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1. 发明授权

US5939419A 2-benzyl-polycyclic guanine derivatives and process for preparing them 失效
标题翻译： 2-苄基 - 多环鸟嘌呤衍生物及其制备方法
公开(公告)号：US5939419A
公开(公告)日：1999-08-17
申请号：US507508
申请日：1995-08-23
申请人： Deen Tulshian , Brian A. McKittrick , Yan Xia , Samuel Chackalamannil
发明人： Deen Tulshian , Brian A. McKittrick , Yan Xia , Samuel Chackalamannil
IPC分类号： C07D239/54 , C07D473/40 , C07D487/14 , C07D487/20 , A61K31/505 , C07D491/22
CPC分类号： C07D487/14 , C07D239/54 , C07D473/40
摘要： Antihypertensive and bronchodilating compounds of the formula or a pharmaceutically acceptable salt thereof, and a process for preparing them are disclosed, wherein:R.sub.1, R.sub.2, R.sub.3, R.sup.a, R.sup.b and R.sup.c as defined in the disclosure;pharmaceutical compositions containing said compounds;methods of treatment using said compounds; anda process for preparing polycyclic guanines comprisinga) reducing a nitrosopyrimidine, and treating the reduced nitrosopyrimidine with an acylating reagent to give the amidopyrimidine;b) reacting the amidopyrimidine with a halogenating/cyclizing reagent to give a halopurine;c) reacting, in the presence of a base, the halopurine with an amine to give the substituted aminopurine; andd) closing the ring of the substituted aminopurine with a suitable dehydrating agent.
摘要翻译： PCT No.PCT / US94 / 01728 Sec。 371日期1996年11月26日 102（e）日期1996年11月26日PCT 1994年2月24日PCT公布。 WO94 / 19351 PCT出版物 1994年9月1日公开了下式的低血压和支气管扩张化合物或其药学上可接受的盐及其制备方法，其中：本发明中定义的R1，R2，R3，Ra，Rb和Rc; 含有所述化合物的药物组合物; 使用所述化合物的治疗方法; 以及制备多环鸟嘌呤的方法，包括a）还原亚硝基嘧啶，用酰化试剂处理还原的亚硝基嘧啶，得到酰胺嘧啶; b）使酰胺嘧啶与卤化/环化试剂反应得到卤代嘌呤; c）在碱的存在下使卤代嘌呤与胺反应，得到取代的氨基嘌呤; 和d）用合适的脱水剂封闭取代的氨基嘌呤的环。

2. 发明授权

US08148363B2 Heterocyclic compounds as factor IXA inhibitors 有权
标题翻译：杂环化合物作为因子IXA抑制剂
公开(公告)号：US08148363B2
公开(公告)日：2012-04-03
申请号：US12993607
申请日：2009-05-18
申请人： Martin C. Clasby , William J. Greenlee , Yan Xia , Tin-Yau Chan , Mariappan V. Chelliah , Samuel Chackalamannil , Haiyan Pu , Keith A. Eagen , Henry Vaccaro , Brian A. McKittrick , Liyuan Wang , Xiaobang Gao
发明人： Martin C. Clasby , William J. Greenlee , Yan Xia , Tin-Yau Chan , Mariappan V. Chelliah , Samuel Chackalamannil , Haiyan Pu , Keith A. Eagen , Henry Vaccaro , Brian A. McKittrick , Liyuan Wang , Xiaobang Gao
IPC分类号： A61K31/55 , A61K31/4184 , A61K31/5377 , A61K31/4192 , A61K31/454 , A61K31/4439 , A61K31/422 , A61K31/506 , A61K31/496 , A61P7/02 , C07D403/14 , C07D413/14 , C07D403/04 , C07D401/14
CPC分类号： C07D487/04 , C07D231/18 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14
摘要： The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
摘要翻译：本发明涉及式I-III的新型杂环化合物; 如本文所公开的或其药学上可接受的盐，溶剂化物，酯，前药或立体异构体。还公开了包含所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓栓塞性疾病的方法。

