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1. 发明申请

WO9820437A3 SYSTEM, METHOD AND COMPUTER PROGRAM PRODUCT FOR IDENTIFYING CHEMICAL COMPOUNDS HAVING DESIRED PROPERTIES 审中-公开
标题翻译：用于识别具有所需特性的化学化合物的系统，方法和计算机程序产品
公开(公告)号：WO9820437A3
公开(公告)日：1998-06-25
申请号：PCT/US9720918
申请日：1997-11-04
申请人： DIMENSIONAL PHARM INC
发明人： AGRAFIOTIS DIMITRIS K , BONE ROGER F , SALEMME FRANCIS R , SOLL RICHARD M
IPC分类号： G01N33/00 , B01J19/00 , C07B61/00 , G01N33/15 , G06F15/18 , G06F17/30 , G06F17/50 , G06F19/00 , G06F19/16 , G06F19/26 , G06N3/00 , G06T11/20 , G06T17/40
CPC分类号： G06T11/206 , B01J19/0046 , B01J2219/00689 , B01J2219/00691 , B01J2219/00695 , B01J2219/007 , B01J2219/00702 , C40B40/00 , G06F19/707 , G06F19/708 , G06K9/6251 , G06K9/6253
摘要： An automatic, partially automatic, and/or manual iterative system, method and/or computer program product for generating chemical entities having desired or specified physical, chemical, functional, and/or bioactive properties. The present invention identifies a set of compounds for analysis; collects, acquires or synthesizes the identified compounds; analyzes the compounds to determine one or more physical, chemical and/or bioactive properties (structure-property data); and uses the structure-property data to identify another set of compounds for analysis in the next iteration. An Experiment Planner generates Selection Criteria and/or one or more Objective Functions for use by a Selector. The Selector searches the Compound Library to identify a subset of compounds (a Directed Diversity Library) that maximizes or minimizes the Objective Functions. The compounds listed in the Directed Diversity Library are then collected, acquired or synthesized, and are analyzed to evaluate their properties of interest. In one embodiment, when a compound in a Directed Diversity Library is available in a Chemical Inventory, the compound is retrieved from the Chemical Inventory instead of re-synthesizing the compound.

2. 发明申请

WO0206248A2 CYCLIC OXYGUANIDINE PYRAZINONES AS PROTEASE INHIBITORS 审中-公开
标题翻译：作为蛋白酶抑制剂的环状氧杂胍吡唑啉酮
公开(公告)号：WO0206248A2
公开(公告)日：2002-01-24
申请号：PCT/US0122302
申请日：2001-07-17
申请人： DIMENSIONAL PHARM INC
发明人： WANG AIHUA , TOMCZUK BRUCE E , LU TIANBAO , SOLL RICHARD M , SPURLINO JOHN C , BONE ROGER FRANCIS
IPC分类号： A61K31/5355 , A61K31/5395 , A61K51/00 , A61L33/00 , A61P7/02 , A61P43/00 , C07D413/12 , C07D413/14 , C07D241/00
CPC分类号： C07D413/12 , C07D413/14
摘要： Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula (I): wherein R , R , R , W, and A are as set forth in the specidification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of protease, especially trypsin-like serine proteases, such as chymotripsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of trombin. Compositions for inhibiting loss of blood platelas, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed labeled and employed fot in vivo imaging of thrombi.
摘要翻译：描述了环状氧胍吡嗪酮化合物，包括式（I）的化合物：其中R 3，R 4，R 5，W和A如分类中所述，以及水合物，溶剂合物或其药学上可接受的盐。本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。某些化合物通过直接选择性抑制凝血酶而表现出抗血栓形成活性。描述了用于抑制血小板丧失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制栓塞形成的组合物。本发明化合物的其它用途是作为抗凝血剂嵌入或物理连接到用于血液采集，血液循环和血液储存的装置的制造中的材料，例如导管，血液透析机，血液采集注射器和管，血线和支架。另外，化合物可以被可检测地标记并且被用于标记并且用于血栓的体内成像。

