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1. 发明授权

US5596105A Therapeutically active naphthalenesulfonic pyrrolecarboxamido derivatives 失效
标题翻译：治疗活性萘磺酰吡咯烷酰胺衍生物
公开(公告)号：US5596105A
公开(公告)日：1997-01-21
申请号：US372872
申请日：1995-01-13
申请人： Nicola Mongelli , Giovanni Biasoli , Maria Grandi , Marina Ciomei , Maria C. Geroni
发明人： Nicola Mongelli , Giovanni Biasoli , Maria Grandi , Marina Ciomei , Maria C. Geroni
IPC分类号： A61K31/40 , A61P31/12 , A61P31/18 , C07D207/34 , C07D207/36
CPC分类号： C07D207/34
摘要： The invention relates to naphthalenesulfonic-pyrrolecarboxamido compounds of formula ##STR1## wherein n is zero or an integer of 1 to 3; R is a sulfonic acid residue; m is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof, which are active as antiviral agents, in particular against Human Immunodeficiency Virus
摘要翻译：本发明涉及式（I）+（其中n为0或1〜3的整数）的萘磺酰 - 吡咯酰胺化合物。 R是磺酸残基; m为1〜3的整数，或其药学上可接受的盐，其作为抗病毒剂具有活性，特别是针对人类免疫缺陷病毒

2. 发明授权

US5587373A 2-acyloxycephem derivatives 失效
标题翻译： 2-酰氧基头孢烯衍生物
公开(公告)号：US5587373A
公开(公告)日：1996-12-24
申请号：US331483
申请日：1994-11-04
申请人： Marco Alpegiani , Pierluigi Bissolino , Ettore Perrone
发明人： Marco Alpegiani , Pierluigi Bissolino , Ettore Perrone
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/16 , C07D501/20 , C07D501/26 , C07D501/36 , C07D501/38 , C07D501/59 , C07D501/04 , C07D501/14 , C07D501/60
CPC分类号： C07D501/00
摘要： The present invention provides cephalosporin sulphones of formula (I) and the pharmaceutically and veterinarily acceptable salts thereof: ##STR1## wherein n is one or two: A and B are both or each independently hydrogen or an organic radical;R.sup.1 represents halogen, A, OA, --S(O).sub.m A wherein m is 0-2, --OC(O)A, --OS(O).sub.2 A, --NHC(O)A or --NH--Z wherein Z is a mono, di- or tripeptide and A is as defined above;R.sup.2 represents a halogen, A, --S(O).sub.m A, --O--A, --C(O)A, --C(O)OA, --CH.sub.2 --OA, --CH.sub.2 S(O).sub.m A, --CH.sub.2 OC(O)A, --CH.sub.2 O--Z, --CH.sub.2 SC(O) A, --CH.sub.2 --N(A)A, --CH.sub.2 N.sup.+ (A)(A')A", --CH.sub.2 NH--C(O)A or --CH.sub.2 NH--Z wherein A and Z are as defined above.The compounds of formula (I) and their salts are elastase inhibitors.
摘要翻译： PCT No.PCT / EP94 / 00529 Sec。 371日期：1994年11月4日 102（e）日期1994年11月4日PCT 1994年2月24日PCT PCT。 WO94 / 20504 PCT出版物 1994年9月15日本发明提供式（I）的头孢菌素砜及其药学上和兽医学上可接受的盐：其中n是一个或两个：A和B都是氢或有机的激进; R1表示卤素，A，OA，-S（O）mA，其中m为0-2，-OC（O）A，-OS（O）2A，-NHC（O）A或-NH-Z，其中Z为单，二或三肽和A如上所定义; R 2表示卤素，A，-S（O）mA，-OA，-C（O）A，-C（O）OA，-CH 2 OA，-CH 2 S（O） -CH 2 SC（O）A，-CH 2 -N（A）A，-CH 2 N +（A）（A'）A“，-CH 2 NH-C（O）A或-CH 2 NH- Z如上所定义。式（I）化合物及其盐是弹性蛋白酶抑制剂。