3. 发明授权

US07638526B2 Azetidine derivatives useful in treating pain, diabetes and disorders of lipid metabolism 失效
标题翻译：可用于治疗疼痛，糖尿病和脂质代谢紊乱的氮杂环丁烷衍生物
公开(公告)号：US07638526B2
公开(公告)日：2009-12-29
申请号：US11854600
申请日：2007-09-13
申请人： Brian A. McKittrick , Elizabeth M. Smith , Chad E. Bennett , Joel M. Harris , Eugenia Y. Kiselgof , Chad E. Knutson , Peter Korakas , Deen Tulshian , Hyunjin Kim
发明人： Brian A. McKittrick , Elizabeth M. Smith , Chad E. Bennett , Joel M. Harris , Eugenia Y. Kiselgof , Chad E. Knutson , Peter Korakas , Deen Tulshian , Hyunjin Kim
IPC分类号： A61K31/438 , C07D471/10
CPC分类号： C07D471/08
摘要： Disclosed are compounds of the formula: and compounds of the formula: wherein R1, R2, R3, R4, R5, u and v are as defined herein. Also disclosed are methods of treating pain (e.g., inflammatory pain, chronic pain, and neuropathic pain), methods of treating diabetes, and methods of inhibiting the absorption of cholesterol using compounds of formula I or IIA.
摘要翻译：公开了下式的化合物和下式的化合物：其中R 1，R 2，R 3，R 4，R 5，u和v如本文所定义。还公开了治疗疼痛（例如炎性疼痛，慢性疼痛和神经性疼痛）的方法，治疗糖尿病的方法，以及使用式I或IIA化合物抑制胆固醇吸收的方法。

4. 发明授权

US5824683A 2'-��4'-h alo-�1,1'-biphenyl!-4-yl!methyl!-5'-methyl-spiro�cyclopentane-1,7' (8'H)-�3H! imidazo�2,1-b!purin!-4' (5'H)-ones 失效
标题翻译： 2' - [[4'-卤代 - [1,1'-联苯] -4-基]甲基] -5'-甲基 - 螺[环戊烷-1,7'（8'H） - [3 H]咪唑并[ 2,1-b]嘌呤] -4'（5'H） - 酮
公开(公告)号：US5824683A
公开(公告)日：1998-10-20
申请号：US756508
申请日：1996-11-26
申请人： Brian A. McKittrick , Deen Tulshian
发明人： Brian A. McKittrick , Deen Tulshian
IPC分类号： C07D487/20 , A61K31/505 , C07D473/18 , C07D473/40 , C07D487/14
CPC分类号： C07D487/20
摘要： Antihypertensive and bronchodilating phosphoclusterose inhibitory compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein X is fluoro, chloro or bromo.
摘要翻译：抗高血压药和支气管扩张型磷酸荧光蛋白抑制化合物或其药学上可接受的盐，其中X是氟，氯或溴。

