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1. 发明申请

US20080213281A1 Butyrylcholinesterase Variants that Alter the Activity of Chemotherapeutic Agents 审中-公开
标题翻译：丁酰胆碱酯酶改变化疗药物活性的变体
公开(公告)号：US20080213281A1
公开(公告)日：2008-09-04
申请号：US10535441
申请日：2003-12-04
申请人： Jeffrey D. Watkins , James D. Pancock
发明人： Jeffrey D. Watkins , James D. Pancock
IPC分类号： A61K39/395 , A61K38/43 , C12N9/00 , C07D471/04 , C07H19/00 , A61P35/00
CPC分类号： C12N9/18 , A61K38/00
摘要： The invention provides a butyrylchinesterase variant, a method of converting a camptothecin derivative to a topoisomerase inhibitor by contacting the camptothecin derivative with a butyrylcholinesterase variant and a method of treating cancer by administering to an individual an effective amount a butyrylcholinesterase variant exhibiting increased capability to convert a camptothecin derivative to a topoisomerase inhibitor compared to butyrylcholinesterase.
摘要翻译：本发明提供丁酰基切割酶变体，通过使喜树碱衍生物与丁酰胆碱酯酶变体接触来将喜树碱衍生物转化为拓扑异构酶抑制剂的方法和通过向个体施用有效量的治疗癌症的方法，所述丁酰胆碱酯酶变体表现出增加的转化能力的丁酰胆碱酯酶变体喜树碱衍生物与拓扑异构酶抑制剂相比，与丁酰胆碱酯酶相比。

2. 发明申请

US20090118167A1 Selective Vpac2 Receptor Peptide Agonists 审中-公开
标题翻译：选择性Vpac2受体肽激动剂
公开(公告)号：US20090118167A1
公开(公告)日：2009-05-07
申请号：US11573917
申请日：2005-08-11
申请人： Bengt Krister Bokvist , John Philip Mayer , Lianshan Zhang , Jorge Alsina-Fernandez , Andrew Mark Vick
发明人： Bengt Krister Bokvist , John Philip Mayer , Lianshan Zhang , Jorge Alsina-Fernandez , Andrew Mark Vick
IPC分类号： A61K38/17 , C07K14/475
CPC分类号： A61K47/60
摘要： The invention provides VPAC2R peptide agonists coupled to at least one polyethylene glycol molecule or derivative thereof, resulting in a biologically active peptide with an extended half-life and a slower clearance when compared to that of unPEGylated peptide.
摘要翻译：本发明提供了与至少一种聚乙二醇分子或其衍生物偶联的VPAC2R肽激动剂，当与未PEG化肽相比时，产生具有延长的半衰期和较慢清除率的生物活性肽。

3. 发明申请

US20080207716A1 Formulations and Dosing Regiment for Ppar-Alpha Modulators 审中-公开
标题翻译： Ppar-α调制剂的配方和配料团
公开(公告)号：US20080207716A1
公开(公告)日：2008-08-28
申请号：US11814487
申请日：2006-01-25
申请人： Eyas Jamal Abu-Raddad , Michael Arthur Derby , Cynthia Joyce Harris , Daniel Charles Howey , Laura Frey Michael
发明人： Eyas Jamal Abu-Raddad , Michael Arthur Derby , Cynthia Joyce Harris , Daniel Charles Howey , Laura Frey Michael
IPC分类号： A61K31/4196 , A61P3/00 , A61P25/00 , A61P9/00 , A61P35/00
CPC分类号： A61K31/4196
摘要： The present invention provides dosing regimens for PPAR-alpha agonist and compositions thereof. A further embodiment of the present invention is a solid oral formulation of Propanoic Acid, 2-[4-[3-[2,5-dihy-dro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxyl-2-methyl- comprising 75 μg or less of Propanoic Acid, 2-[4-[3-[2,5-dihydro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methyl- per dosage unit.
摘要翻译：本发明提供PPAR-α激动剂及其组合物的给药方案。本发明的另一个实施方案是丙酸，2- [4- [3- [2,5-二氢 - 1 - [（4-甲基苯基）甲基] -5-氧代-1H- 1,2,4-三唑-3-基]丙基]苯氧基-2-甲基 - 包含75摩尔或更少的丙酸，2- [4- [3- [2,5-二氢-1 - [（4- 甲基苯基）甲基] -5-氧代-1H-1,2,4-三唑-3-基]丙基]苯氧基] -2-甲基 - 。

