序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
1 蛋白酶抑制剂 CN98806641.6 1998-04-29 CN1261276A 2000-07-26 S·M·哈尔伯特; E·米绍; S·K·汤普森; D·F·韦贝尔
发明提供抑制蛋白酶,包括组织蛋白酶K的式(Ⅰ)化合物,含有式Ⅰ化合物的药用组合物,治疗过量骨丢失或软骨或基质降解的疾病,包括骨质疏松症和龈病包括龈炎和牙周炎,关节炎,特别是骨关节炎和类湿关节炎,paget氏病,高血症或恶性肿瘤以及代谢性骨疾病的方法。
2 生物相容的含N,N-二取代磺酰胺的荧光染料标记 CN200680040360.8 2006-09-01 CN101296927A 2008-10-29 N·纳拉亚南; K·格罗夫斯; J·D·彼得森; M·拉约帕德耶
发明涉及新的荧光化学实体,尤其是包含生物相容性的N,N-二取代磺酰胺荧光染料的荧光分子。本发明还涉及该分子相应的活性形式。本发明也涉及具有部分例如肽、蛋白质、不同生物分子、环和杂环化合物、糖的相应缀合物,以及它们的用途。
3 蛋白酶抑制剂 CN99815093.2 1999-12-21 CN1253441C 2006-04-26 小R·W·马奎斯; 玉汝; D·F·维贝尔; M·D·库明斯; S·K·汤普森; D·雅马施塔
发明提供了抑制包括组织蛋白酶K的蛋白酶的4-基-氮杂环庚烷-3-蛋白酶抑制剂及其可药用盐、合物和溶剂化物,含这些化合物的药物组合物,这些化合物的新的中间体,以及治疗骨损失或者软骨或骨基质降解过度的疾病的方法,这些疾病包括骨质疏松症;包括齿龈炎和牙周炎的齿龈病;关节炎,特别是骨关节炎和类湿性关节炎;佩吉特氏病;恶性血过多;及代谢性骨病,该方法包含给需要的患者施用本发明的化合物来抑制所述骨损失或软骨或骨基质降解过度。
4 丙型肝炎病毒抑制剂 CN201080061374.4 2010-11-10 CN102712628B 2014-10-15 R·拉瓦; J·A·本德; J·L·罗米内; E·H·吕迪格; C·巴尚; O·D·罗佩斯; 陈琦; M·贝勒马; J·F·卡多; L·G·哈曼
申请涉及如在说明书中所定义的式(I)新化合物和包含所述新化合物的组合物。这些化合物是有用的抗病毒剂,尤其可用于抑制由丙型肝炎病毒(HCV)编码的NS5A蛋白的功能。因此,本申请还涉及通过使用这些新化合物或包含所述新化合物的组合物来治疗HCV相关疾病或病症的方法。
5 丙型肝炎病毒抑制剂 CN201080061374.4 2010-11-10 CN102712628A 2012-10-03 R·拉瓦; J·A·本德; J·L·罗米内; E·H·吕迪格; C·巴尚; O·D·罗佩斯; 陈琦; M·贝勒马; J·F·卡多; L·G·哈曼
申请涉及如在说明书中所定义的式(I)新化合物和包含所述新化合物的组合物。这些化合物是有用的抗病毒剂,尤其可用于抑制由丙型肝炎病毒(HCV)编码的NS5A蛋白的功能。因此,本申请还涉及通过使用这些新化合物或包含所述新化合物的组合物来治疗HCV相关疾病或病症的方法。
6 蛋白酶抑制剂 CN99815093.2 1999-12-21 CN1350458A 2002-05-22 小R·W·马奎斯; 玉汝; D·F·维贝尔; M·D·库明斯; S·K·汤普森; D·雅马施塔
发明提供了抑制包括组织蛋白酶K的蛋白酶的4-基-氮杂环庚烷-3-蛋白酶抑制剂及其可药用盐、合物和溶剂化物,含这些化合物的药物组合物,这些化合物的新的中间体,以及治疗骨损失或者软骨或骨基质降解过度的疾病的方法,这些疾病包括骨质疏松症;包括齿龈炎和牙周炎的齿龈病;关节炎,特别是骨关节炎和类湿性关节炎;佩吉特氏病;恶性血过多;及代谢性骨病,该方法包含给需要的患者施用本发明的化合物来抑制所述骨损失或软骨或骨基质降解过度。
7 Substituted benzisoxazole and benzisothiazole herbicide JP4566296 1996-02-08 JP4167731B2 2008-10-22 ピーター・ジヨン・ウエプロ
