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1. 发明申请

WO1998007742A1 SULFONAMIDES 审中-公开
标题翻译：磺胺类药物
公开(公告)号：WO1998007742A1
公开(公告)日：1998-02-26
申请号：PCT/GB1997002222
申请日：1997-08-19
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , BARLAAM, Bernard, Christophe
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07K05/06
CPC分类号： C07D213/70 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07D209/34 , C07D215/36 , C07D217/02 , C07D233/84 , C07D239/88 , C07D261/10 , C07D271/12 , C07D277/54 , C07D333/34 , C07D409/04
摘要： Compounds of formula (I) wherein R is aryl, heterocyclyl or heteroaryl; R is hydrogen, C1-8alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, heteroaryl, heterocyclyl, arylC1-6alkyl, heteroarylC1-6alkyl, heterocyclylC1-6alkyl or C3-8cycloalkylC1-6alkyl; R is C1-6alkyl, C2-6alkenyl, aryl, C1-6alkyl, heteroarylC1-6alkyl or the side-chain of a naturally occurring amino acid; R is hydrogen, C1-6alkyl, C3-8cycloalkyl, C4-8cycloalkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or heterocyclylC1-6alkyl; R is hydrogen or C1-6alkyl; or R and R together with the nitrogen atom to which they are joined form a heterocyclic ring; wherein any group or ring, in R -R , is optionally substituted; or pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, are described as inhibitors of the production of Tumor Necrosis Factor and/or one or more matrix metalloproteinase enzymes. Compositions containing them and their preparation are also described.
摘要翻译：式（I）的化合物，其中R 1是芳基，杂环基或杂芳基; R 2是氢，C 1-8烷基，C 2-6烯基，C 2-6炔基，C 3-8环烷基，杂芳基，杂环基，芳基C 1-6烷基，杂芳基C 1-6烷基，杂环基C 1-6烷基或C 3-8环烷基C 1-6烷基; R 3是C 1-6烷基，C 2-6烯基，芳基，C 1-6烷基，杂芳基C 1-6烷基或天然存在的氨基酸的侧链; R 4是氢，C 1-6烷基，C 3-8环烷基，C 4-8环烯基，芳基C 1-6烷基，杂芳基C 1-6烷基或杂环基C 1-6烷基; R 5是氢或C 1-6烷基; 或R 4和R 5与它们所连接的氮原子一起形成杂环; 其中R 1 -R 5中的任何基团或环任选被取代; 或其药学上可接受的盐或体内可水解的酯被描述为产生肿瘤坏死因子和/或一种或多种基质金属蛋白酶的抑制剂。还描述了含有它们的组合物及其制备方法。

2. 发明申请

WO1997046577A1 NEW AMINO ACID DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS 审中-公开
标题翻译：新型氨基酸衍生物及其作为抑制剂的使用
公开(公告)号：WO1997046577A1
公开(公告)日：1997-12-11
申请号：PCT/SE1997000989
申请日：1997-06-05
申请人： ASTRA AKTIEBOLAG , GUSTAFSSON, David , NYSTRÖM, Jan-Erik
发明人： ASTRA AKTIEBOLAG
IPC分类号： C07K05/06
CPC分类号： C07D401/12 , C07D205/04 , C07D207/16
摘要： There is provided compounds of formula (I), wherein R , R , R , R , Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
摘要翻译：提供式（I）化合物，其中R 1，R 2，R 3，R x，Y，n和B具有在描述中给出的含义，其可用作胰蛋白酶的竞争性抑制剂特别是在需要凝血酶抑制（例如血栓形成）或作为抗凝剂的条件下进行治疗。

