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41. 发明申请

US20080286219A1 Hydroquinone derivative skin brightening compounds 审中-公开
标题翻译：对苯二酚衍生物皮肤增白剂
公开(公告)号：US20080286219A1
公开(公告)日：2008-11-20
申请号：US11804120
申请日：2007-05-17
申请人： Michael Fitzpatrick Wempe , Jeffrey M. Clauson
发明人： Michael Fitzpatrick Wempe , Jeffrey M. Clauson
IPC分类号： A61K8/34 , A61K8/49 , A61Q19/02 , C07C43/178 , C07C59/52 , C07C69/66 , C07D207/16 , C07D277/36
CPC分类号： C07C323/59 , C07C323/20 , C07C323/52 , C07C323/57 , C07C323/60 , C07C2601/08 , C07C2601/14 , C07D207/16 , C07D277/36 , C07D333/18
摘要： Skin brightening compositions based on hydroquinone derivatives and methods of making and using the composition. The hydroquinone derivatives are 2-thio-hydroquinone derivatives.
摘要翻译：基于氢醌衍生物的皮肤增亮组合物和制备和使用该组合物的方法。氢醌衍生物是2-硫代氢醌衍生物。

42. 发明申请

US20080226716A1 AMINO ACID CONJUGATES PROVIDING FOR SUSTAINED SYSTEMIC CONCENTRATION OF GABA ANALOGUES 失效
标题翻译：提供持续的GABA类似物系统浓度的氨基酸联合
公开(公告)号：US20080226716A1
公开(公告)日：2008-09-18
申请号：US12128225
申请日：2008-05-28
申请人： Mark Gallop , Kenneth C. Cundy , Randall A. Scheuerman , Ronald W. Barrett , Noa Zerangue
发明人： Mark Gallop , Kenneth C. Cundy , Randall A. Scheuerman , Ronald W. Barrett , Noa Zerangue
IPC分类号： C07C61/08 , A61K31/195 , A61K31/35 , C07D315/00 , A61K31/38 , A61K31/40 , A61K31/403 , C07D207/00 , A61P25/00 , A61P25/30 , A61P1/00 , A61P29/00 , A61K9/22
CPC分类号： C07D233/64 , A61K38/00 , A61K47/64 , C07C237/12 , C07C237/20 , C07C317/50 , C07C323/59 , C07C323/60 , C07C2601/14 , C07D207/16 , C07K5/0205 , G01N33/566
摘要： Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.
摘要翻译：公开了在口服给予动物后提供持续的全身浓度的GABA类似物的化合物。还公开了药物组合物，以及使用这些化合物的方法。

43. 发明申请

US20080176821A1 LIGANDS FOR METABOTROPIC GLUTAMATE RECEPTORS AND INHIBITORS OF NAALADASE 有权
标题翻译：代谢谷氨酸受体和NAALADASE抑制剂的配体
公开(公告)号：US20080176821A1
公开(公告)日：2008-07-24
申请号：US12029367
申请日：2008-02-11
申请人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
发明人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
IPC分类号： A61K31/664 , A61K31/662 , A61K31/195 , A61K31/225 , A61P25/00 , A61P25/02 , A61P25/18
CPC分类号： C07D257/04 , C07C59/347 , C07C69/716 , C07C271/22 , C07C275/16 , C07C275/26 , C07C323/59 , C07C335/08 , C07F9/301 , C07F9/303
摘要： The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.
摘要翻译：本发明涉及其化合物是代谢型谷氨酸受体或NAALADase酶或两者的配体，例如激动剂或拮抗剂的新化合物及其制剂。本发明还涉及使用本发明的化合物或制剂调节代谢型谷氨酸受体或NAALADase酶或两者的活性的方法，例如在有需要的受试者中。本发明还涉及使用化合物或至少部分由内源性代谢型谷氨酸受体或NAALADase酶或两者的活性异常而治疗患有慢性或急性疾病，疾病或病症的受试者的方法，本发明的制剂。

