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41. 发明申请

WO1997002289A1 PEPTIDE INHIBITORS OF FIBRONECTINE 审中-公开
标题翻译：纤维蛋白抑肽酶
公开(公告)号：WO1997002289A1
公开(公告)日：1997-01-23
申请号：PCT/GB1996001580
申请日：1996-07-02
申请人： ZENECA LIMITED , DUTTA, Anand, Swaroop
发明人： ZENECA LIMITED
IPC分类号： C07K14/78
CPC分类号： C07K7/56 , A61K38/00
摘要： Cyclic dimeric peptides of formula (1) wherein: peptide 1 and peptide 2 independently represent a tetrapeptide of formula -AA1-AA2-AA3-AA4- juxtaposed in parallel or antiparallel orientation; AA1 is an L or D amino acid selected from Ile, Leu and amino analogues thereof selected from Pro, Gly, Tic and Phe; AA2 is an L amino acid selected from Leu and amino acid analogues thereof selected from Ile, Phe and Val; AA3 is an L amino acid selected from Asp, Glu and amino acid analogues thereof; AA4 is an L amino acid selected from Val and amino acid analogues thereof selected from Leu, Ile, Phe and Cha (cyclohexylalanine); L1 and L2 independently represent linking moieties for linking peptides 1 and 2 to form a cyclic dipeptide; or salts thereof. The cyclic dipeptides inhibit the interaction of vascular cell adhesion molecule-1 and fibronectin with integrin very late antigen 4 and have therapeutic applications such as in rheumatoid arthritis, asthma or multiple sclerosis.
摘要翻译：式（1）的环状二聚肽其中：肽1和肽2独立地表示并列或反平行取向并入的式-AA1-AA2-AA3-AA4的四肽; AA1是选自Ile，Leu及其选自Pro，Gly，Tic和Phe的氨基类似物的L或D或D 氨基酸; AA2是选自Leu和其选自Ile，Phe和Val的氨基酸类似物的L9氨基酸; AA3是选自Asp，Glu及其氨基酸类似物的一种氨基酸; AA4是选自Val和其氨基酸类似物的选自Leu，Ile，Phe和Cha（环己基丙氨酸）的L9A氨基酸; L1和L2独立地表示用于连接肽1和2的连接部分以形成环状二肽; 或其盐。环状二肽抑制血管细胞粘附分子-1和纤连蛋白与整联蛋白非常晚的抗原4的相互作用，并具有治疗应用，例如类风湿性关节炎，哮喘或多发性硬化。

