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21. 发明申请

US20070281952A1 Arylsulfonylnaphthalene Derivatives As 5Ht2a Antagonists 失效
标题翻译：芳基磺酰基萘衍生物作为5Ht2a拮抗剂
公开(公告)号：US20070281952A1
公开(公告)日：2007-12-06
申请号：US11791195
申请日：2005-11-28
申请人： Mark Chambers , Neil Curtis , Emanuela Gancia , Myra Gilligan , Alexander Humphries , Tamara Ladduwahetty , Robert Maxey , Kevin Merchant
发明人： Mark Chambers , Neil Curtis , Emanuela Gancia , Myra Gilligan , Alexander Humphries , Tamara Ladduwahetty , Robert Maxey , Kevin Merchant
IPC分类号： A61K31/495 , A61K31/41 , A61K31/415 , A61K31/52 , A61P25/20 , A61P25/24 , A61P27/06 , C07D213/02 , C07D231/10 , C07D473/00 , C07D239/02 , C07D233/00 , C07D221/02 , C07C317/00 , A61P25/30 , A61P25/22 , A61P25/18 , A61K31/435 , A61K31/4353
CPC分类号： C07D401/12 , C07C311/08 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/42 , C07C317/44 , C07C323/65 , C07C2601/04 , C07D213/61 , C07D213/64 , C07D213/70 , C07D215/36 , C07D215/60 , C07D233/64 , C07D241/12 , C07D249/06 , C07D249/08 , C07D249/18 , C07D261/08 , C07D271/10 , C07D277/26 , C07D333/34 , C07D471/04 , C07D473/38
摘要： Compounds of formula (I) are potent and selective 5-HT2A antagonists, useful in treatment of a variety of adverse conditions of the CNS.
摘要翻译：式（I）化合物是有效和选择性的5-HT 2AA拮抗剂，可用于治疗CNS的多种不利条件。

22. 发明授权

US07452899B2 Gamma-secretase inhibitors 失效
标题翻译： γ-分泌酶抑制剂
公开(公告)号：US07452899B2
公开(公告)日：2008-11-18
申请号：US10566486
申请日：2004-07-29
申请人： Michela Bettati , Amanda Louise Boase , Ian Churcher , Tamara Ladduwahetty , Kevin John Merchant , Abdul Quddus
发明人： Michela Bettati , Amanda Louise Boase , Ian Churcher , Tamara Ladduwahetty , Kevin John Merchant , Abdul Quddus
IPC分类号： A01N43/42 , A01N47/00 , A61K31/44 , A61K31/21 , A61K31/26 , A61K43/64 , C07D215/00 , C07D217/00
CPC分类号： C07D231/12 , C07D417/06
摘要： Compounds of Formula (I): inhibit the processing of APP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.
摘要翻译：式（I）的化合物：通过γ-分泌酶抑制APP的加工，因此可用于治疗或预防阿尔茨海默氏病。

23. 发明授权

US06444666B1 Triazolopyridazine Derivatives for treating anxiety and enhancing cognition 失效
标题翻译：用于治疗焦虑和增强认知的三唑并哒嗪衍生物
公开(公告)号：US06444666B1
公开(公告)日：2002-09-03
申请号：US09140948
申请日：1998-08-27
申请人： Tamara Ladduwahetty , Kevin John Merchant , Francine Sternfeld , Leslie Joseph Street
发明人： Tamara Ladduwahetty , Kevin John Merchant , Francine Sternfeld , Leslie Joseph Street
IPC分类号： A61K315025
CPC分类号： C07D487/04
摘要： A compound of formula I, or a salt or prodrug thereof: wherein: Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted; R1 represents an optionally substituted five-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or R1 represents an optionally substituted six-membered heteroaromatic ring selected from pyrazine, pyrimidine and pyridazine; and R2 represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alkyl, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.
摘要翻译：式I的化合物或其盐或前药：其中：Z表示C 1-6烷基，C 3-7环烷基，C 4-7环烯基，芳基，C 3-7杂环烷基，杂芳基或二（C 1-6）烷基氨基，任何其中R 1表示选自恶唑，噻唑，异恶唑，异噻唑，咪唑，吡唑，恶二唑，噻二唑，三唑和四唑的任选取代的五元杂芳环; 或R 1表示选自吡嗪，嘧啶和哒嗪的任选取代的六元杂芳环; 并且R 2表示氰基（C 1-6）烷基，羟基（C 1-6）烷基，C 3-7环烷基（C 1-6）烷基，炔丙基，C 3-7杂环烷基羰基（C 1-6）烷基，芳基（C 1-6）烷基或杂芳基（C 1-6）烷基，其中任何基团可以是任选取代的; 其用于治疗焦虑症和包含它的药物组合物; 还公开了可用于增强认知的化合物的亚类，例如阿尔茨海默氏病。