3. 发明授权

US5571509A Truncated forms of the hepatocyte growth factor (HGF) receptor 失效
标题翻译：截短形式的肝细胞生长因子（HGF）受体
公开(公告)号：US5571509A
公开(公告)日：1996-11-05
申请号：US879384
申请日：1992-05-07
申请人： Paolo Comoglio , Tiziana Crepaldi , Maria Prat
发明人： Paolo Comoglio , Tiziana Crepaldi , Maria Prat
IPC分类号： A61K38/00 , C07K14/00 , C07K14/705 , C07K14/71 , C07K14/82 , C07K16/32 , C07K19/00 , C12N5/06 , C12N9/12 , C12N15/12 , C12P21/02 , C12R1/91 , C12N9/10 , A61K38/45
CPC分类号： C07K14/82 , C07K16/32 , A61K38/00
摘要： A protein, which is useful as an antagonist of hepatocyte growth factor, is composed of two disulphide-linked chains of 50 kDa and 75 or 85 kDa respectively, the 5 kDa chain being the .alpha.-chain of the tyrosine kinase encoded by the MET protooncogene and the 75 or 85 kDa chain being a C-terminal truncated form of the .beta.-chain of the said tyrosine kinase.
摘要翻译：可用作肝细胞生长因子拮抗剂的蛋白质分别由50kDa和75或85kDa的两个二硫键连接的链组成，5kDa链是由MET原癌基因编码的酪氨酸激酶的α-链并且75或85kDa链是所述酪氨酸激酶的β-链的C-末端截短形式。

4. 发明授权

US5563064A Process for preparing daunorubicin 失效
标题翻译：制备柔红霉素的方法
公开(公告)号：US5563064A
公开(公告)日：1996-10-08
申请号：US259924
申请日：1994-06-15
申请人： Charles R. Hutchinson , Krishna M. Madduri , Francesca Torti , Anna L. Colombo
发明人： Charles R. Hutchinson , Krishna M. Madduri , Francesca Torti , Anna L. Colombo
IPC分类号： C12N1/21 , C12N9/10 , C12N15/09 , C12N15/54 , C12P19/56 , C12P19/60 , C12R1/185 , C12R1/465 , C12N15/70
CPC分类号： C12N9/1007 , C12P19/56
摘要： The ability to convert carminomycin to daunorubicin can be conferred on a host by transforming the host with a recombinant vector comprising a DNA having the configuration of restriction sites shown in FIGS. 2, 3 and 4 and a nucleotide sequence shown in FIG. 3 of the accompanying drawings or a restriction fragment derived therefrom containing a gene coding for carminomycin 4-O-methyltransferase.
摘要翻译：通过用包含具有如图1和2所示的限制性位点构型的DNA的重组载体转化宿主，可以将宿主转化为柔红霉素的能力。 2,3和4以及图3所示的核苷酸序列。附图3或其衍生的限制性片段含有编码卡培霉素4-O-甲基转移酶的基因。

5. 发明授权

US5488057A 2-oxindole compounds which have useful tyrosine kinase activity 失效
标题翻译：具有有用的酪氨酸激酶活性的2-羟吲哚化合物
公开(公告)号：US5488057A
公开(公告)日：1996-01-30
申请号：US294350
申请日：1994-08-23
申请人： Franco Buzzetti , Antonio Longo , Maristella Colombo
发明人： Franco Buzzetti , Antonio Longo , Maristella Colombo
IPC分类号： A61K31/16 , A61K31/03 , A61K31/19 , A61K31/22 , A61K31/275 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4178 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61P35/00 , A61P43/00 , C07C57/42 , C07C57/60 , C07C59/52 , C07C59/54 , C07C59/64 , C07C69/017 , C07C209/42 , C07C215/48 , C07C233/11 , C07C235/34 , C07C255/34 , C07C255/36 , C07C255/37 , C07C255/41 , C07C255/52 , C07C255/53 , C07C255/54 , C07C327/44 , C07C327/48 , C07D209/34 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/22 , C07D215/227 , C07D215/233 , C07D215/26 , C07D401/06 , C07D403/06 , C07D417/06 , A61K31/405
CPC分类号： C07D215/227 , C07C235/34 , C07C255/36 , C07C255/41 , C07C327/44 , C07C59/52 , C07C59/54 , C07D209/34 , C07D215/14 , C07D215/20 , C07D215/233 , C07D215/26 , C07D401/06 , C07D403/06 , C07C2102/10
摘要： The present invention provides novel aryl- and heteroarylethenylene derivatives which are useful as tyrosine kinase activity inhibitors.
摘要翻译：本发明提供了可用作酪氨酸激酶活性抑制剂的新型芳基和亚杂亚氨基衍生物。

