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1. 发明申请

US20020037861A1 Anticonvulsant derivatives useful for preventing the development of Type II diabetes mellitus and Syndrome X 有权
标题翻译：用于预防II型糖尿病和X综合征发展的抗惊厥药物
公开(公告)号：US20020037861A1
公开(公告)日：2002-03-28
申请号：US09900567
申请日：2001-07-06
发明人： Carlos Plata-Salaman , Jeffrey Crooke
IPC分类号： A61K031/7024 , A61K031/357 , A61K031/35 , A61K031/255
CPC分类号： A61K31/36 , A61K31/255 , A61K31/35 , A61K31/357 , A61K31/7048
摘要： Anticonvulsant derivatives useful for preventing the development of Type II diabetes mellitus and Syndrome X are disclosed.
摘要翻译：公开了可用于预防II型糖尿病和综合征X发展的抗惊厥药物。

2. 发明申请

US20020091152A1 Medicament for treatment of irritable bowel syndrome 失效
标题翻译：用于治疗肠易激综合征的药物
公开(公告)号：US20020091152A1
公开(公告)日：2002-07-11
申请号：US10022274
申请日：2001-12-20
申请人： MITSUBISHI CHEMICAL CORPORATION
发明人： Michikazu Abe , Ken-Ichi Saito
IPC分类号： A61K031/357
CPC分类号： C07D407/12 , A61K31/357 , A61K31/36 , C07D319/20
摘要： A medicament for preventive and/or therapeutic treatment of irritable bowel syndrome which comprises as an active ingredient a substance selected from the group consisting of an alkylenedioxybenzene derivative represented by the following general formula (I) and a pharmaceutically acceptable salt thereof, and a hydrate thereof and a solvate thereof: 1 wherein m represents an integer of from 2 to 5, and n represents an integer of from 1 to 3 (e.g., 5-null3-null(2S)-(1,4-benzodioxan-2-ylmethyl)aminonullpropoxynull-1,3-benzodioxol).
摘要翻译：一种用于预防和/或治疗肠易激综合征的药物，其包含选自以下通式（I）表示的亚烷基二氧苯衍生物及其药学上可接受的盐及其水合物作为活性成分的物质和其溶剂合物：其中m表示2至5的整数，n表示1至3的整数（例如，5- [3 - [（2S） - （1,4-苯并二恶烷-2-基甲基）氨基]丙氧基] -1,3-苯并间二氧杂环戊烯）。

3. 发明申请

US20020068758A1 Novel orally active iron (III) chelators 有权
标题翻译：新型口服活性铁（III）螯合剂
公开(公告)号：US20020068758A1
公开(公告)日：2002-06-06
申请号：US09944113
申请日：2001-09-04
申请人： BTG International Limited.
发明人： Robert Charles Hider , Gary Stuart Tilbrook , Zudong Liu
IPC分类号： A61K031/357 , C07D319/04
CPC分类号： C07D213/69 , C07D213/81 , C07D309/40 , C07D417/06 , C07D493/04
摘要： A novel 3-hydroxypyridinone compound of formula I is provided 1 wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6 -aryloxy or C7-10 aralkoxy ether thereof, R3 is selected from hydrogen and C1-6 alkyl; and R4 is selected from hydrogen, C1-6 alkyl and a group as described for R2 ; characterized in that R2 is selected from groups (i) nullCONHnullR5 (ii) nullCH2NHCOnullR5 (iii) nullSO2NHnullR5 (iv) nullCH2NHSO2nullR5 (v) nullCR6R6OR7 (viii) nullCONHCOR5 wherein R5 is selected from hydrogen and optionally hydroxy, alkoxy, or aralkoxy substituted C1-13 alkyl, aryl and C7-13 aralkyl, R6 is independently selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl, and R7 is selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl or a pharmaceutically acceptable salt of any such compound with the proviso that when R7 is hydrogen, R6 is not selected from aryl and with the proviso that the compound is not 1-ethyl-2-(1null-hydroxyethyl)-3-hydroxypyridin-4-one.
摘要翻译：提供式I的新颖的3-羟基吡啶酮化合物，其中R是氢或通过体内代谢除去以提供游离羟基化合物的基团，R 1是脂族烃基或被羟基取代的脂族烃基或羧酸酯，磺酸酯或C 1-6烷氧基，C 6芳氧基或C 7-10芳烷氧基醚，R 3选自氢和C 1-6烷基; 并且R 4选自氢，C 1-6烷基和如对于R 2所述的基团; 其特征在于R2选自基团（ⅰ）-CONH-R5（ⅱ）-CH2NHCO-R5（ⅲ）-SO2NH-R5（ⅳ）-CH2NHSO2-R5（ⅴ）-CR6R6OR7（ii）-CONHCOR5，其中选择R5 由氢和任选的羟基，烷氧基或芳烷氧基取代的C 1-13烷基，芳基和C 7-13芳烷基，R 6独立地选自氢，C 1-13烷基，芳基和C 7-13芳烷基，并且R 7选自氢，C 1 -13烷基，芳基和C7-13芳烷基或任何此类化合物的药学上可接受的盐，条件是当R7为氢时，R6不选自芳基，条件是该化合物不是1-乙基-2-（ 1'-羟乙基）-3-羟基吡啶-4-酮

