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1. 发明授权

US08642603B2 Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof 有权
标题翻译：取代的二氢和四氢恶唑啉嘧啶酮，其制备和应用
公开(公告)号：US08642603B2
公开(公告)日：2014-02-04
申请号：US12554129
申请日：2009-09-04
申请人： Bin Cao , Vieroslava Gurunian , Sathapana Kongsamut , Raymond W. Kosley, Jr. , Rosy Sher , Ryan E. Hartung
发明人： Bin Cao , Vieroslava Gurunian , Sathapana Kongsamut , Raymond W. Kosley, Jr. , Rosy Sher , Ryan E. Hartung
IPC分类号： C07D491/04 , A61K31/519 , A61P25/28 , A61P25/22 , A61P25/18 , A61P25/06 , A61P25/02
CPC分类号： C07D498/04
摘要： The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
摘要翻译：本发明涉及一系列取代的二氢和四氢恶唑啉嘧啶酮，特别涉及一系列2-取代-2,3-二氢 - 恶唑并[3,2-a]嘧啶-7-酮和2-取代-2,2-二氧杂唑并[ （I）的3,5,6-四氢恶唑并[3,2-a]嘧啶-7-酮：其中p，n，X，Y，R1，R2，R3，R4，R5，R6， R7和R8如本文所定义。本发明还涉及制备这些化合物的方法，包括新型中间体。本发明的化合物是代谢型谷氨酸受体（mGluR），特别是mGluR2受体的调节剂。因此，本发明的化合物可用作药物，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经变性疾病，精神病，抽搐，焦虑，抑郁症，偏头痛，疼痛，睡眠障碍和呕吐。

2. 发明授权

US07919628B2 CXCR2 inhibitors 有权
标题翻译： CXCR2抑制剂
公开(公告)号：US07919628B2
公开(公告)日：2011-04-05
申请号：US11771958
申请日：2007-06-29
申请人： Stephanie Hachtel , Juergen Dedio , Holger Heitsch , Werngard Czechtizky , Sven Grueneberg , Stephen J. Shimshock , Raymond W. Kosley, Jr. , Carolina L. Lanter , Hui Li , Rosy Sher , Aleksandra Weichsel
发明人： Stephanie Hachtel , Juergen Dedio , Holger Heitsch , Werngard Czechtizky , Sven Grueneberg , Stephen J. Shimshock , Raymond W. Kosley, Jr. , Carolina L. Lanter , Hui Li , Rosy Sher , Aleksandra Weichsel
IPC分类号： C07D277/64 , A61K31/426
CPC分类号： C07D213/68 , C07D207/325 , C07D213/30 , C07D213/65 , C07D213/69 , C07D215/14 , C07D217/26 , C07D231/12 , C07D233/64 , C07D249/06 , C07D249/08 , C07D249/18 , C07D261/08 , C07D263/32 , C07D271/12 , C07D277/24 , C07D277/64 , C07D307/42 , C07D317/54 , C07D319/20 , C07D333/56 , C07D333/70 , C07D409/12 , C07D417/12 , C07D495/04
摘要： The invention relates to compounds of the formula I: in which R1, R2, X, A, B, D and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
摘要翻译：本发明涉及式I化合物：其中R1，R2，X，A，B，D和Y1至Y4具有权利要求中所示的含义，和/或其药学上可接受的盐和/或前药。由于其作为趋化因子受体的抑制剂的特性，特别是作为CXCR2抑制剂，式I化合物及其药学上可接受的盐和前药适用于预防和治疗趋化因子介导的疾病。

3. 发明授权

US07125903B1 Thienoisoxazolyl-and thienylpyrrazolyl-phenoxy substituted propyl derivatives useful as D4 antagonists 失效
标题翻译：噻吩异恶唑基和噻吩基吡唑基 - 苯氧基取代的丙基衍生物，可用作D4拮抗剂
公开(公告)号：US07125903B1
公开(公告)日：2006-10-24
申请号：US10088250
申请日：2000-09-13
申请人： David M. Fink , Brian S. Freed , Nicholas J. Hrib , Raymond W. Kosley, Jr. , George E. Lee , Gregory H. Merriman , Barbara S. Rauckman
发明人： David M. Fink , Brian S. Freed , Nicholas J. Hrib , Raymond W. Kosley, Jr. , George E. Lee , Gregory H. Merriman , Barbara S. Rauckman
IPC分类号： A61K31/42 , A61K31/415 , C07D261/00 , C07D231/00
CPC分类号： C07D495/04
摘要： The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
摘要翻译：这些化合物是类似噻吩并恶唑基和噻吩基吡唑基 - 苯氧基取代的丙基衍生物，可用作D 4 N 4拮抗剂。所述化合物可用于治疗通过抑制D 4受体介导的医学病症。这些病症包括例如注意力缺陷多动障碍，强迫症，精神病，药物滥用，物质依赖性，帕金森病，帕金森综合征，迟发性麻痹症，杜氏综合征，行为障碍和反对性反抗障碍。本发明的另一方面是提供药物组合物，中间体和制备所述类化合物的方法。