4. 发明申请

US20070078166A1 Novel crystalline forms of {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1h-[1,2,3] triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone 有权
标题翻译： {2- [1-（3,5-双 - 三氟甲基 - 苄基）-5-吡啶-4-基-1h - [1,2,3]三唑-4-基] - 吡啶-3-基] （2-氯苯基） - 甲酮
公开(公告)号：US20070078166A1
公开(公告)日：2007-04-05
申请号：US10574712
申请日：2004-10-12
申请人： Alfio Borghese , David Coffey , Pamela Footman , Steven Pedersen , Susan Reutzel-Edens , Shella Tameze , Carsten Timpe , Carsten Weber
发明人： Alfio Borghese , David Coffey , Pamela Footman , Steven Pedersen , Susan Reutzel-Edens , Shella Tameze , Carsten Timpe , Carsten Weber
IPC分类号： A61K31/444 , C07D403/14
CPC分类号： C07D401/14 , C07D213/50
摘要： The present invention provides novel crystalline forms of {2-[1-(3,5-bistrifluoromethylbenzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, compositions thereof, intermediates thereof, methods of using the same, processes for making the same, and processes for making intermediates thereof.
摘要翻译：本发明提供{2- [1-（3,5-双三氟甲基苄基）-5-吡啶-4-基-1H- [1,2,3]三唑-4-基] - 吡啶-3-基] （2-氯苯基） - 甲酮，其组合物，其中间体，其使用方法，制备方法及其制备中间体的方法。

5. 发明申请

US20060293223A1 Uses of melanocortin-3 receptor (mc3r) agonist peptides 审中-公开
标题翻译：黑皮质素-3受体（mc3r）激动剂肽的使用
公开(公告)号：US20060293223A1
公开(公告)日：2006-12-28
申请号：US10556690
申请日：2004-06-17
申请人： Robert Gadski , Mark Heiman , Hansen Hsiung , John Mayer , Liang Yan
发明人： Robert Gadski , Mark Heiman , Hansen Hsiung , John Mayer , Liang Yan
IPC分类号： A61K38/12
CPC分类号： A61K38/12
摘要： The present invention provides methods of treating metabolic disorders, including, for example, obesity, diabetes mellitus, cachexia, sarcopenia, and cardiovascular disorders, methods of inducing weight loss and increasing muscle mass in a patient, by administration of MC3R agonist peptides. Furthermore, the present invention provides the use of an MC3R agonist peptide for the manufacture of a medicament for the treatment of metabolic disorders, including, for example, obesity, diabetes mellitus, cachexia, sarcopenia, and cardiovascular disorders, inducing weight loss and increasing muscle mass in a patient.
摘要翻译：本发明提供了通过施用MC3R激动剂肽来治疗代谢紊乱的方法，包括例如肥胖症，糖尿病，恶病质，肌营养不良和心血管疾病，诱导患者体重减轻和增加肌肉质量的方法。此外，本发明提供了MC3R激动剂肽用于制备用于治疗代谢紊乱的药物的用途，所述代谢紊乱包括例如肥胖，糖尿病，恶病质，肌营养不良和心血管疾病，引起体重减轻和增加肌肉在病人身上。

6. 发明申请

US20060167268A1 Growth hormone secretagogues 审中-公开
公开(公告)号：US20060167268A1
公开(公告)日：2006-07-27
申请号：US10510305
申请日：2003-03-31
申请人： Britta Evers , Ruehter Gerd , Eva Martin De La Nava , Mark Tebbe
发明人： Britta Evers , Ruehter Gerd , Eva Martin De La Nava , Mark Tebbe
IPC分类号： C07D275/02 , C07D207/24
CPC分类号： C07D275/02 , C07D275/06
摘要： This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.