8 Wood storage stability oxathiazine compound JP50778095 1994-08-24 JP2761441B2 1998-06-04 DEEBISU ROBAATO EI; BARUTSUKE ARETSUKUSU AARU EI; BUROWAA UORUTAA JII
9 Wood storage stability oxathiazine compound JP50778095 1994-08-24 JPH08509986A 1996-10-22 エイ. デービス,ロバート; アール.エイ. バルッケ,アレックス; ジー. ブロウワー,ウオルター
(57)【要約】 本発明は、木材および複合木材材料を木材損傷および木材分解作用体に対して長期間保存するのに有用な、或る群の3−アリール−5,6−ジヒドロ−1,4,2−オキサチアジン化合物およびそれらのオキサイドを提供する。 本発明はまた、これらの3−アリール−5,6−ジヒドロ−1,4,2−オキサチアジン化合物およびそれらのオキサイドならびに組成物用の適当な担体を含有する組成物を提供する。 木材の保存方法がまた開示されており、この方法は殺カビまたは殺菌有効量の当該3−アリール−5,6−ジヒドロ−1,4,2−オキサチアジン化合物およびそれらのオキサイドを被処理木材物体に施用することからなる。
10 Substituted benzisoxazole and benzisothiazole herbicide JP4566296 1996-02-08 JPH08253476A 1996-10-01 PIITAA JIYON UEPURO
PROBLEM TO BE SOLVED: To obtain the subject compound for herbicide and useful for control of undesirable plant species after gemmating. SOLUTION: This substance is a compound of formula I [R is H, a halogen, an 1-4C alkyl, 1-4C haloalkyl or 1-4C haloalkoxy; R 1 is a halogen, X 1R 2 or R 2; X and X 1 are each O or S; R 2 is e.g. H or substituted alkyl; and Q is e.g. formula H (R 11 and R 12 are each e.g. H or an alkyl; and A and A 1 are each e.g. O or S)], e.g. 5-(1-cyclohexene-1,2-dicarboxyimide)-1,2-benzisothiazole-3-methyl acetate. A compound of formula I is obtained by make a conversion of an aminobenzisoxazole or aminobenzisothiazole of formula III into an isocyanate, treating it with an amino acid and furthermore treating it with an ethanolic hydrogen chloride or α-bromocarboxyamide. The herbicide is applied to undersirable foliage, seeds, soil and water in the ratio of 0.016 to 4 kg/ha. COPYRIGHT: (C)1996,JPO
11 BIOCOMPATIBLE FLUORESCENT IMAGING AGENTS PCT/US2006/034604 2006-09-01 WO2007028163A1 2007-03-08 RAJOPADHYE, Milind; GROVES, Kevin