3. 发明申请

WO9823565A3 Aminoguandines and alkoxyguandines as protease inhibitors 审中-公开
标题翻译：氨基嘌呤和烷氧基胍作为蛋白酶抑制剂
公开(公告)号：WO9823565A3
公开(公告)日：1998-07-30
申请号：PCT/US9721649
申请日：1997-11-26
申请人： DIMENSIONAL PHARM INC
发明人： TOMCZUK BRUCE E , SOLL RICHARD M , LU TIANBAO , FEDDE CYNTHIA L , ILLIG CARL R , MARKOTAN THOMAS P , STAGNARO THOMAS P
IPC分类号： C07D295/22 , A01N1/02 , A61K20060101 , A61K31/155 , A61K31/165 , A61K31/18 , A61K31/225 , A61K31/255 , A61K31/305 , A61K31/335 , A61K31/341 , A61K31/36 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/535 , A61K33/42 , A61L33/00 , A61P7/00 , A61P7/02 , A61P9/10 , A61P29/00 , C07C20060101 , C07C69/76 , C07C279/00 , C07C279/10 , C07C281/16 , C07C291/04 , C07C303/30 , C07C303/40 , C07C305/00 , C07C309/00 , C07C309/63 , C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/08 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C317/26 , C07C323/17 , C07D20060101 , C07D207/14 , C07D207/16 , C07D207/48 , C07D209/04 , C07D211/22 , C07D211/58 , C07D211/64 , C07D211/96 , C07D213/24 , C07D213/42 , C07D213/74 , C07D215/12 , C07D215/36 , C07D217/12 , C07D217/22 , C07D229/00 , C07D231/04 , C07D237/02 , C07D239/42 , C07D239/72 , C07D243/04 , C07D245/02 , C07D261/02 , C07D263/54 , C07D265/02 , C07D267/04 , C07D269/00 , C07D285/14 , C07D295/12 , C07D307/02 , C07D307/52 , C07D307/66 , C07D311/66 , C07D311/74 , C07D317/08 , C07D317/14 , C07D317/34 , C07D317/40 , C07D317/64 , C07D333/06 , C07D333/34 , C07D333/54 , C07D333/62 , C07D403/04 , C07D413/04 , C07F9/22
CPC分类号： C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C323/66 , C07C2601/02 , C07C2601/14 , C07D211/96 , C07D213/42 , C07D213/74 , C07D215/36 , C07D217/02 , C07D217/22 , C07D239/42 , C07D295/13 , C07D295/26 , C07D307/66
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of formula (I) wherein X is O or NR?9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc¿, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula (I). The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.

