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81. 发明申请

WO00078747A1 ACYLHYDRAZINE DERIVATIVES, PROCESS FOR PREPARING THE SAME AND USE THEREOF 审中-公开
标题翻译：乙酰衍生物衍生物，其制备方法和用途
公开(公告)号：WO00078747A1
公开(公告)日：2000-12-28
申请号：PCT/JP2000/004034
申请日：2000-06-21
IPC分类号： A61P9/10 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D495/04 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D207/273 , C07D241/08 , C07D405/12
CPC分类号： C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D495/04
摘要： Novel acylhydrazine derivatives exhibiting an inhibitory activity against activated blood coagulation factor X, which are compounds of general formula (I) or salts thereof, wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; R and R are each hydrogen or optionally substituted hydrocarbyl, or alternatively R and R or the substituent of X and R may be united to form an optionally substituted ring; X and X are each free valency, optionally substituted alkylene, or optionally substituted imino; D is oxygen or sulfur; A is -N(R )-Y- or -N=Y-; R is hydrogen, optionally substituted hydrocarbyl, or acyl; Y is an optionally substituted chain hydrocarbon group or an optionally substituted cyclic group; and Z is (1) optionally substituted amino, (2) optionally substituted imidoyl, or (3) an optionally substituted nitrogenous heterocycle group.
摘要翻译：对活性凝血因子X具有抑制活性的新型酰肼衍生物，其为通式（I）的化合物或其盐，其中R为任选取代的烃基或任选取代的杂环基; R 1和R 2各自为氢或任选取代的烃基，或者R 1和R 2或X 1和R 2的取代基可以一起形成任选取代的环 ; X 1和X 2各自为任意取代的亚烷基，或任意取代的亚氨基; D是氧或硫; A是-N（R 3）-Y-或-N = Y-; R 3是氢，任选取代的烃基或酰基; Y是任选取代的链烃基或任选取代的环基; 和Z是（1）任选取代的氨基，（2）任选取代的亚氨基，或（3）任选取代的含氮杂环基。

82. 发明申请

WO0008047A8 DEPSIPEPTIDE DERIVATIVES BEARING PIPERAZINONE RINGS 审中-公开
标题翻译：含哌嗪酮环的哌普生衍生物
公开(公告)号：WO0008047A8
公开(公告)日：2000-05-04
申请号：PCT/JP9904205
申请日：1999-08-04
申请人： NISSHIN FLOUR MILLING CO , YANAI MAKOTO , SUZUKI MASASHI , OSHIDA NORIO , KAWAMURA KOJI , HIRAMOTO SHIGERU , YASUDA ORIE , KINOSHITA NOBUHIRO , SHINGAI AKIKO , TAKASU MASAKO
发明人： YANAI MAKOTO , SUZUKI MASASHI , OSHIDA NORIO , KAWAMURA KOJI , HIRAMOTO SHIGERU , YASUDA ORIE , KINOSHITA NOBUHIRO , SHINGAI AKIKO , TAKASU MASAKO
IPC分类号： A61K38/00 , C07K5/02 , C07K5/078 , C07K5/062 , A61K31/50 , A61K38/06 , C07D241/08 , C07K5/072 , C07K5/083
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/0207
摘要： Novel depsipeptide derivatives bearing piperazinone rings in the molecule, represented by general formula (1) wherein X1 is N(R4)-CO, N(R5)-CH2, CH2-CO, CH2-CH2, CH=CH, CH2-CH(OH) or CH(OH)-CH(OH); R1 is C5-C20 alkyl or alkoxy(C5-C15)alkyl(C1-C4); R2 to R5 are each hydrogen or C1-C6 alkyl; and A is (2), (3) or (4): -X2-CH(R11)-X3-CH(R12)-NH-R13. These derivatives exhibit apolipoprotein E production accelerating activities, thus being useful as remedies for nerve injury, dementia and hyperlipidemia.
摘要翻译：由通式（1）表示的分子中带有哌嗪酮环的新型缩酚酸肽衍生物，其中X1是N（R4）-CO，N（R5）-CH2，CH2-CO，CH2-CH2，CH = CH，CH2- OH）或CH（OH）-CH（OH）; R1是C5-C20烷基或烷氧基（C5-C15）烷基（C1-C4）; R2至R5各自为氢或C1-C6烷基; （2），（3）或（4）：-X2-CH（R11）-X3-CH（R12）-NH-R13。这些衍生物表现出载脂蛋白E产生促进活性，因此可用作神经损伤，痴呆和高脂血症的治疗剂。

