作例如抗焦虑剂。在该式中，A是任选取代的亚烷基链，Z是指定的双环含氮杂芳基，R是氢或低级烷基，R 1是芳基或芳基（低级）烷基，R 2和R 3 >是氢或指定的有机基团，或-NR 2 R 3表示杂环。

8. 发明申请

WO1993014076A1 PIPERAZINE DERIVATIVES AS 5-HT RECEPTORS ANTAGONISTS 审中-公开
标题翻译：哌嗪衍生物作为5-HT受体拮抗剂
公开(公告)号：WO1993014076A1
公开(公告)日：1993-07-22
申请号：PCT/GB1992002399
申请日：1992-12-24
申请人： JOHN WYETH & BROTHER LIMITED , CLIFFE, Ian, Anthony
发明人： JOHN WYETH & BROTHER LIMITED
IPC分类号： C07D295/12
CPC分类号： C07D295/13 , C07C2601/14
摘要： Compounds of formula (I) where A is an alkylene chain of 2 to 5 carbon atoms optionally substituted by one or more lower alkyl groups, R represents hydrogen or one or two same or different lower alkyl groups, R1 is a monocyclic aryl or heteroaryl radical, R2 is a mono or bicycle aryl radical and R3 is cycloalkyl and the pharmaceutically acceptable acid addition salts are novel. They are 5-HT¿1A?-antagonists which may be used, for example, in treating anxiety.

9. 发明申请

WO1992006960A1 PIPERAZINE DERIVATIVES 审中-公开
标题翻译：哌嗪衍生物
公开(公告)号：WO1992006960A1
公开(公告)日：1992-04-30
申请号：PCT/GB1991001800
申请日：1991-10-16
申请人： JOHN WYETH & BROTHER LIMITED , CLIFFE, Ian, Anthony , WHITE, Alan, Chapman , IFILL, Anderson, Decourtney
发明人： JOHN WYETH & BROTHER LIMITED
IPC分类号： C07D213/56
CPC分类号： C07D295/185 , C07D213/56
摘要： Compounds of formula (I), where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, R is hydrogen or lower alkyl, R1 is a mono or bicyclic aryl or a heteroaryl radical, R2 is an aryl radical, a heteroaryl radical, or an aryl- or heteroaryl-lower alkyl radical, R3 is hydrogen, lower alkyl or aryl and R4 is hydrogen, lower alkyl, cycloalkyl, cycloalkyl(lower)alkyl, aryl, or aryl(lower)alkyl or R?3 and R4¿ together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom and the dotted line represents a single or double bond, the hydrogen atoms shown in brackets being present when the dotted line represents a single bond and their pharmaceutically acceptable acid addition salts are 5-HT¿1A? binding agents which may be used, for example, for the treatment of CNS disorders such as anxiety.

10. 发明申请

WO1996001656A1 5-HT1A LIGANDS 审中-公开
标题翻译： 5-HT1A配偶
公开(公告)号：WO1996001656A1
公开(公告)日：1996-01-25
申请号：PCT/GB1995001395
申请日：1995-06-15
申请人： JOHN WYETH & BROTHER LIMITED , CLIFFE, Ian, Anthony , FLETCHER, Allan , WHITE, Alan, Chapman
发明人： JOHN WYETH & BROTHER LIMITED
IPC分类号： A61K51/04
CPC分类号： A61K51/0459 , A61K2123/00
摘要： 5-HT1A receptor binding agents which are piperazine derivatives of specified formula are radiolabelled with I, I or F. The radiolabelled compounds are useful in pharmacological screening procedures, in positron emission tomography studies and in single photon emission computed tomography studies.
摘要翻译：作为具有规定式的哌嗪衍生物的5-HT 1A受体结合剂用125 I，125 I或18 F进行放射性标记。放射性标记化合物可用于药物筛选程序，正电子发射断层扫描研究和单光子发射计算机断层扫描研究。

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