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1. 发明申请

US20130123230A1 2-Thiopyrimidinones 有权
公开(公告)号：US20130123230A1
公开(公告)日：2013-05-16
申请号：US13670852
申请日：2012-11-07
申请人： Philip A. Carpino , Edward L. Conn , Robert L. Dow , Matthew S. Dowling , David Hepworth , Daniel Wei-Shung Kung , Suvi Orr , Benjamin N. Rocke , Roger B. Ruggeri , Matthew F. Sammons , Joseph S. Warmus , Yan Zhang
发明人： Philip A. Carpino , Edward L. Conn , Robert L. Dow , Matthew S. Dowling , David Hepworth , Daniel Wei-Shung Kung , Suvi Orr , Benjamin N. Rocke , Roger B. Ruggeri , Matthew F. Sammons , Joseph S. Warmus , Yan Zhang
IPC分类号： C07D239/56 , C07D401/04 , C07D405/10 , C07D403/10 , C07D487/04 , C07D409/10 , C07D417/10 , C07D401/06 , C07D403/06 , C07D413/06 , A61K31/5377 , C07D405/04 , C07D403/04 , C07D409/04 , C07D401/10 , C07D403/12 , A61K31/352 , A61K45/06 , A61K31/513
CPC分类号： C07D239/56 , A61K31/352 , A61K31/37 , A61K31/513 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/10 , C07D409/04 , C07D409/10 , C07D413/06 , C07D417/04 , C07D417/10 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.

2. 发明授权

US08835449B2 2-thiopyrimidinones 有权
标题翻译： 2-硫代嘧啶酮
公开(公告)号：US08835449B2
公开(公告)日：2014-09-16
申请号：US13670852
申请日：2012-11-07
申请人： Edward L. Conn , David Hepworth , Roger B. Ruggeri
发明人： Edward L. Conn , David Hepworth , Roger B. Ruggeri
IPC分类号： C07D239/56 , A61K31/513
CPC分类号： C07D239/56 , A61K31/352 , A61K31/37 , A61K31/513 , A61K31/5377 , A61K45/06 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/10 , C07D409/04 , C07D409/10 , C07D413/06 , C07D417/04 , C07D417/10 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
摘要翻译：髓过氧化物酶抑制剂，含有这些抑制剂的药物组合物以及这些抑制剂用于治疗例如心血管病症的用途。

3. 发明申请

US20130072519A1 2-PHENYL BENZOYLAMIDES 审中-公开
标题翻译： 2-苯基苯甲酰胺
公开(公告)号：US20130072519A1
公开(公告)日：2013-03-21
申请号：US13699230
申请日：2011-05-09
申请人： Edward Lee Conn , David Hepworth , Yingmei Qi , Benjamin Neil Rocke , Roger Benjamin Ruggeri , Yan Zhang
发明人： Edward Lee Conn , David Hepworth , Yingmei Qi , Benjamin Neil Rocke , Roger Benjamin Ruggeri , Yan Zhang
IPC分类号： C07D307/83 , A61K31/4035 , A61K31/435 , C07C235/84 , A61K31/216 , C07D221/04 , C07D209/44 , A61K31/343
CPC分类号： C07D307/83 , A61K31/216 , A61K31/343 , A61K31/4035 , A61K31/435 , C07C235/84 , C07D209/44 , C07D209/49 , C07D221/04 , C07D307/88 , C07D401/12 , C07D471/04
摘要： Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein.
摘要翻译：本文描述抑制微粒体甘油三酯转运蛋白（MTP）和/或载脂蛋白B（Apo B）分泌的式I化合物及其在治疗与动物相关疾病中的用途。