83. 发明申请

WO00008005A2 PIPERAZINONE DERIVATIVES 审中-公开
标题翻译：嗪酮
公开(公告)号：WO00008005A2
公开(公告)日：2000-02-17
申请号：PCT/EP1999/005070
申请日：1999-07-16
IPC分类号： C07D241/08 , C07D413/10 , C07D295/00
CPC分类号： C07D413/10 , C07D241/08
摘要： The present invention relates to new piperazinone derivatives of the formula (I), in which R , R , R , R , R , R , R , R , W and X are such as defined in claim 1, as well as to the salts and solvates thereof. These derivatives are inhibitors of the coagulation factor Xa and can be used for preventing and/or treating thromboembolic disorders.
摘要翻译：式（I）的新的哌嗪酮衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，W 和X具有权利要求（1）中给出的含义，并且它们的盐和溶剂化物是凝血因子Xa的抑制剂并且可以用于预防和/或治疗血栓栓塞性疾病。

84. 发明申请

WO00001678A1 PROCESS FOR THE SYNTHESIS OF SUBSTITUTED PIPERAZINONES VIA MITSUNOBU REACTION 审中-公开
标题翻译：通过MITSUNOBU反应合成替代哌嗪的方法
公开(公告)号：WO00001678A1
公开(公告)日：2000-01-13
申请号：PCT/US1999/014727
申请日：1999-06-29
IPC分类号： C07D241/08 , C07D403/06 , C07D401/04
CPC分类号： C07D403/06 , C07D241/08
摘要： The present invention is directed to a process for synthesizing substituted piperazinones, which are useful intermediates for making farnesyl-protein transferase inhibitors, using a Mitsunobu reaction.
摘要翻译：本发明涉及一种合成取代哌嗪酮的方法，其是使用Mitsunobu反应制备法呢基蛋白转移酶抑制剂的有用中间体。

85. 发明申请

WO00000477A1 NON-PEPTIDYL INHIBITORS OF VLA-4 DEPENDENT CELL BINDING USEFUL IN TREATING INFLAMMATORY, AUTOIMMUNE, AND RESPIRATORY DISEASES 审中-公开
标题翻译： VLA-4依赖性细胞结合的非磷酸抑制剂有助于治疗炎症，自发性和呼吸道疾病
公开(公告)号：WO00000477A1
公开(公告)日：2000-01-06
申请号：PCT/IB1999/000973
申请日：1999-05-31
IPC分类号： C07D277/20 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/443 , A61K31/4439 , A61K31/495 , A61K31/496 , A61P1/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D207/32 , C07D207/333 , C07D231/06 , C07D231/12 , C07D233/54 , C07D241/08 , C07D249/08 , C07D257/04 , C07D261/04 , C07D261/08 , C07D263/10 , C07D263/32 , C07D271/06 , C07D277/26 , C07D277/30 , C07D307/58 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/10 , C07D417/12
CPC分类号： C07D207/333 , C07D231/06 , C07D231/12 , C07D233/64 , C07D241/08 , C07D249/08 , C07D257/04 , C07D261/04 , C07D261/08 , C07D263/10 , C07D263/32 , C07D271/06 , C07D277/26 , C07D277/30 , C07D307/58 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/10 , C07D417/12
摘要： Compounds of Formula (1.0.0) are described, wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably -C(=O)-; B is independently selected from a group of moieties, the most preferred of which are those of partial Formulas (1.1.2) and (1.1.6), and E is a single bond; oxygen; 1,1-cyclopropyl; C(CH3)2; CF2; or a bridging moiety of partial Formula (1.9.0), where R a is hydrogen when R has the meaning of a mono-valent substituent; and R a is a single bond when R has the meaning of a di-valent substituent. Said compounds are useful in methods of treating or preventing an inflammatory, autoimmune or respiratory disease by inhibiting cell adhesion and consequent or associated pathogenic processes subsequently mediated by VLA-4.
摘要翻译：描述式（1.0.0）的化合物，其中A为例如芳基，杂芳基或杂环基，Y优选为-C（= O） - ; B独立地选自一组部分，其中最优选的是部分式（1.1.2）和（1.1.6）的那些，并且E是单键; 氧; 1,1-环丙基; C（CH 3）2; CF2; 或部分式（1.9.0）的桥连部分，其中当R 1具有1价取代基的含义时，R 1a是氢; 并且当R 1具有二价取代基的含义时，R 1a是单键。所述化合物可用于通过抑制随后由VLA-4介导的细胞粘附和随后或相关的致病过程来治疗或预防炎性，自身免疫性或呼吸系统疾病的方法。