5. 发明授权

US5476847A Derivatives of phosphinic acid useful as endothelin converting enzyme inhibitors 失效
标题翻译：次膦酸的衍生物可用作内皮素转化酶抑制剂
公开(公告)号：US5476847A
公开(公告)日：1995-12-19
申请号：US267630
申请日：1994-06-29
申请人： Brian A. McKittrick , Michael F. Czarniecki , Samuel Chackalamannil , Shin Chung , Shawn DeFrees , Andrew W. Stamford
发明人： Brian A. McKittrick , Michael F. Czarniecki , Samuel Chackalamannil , Shin Chung , Shawn DeFrees , Andrew W. Stamford
IPC分类号： A61K31/66 , A61P1/00 , A61P3/08 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07F9/30 , C07F9/572 , C07F9/6558 , A61K31/405 , C07D209/14 , C07F9/36
CPC分类号： C07F9/65583 , C07F9/303 , C07F9/5728
摘要： Phosphinic acid derivatives of the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R.sub.1 and R.sub.2 form a cycloalkyl ring of 3-8 members and R.sub.3 and R.sub.4 are as defined; or R.sub.3 and R.sub.4 form a cycloalkyl ring of 3-7 members and R.sub.1 and R.sub.2 are as defined; or R.sub.1 and R.sub.2 together, and R.sub.3 and R.sub.4 together, each form a cycloalkyl ring;R.sub.5 is --OR.sub.9 or --NHR.sub.9, wherein R.sub.9 is hydrogen or alkyl;n is 0 or 1;A.sub.1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A.sub.1 and R.sub.5 together form a radical of an .alpha.-aminoacyl derivative; andR.sub.6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or --A.sub.2 --R.sub.7, wherein A.sub.2 is a divalent .alpha.-aminoacyl radical, and R.sub.7 is a substituent on the .alpha.-amino atom selected from H, R.sub.8 OCO--, R.sub.8 SO.sub.2 -- and R.sub.8 NHCO--, wherein R.sub.8 is aryl, arylmethyl or (C.sub.1 -C.sub.8)alkyl;are disclosed for use as endothelin converting enzyme inhibitors; also disclosed are a genus of novel compounds wherein R.sup.3 and R.sup.4 form a cycloalkyl ring, and pharmaceutical compositions comprising said novel compounds.
摘要翻译：结构式为“IMAGE”的次膦酸衍生物或其药学上可接受的盐，其中R为H，烷基或烷酰氧基亚甲基; R 1，R 2，R 3和R 4是H，烷基，烯基，链烯基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，羟基烷基，羧基烷基，硫代烷基，烷氧基硫代烷基，氨基烷基，烷基氨基烷基，环烷基取代的烷基或杂环烷基。或R 1和R 2形成3-8成员的环烷基环，并且R 3和R 4如所定义; 或R 3和R 4形成3-7成员的环烷基环，并且R 1和R 2如所定义; 或R 1和R 2一起，并且R 3和R 4一起形成环烷基环; R5是-OR9或-NHR9，其中R9是氢或烷基; n为0或1; A1是对氨基苯甲酰基或对氨基苯磺酰基，或者A1和R5一起形成α-氨基酰基衍生物的基团; R6为苯基甲氧基羰基，芳基羰基，杂芳基羰基或-A2-R7，其中A2为二价α-氨基酰基，R7为选自H，R8OCO-，R8SO2-和R8NHCO-的α-氨基原子上的取代基，其中R8 是芳基，芳甲基或（C1-C8）烷基; 被公开用作内皮素转化酶抑制剂; 还公开了一种其中R3和R4形成环烷基环的新化合物，以及包含所述新化合物的药物组合物。

6. 发明授权

US08426403B2 Gamma secretase modulators 有权
标题翻译：伽玛分泌酶调节剂
公开(公告)号：US08426403B2
公开(公告)日：2013-04-23
申请号：US12601322
申请日：2008-05-28
申请人： Zhaoning Zhu , William J. Greenlee , Xianhai Huang , Brian A. McKittrick , John W. Clader , Mark D. McBriar , Anandan Palani
发明人： Zhaoning Zhu , William J. Greenlee , Xianhai Huang , Brian A. McKittrick , John W. Clader , Mark D. McBriar , Anandan Palani
IPC分类号： A61K31/5365 , A61K31/5395 , C07D498/04 , A61P25/28
CPC分类号： C07D498/04 , C07D403/10 , C07D471/04 , C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。

7. 发明申请

US20080188485A1 PIPERIDINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS 有权
标题翻译：哌啶衍生物作为CCR5拮抗剂有用
公开(公告)号：US20080188485A1
公开(公告)日：2008-08-07
申请号：US12055900
申请日：2008-03-26
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
IPC分类号： A61K31/496 , A61P1/00 , A61P19/02
CPC分类号： C07D401/06 , A61K31/496 , A61K45/06 , C07D211/58 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroarylalkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，芴基，二苯甲基或任选取代的苯基或杂芳基烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5和R 7是氢或烷基; R 6是氢，烷基或链烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