24. 发明授权

US06297235B1 Triazolopyridazine derivatives for treating anxiety and enhancing cognition 失效
标题翻译：用于治疗焦虑和增强认知的三唑并哒嗪衍生物
公开(公告)号：US06297235B1
公开(公告)日：2001-10-02
申请号：US09190751
申请日：1998-11-12
申请人： Tamara Ladduwahetty , Kevin John Merchant , Francine Sternfeld , Leslie Joseph Street
发明人： Tamara Ladduwahetty , Kevin John Merchant , Francine Sternfeld , Leslie Joseph Street
IPC分类号： A61K315025
CPC分类号： C07D487/04
摘要： A compound of formula I, or a salt or prodrug thereof: wherein: Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted; R1 represents an optionally substituted five-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or R1 represents an optionally substituted six-membered heteroaromatic ring selected from pyrazine, pyrimidine and pyridazine; and R2 represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alky, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.
摘要翻译：式I的化合物或其盐或前药：其中：Z表示C 1-6烷基，C 3-7环烷基，C 4-7环烯基，芳基，C 3-7杂环烷基，杂芳基或二（C 1-6）烷基氨基，任何其中R 1表示选自恶唑，噻唑，异恶唑，异噻唑，咪唑，吡唑，恶二唑，噻二唑，三唑和四唑的任选取代的五元杂芳环; 或R 1表示选自吡嗪，嘧啶和哒嗪的任选取代的六元杂芳环; 和R 2表示氰基（C 1-6）烷基，羟基（C 1-6）烷基，C 3-7环烷基（C 1-6）烷基，炔丙基，C 3-7杂环烷基羰基（C 1-6）烷基，芳基（C 1-6）烷基或杂芳基（C 1-6）烷基，其中任何基团可以是任选取代的; 其用于治疗焦虑症和包含它的药物组合物; 还公开了可用于增强认知的化合物的亚类，例如阿尔茨海默氏病。

25. 发明申请

US20120004221A1 Antibacterial Compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US20120004221A1
公开(公告)日：2012-01-05
申请号：US13154485
申请日：2011-06-07
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/437 , A01N43/90 , A61K31/497 , A01P1/00 , A61K31/5377 , A61K31/506 , A61K31/5383 , A61P31/04 , C07D513/04 , A61K31/496
CPC分类号： A61K31/437 , A01N47/36 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5383
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N; R2 and R3 are as defined in the description.
摘要翻译：式（I）化合物具有抗菌活性：其中：m为0或1; Q是氢或环丙基; Alk是可以含有醚（-O-），硫醚（-S-）或氨基（-NR） - 连接的任意取代的二价C1-C6亚烷基，亚烯基或亚炔基，其中R是氢，-CN或 C1-C3烷基; X是-C（= O）NR 6 - ， - S（O）NR 6 - ， - C（= O）O-或-S（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N; R2和R3如说明书中所定义。

26. 发明授权

US5624947A Phenyl derivatives useful as tachykinin antagonists 失效
标题翻译：可用作速激肽拮抗剂的苯基衍生物
公开(公告)号：US5624947A
公开(公告)日：1997-04-29
申请号：US481503
申请日：1995-06-20
申请人： Linda E. Keown , Tamara Ladduwahetty , Monique B. Van Niel
发明人： Linda E. Keown , Tamara Ladduwahetty , Monique B. Van Niel
IPC分类号： C07D207/32 , C07D207/325 , C07D211/88 , C07D233/60 , C07D233/88 , C07D233/91 , C07D295/084 , C07D521/00 , A61K31/415
CPC分类号： C07D207/325 , C07D211/88 , C07D231/12 , C07D233/56 , C07D233/88 , C07D233/91 , C07D249/08 , C07D295/092
摘要： Compounds of formula (I), or a salt or prodrug thereof are tachykinin antagonists.
摘要翻译： PCT No.PCT / GB93 / 02559 Sec。 371日期：1995年6月20日 102（e）1995年6月20日PCT 1993年12月15日PCT PCT。 WO94 / 14767 PCT出版物（I）式（I）化合物或其盐或前药是速激肽拮抗剂。

