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1. 发明授权

US5256811A Certain intermediates for the preparation of neuinic acid derivatives 失效
标题翻译：用于制备神经酸衍生物的某些中间体
公开(公告)号：US5256811A
公开(公告)日：1993-10-26
申请号：US804075
申请日：1991-12-06
申请人： Richard S. Todd , Maxwell Reeve
发明人： Richard S. Todd , Maxwell Reeve
IPC分类号： C07C69/013 , C07C69/732 , C07C69/757 , C07D309/30 , C07C321/22 , C07C69/608
CPC分类号： C07C69/013 , C07C69/732 , C07C69/757 , C07D309/30 , Y02P20/55
摘要： compounds of formula I ##STR1## wherein R.sup.1 represents a C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, C.sub.3-8 cycloalkyl(C.sub.1-8)alkyl, C.sub.1-8 hydroxyalkyl, C.sub.1-8 alkylthio, phenyl or substituted phenyl;R.sup.3 represents a C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, CO2(C.sub.1-8)alkyl, CO.sub.2 (C.sub.2-8) alkenyl, C.sub.1-8 alkylthio, (C.sub.1-2)alkyl CO.sub.2 (C.sub.1-8) alkyl or C.sub.1-8 aldehydroalkyl where the aldehyde function is protected by a suitable protecting group (for example, an acetal such as a dimethyl acetal);R.sup.4 represents a hydrogen atom, C.sub.1-8 alkyl or C.sub.2-8 alkenyl;Z represents a group (CH.sub.2).sub.n or a branched alkyl chain;n is 1 to 8;and each of a, b and c is independently a single or a double bond;can be prepared relatively easily and in good xxx at room temperature by reacting a compound of general formula II ##STR2## wherein R.sup.2, R.sup.3, R.sup.4, Z, a, b and c are as define din general formula I; with a compound of general formula IIICHI.sub.2 R.sup.1 (III)wherein R.sup.1 is as defined in general formula I;in the presence of metal ions such as chromium (II) ions. The sever conditions of the Wittig reaction can therefore be avoided.Compounds of formula I are useful intermediates in the synthesis of mevinic acids, which are potent inhibitors of HMG-CoA reductase and which are useful in the treatment of hypocholesterolaemia an hyperlipidaemia.
摘要翻译：式I的化合物其中R 1表示C 1-8烷基，C 2-8烯基，C 2-8炔基，C 3-8环烷基（C 1-8）烷基，C 1-8羟烷基，C 1-8烷硫基，苯基或取代苯基; R 3表示C 1-8烷基，C 2-8烯基，C 2-8炔基，CO 2（C 1-8）烷基，CO 2（C 2-8）烯基，C 1-8烷硫基，（C 1-2）烷基CO 2 ）烷基或C 1-8脱氢烷基，其中醛官能团被合适的保护基保护（例如缩醛如二甲基缩醛）; R 4表示氢原子，C 1-8烷基或C 2-8烯基; Z表示基团（CH 2）n或支链烷基链; n为1至8; a，b和c各自独立地为单键或双键; 其中R 2，R 3，R 4，Z，a，b和c如通式I所定义;通式II的化合物其中R2，R3，R4，Z，a，与通式III的化合物CHI 2 R 1（III）其中R 1如通式I中所定义; 在金属离子如铬（II）离子的存在下。因此可以避免维蒂希反应的严重条件。式I化合物是合成有效的中间体，它是HMG-CoA还原酶的有效抑制剂，可用于治疗高胆固醇血症的低胆固醇血症。