This invention relates to new fluorescent chemical entities that are designed to attach to biocompatible molecules to form in vivo optical imaging agents.

12 TRICYCLIC QUINOXALINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS PCT/US1998/016232 1998-08-04 WO99007701A1 1999-02-18
The present invention relates to tricyclic quinoxaline compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein tyrosine kinases and therefore should be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.
13 METHOD OF TREATMENT EP01966474 2001-08-31 EP1320370A4 2008-10-22 TEW DAVID G; THOMPSON SCOTT K; VEBER DANIEL F
The present invention relates to methods of treating parasitic diseases which are mediated by cysteine proteases by administration of 4-amino-azepan-3-one protease inhibitors. In particular, the present invention relates to a method of treating malaria by inhibiting the cysteine protease falcipain.
14 BIOCOMPATIBLE N, N-DISUBSTITUTED SULFONAMIDE-CONTAINING FLUORESCENT DYE LABELS EP06802829.9 2006-09-01 EP1934211A1 2008-06-25 NARAYANAN, Narasimhachari; GROVES, Kevin; PETERSON, Jeffrey, D.; RAJOPADHYE, Milind
This invention relates to new fluorescent chemical entities, especially fluorescent molecules that comprise biocompatible N,N-disubstituted sulfonamide fluorochromes. This invention also relates to the corresponding reactive versions of such molecules. This invention also relates to the corresponding conjugates with moieties such as peptides, proteins, various biomolecules, carbocyclic and heterocyclic compounds, sugars, and their uses thereof.
15 6-AZAINDOLE COMPOUND EP05732504.5 2005-04-04 EP1732566A2 2006-12-20 HORIGUCHI, Yoshiaki; IMOTO, Hiroshi, Takeda Pharmaceutical Company Ltd.; WOLF, Mark, A.
A compound represented by the formula (I) wherein R1, R2, R3 and R6 are the same or different and each is a hydrogen atom or a substituent; one of R4 and R5 is a hydrogen atom and the other is a group represented by the formula: -C(=X)-R7 wherein X is N-O-R8 or N-NH-R9 wherein R8 and R9 are the same or different and each is a hydrogen atom or a group bonded via a carbon atom; and R7 is a hydrogen atom or a substituent, and the like and a salt thereof have a superior IκB kinase inhibitory activity, and useful as pharmaceutical agents such as agents for preventing or treating diabetes and the like.
16 PHOSPHATASE BINDING COMPOUNDS AND METHODS OF USING SAME EP20738072.6 2020-01-08 EP3908306A1 2021-11-17 CREWS, Craig; GERRITZ, Samuel W.; EASTMAN, Kyle J.; KAYSER-BRICKER, Katherine J.; CHEN, Jinshan M.; PULEO, David E.
The present invention provides bifunctional compounds that efficiently dephosphorylate certain phospho-activated target proteins. Such target proteins can be any protein involved in the pathway of a disease or disorder, such as but not limited to cancer, neurodegeneration, metabolic disease, diabetes, insulin resistance, and so forth.
17 BIOCOMPATIBLE FLUORESCENT IMAGING AGENTS EP06802988.3 2006-09-01 EP1937676B1 2016-11-30 RAJOPADHYE, Milind; GROVES, Kevin
18 METHOD OF TREATMENT EP01966474.7 2001-08-31 EP1320370A1 2003-06-25 TEW, David G.; THOMPSON, Scott, K.; VEBER, Daniel, F.
The present invention relates to methods of treating parasitic diseases which are mediated by cysteine proteases by administration of 4-amino-azepan-3-one protease inhibitors. In particular, the present invention relates to a method of treating malaria by inhibiting the cysteine protease falcipain.
19 Phosphatase Binding Compounds and Methods of Using Same PCT/US2020/012700 2020-01-08 WO2020146470A1 2020-07-16 CREWS, Craig; GERRITZ, Samuel W.; EASTMAN, Kyle J.; KAYSER-BRICKER, Katherine J.; CHEN, Jinshan M.; PULEO, David E.

The present invention provides bifunctional compounds that efficiently dephosphorylate certain phospho-activated target proteins. Such target proteins can be any protein involved in the pathway of a disease or disorder, such as but not limited to cancer, neurodegeneration, metabolic disease, diabetes, insulin resistance, and so forth.

20 HEPATITIS C VIRUS INHIBITORS PCT/US2010/056114 2010-11-10 WO2011060000A1 2011-05-19 LAVOIE, Rico; BENDER, John A.; ROMINE, Jeffrey Lee; RUEDIGER, Edward H.; BACHAND, Carol; LOPEZ, Omar D.; CHEN, Qi; BELEMA, Makonen; KADOW, John F.; HAMANN, Lawrence G.

This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.

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