86. 发明申请

WO99043662A1 SOLID SUPPORT SYNTHESIS OF 2-OXOPIPERAZINES 审中-公开
标题翻译： 2-OXOPIPERAZINES的固体支持合成
公开(公告)号：WO99043662A1
公开(公告)日：1999-09-02
申请号：PCT/US1999/002734
申请日：1999-02-08
IPC分类号： C07D241/08 , C07D243/08 , C07D245/02
CPC分类号： C07D243/08 , C07D241/08 , Y02P20/55
摘要： The subject invention involves processes for making 2-oxopiperazine and homologous compounds using a solid support resin by (a) removing the protecting group from an N-protected amino acid ester of the resin (if present), (b) reacting the resulting unprotected resin ester with a N-protected alpha -amino aldehyde, (c) optionally modifying the resulting intermediate by substituting a non-hydrogen moiety on the N from the amino acid, (d) removing the remaining N-protecting group from the N from the amino aldehyde, and (e) cleaving/cyclizing the product from the resin.
摘要翻译：本发明涉及使用固体支持树脂制备2-氧代哌嗪和同系化合物的方法，该方法是通过（a）从保护的树脂的N-保护的氨基酸酯（如果存在）中除去保护基团，（b）使得到的未保护的树脂酯与N-保护的α-氨基醛反应，（c）任选地通过从氨基酸取代N上的非氢部分来修饰所得中间体，（d）从氨基中除去剩余的N-保护基团，醛，和（e）从树脂中切割/环化产物。

87. 发明申请

WO99023062A1 IRON ALKALI SALT OF S,S-ETHYLENEDIAMINE-N,N'-DISUCCINIC ACID AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：硫辛酸盐，S-乙烯基胺-N，N'-错酸及其生产方法
公开(公告)号：WO99023062A1
公开(公告)日：1999-05-14
申请号：PCT/JP1998/004917
申请日：1998-10-30
IPC分类号： C07C227/18 , C07C227/40 , C07C229/24 , C07D241/06 , C07D241/08 , C07C229/16
CPC分类号： C07D241/06 , C07C227/18 , C07C227/40 , C07C229/24 , C07D241/08
摘要： An iron alkali salt of S,S-ethylenediamine-N,N'-disuccinic acid wherein the content of a lactam compound of general formula (1), wherein M represents an ammonium or alkali metal ion, and the content of an ethylenediaminemonosuccinic acid of general formula (2), wherein M represents an ammonium or alkali metal ion, are respectively 7 % by weight or less.
摘要翻译：一种S，S-乙二胺-N，N'-二琥珀酸的碱金属盐，其中通式（1）的内酰胺化合物的含量，其中M表示铵或碱金属离子，以及乙二胺一琥珀酸的含量其中M表示铵或碱金属离子的通式（2）分别为7重量％以下。