2. 发明授权

US5200412A Heterobicyclic containing benzene sulfonamides which are platelet activating factor antagonists 失效
标题翻译：含有苯甲酸甲酯的异环己烯体活性成分因子拮抗剂
公开(公告)号：US5200412A
公开(公告)日：1993-04-06
申请号：US745471
申请日：1991-08-15
申请人： Mark Whittaker , Andrew Miller
发明人： Mark Whittaker , Andrew Miller
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/435 , A61K31/4375 , A61K31/535 , A61K31/5355 , A61P9/02 , A61P9/10 , A61P11/00 , A61P29/00 , A61P43/00 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/26 , C07D235/28 , C07D401/12 , C07D403/12 , C07D471/04 , C07F7/18
CPC分类号： C07D401/12 , A61K31/415 , C07D235/08 , C07D403/12 , C07D471/04 , C07F7/1856
摘要： Compounds of general formula I; ##STR1## wherein: A.sup.1 is .dbd.N--, .dbd.CH-- or .dbd.CR.sup.1 --;A.sup.2 is --N.dbd., --CH.dbd. or --CR.sup.2 .dbd.;provided that, when one of A.sup.1 and A.sup.2 is a nitrogen atom, the other of A.sup.1 and A.sup.2 is other than a nitrogen atom;the rest of the variables are described in the specification;and their pharmaceutically and veterinarily acceptable acid addition salts and hydrates are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or disorders mediated by PAF.
摘要翻译：通式I的化合物; 其中：A1为= N-，= CH-或CR1-; A2是-N =，-CH =或-CR2 = 条件是当A1和A2之一是氮原子时，A1和A2中的另一个不是氮原子; 其余的变量在说明书中描述; 其药物和兽医学上可接受的酸加成盐和水合物是血小板活化因子（PAF）的拮抗剂，因此可用于治疗或改善由PAF介导的各种疾病或病症。

3. 发明授权

US5158877A Gene synthesis 失效
标题翻译：基因合成
公开(公告)号：US5158877A
公开(公告)日：1992-10-27
申请号：US582926
申请日：1990-10-11
申请人： Richad M. Edwards , Sally E. Adams
发明人： Richad M. Edwards , Sally E. Adams
IPC分类号： C12N15/09 , C07K14/16 , C12N15/10 , C12Q1/68
CPC分类号： C07K14/005 , C12N15/10 , C12Q1/686 , C12N2740/16322
摘要： Double stranded DNA (ds-DNA) can be prepared by preparing a hybrid DNA containing a single stranded portion and a double stranded portion and carrying out in vivo gap repair on the hybrid DNA. The hybrid DNA is prepared by synthesizing a single strand of DNA and introducing the single strand into double stranded DNA. This method of synthesis can be used to make synthetic genes, including synthetic DNA coding for the TAT protein of HIV-I, and incorporates useful restriction sites. Also included are flanking restriction sites to simplify the incorporation of the gene into any desired expression system.
摘要翻译： PCT No.PCT / GB89 / 00384 Sec。 371 1990年10月11日第 102（e）1990年10月11日PCT PCT 1989年4月14日提交PCT公布。出版物WO89 / 09824 日期为1989年10月19日。双链DNA（ds-DNA）可以通过制备含有单链部分和双链部分并在杂交DNA上进行体内间隙修复的杂交DNA来制备。通过合成单链DNA并将单链引入双链DNA来制备杂交DNA。这种合成方法可用于制备合成基因，包括编码HIV-1 TAT蛋白的合成DNA，并结合有用的限制性位点。还包括侧翼限制位点以简化基因并入任何所需的表达系统。

4. 发明授权

US5736363A IGF-II analogues 失效
标题翻译： IGF-II类似物
公开(公告)号：US5736363A
公开(公告)日：1998-04-07
申请号：US190029
申请日：1994-02-28
申请人： Richard Mark Edwards , Lindsay Bawden
发明人： Richard Mark Edwards , Lindsay Bawden
IPC分类号： A61K38/00 , C07K14/65 , C12N1/21 , C12N9/08 , C12N15/16 , C12P21/06 , A61K38/30
CPC分类号： C12N9/0065 , C07K14/65 , A61K38/00 , C07K2319/00 , C07K2319/035 , C07K2319/75
摘要： Insulin-like Growth Factor II (IGF-II) analogues in which at least one of R37 and R38 is replaced with another amino add residue, the most preferred being IGF-II R37Q R38Q, can readily be produced in E. coli, unlike natural IGF-II, which is cleaved on secretion. The analogues retain activity on the type I and type II IGF receptors but have lower affinity for the insulin receptor; they are therefore more specific in their action.
摘要翻译： PCT No.PCT / GB92 / 01389 371日期1994年2月28日 102（e）1994年2月28日PCT PCT 1992年7月27日PCT公布。出版物WO93 / 03152 日期：1993年2月18日胰岛素样生长因子II（IGF-II）类似物，其中R37和R38中的至少一个被另一个氨基加成残基替代，最优选的是IGF-II R37Q R38Q，可容易地在E中产生大肠杆菌，不同于天然IGF-II，其在分泌物上被切割。类似物保留对I型和II型IGF受体的活性，但对胰岛素受体具有较低的亲和力; 因此，他们的行动更具体。