4. 发明授权

US06316439B1 Galanthamine derivatives as acetylcholinesterase inhibitors 失效
标题翻译： Galanthamine衍生物作为乙酰胆碱酯酶抑制剂
公开(公告)号：US06316439B1
公开(公告)日：2001-11-13
申请号：US08137444
申请日：1993-10-15
申请人： Raymond W. Kosley, Jr. , Larry Davis , Veronica Taberna
发明人： Raymond W. Kosley, Jr. , Larry Davis , Veronica Taberna
IPC分类号： C07D49106
CPC分类号： C07D491/10
摘要： This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12)alkylcarbonyl, (C1-C12)alkoxycarbonyl, aryl(C1-C12)alkylaminocarbonyl, mono(C1-C18)alkylaminocarbonyl or di(C1-C8)alkylaminocarbonyl; R2 is (C1-C12)alkylcarbonyloxy, aryl(C1-C4)alkylcarbonyloxy, (C1-C12)alkoxycarbonyloxy, arylcarbonyloxy, hydroxy, (C1-C6)alkoxycarbonyl(C1-C6)alkoxy or hydroxy(C1-C10)alkoxy; R3 is hydrogen or halo; and pharmaceutically acceptable addition salts; with the proviso that when R2 is hydroxy, R1 and R3 are not both hydrogen or when R2 is hydroxy and R3 is hydrogen, R1 is not methylcarbonyl; which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing the compounds and methods for making and using the compounds.
摘要翻译：本申请涉及式（Ⅳ）化合物，其中R1是氢，（C1-C12）烷基羰基，（C1-C12）烷氧基羰基，芳基（C1-C12）烷基氨基羰基，单（C1-C18）烷基氨基羰基或二（C1-C8）烷基氨基羰基; R2是（C1-C12）烷基羰基氧基，芳基（C1-C4）烷基羰基氧基，（C1-C12）烷氧基羰氧基，芳基羰基氧基，羟基，（C1-C6）烷氧羰基（C1-C6）烷氧基或羟基（C1-C10）是氢或卤素; 和药学上可接受的加成盐; 条件是当R 2是羟基时，R 1和R 3不是氢或当R 2是羟基且R 3是氢时，R 1不是甲基羰基;这些化合物可用于治疗以胆碱能功能降低为特征的记忆功能障碍，含有化合物的制备和使用方法。

5. 发明授权

US5565579A (1H-indol-1-yl)-2-(amino)acetamides and related (1H-indol-1-yl)-(aminoalkyl)amides 失效
标题翻译：（1H-吲哚-1-基）-2-（氨基）乙酰胺和相关的（1H-吲哚-1-基） - （氨基烷基）酰胺
公开(公告)号：US5565579A
公开(公告)日：1996-10-15
申请号：US218211
申请日：1994-03-25
申请人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
发明人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P25/00 , C07D209/08 , C07D209/12 , C07D209/30
CPC分类号： C07D209/08 , A61K31/40 , C07D209/12 , C07D209/30
摘要： There are disclosed compounds having the formula ##STR1## wherein X, Y, Z and R.sub.1 -R.sub.6 are defined in the specification and pharmaceutically acceptable addition salts thereof, or where applicable, the optical or geometrical isomers or racemic mixtures thereof, intermediates in the process for making the compounds, a process for making the compounds and pharmaceutical compositions and method of use as neuroprotective agents.
摘要翻译：公开了具有式“IMAGE”的化合物，其中X，Y，Z和R 1 -R 6在本说明书及其药学上可接受的加成盐中定义，或适用时，其光学或几何异构体或外消旋混合物，该方法中的中间体用于制备化合物，制备化合物的方法和药物组合物以及用作神经保护剂的方法。

6. 发明授权

US5274116A 1-aminoacetamidopyrroles and 1-aminoacetamido-2-(substituted)pyrroles and related compounds 失效
标题翻译： 1-氨基乙酰胺吡咯和1-氨基乙酰胺基-2-（取代）吡咯及相关化合物
公开(公告)号：US5274116A
公开(公告)日：1993-12-28
申请号：US922291
申请日：1992-07-30
申请人： Lawrence Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
发明人： Lawrence Martin , Raymond W. Kosley, Jr. , Denise M. Flanagan , Gert U. Kuerzel , Peter A. Nemoto , David G. Wettlaufer
IPC分类号： A61K31/40 , A61K31/00 , A61K31/4025 , A61P25/28 , C07D207/335 , C07D207/34 , C07D207/50 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/06 , C07D409/14 , C07D401/06
CPC分类号： C07D403/04 , C07D207/50 , C07D409/06
摘要： There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)-pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.