27. 发明授权

US5496833A Piperidine tachykinin receptor antagonists 失效
公开(公告)号：US5496833A
公开(公告)日：1996-03-05
申请号：US387684
申请日：1995-02-13
申请人： Reymond Baker , Tamara Ladduwahetty , Eileen M. Seward , Christopher J. Swain
发明人： Reymond Baker , Tamara Ladduwahetty , Eileen M. Seward , Christopher J. Swain
IPC分类号： C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , A61K31/445
CPC分类号： C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein n is 1, 2 or 3;X represents O or S;Y represents a hydrocarbon chain of 1, 2, 3 or 4 carbon atoms optionally substituted by oxo;R.sup.1 is phenyl optionally substituted by 1, 2 or 3 of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, --OR.sup.a, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b ;R.sup.2 is phenyl, indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl, quinolyl, benzhydryl, or benzyl;R.sup.4 and R.sup.5 each independently represent H, halo, C.sub.1-6 alkyl, oxo, CH.sub.2 OR.sup.a, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ;R.sup.8 represents an optionally substituted aromatic heterocycle; andR.sup.a and R.sup.b are H, trifluoromethyl, C.sub.1-6 alkyl or phenyl optionally substituted by C.sub.1-6 alkyl, halo or trifluoromethyl;are tachykinin antagonists useful in medicine.

28. 发明授权

US08389516B2 Antibacterial compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US08389516B2
公开(公告)日：2013-03-05
申请号：US13154592
申请日：2011-06-07
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/5377 , A61K31/501 , A61K31/497 , A61K31/496 , A61K31/506 , A61K31/4436 , A61K31/428 , A61K31/429 , C07D239/42
CPC分类号： C07D417/04 , C07D417/14 , Y02P20/582
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
摘要翻译：式（I）化合物具有抗菌活性：其中：m为0或1; Q是氢或环丙基; Alk是可以含有醚（-O-），硫醚（-S-）或氨基（-NR） - 连接的任意取代的二价C1-C6亚烷基，亚烯基或亚炔基，其中R是氢，-CN或 C1-C3烷基; X是-C（= O）NR 6 - ， - S（O）NR 6 - ， - C（= O）O-或-S（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N或CH，或CF; R2和R3如说明书中所定义。

29. 发明授权

US07977340B2 Antibacterial compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US07977340B2
公开(公告)日：2011-07-12
申请号：US12304303
申请日：2007-06-21
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/4412 , A61K31/4436 , A61K31/497 , A61K31/506 , C07D403/14 , C07D417/14
CPC分类号： C07D417/04 , C07D417/14 , Y02P20/582
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
摘要翻译：式（I）化合物具有抗菌活性：其中：m为0或1; Q是氢或环丙基; Alk是可以含有醚（-O-），硫醚（-S-）或氨基（-NR） - 连接的任意取代的二价C 1 -C 6亚烷基，亚烯基或亚炔基，其中R是氢，-CN或 C1-C3烷基; X是-C（= O）NR 6 - ， - S（O）NR 6 - ， - C（= O）O-或-S（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N或CH，或CF; R2和R3如说明书中所定义。

30. 发明授权

US5922706A Morpholine and thiomorpholine tachykinin receptor antagonists 失效
公开(公告)号：US5922706A
公开(公告)日：1999-07-13
申请号：US969685
申请日：1997-11-13
申请人： Conrad P. Dorn , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Tamara Ladduwahetty
发明人： Conrad P. Dorn , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Tamara Ladduwahetty
IPC分类号： C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , A61K31/535 , A61K31/54 , C07D417/04
CPC分类号： C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , Y10S514/825
摘要： Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

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