5. 发明授权

US5434073A Fibrinolytic and anti-thrombotic cleavable dimers 失效
标题翻译：纤维蛋白溶解和抗血栓形成的切割二聚体
公开(公告)号：US5434073A
公开(公告)日：1995-07-18
申请号：US854596
申请日：1992-06-03
申请人： Keith Dawson , Michael G. Hunter , Lloyd G. Czaplewski
发明人： Keith Dawson , Michael G. Hunter , Lloyd G. Czaplewski
IPC分类号： A61K38/46 , A61K38/00 , A61K38/48 , A61K38/55 , A61P7/02 , C07K7/64 , C07K14/00 , C07K14/315 , C07K14/745 , C07K14/81 , C07K14/815 , C07K19/00 , C12N20060101 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/48 , C12N9/64 , C12N9/68 , C12N9/70 , C12N9/72 , C12N15/09 , C12N15/15 , C12N15/57 , C12N15/62 , C12N15/81 , C12N15/85 , C12P21/02
CPC分类号： C12N9/6435 , C07K14/3153 , C07K14/815 , C07K7/64 , C12N15/62 , C12N15/625 , C12N15/81 , C12N15/85 , C12N9/48 , C12N9/6459 , C12Y304/21007 , C12Y304/21069 , A61K38/00 , C07K2319/00 , C12N2800/108 , C12N2830/002 , C12N2830/15 , C12N2830/32 , C12N2830/55 , C12N2830/704 , C12N2840/107
摘要： Relatively inactive fusion proteins are activatable by enzymes of the clotting cascade to have fibrinolytic and/or clot formation inhibition activity. For example, a fusion protein comprising two hirudin or streptokinase molecules, linked by a cleavable linkage sequence, may be cleaved to yield anti-thrombotic hirudin or fibrinolytic streptokinase by thrombin or Factor Xa. Fibrinolytic or clot formation inhibition activity is therefore directed to the site of clot formation. Cleavable streptokinase/hirudin heterodimers are claimed.
摘要翻译： PCT No.PCT / GB90 / 01911 Sec。 371日期：1992年6月3日 102（e）日期1992年6月3日PCT 1990年12月7日PCT PCT。公开号WO91 / 09125 日期1991年6月27日。相对无活性的融合蛋白可通过凝血级联的酶激活以具有纤维蛋白溶解和/或凝块形成抑制活性。例如，通过可切割连锁序列连接的包含两个水蛭素或链激酶分子的融合蛋白可能被切割，以通过凝血酶或因子Xa产生抗血栓形成水蛭素或纤维蛋白溶解性链激酶。因此，纤维蛋白溶解或凝块形成抑制活性指向凝块形成部位。可剥夺的链激酶/水蛭素异二聚体。