4. 发明授权

US07902188B2 Morpholine dopamine agonists 有权
标题翻译：吗啉多巴胺激动剂
公开(公告)号：US07902188B2
公开(公告)日：2011-03-08
申请号：US12496864
申请日：2009-07-02
申请人： Charlotte Moira Norfor Allerton , Andrew Douglas Baxter , Andrew Simon Cook , David Hepworth , Stephen Kwok-Fung Wong
发明人： Charlotte Moira Norfor Allerton , Andrew Douglas Baxter , Andrew Simon Cook , David Hepworth , Stephen Kwok-Fung Wong
IPC分类号： A61K31/5375 , C07D265/30
CPC分类号： C07D265/30 , C07D413/04
摘要： The present invention provides for compounds of formula (I), (Ia) and (Ib) Wherein: A is selected from C—X and N, B is selected from C—Y and N, R1 is selected from H and (C1-C6)alkyl, R2 is selected from H and (C1-C6)alkyl, X is selected from H, HO, C(O)NH2, NH2 Y is selected from H, HO, NH2, Br, Cl and F Z is selected from H, HO, F, CONH2 and CN; And pharmaceutically acceptable salts, solvates and prodrugs thereof; With the provisos that: for a compound of formula (I), (Ia) or (Ib), when A is C—X, B is C—Y, R1 is H or (C1-C6)alkyl and R2 is H or (C1-C6)alkyl at least one of X, Y and Z must be OH; for a compound of formula (I), when A is C—X and B is C—Y, Y is H, Z is H, R1 is H and R2 is H, then X cannot be OH; these compounds are useful as a medicament.
摘要翻译：本发明提供式（I），（Ia）和（Ib）的化合物，其中A选自C-X和N，B选自C-Y和N，R 1选自H和（C1- C6）烷基，R2选自H和（C1-C6）烷基，X选自H，HO，C（O）NH 2，NH 2 Y选自H，HO，NH 2，Br，Cl和FZ选自 H，HO，F，CONH 2和CN; 其药学上可接受的盐，溶剂合物和前药; 条件是：对于式（I），（Ia）或（Ib）的化合物，当A是C-X时，B是C-Y，R1是H或（C1-C6）烷基，R2是H或（C1-C6）烷基，X，Y和Z中的至少一个必须是OH; 对于式（I）化合物，当A为C-X且B为C-Y时，Y为H，Z为H，R 1为H且R 2为H，则X不能为OH; 这些化合物可用作药物。

5. 发明授权

US07649002B2 (3,5-dimethylpiperidin-1yl)(4-phenylpyrrolidin-3-yl)methanone derivatives as MCR4 agonists 有权
标题翻译：（3,5-二甲基哌啶-1-基）（4-苯基吡咯烷-3-基）甲酮衍生物作为MCR4激动剂
公开(公告)号：US07649002B2
公开(公告)日：2010-01-19
申请号：US11051144
申请日：2005-02-03
申请人： Andrew Antony Calabrese , David Sebastien Fradet , David Hepworth , Mark Lansdell
发明人： Andrew Antony Calabrese , David Sebastien Fradet , David Hepworth , Mark Lansdell
IPC分类号： A61K31/454 , C07D403/02
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
摘要翻译：本发明涉及一类通式（I）的黑皮质素MCR4激动剂，其中R1，R2，R3，R4和R5如本文所定义，特别是涉及选择性MCR4激动剂化合物在医药中的用途，含有它们的组合物，其制备方法和在这些方法中使用的中间体。