88. 发明申请

WO98035930A1 METHOD OF PREPARING AMINO CARBOXYLIC ACIDS 审中-公开
标题翻译：制备氨基羧酸的方法
公开(公告)号：WO98035930A1
公开(公告)日：1998-08-20
申请号：PCT/US1998/002882
申请日：1998-02-12
IPC分类号： B01J31/24 , B01J31/20 , C07B61/00 , C07C227/00 , C07C227/20 , C07C229/16 , C07C231/08 , C07C233/36 , C07C233/47 , C07C273/18 , C07C275/16 , C07D241/08 , C07D241/18 , C07D251/04 , C07D251/14 , C07F9/38 , C07F9/40 , C07F9/6509 , C07C62/00 , C07C61/09 , C07C61/10 , C07C61/24 , C07C233/00 , C07C235/00 , C07C237/00 , C07F9/22 , C07F9/28
CPC分类号： C07F9/3813 , C07C227/00 , C07C275/16 , C07D241/18 , C07D251/04 , C07D251/14
摘要： Process for the preparation of an N-acyl amino carboxylic acid by means of a carboxymethylation reaction. In this reaction, a reaction mixture is formed which contains a base pair, carbon monoxide, hydrogen and an aldehyde with the base pair conprising a carbamoyl compound and a carboxymethylation catalyst precursor. In a preferred embodiment, the carbamoyl compound and aldehyde are selected to yield an N-acyl amino carboxylic acid which is readily converted to N-(phosphonomethyl)glycine, or a salt or ester thereof.
摘要翻译：通过羧甲基化反应制备N-酰基氨基羧酸的方法。在该反应中，形成含有碱基对，一氧化碳，氢气和醛的反应混合物，碱基对具有氨基甲酰基化合物和羧甲基化催化剂前体。在优选的实施方案中，选择氨基甲酰基化合物和醛以产生N-酰基氨基羧酸，其易于转化为N-（膦酰基甲基）甘氨酸或其盐或酯。

89. 发明申请

WO1997048685A1 METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：金属蛋白酶抑制剂
公开(公告)号：WO1997048685A1
公开(公告)日：1997-12-24
申请号：PCT/GB1997001633
申请日：1997-06-17
申请人： GLAXO GROUP LIMITED
发明人： GLAXO GROUP LIMITED , CAMPBELL, David, Alan , LOOK, Gary, Charles , SZARDENINGS, Anna, Katrin , PATEL, Dinesh, Vinubhai
IPC分类号： C07D241/08
CPC分类号： C07D401/06 , C07D241/08 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/06 , C07D409/14 , C40B40/00
摘要： Novel inhibitors of metalloproteases are disclosed. Such compounds are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, such as rheumatoid arthritis.
摘要翻译：公开了新的金属蛋白酶抑制剂。这些化合物可用于治疗或控制涉及组织分解的疾病状态或病症的药物组合物和方法，例如类风湿性关节炎。

90. 发明申请

WO1997042177A1 PROCESS FOR THE PREPARATION OF UREIDE DERIVATIVES AND NEW INTERMEDIATES OF SYNTHESIS 审中-公开
标题翻译：制备尿苷衍生物的方法和新的合成中间体
公开(公告)号：WO1997042177A1
公开(公告)日：1997-11-13
申请号：PCT/EP1997002221
申请日：1997-04-30
申请人： ABRES ASSOCIATED BIOTECHNOLOGY RESEARCH S.R.L. , TASSONE, Giuseppe , RIZZA, Victor
发明人： ABRES ASSOCIATED BIOTECHNOLOGY RESEARCH S.R.L.
IPC分类号： C07D241/08
CPC分类号： C07D241/08 , C07D499/00 , C07D501/00
摘要： A new process is described for the synthesis of ureide derivatives having formula (I) where the P ring is a saturated or unsaturated nitrogen heterocycle with 5 or 6 members, possibly containing, in addition, one or more hetero-atoms chosen from N, O and S, and in which -L is the radical of a compound containing a primary amine group. The process according to the invention comprises the condensation of said PN-H nitrogen heterocycle and of said L-NH2 compound containing a primary amine group with chloro-carbonyl derivatives. In particular, said process enables the low environmental impact and economically advantageous synthesis of beta -lactam antibiotics, using new intermediates of synthesis.
摘要翻译：描述了用于合成具有式（I）的脲衍生物的新方法，其中P环是具有5或6个成员的饱和或不饱和的氮杂环，可能还含有一个或多个选自N，O的杂原子和S，其中-L是含有伯胺基的化合物的基团。根据本发明的方法包括所述PN-H氮杂环和所述含伯胺基的L-NH 2化合物与氯羰基衍生物的缩合。特别地，所述方法能够使用新的合成中间体来实现对β-内酰胺抗生素的低环境影响和经济上有利的合成。

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