42. 发明申请

WO1997000864A1 AROMATIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：芳香化合物和含有它们的药物组合物
公开(公告)号：WO1997000864A1
公开(公告)日：1997-01-09
申请号：PCT/GB1996001443
申请日：1996-06-17
申请人： ZENECA LIMITED , BREAULT, Gloria, Anne
发明人： ZENECA LIMITED
IPC分类号： C07D237/24
CPC分类号： C07D213/80 , C07D213/82 , C07D237/18 , C07D237/24 , C07D401/04 , C07D403/04 , C07D413/04 , C07D413/12 , C07D417/12
摘要： The invention relates to compounds of formula (I), wherein A is an optionally substituted, ring system provided that the -CH(R )N(R )B-R and -OD groups are positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the -OD linking group (and therefore in the 3-position relative to the -CHR NR linking group) is not substituted; B is an optionally substituted ring system; R is positioned on ring B in a 1,3 or 1,4 relationship with the -CH(R )N(R )- linking group and is as defined in the description; R is hydrogen, C1-6alkyl, optionally substituted by hydroxy, cyano or trifluoromethyl, C2-6alkenyl (provided the double bond is not in the 1-position), (C2-6alkynyl (provided the triple bond is not in the 1-position), phenylC1-3alkyl or pyridylC1-3alkyl; R is hydrogen, methyl or ethyl; D is hydrogen, an optionally substituted 5-7 membered carbocyclic ring containing one double bond, C1-3alkyl substituted by an optionally substituted 5-7 membered carbocyclic ring containing one double bond or D is of the formula -(CH2)nCH(R )C(R )=C(R )R and N-oxides of -NR where chemically possible; and S-oxides of sulphur containing rings where chemically possible; and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof; excluding 4-[5-carboxy-2-hydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]benzoic acid, 5-[2-hydroxybenzylamino]-2-hydroxybenzoic acid, 3-[2,5-dihydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]benzenecarboxamide, 3-[2-hydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]-2-hydroxybenzoic acid, 4-[hydroxybenzylamino]-2-hydroxybenzoic acid and 4[2-hydroxybenzylamino]benzoic acid. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）化合物，其中A是任选取代的环系，条件是-CH（R 3）N（R 2）BR 1和-OD基团位于在环碳原子上彼此相关，并且位于-OD连接基团（因此相对于-CHR 3 NR 2连接基团的3位）的环原子未被取代 ; B是任选取代的环系; R 1与-CH（R 3）N（R 2） - 连接基以1,3或1,4个关系位于环B上，并且如说明书中所定义; R 2是氢，任选被羟基，氰基或三氟甲基取代的C 1-6烷基，C 2-6烯基（提供双键不在1-位），（C 2-6炔基（条件是三键不在 1-位），苯基C 1-3烷基或吡啶基C 1-3烷基; R 3是氢，甲基或乙基; D是氢，任选取代的含有一个双键的5-7元碳环，被任选取代的C 1-3烷基含有一个双键的5-7元碳环或D具有式 - （CH 2）n CH（R 4）C（R 5）= C（R 6）R 7和N-氧化物其中化学上可能的是-NR 2，和其中化学可能的含硫环的S-氧化物;及其药学上可接受的盐和体内可水解的酯和酰胺;不包括4- [5-羧基-2-羟基苄基氨基]苯甲酸， 4- [2,5-二羟基苄基氨基]苯甲酸，5- [2-羟基苄基氨基] -2-羟基苯甲酸，3- [2,5-二羟基苄基氨基]苯甲酸，4- [2,5-二羟基苄基氨基]苯甲醛 de，3- [2-羟基苄基氨基]苯甲酸，4- [2,5-二羟基苄基氨基] -2-羟基苯甲酸，4- [羟基苄基氨基] -2-羟基苯甲酸和4 [2-羟基苄基氨基]苯甲酸。其制备方法，制备中的中间体，作为治疗剂的用途和含有它们的药物组合物。

43. 发明申请

WO1996039822A1 DRY WATER-DISPERSIBLE COMPOSITIONS OF MICROENCAPSULATED PESTICIDES 审中-公开
标题翻译：微乳化农药的干水分散组合物
公开(公告)号：WO1996039822A1
公开(公告)日：1996-12-19
申请号：PCT/GB1996001310
申请日：1996-06-03
申请人： ZENECA LIMITED
发明人： ZENECA LIMITED , SCHER, Herbert, Benson , CHEN, Jin, Ling , LO, Ray, Jia
IPC分类号： A01N25/14
CPC分类号： A01N25/28 , A01N25/14
摘要： Solid water-dispersible compositions containing microencapsulated pesticides are produced by spray-drying an aqueous suspension of said pesticides in the presence of a water-soluble polymer, preferably polyvinyl alcohol.
摘要翻译：通过在水溶性聚合物，优选聚乙烯醇存在下，将所述杀虫剂的水性悬浮液喷雾干燥来制备含微囊化农药的固体水分散性组合物。

44. 发明申请

WO1996038416A1 (-)-(3R)-3-METHYL-4-{4-[4-(4-PYRIDYL)PIPERAZIN-1-YL]PHENOXY} BUTYRIC ACID AS CELLULAR ADHESION INHIBITOR 审中-公开
标题翻译：（ - ） - （3R）-3-甲基-4- {4- [4-（4-吡啶基）哌嗪-1-基]苯基}丁酸作为细胞粘附抑制剂
公开(公告)号：WO1996038416A1
公开(公告)日：1996-12-05
申请号：PCT/GB1996001260
申请日：1996-05-28
申请人： ZENECA LIMITED
发明人： ZENECA LIMITED , MILLS, Stuart, Dennett
IPC分类号： C07D213/74
CPC分类号： C07D213/74
摘要： The novel optically active compound (-)-(3R)-3-methyl-4-{4-[4-(4-pyridyl)-piperazin-1-yl]phenoxy}butyric acid, and pharmaceutically-acceptable salts, esters, amides or solvates thereof. Processes for the preparation of the compound, pharmaceutical compositions containing the compound and its use to inhibit cellular adhesion, for example platelet aggregation.
摘要翻译：新的光学活性化合物（ - ） - （3R）-3-甲基-4- {4- [4-（4-吡啶基） - 哌嗪-1-基]苯氧基}丁酸及其药学上可接受的盐，酯，酰胺或溶剂化物。用于制备化合物的方法，含有该化合物的药物组合物及其抑制细胞粘附的用途，例如血小板聚集。