44. 发明申请

US20080108692A1 Organoselenium compound for cancer chemoprevention 失效
标题翻译：有机硒化合物用于癌症化学预防
公开(公告)号：US20080108692A1
公开(公告)日：2008-05-08
申请号：US11980875
申请日：2007-10-30
申请人： Luke Lam , Nayaz Ahmed
发明人： Luke Lam , Nayaz Ahmed
IPC分类号： A61K31/26 , C07C391/00 , C07C323/57 , A61K31/381 , A61K31/33 , A61P35/00 , A61K31/341 , C07K5/06 , C07K5/08
CPC分类号： C07D333/14 , A23L33/10 , A61K38/00 , C07C323/58 , C07C323/59 , C07C391/00 , C07D333/20 , C07D333/22 , C07D345/00 , C07K5/0215 , C07K5/0606
摘要： A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.
摘要翻译：含有亚硒基异氰酸酯或亚烷基异氰酸酯部分的化合物有效地防止癌症或癌前病症的发生或发展。化合物可以以药物组合物，化妆品，食品添加剂，补充剂等的形式提供和施用。还提供了本发明的化学预防化合物的合成和使用方法。

45. 发明授权

US07358248B2 Substituted amino carboxylic acids 失效
标题翻译：取代的氨基羧酸
公开(公告)号：US07358248B2
公开(公告)日：2008-04-15
申请号：US10835817
申请日：2004-04-30
申请人： Darren Whitehouse , Shaojing Hu , Michael C. Van Zandt , Garrett Parker , Thomas G. Meskill
发明人： Darren Whitehouse , Shaojing Hu , Michael C. Van Zandt , Garrett Parker , Thomas G. Meskill
IPC分类号： A61K31/5355 , C07D265/30 , C07D295/02 , C07D307/79 , C07D323/02
CPC分类号： C07D239/26 , C07C323/59 , C07D209/08 , C07D307/79 , C07D307/81 , C07D307/91 , C07D317/56 , C07D333/76 , C07D405/04 , C07D405/12 , C07D417/04
摘要： Disclosed are compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
摘要翻译：公开了式（I）的化合物和药学上可接受的盐：其可用于治疗与胰岛素抵抗，瘦素抗性或高血糖相关的代谢紊乱。本发明的化合物包括可用于治疗糖尿病和其它PTP介导的疾病如癌症，神经变性疾病等的蛋白质酪氨酸磷酸酶抑制剂，特别是蛋白质酪氨酸磷酸酶-1B（PTP-1B）。还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。

46. 发明授权

US07348319B2 Nitric oxide-releasing amidine diazeniumdiolates, compositions and uses thereof and method of making same 失效
标题翻译：一氧化氮释放脒二氮烯二硫氰酸盐，其组成及用途及其制备方法
公开(公告)号：US07348319B2
公开(公告)日：2008-03-25
申请号：US11208313
申请日：2005-08-19
申请人： Joseph A Hrabie , Larry K Keefer , Ernst V Arnold
发明人： Joseph A Hrabie , Larry K Keefer , Ernst V Arnold
IPC分类号： A61K31/675 , A61K31/655
CPC分类号： A61K31/655 , A61K31/13 , A61K38/00 , C07C291/02 , C07C323/59
摘要： The present invention relates to nitric oxide-releasing amidine diazeniundiolates, compositions comprising same, methods of using same, and a method for preparing same from imidate diazeniumdiolates and primary or secondary amines.
摘要翻译：本发明涉及一氧化氮释放脒二氮烯二十一碳二烯酸酯，包含其的组合物，其使用方法及其制备方法，由酰亚胺二氮烯二硫鎓和伯胺或仲胺。