6. 发明授权

US06610747B2 Phenoxybenzylamine derivatives as SSRIs 失效
标题翻译：苯氧基苄胺衍生物作为SSRIs
公开(公告)号：US06610747B2
公开(公告)日：2003-08-26
申请号：US09941177
申请日：2001-08-27
申请人： Mavis Diane Adam , Mark David Andrews , Mark Leonard Elliott , Geoffrey Edward Gymer , David Hepworth , Harry Ralph Howard, Jr. , Donald Stuart Middleton , Alan Stobie
发明人： Mavis Diane Adam , Mark David Andrews , Mark Leonard Elliott , Geoffrey Edward Gymer , David Hepworth , Harry Ralph Howard, Jr. , Donald Stuart Middleton , Alan Stobie
IPC分类号： A61K3118
CPC分类号： C07D277/62 , A61K31/135 , A61K31/343 , A61K31/381 , A61K31/39 , A61K31/47 , C07C311/08 , C07C323/20 , C07C2602/08 , C07D215/20 , C07D239/74 , C07D307/87 , C07D327/06 , C07D333/54 , C07D333/72
摘要： A compound of general formula (I) wherein R1 and R2 are H, C1-C6alkyl or (CH2)d(C3-C6cycloalkyl) wherein d=0, 1, 2 or 3; or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; Z or Y is —SR3 and the other Z or Y is halogen or —R3; wherein R3 is C1-C4 alkyl optionally substituted with fluorine; except that R3 is not CF3; or Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; R4 and R5, which may be the same or different, are: A—X, wherein A=—CH═CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(═O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R13; wherein R13 is hydroxy, C1-C4alkoxy, F, C1-C6alkyl, haloalkyl, haloalkoxy, —NH2, —NH(C1-C6alkyl) or —N(C1-C6alkyl)2.
摘要翻译：通式（I）的化合物，其中R 1和R 2是H，C 1 -C 6烷基或（CH 2）d（C 3 -C 6环烷基），其中d = 0,1,2或3; 或R 1和R 2与它们所连接的氮一起形成氮杂环丁烷环; Z或Y是-SR 3，另一个Z或Y是卤素或-R 3; 其中R 3是任选被氟取代的C 1 -C 4烷基; 除了R3不是CF3; 或Z和Y连接，使得与互连原子一起形成稠合的5至7元碳环或杂环，并且其中当Z和Y除碳原子之外形成杂环时，连接含有一个或两个独立地选自氧，硫和氮的杂原子; R 4和R 5可以相同或不同，为：A-X，其中A = -CH = CH-或 - （CH 2）p - ，其中p为0,1或2; X是氢，F，Cl，Br，I，CONR6R7，SO2NR6R7，SO2NHC（= O）R6，OH，C1-4烷氧基，NR8SO2R9，NO2，NR6R11，CN，CO2R10，CHO，SR10，S（O）R9或SO2R10 ; 或含有1,2或3个选自N，S和O的杂原子的5-或6-元杂环，任选被一个或多个R 13独立地取代; 其中R 13是羟基，C 1 -C 4烷氧基，F，C 1 -C 6烷基，卤代烷基，卤代烷氧基，-NH 2，-NH（C 1 -C 6烷基）或-N（C 1 -C 6烷基）2。

7. 发明申请

US20090005354A1 New Amino Derivatives and Their Use as Pharmaceuticals 审中-公开
标题翻译：新型氨基衍生物及其作为药物的用途
公开(公告)号：US20090005354A1
公开(公告)日：2009-01-01
申请号：US12208148
申请日：2008-09-10
申请人： Charlotte Moira Norfor Allerton , Andrew Simon Cook , David Hepworth , Duncan Charles Miller
发明人： Charlotte Moira Norfor Allerton , Andrew Simon Cook , David Hepworth , Duncan Charles Miller
IPC分类号： A61K31/397 , C07D413/02 , A61K31/5377 , A61P25/00 , A61P15/00 , C07D401/02
CPC分类号： C07D413/04 , C07D401/04
摘要： The present invention provides for compounds of formula (I): which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.
摘要翻译：本发明提供了式（I）化合物：其是一类多巴胺激动剂，更特别的是在D2上对D3具有选择性的一类激动剂。这些化合物可用于治疗和/或预防性功能障碍，例如女性性功能障碍（FSD），特别是女性性唤起障碍（FSAD），性欲低下症（HSDD;对性不感兴趣），女性高潮无效（FOD;无法达到性高潮）; 男性性功能障碍，特别是男性勃起功能障碍（MED）。本文所提及的男性性功能障碍意在包括射精性疾病，例如早泄，无汗（无法达到性高潮）或期望障碍，如性欲低下症（HSDD;对性不感兴趣）。这些化合物也可用于治疗神经精神障碍和神经变性疾病。