45. 发明申请

WO1996036587A1 CATALYTIC NITRATION 审中-公开
标题翻译：催化硝化
公开(公告)号：WO1996036587A1
公开(公告)日：1996-11-21
申请号：PCT/GB1996001186
申请日：1996-05-17
申请人： ZENECA LIMITED , DEBOOS, Gareth, Andrew , SMITH, Keith , MUSSON, Adam, Johnathon
发明人： ZENECA LIMITED
IPC分类号： C07C201/08
CPC分类号： C07C201/08 , C07D333/42 , Y02P20/582 , C07C205/06 , C07C205/12 , C07C205/37
摘要： A solvent free process for the nitration of an aromatic compound using an aluminosilicate catalyst which has been treated with nitric acid and an acid anhydride. The process enables nitrated aromatic compounds to be produced in high yields and with good regioselectivity. The process also avoids the need to recover the nitrated product from large volumes of solvent and avoids treatment of inorganic acid waste, both of which may be undesirable for environmental reasons.
摘要翻译：使用已经用硝酸和酸酐处理的硅铝酸盐催化剂硝化芳族化合物的无溶剂方法。该方法能够以高产率和良好的区域选择性生产硝化芳族化合物。该方法还避免了从大量溶剂中回收硝化产物的需要，并且避免了无机酸废物的处理，因为这两个因素在环境方面都是不希望的。

46. 发明申请

WO1996031444A1 METHOD OF COATING OPTICAL FIBRES 审中-公开
标题翻译：涂布光纤的方法
公开(公告)号：WO1996031444A1
公开(公告)日：1996-10-10
申请号：PCT/GB1996000755
申请日：1996-03-29
申请人： ZENECA LIMITED , BROWN, Beverley, Anne , EDWARDS, Martin, Russell
发明人： ZENECA LIMITED
IPC分类号： C03C25/02
CPC分类号： C03C25/1065
摘要： A "wet-on-wet" method of coating an optical glass fibre, so as to provide thereon an ultra violet radiation-cured clear primary coating and an ultra violet radiation-cured pigmented secondary coating, comprises: a) applying to the fibre a clear primary curable liquid coating composition, b) applying directly onto the curable primary composition a pigmented curable secondary liquid coating composition, and c) simultaneously curing both the primary and secondary coating compositions using ultra violet radiation, and acylphosphine photoinitiator being used as an initiator during the curing of the primary coating composition.
摘要翻译：一种涂覆光学玻璃纤维的“湿法湿式”方法，以便在其上提供紫外线辐射固化的透明一级涂层和紫外线辐射固化的着色二次涂层，包括：a）施加到纤维a 透明的主要可固化液体涂料组合物，b）将直接涂覆到可固化的初级组合物上的着色的可固化的次级液体涂料组合物，和c）使用紫外线辐射同时固化所述主要和次要的涂料组合物，并且使用酰基膦光引发剂作为引发剂初级涂料组合物的固化。