4. 发明申请

US20020068075A1 Citral Acetal 有权
标题翻译：柠檬醛缩醛
公开(公告)号：US20020068075A1
公开(公告)日：2002-06-06
申请号：US09973017
申请日：2001-10-10
申请人： Kao Corporation
发明人： Sakuya Tanaka , Shigeyoshi Tanaka , Shunichi Akiba , Katsutoshi Ara , Hirohiko Ishida
IPC分类号： A61K031/357 , A61K007/00 , A61K007/46 , C07D317/18
CPC分类号： C07D317/22 , A61K8/4973 , A61K2800/782 , A61Q13/00 , A61Q15/00 , A61Q19/00
摘要： The present invention provides a citral acetal capable of sustaining a lemon aroma unique to citral and a perfume composition comprising the citral acetal, as well as an LDH inhibitor and a deodorant, cosmetics and a skin agent for external application, comprising the LDH inhibitor. The citral acetal of the present invention is represented by formula (1): 1 wherein the wavy line represents a cis and/or trans form, and R represents a C1, to C9, linear or branched alkyl group.
摘要翻译：本发明提供了能够维持柠檬醛独特的柠檬香气和包含柠檬醛缩醛的香料组合物的柠檬醛缩醛，以及包含LDH抑制剂的LDH抑制剂和用于外用的除臭剂，化妆品和皮肤剂。本发明的柠檬醛缩醛由式（1）表示：其中波浪线表示顺式和/或反式，R表示C1至C9直链或支链烷基。

5. 发明申请

US20040058981A1 Methods of using artemisinin-like compounds to prevent or delay the appearance of cancer 审中-公开
标题翻译：使用青蒿素样化合物预防或延缓癌症的出现的方法
公开(公告)号：US20040058981A1
公开(公告)日：2004-03-25
申请号：US10457079
申请日：2003-06-06
申请人： University of Washington
发明人： Henry C. Lai , Narendra P. Singh
IPC分类号： A61K031/357
CPC分类号： A61K31/555 , A61K31/00 , A61K31/295 , A61K31/335 , A61K31/357 , A61K38/40 , A61K2300/00
摘要： The invention provides methods for preventing or delaying the development of cancer by administering free radical-generating agents to a subject. Representative free radical-generating agents include endoperoxide compounds, such as endoperoxides bearing sesquiterpene compounds such as artemisinin and its analogs, arteflene and its analogs, 1,2,4-trioxanes and 1,2,4,5-tetraoxanes. Intracellular iron concentrations may be enhanced by the administration of iron salts or complexes.
摘要翻译：本发明提供了通过向受试者施用自由基产生剂来预防或延缓癌症发展的方法。代表性的自由基产生剂包括内过氧化物化合物，例如含有倍半萜烯化合物如青蒿素及其类似物的内过氧化物，芳香烯及其类似物，1,2,4-三恶烷和1,2,4,5-四氧杂环己烷。通过施用铁盐或络合物可增强细胞内铁的浓度。

6. 发明申请

US20020128231A1 Aryl-indane compounds 审中-公开
标题翻译：芳基 - 茚满化合物
公开(公告)号：US20020128231A1
公开(公告)日：2002-09-12
申请号：US09976929
申请日：2001-10-11
发明人： Anita Melikian-Badalian
IPC分类号： A61K031/695 , A61K031/137 , A61K031/357 , A61K031/195
CPC分类号： C07D295/185 , C07C62/34 , C07C69/734 , C07C69/757 , C07C217/74 , C07C233/78 , C07C235/40 , C07C235/50 , C07C235/60 , C07C275/24 , C07C311/17 , C07C2602/08 , C07D295/096 , C07D295/205 , C07F7/1804
摘要： A new family of compounds, particularly aryl-indane compounds, is disclosed. The compounds may be used as inhibitors of P-glycoprotein-mediated transport. Use of the compounds to enhance bioavailability and to modulate multi-drug resistance to chemotherapeutic agents is disclosed.
摘要翻译：公开了一系列化合物，特别是芳基 - 二氢化茚化合物。这些化合物可以用作P-糖蛋白介导的转运的抑制剂。公开了使用该化合物以提高生物利用度和调节对化学治疗剂的多药耐药性。