8. 发明申请

US20080075900A1 Biocomposite Material 有权
标题翻译：生物复合材料
公开(公告)号：US20080075900A1
公开(公告)日：2008-03-27
申请号：US11791221
申请日：2005-11-10
申请人： David Hepworth , Eric Whale
发明人： David Hepworth , Eric Whale
IPC分类号： B27N5/02 , B05D7/00 , D02G3/00
CPC分类号： C08J5/045 , C08J5/12 , C08J2301/02 , C08L1/02 , D21C5/005 , D21C9/002 , D21C9/10 , D21H11/20 , D21H27/34 , Y10T156/10 , Y10T428/13 , Y10T428/1303 , Y10T428/1348 , Y10T428/1352 , Y10T428/1359 , Y10T428/139 , Y10T428/2929
摘要： A biocomposite material (1) and methods of production thereof are described. The biocomposite material (1) exhibits a physical stiffness, strength and toughness comparable to known glass fibre composites while its composition makes it inherently impermeable to water. A general formulation for the biocomposite material (1) is given by the expression: Cel(1-x-y) HPIx HPOy where “Cel” represents cellulose fragments (2), “HPI” represents hydrophilic binders (4), “HPO” represents hydrophobic binders (5) and (x) and (y) quantify the percentage by weight of the hydrophilic (4) and hydrophobic binders (5) present within a material, respectively. The described properties of the biocomposite material (1) are achieved when (x) is within the range of from 0.05 to 0.55 and (y) is within the range of from 0.05 to 0.65.
摘要翻译：描述生物复合材料（1）及其生产方法。生物复合材料（1）具有与已知的玻璃纤维复合材料相当的物理刚度，强度和韧性，而其组成使得其固有地不透水。生物复合材料（1）的一般配方由以下表达式给出：Cel（1-xy）HPI x HPO Y y / “代表纤维素片段（2），”HPI“代表亲水性粘合剂（4），”HPO“表示疏水性粘合剂（5）和（x）和（y）定量亲水性（4）和疏水性粘合剂 5）分别存在于材料内。当（x）在0.05至0.55的范围内且（y）在0.05至0.65的范围内时，可以实现生物复合材料（1）的描述性质。

9. 发明申请

US20050267096A1 New indazole and indolone derivatives and their use pharmaceuticals 审中-公开
标题翻译：新吲唑和吲哚酮衍生物及其用途药物
公开(公告)号：US20050267096A1
公开(公告)日：2005-12-01
申请号：US11138706
申请日：2005-05-26
申请人： Charlotte Moira Allerton , David Hepworth , Duncan Miller
发明人： Charlotte Moira Allerton , David Hepworth , Duncan Miller
IPC分类号： A61K31/404 , A61K31/416 , A61K31/454 , A61K31/5377
CPC分类号： C07D413/04 , C07D231/54 , C07D401/04 , C07D403/04
摘要： The present invention provides for compounds of formula (I), which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.
摘要翻译：本发明提供式（I）化合物，其是一类多巴胺激动剂，更特别的是一类在D2上对D3具有选择性的激动剂。这些化合物可用于治疗和/或预防性功能障碍，例如女性性功能障碍（FSD），特别是女性性唤起障碍（FSAD），性欲低下症（HSDD;对性不感兴趣），女性高潮无效（FOD;无法达到性高潮）; 男性性功能障碍，特别是男性勃起功能障碍（MED）。本文所提及的男性性功能障碍意在包括射精性疾病，例如早泄，无汗（无法达到性高潮）或期望障碍，如性欲低下症（HSDD;对性不感兴趣）。这些化合物也可用于治疗神经精神障碍和神经变性疾病。

10. 发明申请

US20050176772A1 Pharmaceutically active compounds 有权
标题翻译：药物活性化合物
公开(公告)号：US20050176772A1
公开(公告)日：2005-08-11
申请号：US11051144
申请日：2005-02-03
申请人： Andrew Calabrese , David Fradet , David Hepworth , Mark Lansdell
发明人： Andrew Calabrese , David Fradet , David Hepworth , Mark Lansdell
IPC分类号： A61K31/454 , C07D401/06 , C07D401/14 , C07D405/14 , C07D43/02
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
摘要翻译：本发明涉及一类通式（I）的黑皮质素MCR4激动剂，其中R 1，R 2，R 3，R 3， SUP> 4和R 5如本文所定义，特别是选择性MCR4激动剂化合物，其在医学上的用途，含有它们的组合物，其制备方法和用于这样的过程。

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