3. 发明申请

WO1997043305A1 INHIBITORS OF PICORNAVIRUS 3C PROTEASES AND METHODS FOR THEIR USE AND PREPARATION 审中-公开
标题翻译： PICORNAVIRUS 3C蛋白质的抑制剂及其使用和制备方法
公开(公告)号：WO1997043305A1
公开(公告)日：1997-11-20
申请号：PCT/US1997008112
申请日：1997-05-13
申请人： AGOURON PHARMACEUTICALS, INC.
发明人： AGOURON PHARMACEUTICALS, INC. , WEBBER, Stephen, E. , DRAGOVICH, Peter, S. , PRINS, Thomas, J. , REICH, Siegfried, H. , LITTLE, Thomas, L., Jr. , LITTLEFIELD, Ethel, S. , MARAKOVITS, Joseph, T. , BABINE, Robert, E. , BLECKMAN, Ted, M.
IPC分类号： C07K05/06
CPC分类号： C07K5/06139 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06052
摘要： Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.
摘要翻译：通过化学合成获得的微小RNA病毒3C蛋白酶抑制剂抑制或阻断小核糖核酸病毒3C蛋白酶的生物学活性。这些化合物以及含有这些化合物的药物组合物适用于治疗感染了一种或多种微小核糖核酸病毒的患者或宿主。可以使用几种新的方法和中间体来制备本发明的新型微核糖核酸病毒3C蛋白酶抑制剂。

4. 发明申请

WO1997040066A1 SUPPRESSION OF IMMUNE RESPONSE VIA INHIBITION OF CATHEPSIN S 审中-公开
标题翻译：通过抑制CATHEPSIN S抑制免疫反应
公开(公告)号：WO1997040066A1
公开(公告)日：1997-10-30
申请号：PCT/US1997006865
申请日：1997-04-22
申请人： MASSACHUSETTS INSTITUTE OF TECHNOLOGY , BRIGHAM & WOMEN'S HOSPITAL, INC. , PLOEGH, Hidde, L. , CHAPMAN, Harold, A. , RIESE, Richard, J. , WOLF, Paula, R. , BOGYO, Matthew, S.
发明人： MASSACHUSETTS INSTITUTE OF TECHNOLOGY , BRIGHAM & WOMEN'S HOSPITAL, INC.
IPC分类号： C07K05/06
CPC分类号： C07K5/06113 , A61K38/55 , C07K5/06043 , C07K5/06095 , C07K5/0819 , Y10S424/81 , Y10S514/885
摘要： Methods and products for suppressing a class II MHC-restricted immune response in a mammal, or in mammalian cells, are described. The methods depend upon inhibiting invariant chain proteolysis by cathepsin S from class II MHC/invariant chain complexes, thereby reducing the competency of class II MHC molecules for binding antigenic peptides, reducing presentation of antigenic peptides by class II MHC molecules, and suppressing immune responses. The methods may be employed in the treatment of autoimmune diseases, allergic responses, and organ or tissue graft rejection. New pharmaceutical and therapeutic compositions which are peptide-based inhibitors of cathepsin S are also described.
摘要翻译：描述了用于抑制哺乳动物或哺乳动物细胞中II类MHC限制性免疫应答的方法和产品。该方法取决于来自II类MHC /不变链复合物的组织蛋白酶S的不变链蛋白酶解，从而降低II类MHC分子与抗原肽结合的能力，减少II类MHC分子呈递抗原肽，并抑制免疫应答。该方法可用于治疗自身免疫疾病，过敏反应和器官或组织移植物排斥。还描述了组合蛋白酶S的基于肽的抑制剂的新的药物和治疗组合物。

5. 发明申请

WO1997029122A1 (N)-(S)-1-PHENYL-1-ALKANAMIDE (N)-(3,3-DIMETHYLBUTYL)-L-ASPARTYL-D-'alpha' AMINOALKANOIC ACID FOR USE AS A SWEETENER 审中-公开
标题翻译：（N） - （S）-1-苯基-1-烷酰胺（N） - （3,3-二甲基丁基）-L-谷氨酰-D-氨基亚氨基酸用作SWERTENER
公开(公告)号：WO1997029122A1
公开(公告)日：1997-08-14
申请号：PCT/FR1997000245
申请日：1997-02-07
申请人： NOFRE, Claude , TINTI, Jean-Marie
IPC分类号： C07K05/06
CPC分类号： C07K5/06113 , A23L27/30
摘要： Compounds of formula (I), wherein Y is C2H5, CH(CH3)2 or (R) CH(OH)CH3, and R" is (S) CH(C2H5)C6H5, (S) CH(CH3)C6H5, or (R) CH(CH2OCH3)C6H5, are disclosed. The compounds are useful as sweeteners.
摘要翻译：式（I）化合物，其中Y为C 2 H 5，CH（CH 3）2或（R）CH（OH）CH 3，R“为（S）CH（C 2 H 5）C 6 H 5，（S）CH（CH 3）（CH 2 CH 2 OCH 3）C 6 H 5，这些化合物可用作甜味剂。