7. 发明申请

US20070105845A1 Quinolone derivatives 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：US20070105845A1
公开(公告)日：2007-05-10
申请号：US10551272
申请日：2004-04-15
申请人： Nicholas Camp , Roberta Penariol , Christopher Beadle
发明人： Nicholas Camp , Roberta Penariol , Christopher Beadle
IPC分类号： A61K31/5415 , A61K31/538 , A61K31/4704
CPC分类号： C07D215/227 , C07D409/04
摘要： This invention relates to compounds of formula (I) where —X—, n, R1, R3 and Ar— have the values defined herein, their preparation, and use as pharmaceuticals.
摘要翻译：本发明涉及式（I）的化合物，其中-X-，n，R 1，R 3和Ar-具有本文定义的值，其制备和用途作为药物。

8. 发明申请

US20070088288A1 Fixed dose medication dispensing device 有权
标题翻译：固定剂量药物分配装置
公开(公告)号：US20070088288A1
公开(公告)日：2007-04-19
申请号：US10575502
申请日：2004-10-15
申请人： Traci Barron , Andrew Burroughs , David Hixson
发明人： Traci Barron , Andrew Burroughs , David Hixson
IPC分类号： A61M5/00
CPC分类号： A61M5/3158 , A61M5/24 , A61M5/31541 , A61M5/3155 , A61M5/31551 , A61M2005/3125 , A61M2205/581 , A61M2205/583 , A61M2205/585
摘要： A guide and follower cooperate to promote a user moving the driver relative to the housing along a travel path that operates the apparatus. The cooperating elements of the nut and the driver are disengaged when the driver is disposed in a reset segment of the travel path, and the cooperating elements of the nut and the driver become engaged when the driver is shifted through a nut engaging segment of the travel path from the reset segment to a nut rotating segment of the travel path. The engagement of the cooperating elements of the nut and the driver cause the nut to screw proximally along the threaded shaft of the drive member when the driver is shifted through the nut rotating segment from the nut engaging segment to an injecting section of the travel path. When the driver is shifted through the injecting section from the nut rotating segment to the reset segment, the nut and the drive member are shifted in the distal direction to axially advance a fluid container piston to dispense medicine, and the cooperating elements of the nut and the driver become disengaged.
摘要翻译：引导和跟随器协作以促进使用者沿着操作该装置的行进路径相对于壳体移动驾驶员。当驾驶员设置在行进路径的复位段中时，螺母和驾驶员的配合元件脱开，并且当驾驶员通过行进的螺母接合部分移动时，螺母和驾驶员的配合元件接合从复位段到行进路径的螺母旋转段的路径。当驾驶员通过螺母旋转部分从螺母接合部分移动到行进路径的注入部分时，螺母和驱动器的配合元件的接合使螺母沿着驱动部件的螺纹轴向近侧螺旋。当驾驶员通过注射部分从螺母旋转段移动到复位段时，螺母和驱动构件在远端方向上移动以轴向前进流体容器活塞以分配药物，并且螺母的协作元件司机变得脱离了。