6. 发明授权

US5473055A Polymer-bound paclitaxel derivatives 失效
标题翻译：聚合物结合紫杉醇衍生物
公开(公告)号：US5473055A
公开(公告)日：1995-12-05
申请号：US263832
申请日：1994-06-22
申请人： Nicola Mongelli , Francesco Angelucci , Enrico Pesenti , Antonino Suarato , Giovanni Biasoli
发明人： Nicola Mongelli , Francesco Angelucci , Enrico Pesenti , Antonino Suarato , Giovanni Biasoli
IPC分类号： A61K38/00 , A61K38/02 , A61K47/48 , A61P35/00 , C07D305/14 , C07K5/062 , C07K5/065 , C07K5/083 , C07K5/087 , C07K5/103 , C07K5/107 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/08
CPC分类号： A61K47/48176 , C07D305/14
摘要： A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta.Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,Gly-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.beta., Phe-Phe-Gly .beta.Ala, Phe-Leu-Gly-Phe-.beta.Ala or Gly-Phe-Leu-Gly-Phe-.beta.Ala. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：一种聚合物共轭物，其基本上由以下组成：90至99.9摩尔％的由式（IMAGE）表示的单元，为0.1至5摩尔％的由式IMA图示的单元，其中R 1和R 2之一是式，另一个是氢原子; 其中R是苯基或叔丁氧基，R3是H或乙酰基，A和A1可以相同或不同，表示化学单键，选自βAla，Gly，Phe-Gly，Phe-Phe-，Leu-Gly，Val-Ala，Phe-Ala，Leu-Phe，Leu-Ala，Phe-Leu-Gly的氨基酸残基或肽间隔子， Phe-Phe-Leu，Leu-Leu-Gly，Phe-Tyr-Ala，Phe-Gly-Phe，Phe-Phe-Gly，Phe-Leu-Gly-Phe，Gly-Phe-Leu-Gly-Phe， βAla，Phe-Gly-βAla，Phe-Phe-βAla，Leu-Gly-βAla，Val-Ala-Ala，Phe-Ala-Ala，Leu-Phe-βAla，Leu-Gly-β Ala，Phe-Leu-Gly-βAla，Phe-Phe-LeuβAla，Leu-Leu-Gly-βAla，Phe-Tyr-Ala-βAla，Phe-Gly-Phe-β，Phe-Phe-Gly β-Ala，Phe-Leu-Gly-Phe-β-Ala或Gly-Phe-Leu-Gly-Phe-β-Ala。与紫杉醇或其已知的类似物相比，这些化合物具有抗肿瘤活性，。还描述了其制备方法和含有它们的药物组合物。

7. 发明授权

US5449692A Substituted (arylalkylaminobenzyl) aminopropionamide derivatives and process for their preparation 失效
标题翻译：取代的（芳基烷基氨基苄基）氨基丙酰胺衍生物及其制备方法
公开(公告)号：US5449692A
公开(公告)日：1995-09-12
申请号：US215694
申请日：1994-03-22
申请人： Mario Varasi , Philippe Dostert , Paolo Pevarello , Alberto Bonsignori
发明人： Mario Varasi , Philippe Dostert , Paolo Pevarello , Alberto Bonsignori
IPC分类号： A61K31/165 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07C231/10 , C07C237/06 , C07C233/05
CPC分类号： C07C237/06
摘要： The invention provides new compounds of formula (I) ##STR1## wherein n is an integer of 1 to 4; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R2 is hydrogen or C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable salts thereof; and wherein when, at the same time, R is hydrogen, R.sub.1 is hydrogen or halogen and n is one, then R.sub.2 is other than hydrogen or methyl; and of formula (IA) ##STR2## wherein R.sub.3 is halogen, and a pharmaceutical acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.
摘要翻译：本发明提供新的式（I）化合物其中n为1至4的整数; R和R 1可以相同或不同，为氢，卤素，三氟甲基或C 1 -C 4烷氧基; R2是氢或C1-C4烷基; 及其药学上可接受的盐; 并且其中当R同时为氢时，R 1为氢或卤素且n为1，则R 2为氢或甲基; 和式（IA）其中R 3是卤素的式（IA）及其药学上可接受的盐，其在中枢神经系统（CNS）上是有活性的，可用于治疗作为抗癫痫药，抗帕金森病，神经保护，抗抑郁药，抗痉挛药和催眠药。