4. 发明申请

WO0125241A3 FUSED 1-(2,6-DICHLORO-4-TRIFLUOROMETHYLPHENYL)-PYRAZOLES, THE SYNTHESIS THEREOF AND THE USE THEREOF AS PESTICIDES 审中-公开
标题翻译：熔融的1-（2,6-二氯-4-三氟甲基苯基） - 吡唑，其合成及其作为农药的用途
公开(公告)号：WO0125241A3
公开(公告)日：2001-12-13
申请号：PCT/US0027588
申请日：2000-10-06
申请人： DIMENSIONAL PHARM INC , HESKA CORP , DHANOA DALJIT S , MEEGALLA SANATH , SOLL RICHARD M , DOLLER DARIO , SHA DEYOU , LIU RUIPING , SILVER GARY
发明人： DHANOA DALJIT S , MEEGALLA SANATH , SOLL RICHARD M , DOLLER DARIO , SHA DEYOU , LIU RUIPING , SILVER GARY
IPC分类号： A01N43/56 , A01N43/90 , C07D231/54 , C07D231/56 , C07D491/04 , C07D491/10 , C07D495/04 , C07D495/10 , C07D513/04
CPC分类号： C07D495/10 , A01N43/56 , A01N43/90 , C07D231/54 , C07D231/56 , C07D491/04 , C07D491/10 , C07D495/04 , C07D513/04
摘要： The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula (I) or a salt thereof, where R is amino, hydrogen, alkyl, hydroxy, halo, alkoxy, alkylamino, dialkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, trifluoroalkylsulfinyl, trifluoroalkylsulfonyl, hydroxy, amino, trifluoromethyl, acetylamino, -OSO2R , -OS(O)R , -OC(O)R , -OC(O)NHR , or -NHC(O)NHR where R is C1-4 alkyl or optionally substituted aryl; X, Y and Z are each independently (CH)n, (CR R )n,S, S(O), or SO2, wherein n is 1-2, R and R are defined herein; Q is N or C-R , wherein R is fluoro, chloro, bromo, or iodo; R is halo, C1-C6alkyl, C1-C4alkenyl, C1-C4alkoxy, C1-C4alkylamino, C1-C4dialkylamino, C1-C4alkylthio, C1-C4alkylsulfinyl, C1-C4alkylsulfonyl, C1-C4trifluoroalkylsufinyl, C1-C4trifluoroalkylsulfonyl, hydroxy, amino, or trifluoromethyl; and with the proviso that only one of X, Y and Z can be S, S(O) or SO2.
摘要翻译：本发明涉及新颖的吡唑衍生物及其作为杀虫剂的用途。吡唑衍生物具有式（I）或其盐，其中R 1是氨基，氢，烷基，羟基，卤素，烷氧基，烷基氨基，二烷基氨基，烷硫基，烷基亚磺酰基，烷基磺酰基，三氟烷基亚磺酰基，三氟烷基磺酰基，羟基，，乙酰氨基，-OSO 2 R 2，-OS（O）R 2，-OC（O）R 2，-OC（O）NHR 2或-NHC（O）NHR 2 R 2是C 1-4烷基或任选取代的芳基; X，Y和Z各自独立为（CH）n，（CR 3 R 4）n，S，S（O）或SO 2，其中n为1-2，R 3和R 4 >在本文中定义; Q是N或C-R 6，其中R 6是氟，氯，溴或碘; R 5是卤素，C 1 -C 6烷基，C 1 -C 4烯基，C 1 -C 4烷氧基，C 1 -C 4烷基氨基，C 1 -C 4二烷基氨基，C 1 -C 4烷硫基，C 1 -C 4烷基亚磺酰基，C 1 -C 4烷基磺酰基，C 1 -C 4三氟烷基亚磺酰基，C 1 -C 4三氟烷基磺酰基，，或三氟甲基; 并且条件是X，Y和Z中只有一个可以是S，S（O）或SO 2。

5. 发明公开

EP0831800A4 ARYLSULFONYLAMINOBENZENE DERIVATIVES AND THE USE THEREOF AS FACTOR Xa INHIBITORS 失效
标题翻译：芳族聚酰胺苯并恶唑衍生物（DYEN VERWENDUNG ALS FAKTOR XA INHIBITOREN
公开(公告)号：EP0831800A4
公开(公告)日：1999-03-10
申请号：EP96921529
申请日：1996-06-07
申请人： DIMENSIONAL PHARM INC
发明人： ILLIG CARL R , SOLL RICHARD M , SALVINO JOSEPH M , TOMCZUK BRUCE E , LU TIANBAO , SUBASINGHE NALIN L
IPC分类号： A61K31/18 , A61K31/195 , A61K31/245 , A61K31/27 , A61K31/435 , A61K31/44 , A61P25/00 , A61P29/00 , A61P35/00 , C07C311/21 , C07C311/44 , C07D213/40 , C07D453/02 , A61K31/165 , A61K31/24 , C07C229/00 , C07C307/02 , C07C317/14 , C07C381/04 , C07D211/82
CPC分类号： C07D213/40 , C07C311/21 , C07C311/44 , C07D453/02