6. 发明申请

WO1996040742A1 PEPTIDYL HETEROCYCLES USEFUL IN THE TREATMENT OF THROMBIN RELATEDDISORDERS 审中-公开
标题翻译：用于治疗相关幽门螺杆菌的肽类异构体
公开(公告)号：WO1996040742A1
公开(公告)日：1996-12-19
申请号：PCT/US1996008430
申请日：1996-06-03
申请人： ORTHO PHARMACEUTICAL CORPORATION
发明人： ORTHO PHARMACEUTICAL CORPORATION , COSTANZO, Michael, J. , MARYANOFF, Bruce, E.
IPC分类号： C07K05/06
CPC分类号： C07D277/68 , A61K38/00 , C07D263/22 , C07D277/56 , C07D417/06 , C07K5/06078 , C07K5/06191
摘要： Compounds of Formula (I) useful in the treatment of thrombin and trypsin related disorders.
摘要翻译：用于治疗凝血酶和胰蛋白酶相关疾病的式（I）化合物。

7. 发明申请

WO1996031527A1 PROTEASE INHIBITING SUCCINIC ACID DERIVATIVES 审中-公开
标题翻译： PROTEASE INHIBIATION SUCCINIC ACID DERIVATIVES
公开(公告)号：WO1996031527A1
公开(公告)日：1996-10-10
申请号：PCT/CA1996000181
申请日：1996-03-27
申请人： BIO-MEGA/BOEHRINGER INGELHEIM RECHERCHE INC.
发明人： BIO-MEGA/BOEHRINGER INGELHEIM RECHERCHE INC. , BEAULIEU, Pierre, Louis , GUSE, Ingrid
IPC分类号： C07K05/06
CPC分类号： C07K5/06139 , C07C233/36 , C07C233/78 , C07C235/20 , C07C237/22 , C07C237/34 , C07C271/22
摘要： Disclosed herein are compounds which inhibit human immunodeficiency virus (HIV) protease activity and inhibit HIV replication in human cells. Thus, the compounds are indicated for the treatment of HIV infections. The compounds can be represented by formula (I), wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an arylalkyl carbamoyl; A is absent or an amino acid or a derived amino acid; either R or R is hydrogen while the other is alkyl or R and R are joined to form a cyclohexane; Q is hydrogen, hydroxy, halo or lower alkoxy; and Y is a terminal group, for example, an alkylamino, alkoxy or an optionally substituted anilino.
摘要翻译：本文公开了抑制人免疫缺陷病毒（HIV）蛋白酶活性并抑制人类细胞中的HIV复制的化合物。因此，这些化合物被指示用于治疗HIV感染。化合物可由式（I）表示，其中X为末端基，例如芳氧基羰基，烷酰基或芳基烷基氨基甲酰基; A不存在或氨基酸或衍生的氨基酸; R 1或R 2是氢，而另一个是烷基或R 1和R 2连接形成环己烷; Q是氢，羟基，卤代或低级烷氧基; 并且Y是末端基团，例如烷基氨基，烷氧基或任选取代的苯胺基。