47. 发明申请

US20070282002A1 ACYLAMIDE COMPOUNDS HAVING SECRETAGOGUE OR INDUCER ACTIVITY OF ADIPONECTIN 失效
标题翻译：具有ADIPONECTIN的秘密活性或诱导活性的酰亚胺化合物
公开(公告)号：US20070282002A1
公开(公告)日：2007-12-06
申请号：US11835029
申请日：2007-08-07
申请人： Katsumi MAEZONO , Toshihiko Yoshimura , Nozomu Ishida , Naoyuki Fukuchi , Toshihiro Hatanaka , Osamu Ikehara , Yayoi Kawato , Hideyuki Tanaka
发明人： Katsumi MAEZONO , Toshihiko Yoshimura , Nozomu Ishida , Naoyuki Fukuchi , Toshihiro Hatanaka , Osamu Ikehara , Yayoi Kawato , Hideyuki Tanaka
IPC分类号： A61K31/198 , C07C235/12
CPC分类号： C07C233/47 , A23L33/10 , C07C323/59
摘要： The present invention provides an acylamide compound of the following formula (1), prodrugs thereof, or pharmaceutically acceptable salts thereof; and an adiponectin inducer or secretagogue, therapeutic agent of metabolic syndromes, therapeutic agent of hypoadiponectinemia, therapeutic agent of hyperlipemia, preventive/therapeutic agent of diabetes, improving agent of impaired glucose tolerance, improving agent of insulin resistance, enhancing agent of insulin sensitivity, therapeutic agent of hypertension, preventive/therapeutic agent of vascular disorders, an anti-inflammatory agent, therapeutic agent of hepatic inflammation, therapeutic agent of fatty liver, therapeutic agent of hepatic fibrosis, therapeutic agent of liver cirrhosis, preventive/therapeutic agent of non-alcoholic/nonviral steatohepatitis (NASH) or non-alcoholic/nonviral fatty liver disease (NAFLD), or therapeutic agent of obesity, each of which has the above compounds as an active ingredient.
摘要翻译：本发明提供下式（1）的酰胺化合物，其前体药物或其药学上可接受的盐; 和脂联素诱导剂或促分泌素，代谢综合征的治疗剂，低脂联素血症的治疗剂，高脂血症的治疗剂，糖尿病的预防/治疗剂，葡萄糖耐量降低的改善剂，胰岛素抵抗的改善剂，胰岛素敏感性的增强剂，治疗高血压药物，血管疾病的预防/治疗剂，抗炎剂，肝脏炎症治疗剂，脂肪肝治疗剂，肝纤维化治疗剂，肝硬化治疗剂，非酒精性预防/治疗剂 /非病毒性脂肪性肝炎（NASH）或非酒精性/非病毒性脂肪性肝病（NAFLD）或肥胖症治疗剂，其各自具有上述化合物作为活性成分。

48. 发明申请

US20070265323A1 COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
标题翻译：用于治疗代谢性疾病的化合物
公开(公告)号：US20070265323A1
公开(公告)日：2007-11-15
申请号：US11772556
申请日：2007-07-02
申请人： Shalini Sharma , Reid von Borstel , Kirvin Hodge , Michael Bamat , Stephen Wolpe
发明人： Shalini Sharma , Reid von Borstel , Kirvin Hodge , Michael Bamat , Stephen Wolpe
IPC分类号： A61K31/41 , A61K31/192 , A61P3/10 , A61P7/12 , A61K31/216
CPC分类号： C07B41/12 , A01N37/10 , A61K31/165 , A61K31/192 , A61K31/216 , A61K31/235 , A61K31/41 , A61K31/4196 , A61K31/44 , A61K31/445 , A61K31/535 , A61K31/54 , C07C59/68 , C07C59/90 , C07C67/47 , C07C69/738 , C07C209/68 , C07C217/22 , C07C233/31 , C07C233/47 , C07C235/78 , C07C235/84 , C07C259/06 , C07C323/52 , C07C323/59 , C07C2601/02 , C07C2601/04 , C07C2602/04 , C07D213/30 , C07D213/55 , C07D249/10 , C07D249/12 , C07D257/04 , C07D333/16 , C07D333/24 , Y10S514/866
摘要： Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
摘要翻译：公开了可用于治疗各种代谢紊乱（例如胰岛素抵抗综合征，糖尿病，高脂血症，脂肪肝疾病，恶病质，肥胖症，动脉粥样硬化和动脉硬化）的化合物。