6. 发明授权

US5308864A 6-(hydronaphtyl-1-ethyl)-4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones and the corresponding hydroxy acids 失效
标题翻译： 6-（氢化萘基-1-乙基）-4-羟基-3,4,5,6-四氢-2H-吡喃-2-酮和相应的羟基酸
公开(公告)号：US5308864A
公开(公告)日：1994-05-03
申请号：US773657
申请日：1991-10-15
申请人： Christopher N. Lewis , Alan H. Davidson , Christopher D. Floyd , Jonathan P. Dickens
发明人： Christopher N. Lewis , Alan H. Davidson , Christopher D. Floyd , Jonathan P. Dickens
IPC分类号： A61K31/215 , A61K31/23 , A61K31/365 , A61K47/48 , A61P3/06 , A61P9/10 , C07C69/28 , C07C69/732 , C07C69/738 , C07D309/00 , C07D309/30 , A61K31/35 , A61K31/225
CPC分类号： C07C69/732 , C07C69/738 , C07D309/30
摘要： Compounds of either of general formulae (I) and (II), wherein: R.sup.1 represents a C.sub.1-8 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl(C.sub.1-8)alkyl, C.sub.2-8 alkenyl, or C.sub.1-6 alkyl substituted phenyl group; R.sup.2 represents a C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl group or a C.sub.1-5 alkyl, C.sub.2-5 alkenyl or C.sub.2-5 alkynyl group substituted with a substituted phenyl group; R.sup.3 represents a hydrogen atom or a substituent R.sup.4 or M; R.sup.4 represents a C.sub.1-5 alkyl group, or C.sub.1-5 alkyl group substituted with a group chosen from substituted phenyl, dimethylamino and acetylamino; R.sup.5 represents a hydrogen atom or a methyl or ethyl group except that when R.sup.2 is methyl then R.sup.5 is not methyl; M represents a cation capable of forming a pharmaceutically acceptable salt; Q represents C.dbd.O or CHOH; and each of a, b, c, and d, is independently a single or double bond except that when a and c are double bonds then b is a single bond; are inhibitors of the enzyme 24 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate limiting enzyme in the biosynthesis of cholesterol in mammals including man, and as such are useful in the treatment of hypercholesterolemia in general and arteriosclerosis, familiar hypercholesterolemia or hyperlipidemia in particular.
摘要翻译： PCT No.PCT / GB90 / 01030 Sec。 371日期1991年10月15日 102（e）1991年10月15日PCT PCT 1990年7月4日PCT公布。公开号WO91 / 00280 1991年1月10日。通式（I）和（II）的化合物，其中：R1表示C1-8烷基，C3-8环烷基，C3-8环烷基（C1-8）烷基，C2-8 烯基或C 1-6烷基取代的苯基; R2表示被取代的苯基取代的C1-8烷基，C2-8烯基，C2-8炔基或C1-5烷基，C2-5烯基或C2-5炔基; R3表示氢原子或取代基R4或M; R4表示C1-5烷基或被选自取代的苯基，二甲基氨基和乙酰氨基的基团取代的C1-5烷基; R5表示氢原子或甲基或乙基，不同之处在于当R 2为甲基时，R 5不是甲基; M表示能够形成药学上可接受的盐的阳离子; Q表示C = O或CHOH; a，b，c和d各自独立地为单键或双键，不同之处在于当a和c为双键时，b为单键; 是酶24-羟基-3-甲基戊二酰辅酶A还原酶（HMG-CoA还原酶）的抑制剂，包括人在内的哺乳动物的胆固醇生物合成中的限速酶，因此可用于一般治疗高胆固醇血症，动脉硬化，熟悉的高胆固醇血症或高脂血症。

7. 发明授权

US5300674A P2'-modified hydroxamic acid collagenase inhibitors 失效
标题翻译： P2'-修饰的异羟肟酸胶原酶抑制剂
公开(公告)号：US5300674A
公开(公告)日：1994-04-05
申请号：US760741
申请日：1991-09-16
申请人： M. J. Crimmin , A. H. Davidson , R. P. Beckett
发明人： M. J. Crimmin , A. H. Davidson , R. P. Beckett
IPC分类号： A61K31/165 , A61K31/19 , A61K31/215 , A61K31/275 , A61K31/38 , A61K31/381 , A61P1/02 , A61P19/10 , A61P27/02 , A61P29/00 , A61P43/00 , C07C237/22 , C07C259/06 , C07C323/60 , C07D333/34 , C07C229/34
CPC分类号： C07C259/06 , C07C237/22 , C07C323/60 , C07D333/34
摘要： Compounds of general formula I: ##STR1## Wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are variables.These compounds have collagenase inhibition activity and are useful in the management of disease involving collagen degradation. Its uses include rheumatoide arthritis, corneal ulceration, osteoporosis, periodontitis, gingivitis and tumour invasion.
摘要翻译：通式I的化合物：（*化学结构*）其中R1，R2，R3，R4，R5和R6是变量。这些化合物具有胶原酶抑制活性，可用于治疗涉及胶原降解的疾病。其用途包括风湿关节炎，角膜溃疡，骨质疏松症，牙周炎，牙龈炎和肿瘤侵袭。

8. 发明授权

US5300524A Spirocyclic PAF antagonists 失效
标题翻译：螺环PAF拮抗剂
公开(公告)号：US5300524A
公开(公告)日：1994-04-05
申请号：US760726
申请日：1991-09-16
申请人： Alan H. Davidson , Mark Whittaker , Zoe M. Spavold
发明人： Alan H. Davidson , Mark Whittaker , Zoe M. Spavold
IPC分类号： C07D307/94 , C07D405/06 , A61K31/34 , C07D311/96
CPC分类号： C07D405/06 , C07D307/94
摘要： Compounds of general formula I; ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are variables.These compounds are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or disorders mediated by PAF.
摘要翻译：通式I的化合物; （*化学结构*）I其中R1，R2，R3，R4，R5，R6和R7是变量。这些化合物是血小板活化因子（PAF）的拮抗剂，因此可用于治疗或改善由PAF介导的各种疾病或病症。