9. 发明申请

US20060211755A1 3-oxo-1, 3-dihydro-indazole-2-carboxylic acid amide derivatives as phospholipase inhibitors 审中-公开
公开(公告)号：US20060211755A1
公开(公告)日：2006-09-21
申请号：US10544910
申请日：2004-03-25
申请人： Patrick Eacho , Patricia Foxworthy-Mason , Ho-Shen Lin , Jose Lopez , Marian Mosior , Michael Richett
发明人： Patrick Eacho , Patricia Foxworthy-Mason , Ho-Shen Lin , Jose Lopez , Marian Mosior , Michael Richett
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： C07D231/56 , C07D405/12 , C07D409/12
摘要： The present invention provides a compound of formula I (1) wherein; R, is selected from the group consisting of C5-C13alkyl; C,—C,2haloalkyl, C4C,2alkenyl, C4-C12alkynyl, or C,—C5alkylcycloalkyl, C3-C8cycloalkyl, C, C5alkylheterocyclic, and aryl, wherein the, cycloalkyl, cycloalkenyl, heterocyclic and aryl substituents are optionally substituted with one to three substituents independently selected from C,—C8a)kyl, C,—C8haloalkyl, ′C2-CBalkenyl, C2-C8a)kynyl, phenyl, benzyl, hydroxy, C,—C5 alkoxy, (C}12)m000C,—Csalkyl, (CH2)mNRaRb, and C,C4alkylcycloalkyl; wherein W and Rb are independently selected from hydrogen, C,CBalkyl, C2-CBalkenyl, C2-CBalkynyl, and C,—C5alkylcycloalkyl; R2 is hydrogen; R3, R4, R5, and R6, are independently selected from hydrogen, C,—C12alkyl, C2C,2haloalkyl, C2-C,2 alkenyl, C2-C12alkynyl, C,—C12alkylaryl, C,—C12alkylcyclohexyl, C, C12alkylcyclopentyl, C,—C12alkylheterocyclic, (CH2)m000H, (CH2)mC0(C,—C,o)alkyl, (CH2)m COO(C,—C,o)alkyl, (CH2)mCOO(C1-C,o)alkylaryl, C,—C,oalkylamino, halo, (CH2)mCONH2, (CH2)rCONRaRb, phenyl, or aryl wherein each of the phenyl or aryl groups is optionally substituted with one to three groups independently selected from CBalkyl, C,—CBhaloalkyl, C2-CBalkenyl, CZCBalkynyl, phenyl, benzyl, hydroxy, C,—C5 alkoxy, (CH2)m000C,—Csalkyl, and C,—C4alkylcycloalkyl; and wherein m is 0, 1, 2, or 3; R7 is selected from the group consisting of hydrogen, C,—Cloalkyl, C,C,ohaloalkyl, C2-C,oalkenyl, C2-C,oalkynyl, C,—C6alkylaryl, C,—C6alkylcyclohexyl, C—C6aikylcyclopentyl, C,—C6alkylheterocyclic, or aryl; or a pharmaceutically acceptable sallvate thereofi together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase-mediated diseases.

10. 发明申请

US20060084663A1 Peroxisome proliferator activated receptor modulators 失效
标题翻译：过氧化物酶体增殖物激活受体调节剂
公开(公告)号：US20060084663A1
公开(公告)日：2006-04-20
申请号：US10505103
申请日：2003-02-13
申请人： Scott Conner , Nathan Mantlo , Guoxin Zhu
发明人： Scott Conner , Nathan Mantlo , Guoxin Zhu
IPC分类号： A61K31/506 , A61K31/501 , A61K31/497 , A61K31/4439 , C07D417/02
CPC分类号： C07D413/04 , C07D263/32 , C07D277/24 , C07D277/26 , C07D413/10 , C07D417/04 , C07D417/10
摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, substituted aryl(C0-C4)alkyl, substituted aryloxy(C0-C4)alkyl, substituted arylthio(C0-C4)alkyl, unsubstituted aryl(C0-C4)alkyl, unsubstituted aryloxy(C0-C4)alkyl, and unsubstituted arylthio(C0-C4)alkyl; (b) T1 is C or N; (c) Q is selected from the group consisting of O, a single bond, O(CH2)q and C; (d) q is 1 or 2; (e) W is selected from the group consisting of O, S, (CH2)rN(R20)(CH2)k, NHSO2, C(O)N(R20)(CH2)r, (CH2)rN(R20)C(O), and SO2; (f) X is CmH2m; (g) m is 0, 1 or 2; (h) A is an functional group selected from the group consisting of carboxyl, C1-C3 alkylnitrile, carboxamide, and (CH2)nCOOR19; and (i) R19 is selected from the group consisting of hydrogen, optionally substituted C1-C4alkyl and optionally substituted arylmethyl.
摘要翻译：本发明涉及由以下结构式表示的化合物及其药学上可接受的盐，式I：其中：（a）R 5选自（C 1 -C 3）（C 1 -C 6）烷基，（C 1 -C 6 -C 6）链烯基，取代的芳基（C 0 -C 6 - 取代的芳氧基（C 0 -C 4 -C 4烷基）烷基，取代的芳硫基（C 0 -C 4 - 烷基，未取代的芳基（C 0 -C 4 -C 4）烷基，未取代的芳氧基（C 0 -C 4 - 烷基和未取代的芳硫基（C 0 -C 4 -C 4）烷基; （b）T1为C或N; （c）Q选自O，单键，O（CH 2 CH 2）q C和C; （d）q为1或2; （e）W选自O，S，（CH 2）n N（R 20）（CH 2 CH 2） C（O）N（R 20）（CH 2）n），（CH

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