7. 发明公开

EP0781436A4 SYSTEM AND METHOD OF AUTOMATICALLY GENERATING CHEMICAL COMPOUNDS WITH DESIRED PROPERTIES 失效
标题翻译：系统和方法自动生成的化合物具有所需性能
公开(公告)号：EP0781436A4
公开(公告)日：1999-08-25
申请号：EP95933748
申请日：1995-09-11
申请人： DIMENSIONAL PHARM INC
发明人： AGRAFIOTIS DIMITRIS K , BONE ROGER F , SALEMME FRANCIS R , SOLL RICHARD M
IPC分类号： A61K38/55 , A61P7/02 , B01J19/00 , C07B61/00 , C07K1/04 , C40B30/02 , C40B40/10 , C40B50/02 , C40B50/08 , G06F17/50 , G06F19/00
CPC分类号： C40B30/02 , B01J19/0046 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/00599 , B01J2219/00689 , B01J2219/00691 , B01J2219/00695 , B01J2219/00698 , B01J2219/007 , B01J2219/0072 , B01J2219/00725 , C07K1/047 , C40B40/10 , C40B50/02 , C40B50/08 , G06F19/702 , G06F19/704 , G06F19/707 , Y10T436/11
摘要： A computer-based, iterative process for generating chemical entities with defined physical, chemical and/or bioactive properties. During each iteration of the process, a directed diversity chemical library (208) is robotically generated in accordance with robotic synthesis instructions (204); the compounds in the directed diversity chemical library (208) are analyzed to identify compounds with the desired properties; structure-property data (210) are used to select compounds to be synthesized in the next iteration; and new robotic synthesis instructions are automatically generated to control the synthesis of the directed diversity chemical library (208) for the next iteration.

8. 发明公开

EP0883405A4 AMIDINO PROTEASE INHIBITORS 失效
标题翻译： AMIDINO PROTEASEINHIBITOREN
公开(公告)号：EP0883405A4
公开(公告)日：1999-04-28
申请号：EP96944847
申请日：1996-12-20
申请人： DIMENSIONAL PHARM INC
发明人： LU TIANBAO , TOMCZUK BRUCE E , ILLIG CARL , SOLL RICHARD M
IPC分类号： C07D295/14 , A61K31/00 , A61K31/18 , A61K31/24 , A61K31/445 , A61K31/495 , A61P1/00 , A61P1/18 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P29/00 , A61P43/00 , C07C309/73 , C07C311/21 , C07D211/22 , C07D211/26 , C07D211/28 , C07D295/195 , A61K38/05
CPC分类号： C07D295/195 , C07C309/73 , C07C311/21 , C07D211/22 , C07D211/26

9. 发明公开

EP0841918A4 THROMBIN INHIBITORS 失效
标题翻译：脑啡肽抑制剂
公开(公告)号：EP0841918A4
公开(公告)日：1998-10-21
申请号：EP96918410
申请日：1996-06-07
申请人： DIMENSIONAL PHARM INC
发明人： BONE ROGER F , SOLL RICHARD M , ILLIG CARL R , LU TIANBAO , SUBASINGHE NALIN L
IPC分类号： A61K38/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P29/00 , C07D207/16 , C07K5/065 , A61K31/40 , C07D207/08
CPC分类号： C07D207/16

10. 发明公开

EP1073449A4 AMINO ACID AMIDINOHYDRAZONES, ALKOXYGUANIDINES AND AMINOGUANIDINES AS PROTEASE INHIBITORS 审中-公开
标题翻译：氨基酸脒基，alkoxyguanidines氨基胍作为蛋白酶抑制剂
公开(公告)号：EP1073449A4
公开(公告)日：2003-01-02
申请号：EP99921434
申请日：1999-04-22
申请人： DIMENSIONAL PHARM INC
发明人： LU TIANBAO , TOMCZUK BRUCE , MARKOTAN THOMAS P , SOLL RICHARD M
IPC分类号： C07D223/16 , A61K31/40 , A61K38/00 , A61K51/00 , A61L33/00 , A61P7/02 , C07C279/24 , C07D207/16 , C07K5/02 , C07K5/06 , C07K5/065 , C07F9/06
CPC分类号： C07K5/06078 , A61K38/00 , C07D207/16 , C07K5/0222

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