9. 发明授权

US5232847A Human tissue plasminogen activator analogue having substitutions at amino acid positions 66, 67 and 68 失效
标题翻译：在氨基酸位置66,67和68上具有取代基的人组织PLASMINOGEN激活剂模拟物
公开(公告)号：US5232847A
公开(公告)日：1993-08-03
申请号：US613908
申请日：1990-12-11
申请人： Richard M. Edwards , Keith Dawson , Anthony Fallon , Stewart Craig
发明人： Richard M. Edwards , Keith Dawson , Anthony Fallon , Stewart Craig
IPC分类号： C12N15/09 , A61K38/00 , A61K38/46 , A61P7/02 , C07H21/04 , C12N20060101 , C12N1/00 , C12N5/10 , C12N9/00 , C12N9/64 , C12N9/72 , C12N15/58 , C22B4/02 , C22B4/06 , C22C1/02
CPC分类号： C12N9/6459 , C12Y304/21069 , A61K38/00
摘要： Tissue plasminogen activator (t-PA) analogues have at least one substitution in the growth factor (GF) domain that at least partially reduces hepatic receptor binding without substantially jeopardising physico-chemical stability in blood or fibrinolytic activity. This results in a longer plasma half life. Substitutions in the beta-sheet encompassing residues 63-72, especially at Leu 66 and/or Tyr 67 and/or Phe 68, are particularly preferred.

10. 发明授权

US5637595A Cyclic ether acetal PAF antagonists 失效
公开(公告)号：US5637595A
公开(公告)日：1997-06-10
申请号：US175411
申请日：1993-12-30
申请人： Mark Whittaker , Andrew Miller , Stephen A. Bowles
发明人： Mark Whittaker , Andrew Miller , Stephen A. Bowles
IPC分类号： C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , A61K31/425 , A61K31/44
CPC分类号： C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04
摘要： Compounds of general formula (I), wherein W represents a 5- or 6-membered aromatic heterocyclic ring containing one or more non-quaternised sp2 nitrogen atoms in its ring, which heterocyclic ring may be optionally fused to a benzene ring or to a further 5- or 6-membered aromatic heterocyclic ring containing one or more nitrogen atoms, wherein at least one of the said heterocyclic rings may also contain an oxygen or sulphur atom, and wherein any of the rings may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; Z represents a) a divalent alkanediyl group from 1 to 8 carbon atoms which may be a straight or branched-chain, wherein the said group is either unsubstituted or substituted by one or more substituents selected from hydroxy, --OC.sub.1 -C.sub.6 alkyl, --SC.sub.1 -C.sub.6 alkyl and halo; or b) a divalent alkenediyl or alkynediyl group from 2 to 8 carbon atoms which may be a straight or branched-chain, wherein the said group is either unsubstituted or subtituted by one or more substituents selected from hydroxy, --OC.sub.1 -C.sub.6 alkyl, --SC.sub.1 -C.sub.6 alkyl and halo; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 each represents a hydrogen atom, a --C.sub.1 -C.sub.18 alkyl or a --C.sub.2 -C.sub.18 alkenyl group; or R.sup.3 and R.sup.5 together with the carbon atoms to which they are attached can form a five to ten membered monocycycloalkyl or bicycloalkyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; or R.sup.3, R.sup.4 and R.sup.5, R.sup.6 and the carbon atoms to which they are attached form a phenyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; X represents a bond, an oxygen atom, a sulphur atom, a --NH-- group, a --N(C.sub.1 -C.sub.6 alkyl)-- group, a --(CH.sub.2).sub.n -- group or a --CR.sup.7 R.sup.8 -- group; n represents an integer of 1, 2 or 3; R.sup.7 and R.sup.8 each represents a --C.sub.1 -C.sub.18 alkyl or a --C.sub.2 -C.sub.18 alkenyl group; or R.sup.3 and R.sup.7 together with the carbon atoms to which they are attached can form a five to ten membered monocycloalkyl or bicycloalkyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; or R.sup.3, R.sup.4 and R.sup.7, R.sup.8 and the carbon atoms to which they are attached form a phenyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; and their pharmaceutically and veterinarily acceptable acid addition salts and hydrates are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or conditions mediated by PAF.

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