7. 发明授权

US4999351A 7-aryl and heteroaryl ethers of desacetylforskolin 失效
标题翻译：去乙酰福斯克林的7-芳基和杂芳基醚
公开(公告)号：US4999351A
公开(公告)日：1991-03-12
申请号：US295840
申请日：1989-01-11
申请人： Raymond W. Kosley, Jr. , Gerard O'Malley , Bettina Spahl
发明人： Raymond W. Kosley, Jr. , Gerard O'Malley , Bettina Spahl
IPC分类号： C07D311/92 , C07D405/12 , C07D413/12 , C07D417/12 , C07D473/00 , C07D493/06 , C07D493/10
CPC分类号： C07D405/12 , C07D311/92 , C07D473/00 , C07D493/10
摘要： Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.

8. 发明授权

US4851397A Labdanes, pharmaceutical compositions, and their use 失效
标题翻译： Labdanes，药物组合物及其用途
公开(公告)号：US4851397A
公开(公告)日：1989-07-25
申请号：US204791
申请日：1988-06-10
申请人： Raymond W. Kosley, Jr. , Robert J. Cherill
发明人： Raymond W. Kosley, Jr. , Robert J. Cherill
IPC分类号： C07D311/92 , C07D407/12 , C07D493/04 , C07D493/10 , C07D493/20 , C07F7/18 , C07F9/655
CPC分类号： C07D407/12 , C07D311/92 , C07D493/04 , C07D493/10 , C07F7/1856 , C07F9/65502
摘要： Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
摘要翻译：公开了新颖的实验室，其中间体及其制备方法，以及利用化合物或其组合物降低眼内压的方法。

9. 发明授权

US4639443A Labdane compounds, pharmaceutical compositions and use 失效
公开(公告)号：US4639443A
公开(公告)日：1987-01-27
申请号：US848053
申请日：1986-04-04
申请人： Raymond W. Kosley, Jr. , Robert J. Cherill
发明人： Raymond W. Kosley, Jr. , Robert J. Cherill
IPC分类号： C07D311/92 , C07D407/12 , C07D493/04 , C07D493/10 , C07D493/20 , C07F7/18 , C07F9/655 , A61K31/35 , A61K31/535 , C07D319/04 , C07D413/06
CPC分类号： C07D407/12 , C07D311/92 , C07D493/04 , C07D493/10 , C07F7/1856 , C07F9/65502
摘要： Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.

10. 发明授权

US4518713A Analgesic substituted-1-aminoalkylamino-4-aryloxypiperidines 失效
标题翻译：止痛性取代的-1-氨基烷基氨基-4-芳氧基哌啶
公开(公告)号：US4518713A
公开(公告)日：1985-05-21
申请号：US600265
申请日：1984-04-13
申请人： Raymond W. Kosley, Jr. , Richard C. Allen
发明人： Raymond W. Kosley, Jr. , Richard C. Allen
IPC分类号： A61K31/443 , A61K31/445 , A61P25/04 , C07D211/46 , C07D317/00 , C07D317/28 , C07D405/12
CPC分类号： C07D405/12 , C07D211/46 , C07D317/28
摘要： There are described analgesic substituted-1-aminoalkylamino-4-aryloxypiperidines of the formula ##STR1## where X is hydrogen, loweralkyl, CF.sub.3, acetyl or halogen; n is 1 or 2; R.sub.1 is H.sub.2 or oxygen; R.sub.2 is H, loweralkyl or benzyl; and R.sub.3 is oxygen or --OCH.sub.2 CH.sub.2 O--, which are useful as analgesic agents and intermediate compounds therefor.
摘要翻译：描述了式为“IMAGE”的镇痛取代的-1-氨基烷基氨基-4-芳氧基哌啶，其中X是氢，低级烷基，CF 3，乙酰基或卤素; n为1或2; R1是H2或氧; R2是H，低级烷基或苄基; 并且R 3为氧或-OCH 2 CH 2 O-，其可用作止痛剂及其中间体化合物。

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