8. 发明申请

WO1996017860A1 NEW DIPEPTIDE P-AMIDINOBENZYLAMIDES WITH N-TERMINAL SULFONYL OR AMINOSULFONYL RADICALS 审中-公开
标题翻译：具有N-末端磺酰OR NEW二肽P AMIDINOBENZYLAMIDE AMINOSULFONYLRESTEN
公开(公告)号：WO1996017860A1
公开(公告)日：1996-06-13
申请号：PCT/EP1995004646
申请日：1995-11-25
申请人： BASF AKTIENGESELLSCHAFT , BÖHM, Hans, Joachim , KOSER, Stefan , MACK, Helmut , PFEIFFER, Thomas , SEITZ, Werner , HÖFFKEN, Hans, Wolfgang , HORNBERGER, Wilfried , ZIERKE, Thomas
发明人： BASF AKTIENGESELLSCHAFT
IPC分类号： C07K05/06
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/06026 , C07K5/06043 , C07K5/06078 , C07K5/06113
摘要： The invention pertains to compounds of formula (I), wherein R , A and B are as indicated in the description, and to their preparation. The new compounds can be used for combatting diseases.
摘要翻译：是式（I）化合物，其中R <1>，A和B具有在说明书中给出的含义，并且它们的生产。的新的化合物适于防治疾病。

9. 发明申请

WO1995035309A1 NEW THROMBIN INHIBITORS, THEIR PREPARATION AND USE 审中-公开
标题翻译：新凝血酶抑制剂，生产和使用
公开(公告)号：WO1995035309A1
公开(公告)日：1995-12-28
申请号：PCT/EP1995002135
申请日：1995-06-06
申请人： BASF AKTIENGESELLSCHAFT , BÖHM, Hans-Joachim , KOSER, Stefan , MACK, Helmut , PFEIFFER, Thomas , SEITZ, Werner , HÖFFKEN, Hans, Wolfgang , HORNBERGER, Wilfried
发明人： BASF AKTIENGESELLSCHAFT
IPC分类号： C07K05/06
CPC分类号： C07K5/0812 , A61K38/00 , A61K47/64 , C07D205/04 , C07D207/16 , C07D207/48 , C07D211/60 , C07K5/06026 , C07K5/0606 , C07K5/06078 , C07K5/06104 , C07K5/06113
摘要： Compounds having the formula (I) are disclosed, in which the substituents have the meanings given in the description, as well as their salts with physiologically acceptable acids and their stereoisomers, and intermediate products for producing the same. These compounds are useful for treating diseases.
摘要翻译：它将与生理上相容的酸和它们的式（I）和它们的盐的化合物，其中取代基具有本说明书中给出的含义的立体异构体进行说明。接着中间体公开了用于它们的制备。所述化合物适于防治疾病。

10. 发明申请

WO1995017418A2 NOVEL INTERMEDIATES FOR THE SYNTHESIS OF L-ASPARTYL-D-'alpha'-AMINOALKANOYL-(S)-N-'alpha'-ALKYLBENZYL AMIDES USEFUL AS ARTIFICIAL SWEETENERS 审中-公开
标题翻译：用于合成作为人工维生素的L-阿糖基-D-α-氨基戊酰-L-（S）-N-甲基苄基苯胺的新型中间体
公开(公告)号：WO1995017418A2
公开(公告)日：1995-06-29
申请号：PCT/US1994014770
申请日：1994-12-22
申请人： THE COCA-COLA COMPANY
发明人： THE COCA-COLA COMPANY , D'ANGELO, Lihong , SWEENY, James, G. , KING, George, A., III
IPC分类号： C07K05/06
CPC分类号： C07D263/18 , C07C237/06 , C07C271/22 , C07K5/06113
摘要： The present invention relates to chemical compounds that are useful for the preparation of artificial sweetener compounds, in particular, chemical intermediates that are useful for the preparation of L-aspartyl-D- alpha -aminoalkanoyl-(S)-N- alpha -alkylbenzyl amides.
摘要翻译：本发明涉及可用于制备人造甜味剂化合物的化合物，特别是可用于制备L-天冬氨酰-D-α-氨基烷酰基 - （S）-N-α-烷基苄基酰胺的化学中间体。

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