7. 发明申请

US20020049221A1 Synthesis and methods of use of new antimitotic agents 失效
标题翻译：新型抗有丝分裂剂的合成和使用方法
公开(公告)号：US20020049221A1
公开(公告)日：2002-04-25
申请号：US09910195
申请日：2001-07-19
发明人： John S. Lazo , Peter Wipf , Billy W. Day
IPC分类号： A61K031/4747 , A61K031/357 , C07D47/02
CPC分类号： C07D317/72 , A61K31/357 , A61K31/426 , C07D319/08 , C07D403/12 , C07D405/06 , C07D405/12 , C07D493/10
摘要： Oxidative cyclization of bis-naphthyl ethers allows concise total syntheses of palmarumycin CP, and deoxypreussomerin A in 8-9 steps and 15-35% overall yield from 5-hydroxy-8-methoxy-1 -tetralone. A small library of palmarumycin analogs was created. Biological evaluation of these naphthoquinone spiroketals against MCF-7 and MDA-MB-23 1 human breast cancer cells revealed several low-micromolar growth inhibitors. A number of the analogs inhibit the thioredoxin -thioredoxin reductase system.
摘要翻译：双萘基醚的氧化环化允许5-9个步骤中的棕榈霉素CP和脱氧阿司咪霉素A的简明综合，5-羟基-8-甲氧基-1-四氢萘酮的总产率为15-35％。创建了一个古老的棕榈霉素类似物库。这些萘醌螺旋酮对MCF-7和MDA-MB-23 1人乳腺癌细胞的生物学评价显示出几种低微摩尔生长抑制剂。许多类似物抑制硫氧还蛋白 - 硫氧还蛋白还原酶系统。

8. 发明申请

US20020016361A1 Beta-amino acid nitrile derivatives as cathepsin K inhibitors 失效
标题翻译： β-氨基酸腈衍生物作为组织蛋白酶K抑制剂
公开(公告)号：US20020016361A1
公开(公告)日：2002-02-07
申请号：US09872927
申请日：2001-06-01
发明人： Tobias Gabriel , Michael Pech , Rosa Maria Rodriguez Sarmiento
IPC分类号： A61K031/357 , A61K031/277 , A61K031/275 , C07D317/44 , C07C255/42
CPC分类号： C07C311/20 , C07C255/29 , C07C255/44 , C07C271/24 , C07C311/13 , C07C311/46 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07D307/85 , C07D317/60 , C07D333/32
摘要： The present invention relates to beta-amino acid nitrile derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are cysteine protease inhibitors useful for the treatment of diseases associated with cysteine proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.
摘要翻译：本发明涉及β-氨基酸腈衍生物及其药学上可接受的盐和/或其药学上可接受的酯。该化合物是半胱氨酸蛋白酶抑制剂，可用于治疗与半胱氨酸蛋白酶相关的疾病，例如骨质疏松症，骨关节炎，类风湿性关节炎，肿瘤转移，肾小球性肾炎，动脉粥样硬化，心肌梗塞，心绞痛，不稳定性心绞痛，中风，斑块破裂，短暂性脑缺血攻击，黑斑病，外周动脉闭塞性疾病，血管成形术和支架置入后再狭窄，腹主动脉瘤形成，炎症，自身免疫性疾病，疟疾，眼底组织细胞病变和呼吸系统疾病。

9. 发明申请

US20030013660A1 Dioxolane analogs for improved inter-cellular delivery 审中-公开
标题翻译：二氧杂环戊烷类似物用于改善细胞内递送
公开(公告)号：US20030013660A1
公开(公告)日：2003-01-16
申请号：US09976249
申请日：2001-10-15
申请人： Shire BioChem Inc.
发明人： Giorgio Attardo , Boulos Zacharie , Rabindra Rej , Jean-Francois Lavallee , Louis Vaillancourt , Real Denis , Sophie Levesque
IPC分类号： A61K031/675 , A61K031/665 , A61K031/522 , A61K038/05 , A61K038/06 , A61K031/513 , A61K031/404 , A61K031/4025 , A61K031/357
CPC分类号： C07D405/04 , C07D473/18 , C07F9/65515 , C07F9/65586 , C07F9/65616
摘要： Dioxolane analogs of the following formula: 1 wherein R1 and R2 are defined herein, are useful in the treatment of cancer. For example, the compounds can be used to treat patients with cancer in which the cancer cells are deficient in nucleoside or nucleoside base transporters.
摘要翻译：下式的二氧杂环戊烷类似物：其中R1和R2如本文所定义，可用于治疗癌症。例如，这些化合物可用于治疗癌细胞中核苷或核苷碱基转运蛋白缺乏的癌症患者。

10. 发明申请

US20020151580A1 Synthetic spiroketal pyranes as potent anti-cancer agents and use 失效
标题翻译：合成螺旋缩酮作为有效的抗癌剂和用途
公开(公告)号：US20020151580A1
公开(公告)日：2002-10-17
申请号：US09974070
申请日：2001-10-09
申请人： Parker Hughes Institute
发明人： Fatih M. Uckun , Chen Mao , He Huang
IPC分类号： A61K031/357
CPC分类号： C07D493/10 , C07C323/41 , C07D307/12 , C07D307/42 , C07K14/47
摘要： Novel tubulin binding compounds (SPIKETS) having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel SP binding pocket on tubulin, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.
摘要翻译：新型微管蛋白结合化合物（SPIKETS）具有强大的微管蛋白解聚活性和对微管蛋白聚合的抑制活性。这些化合物是抑制细胞增殖的有效剂，例如在癌细胞中。该化合物适于与微管蛋白上的新型SP结合袋有利地相互作用，该口袋可用于筛选抗微管蛋白，抗增殖和抗癌药物。

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