49. 发明授权

US07183440B2 Pharmaceutically useful compounds 有权
标题翻译：药用有用化合物
公开(公告)号：US07183440B2
公开(公告)日：2007-02-27
申请号：US11059086
申请日：2005-02-07
申请人： Stanley Michael Roberts , Maria Gabriella Santoro , Vasudev Jadhav , Alan Michael Happe , Jérôme Dauvergne
发明人： Stanley Michael Roberts , Maria Gabriella Santoro , Vasudev Jadhav , Alan Michael Happe , Jérôme Dauvergne
IPC分类号： C07C315/00 , C07C49/00 , A61K31/12 , A61K31/095
CPC分类号： C07C323/59 , C07C45/673 , C07C49/647 , C07C49/653 , C07C49/657 , C07C49/753 , C07C205/45 , C07C225/20 , C07C233/32 , C07C233/76 , C07C271/24 , C07C271/36 , C07C271/56 , C07C271/66 , C07C311/20 , C07C311/53 , C07C323/43 , C07C2601/08 , C07C2601/10
摘要： A compound of formula (I) or (II): wherein A is hydrogen or CR1R2; Y and Z are each, independently, hydrogen or a halogen; X is —NR4R5, or R7; R1 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1–4 carbon atoms; when X is —NR4R5, R2 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1–12 carbon atoms; when X is R7, R2 is an unsubstituted alkyl, alkenyl or alkynyl group, or a substituted or unsubstituted aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1–12 carbon atoms; R3 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1–12 carbon atoms; R4 is hydrogen, a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1–12 carbon atoms, —COOR8, or —COR8; R5 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1–5 carbon atoms; R7 is an unsubstituted alkyl, alkenyl, or alkynyl group, that contains 1–4 carbon atoms; and, R8 is an unsubstituted or halo-substituted alkyl, aryl, or aralkyl group, that contains 1–12 carbon atoms
摘要翻译：式（I）或（II）的化合物：其中A是氢或CR 1 R 2; Y和Z各自独立地为氢或卤素; X是-NR 4 R 5或R 7; R 1是氢或含有1-4个碳原子的取代或未取代的烷基或链烯基; 当X是-NR 4 R 5时，R 2是取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基基团，其任选地在其碳骨架中包含至少一个杂原子并且含有1-12个碳原子; 当X是R 7时，R 2是未取代的烷基，烯基或炔基，或取代或未取代的芳基，芳烷基芳烯基或芳炔基，其任选地包括在其碳骨架中至少有一个杂原子，含有1-12个碳原子; R 3是取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子; R 4是氢，取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子， -COOR 8或-COR 8; R 5是氢或含有1-5个碳原子的取代或未取代的烷基或链烯基; R 7是含有1-4个碳原子的未取代的烷基，烯基或炔基; 并且R 8是含有1-12个碳原子的未取代或卤素取代的烷基，芳基或芳烷基

50. 发明授权

US07074831B2 Compounds, methods for their preparation and use thereof 失效
标题翻译：化合物，其制备方法和用途
公开(公告)号：US07074831B2
公开(公告)日：2006-07-11
申请号：US11050430
申请日：2005-02-04
申请人： Stig Jönsson , Gunnar Andersson , Ulf Wellmar , Ingela Fritzson
发明人： Stig Jönsson , Gunnar Andersson , Ulf Wellmar , Ingela Fritzson
IPC分类号： A61K31/192 , C07C65/105
CPC分类号： C07C233/54 , C07C233/63 , C07C233/75 , C07C235/56 , C07C275/36 , C07C323/59 , C07C323/63 , C07C2601/02 , C07D207/06 , C07D211/14 , C07D295/096 , C07D295/155
摘要： Compounds of formula (I) for clinical treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection and malignant neoplasia. A pharmaceutical composition comprising a compound of formula (I) in an amount giving a daily dosage of from 0.005 mg/kg to 10 mg/kg body weight, in particular from 0.025 mg/kg to 2 mg/kg body weight.
摘要翻译：用于临床治疗自身免疫疾病，炎性疾病，器官移植排斥和恶性肿瘤的式（I）化合物。一种药物组合物，其包含给予每日剂量为0.005mg / kg至10mg / kg体重，特别是0.025mg / kg至2mg / kg体重的式（I）化合物。

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