47. 发明申请

WO1996025452A1 PRODUCTION OF A POLYMER COMPOSITION 审中-公开
标题翻译：生产聚合物组合物
公开(公告)号：WO1996025452A1
公开(公告)日：1996-08-22
申请号：PCT/GB1996000305
申请日：1996-02-12
申请人： ZENECA LIMITED , LIDDELL, John, Macdonald , GEORGE, Neil , TURNER, Peter, Deryck
发明人： ZENECA LIMITED
IPC分类号： C08J03/03
CPC分类号： C12P7/625 , C08G63/89 , C08J3/07 , C08J2367/04
摘要： A process of making a polyhydroxyalkanoate PHA latex comprises making a liquid-form solution of such PHA in a water soluble liquid and contacting that solution with water under shear. Suitably the solution is prepared at a temperature between the boiling point of water and 10 DEG C below the melting point of the PHA as measured by DSC for example by melt separating PHA from a microbiologicalsuspension thereof, dissolving it in the water soluble liquid, and then contacting the solution at over 100 DEG C with water at 50-95 DEG C. The water-soluble liquid may be for example 1,2-propandiol or a liquid more volatile than water such as ethanol, propanol or tertiary butanol. A surfactant may be present or added after contacting, for example one providing steric stabilisation such as an acrylic graft copolymer emulsifier.
摘要翻译：制备聚羟基链烷酸酯PHA胶乳的方法包括将这种PHA的液体形式的溶液制成水溶性液体，并在剪切下使该溶液与水接触。适当地，溶液在沸点水和低于PHA熔点10℃之间的温度下制备，例如通过DSC测量，例如通过将PHA与其微生物悬浮液熔融分离，将其溶解在水溶性液体中，然后在100℃以上的溶液与水在50-95℃下接触。水溶性液体可以是例如1,2-丙二醇或比水如乙醇，丙醇或叔丁醇更易挥发的液体。在接触之后可以存在或加入表面活性剂，例如提供空间稳定剂的表面活性剂，例如丙烯酸接枝共聚物乳化剂。

48. 发明申请

WO1996023812A1 PROLINE DERIVATIVES USEFUL AS INHIBITORS OF HUMAN LEUKOCYTE ELASTASE 审中-公开
标题翻译：丙泊酚衍生物作为人类白细胞抗原的抑制剂有用
公开(公告)号：WO1996023812A1
公开(公告)日：1996-08-08
申请号：PCT/GB1996000193
申请日：1996-01-30
申请人： ZENECA LIMITED
发明人： ZENECA LIMITED , BERNSTEIN, Peter, Robert , VEALE, Chris, Allan , DAVIES, Elwyn, Peter
IPC分类号： C07K05/083
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to particular forms of a novel 1-substituted-N-[2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide of formula (I) which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes pharmaceutical compositions containing such forms, processes for preparing the forms and intermediates useful in the synthesis of the forms.
摘要翻译：本发明涉及作为人类白细胞弹性蛋白酶（HLE）抑制剂的式（I）的新的1-取代-N- [2-甲基-1-（三氟乙酰基）丙基]吡咯烷-2-甲酰胺的具体形式，被称为人嗜中性粒细胞弹性蛋白酶（HNE），使得它们在需要这种抑制时是有用的，例如用于药物，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗。本发明还包括含有这种形式的药物组合物，用于制备可用于合成形式的形式和中间体的方法。

49. 发明申请

WO1996022334A1 MONOAZO PIGMENTS 审中-公开
标题翻译： MONOAZO颜料
公开(公告)号：WO1996022334A1
公开(公告)日：1996-07-25
申请号：PCT/GB1995002833
申请日：1995-12-05
申请人： ZENECA LIMITED , CHORLTON, Alan, Patrick , MASON, James
发明人： ZENECA LIMITED
IPC分类号： C09B63/00
CPC分类号： C09B69/045 , C09B29/366 , C09B63/005 , C09B67/0029 , Y10S534/04
摘要： An azo pyrazolone compound of formula (1) in the form of a salt, and its use as a pigment.
摘要翻译：盐形式的式（1）的偶氮吡唑啉酮化合物及其作为颜料的用途。

50. 发明申请

WO1996022023A1 COMPOSITION AND USE 审中-公开
标题翻译：组成和使用
公开(公告)号：WO1996022023A1
公开(公告)日：1996-07-25
申请号：PCT/GB1995002951
申请日：1995-12-18
申请人： ZENECA LIMITED , AUSTIN, Peter, William
发明人： ZENECA LIMITED
IPC分类号： A01N43/80
CPC分类号： C07D275/04 , A01N43/80 , C08K5/0058 , C08K5/47
摘要： The use of a 2-(C3-5-alkyl)-BIT or 2-aralkyl-BIT such as 2-phenylethyl-BIT as a fungicide for plastics materials. 2-n-butyl-BIT is preferred.
摘要翻译：使用2-（C 3-8 - 烷基）-BIT或2-芳烷基-BIT如2-苯基乙基-BIT作为塑料材料的杀真菌剂。 2-正丁基-BIT是优选的。

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