8. 再颁专利

USRE37721E1 Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents 有权
标题翻译：用作降胆固醇药的羟基取代的氮杂环丁酮化合物
公开(公告)号：USRE37721E1
公开(公告)日：2002-05-28
申请号：US09594996
申请日：2000-06-15
申请人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
发明人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
IPC分类号： C07D20508
CPC分类号： C07D205/08 , A61K9/2018 , A61K9/4858 , A61K31/21 , A61K31/35 , A61K31/395 , A61K31/40 , A61K45/06 , Y02P20/55 , Y10S514/824 , A61K2300/00
摘要： Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X, Y and Z are —CH2—, —CH(lower alkyl)— or —C(dilower alkyl)—; R and R2 are —OR6, —O(CO)R6, —O(CO)OR9 or —O(CO)NR6R7; R1 and R3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5; R4 is selected from lower alkyl, R5, —CF3, —CN, —NO2 and halogen R5 is selected from —OR6, —O(CO)R6, —O(CO)OR9, —O(CH2)1-5OR6, —O(CO)NR6R7, —NR6R7, —NR6(CO)R7, —NR6(CO)OR9, —NR6(CO)NR7R8, —NR6SO2R9, —COOR6, —CONR6R7, —COR6, —SO2NR6R7, S(O)0-2R9, —O(CH2)1-10—COOR6, —O(CH2)1-10CONR6R7, —(lower alkylene)COOR6 and —CH═CH—COOR6; R6, R7 and R8 are H, lower alkyl or aryl-substituted Ic R9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them; and a process for preparing them.
摘要翻译：羟基取代的氮杂环丁酮低胆固醇血症药或其药学上可接受的盐，其中：Ar1和Ar2是芳基或R4取代的芳基; Ar3是芳基或R5-取代的芳基; X，Y和Z是-CH2-，-CH（低级烷基） - 或-C（二卤代烷基） - ; R和R 2为-OR 6，-O（CO）R 6，-O（CO）OR 9或-O（CO）NR 6 R 7; R 1和R 3为H或低级烷基; q为0或1; r为0或1; m，n和p为0-4; 条件是q和r中的至少一个为1，m，n，p，q和r的和为1-6; 并且条件是当p为O且r为1时，m，q和n的和为1-5; R 4选自低级烷基，R 5，-CF 3，-CN，-NO 2，卤素R 5选自-OR 6 ，-O（CO）R 6，-O（CO）OR 9，-O（CH 2）1-5 OR 6，-O（CO）NR 6 R 7，-NR 6 R 7，-NR 6（CO）R 7，-NR 6（CO）OR 9，-NR 6 （CO）NR7R8，-NR6SO2R9，-COOR6，-CONR6R7，-COR6，-SO2NR6R7，S（O）0-2R9，-O（CH2）1-10-COOR6，-O（CH2）1-10CONR6R7， - （低级亚烷基）COOR 6和-CH = CH-COOR 6; R6，R7和R8是H，低级烷基或芳基取代的IcR9是低级烷基，芳基或芳基取代的低级烷基;以及降低血清的方法通过单独或与胆固醇生物合成抑制剂组合施用所述化合物，含有它们的药物组合物; 和一个准备它们的过程。

9. 发明授权

US4785015A Substituted 1,3,4,9-tetrahydropyrano [3,4-B]indole-1-acetic acids 失效
标题翻译：取代的1,3,4,9-四氢吡喃并[3,4-B]吲哚-1-乙酸
公开(公告)号：US4785015A
公开(公告)日：1988-11-15
申请号：US117775
申请日：1987-11-05
申请人： Brian A. McKittrick , Alan H. Katz
发明人： Brian A. McKittrick , Alan H. Katz
IPC分类号： A61K31/40 , A61P25/04 , A61P29/00 , C07D491/04 , C07D491/052
CPC分类号： C07D491/04
摘要： Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1-, 4-, 5-, 6-, 7- and 8- are disclosed. The derivatives are useful anti-inflammatory and analgesic agents and methods for their preparation and use are also disclosed.

10. 发明授权

US07902157B2 Azetidine and azetidone derivatives useful in treating pain and disorders of lipid metabolism 失效
标题翻译：用于治疗疼痛和脂质代谢紊乱的氮杂环丁烷和氮杂环丁烷衍生物
公开(公告)号：US07902157B2
公开(公告)日：2011-03-08
申请号：US11854711
申请日：2007-09-13
申请人： Duane A. Burnett , Brian A. McKittrick
发明人： Duane A. Burnett , Brian A. McKittrick
IPC分类号： C07D471/10 , A61K31/438 , A61P3/06 , A61P25/04
CPC分类号： C07D487/10
摘要： Disclosed are compounds of the formula wherein Z1 is —CH2—or —C(O)—, R4 and R5 are carbon chains (and optionally, together can form a C2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R2 is heteroaryl, and R1 and R3 are as defined herein. Also disclosed are methods of treating pain, and methods of inhibiting the absorption of cholesterol using a compound of formula I.
摘要翻译：公开了下式的化合物其中Z 1是-CH 2 - 或-C（O） - ，R 4和R 5是碳链（并且可以一起形成C 2桥），u和v独立地是0-3的整数总和为3至5，并且R 2为杂芳基，且R 1和R 3如本文所定义。还公开了治疗疼痛的方法，以及使用式I化合物抑制胆固醇吸收的方法。

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