8. 发明授权

US5439820A Anti-thrombin polypeptides 失效
标题翻译：抗凝血酶多肽
公开(公告)号：US5439820A
公开(公告)日：1995-08-08
申请号：US264485
申请日：1994-06-23
申请人： Paolo Sarmientos , Philippe De Taxis du Poet , Giampaolo Nitti , Emanuela Scacheri
发明人： Paolo Sarmientos , Philippe De Taxis du Poet , Giampaolo Nitti , Emanuela Scacheri
IPC分类号： A61K35/62 , A61K38/00 , A61K38/55 , A61K38/58 , A61P7/02 , A61P9/00 , C07K7/08 , C07K14/00 , C07K14/01 , C07K14/145 , C07K14/81 , C07K14/815 , C07K19/00 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/15 , C12N15/866 , C12P21/02 , C12R1/19 , C12R1/91 , C12N5/00 , C07H19/00 , C12P21/06
CPC分类号： C12N15/86 , C07K14/005 , C07K14/815 , A61K38/00 , C07K2319/00 , C07K2319/02 , C07K2319/035 , C07K2319/33 , C12N2710/14122 , C12N2710/14143 , C12N2760/20222
摘要： The present invention relates to anti-thrombin polypeptides isolated from the leech Hirudinaria manillensis and to processes for their preparation. The polypeptides of the invention may be modified by way of amino acid extension at either or each end, and may be subjected to post-translational modification. The anti-thrombin polypeptides may be prepared by isolating them from the tissue or secretions of the leech Hirudinaria manillensis but they also may be synthetized by recombinant DNA methods. According to this latter aspect, the invention provides DNA sequences, expression vectors and host cell lines for the recombinant preparation of the polypeptides. The anti-thrombin polypeptides of the invention find an useful application in the treatment of venous thrombosis, vascular shunt occlusion and thrombin-induced disseminated intravascular coagulation.
摘要翻译：本发明涉及从水蛭Hirudinaria manillensis分离的抗凝血酶多肽及其制备方法。本发明的多肽可以在任一个或每个末端通过氨基酸延伸进行修饰，并且可以进行翻译后修饰。抗凝血酶多肽可以通过将它们与水蛭水蛭水蛭的组织或分泌物分离而制备，但也可以通过重组DNA方法合成。根据后一方面，本发明提供用于重组制备多肽的DNA序列，表达载体和宿主细胞系。本发明的抗凝血酶多肽在治疗静脉血栓形成，血管分流闭塞和凝血酶诱导的弥散性血管内凝血中是有用的。

9. 发明授权

US5229383A Piperazine-substituted 1,4-benzoxazine derivatives and their use in treating disorders of the central nervous system 失效
标题翻译：哌嗪取代的1,4-苯并恶嗪衍生物及其在治疗中枢神经系统疾病中的应用
公开(公告)号：US5229383A
公开(公告)日：1993-07-20
申请号：US748221
申请日：1991-08-20
申请人： Mario Varasi , Piero Melloni , Maria A. Cervini , Alberto Bonsignori , Roberto Commisso
发明人： Mario Varasi , Piero Melloni , Maria A. Cervini , Alberto Bonsignori , Roberto Commisso
IPC分类号： C07D265/36 , C07D279/16 , C07D471/10
CPC分类号： C07D471/10 , C07D265/36 , C07D279/16
摘要： The present invention relates to compounds having the following formula (I) ##STR1## wherein X represents --O-- or --S--;each of R and R.sub.1, independently, is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, nitro or trihalo-C.sub.1 -C.sub.6 alkyl;each of R.sub.2 and R.sub.3, independently, is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or phenyl-C.sub.1 -C.sub.6 alkyl; or R.sub.2 and R.sub.3, taken together with the nitrogen atom to which they are linked, form an unsubstituted or substituted, 6-membered, saturated, heteromonocyclic ring optionally containing a further heteroatom chosen from oxygen, sulphur and nitrogen;each of R.sub.4 and R.sub.5, independently, is hydrogen, halogen, nitro, amino or trihalo-C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful in therapy as major tranquilizers e.g., in the management of psychotic disorders.
摘要翻译：本发明涉及具有下式（I）的化合物：其中X表示-O-或-S-; R和R 1各自独立地是氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，氨基，硝基或三卤代-C 1 -C 6烷基; R 2和R 3各自独立地是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或苯基-C 1 -C 6烷基; 或R 2和R 3与它们所连接的氮原子一起形成任选含有另外选自氧，硫和氮的杂原子的未取代或取代的6元饱和的杂单环; R 4和R 5各自独立地是氢，卤素，硝基，氨基或三卤代-C 1 -C 6烷基; 及其药学上可接受的盐。本发明的化合物可用于作为主要镇静剂的治疗，例如在精神病性障碍的治疗中。

10. 发明授权

US5212166A Unsaturated 17.beta.-subsituted 3-carboxy steroids 失效
标题翻译：不饱和的17（BETA） - 使用的3-CARBOXY STEROIDS
公开(公告)号：US5212166A
公开(公告)日：1993-05-18
申请号：US886574
申请日：1992-05-21
申请人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
发明人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
IPC分类号： A61K31/565 , A61K31/56 , A61K31/58 , A61P5/24 , A61P5/28 , A61P13/02 , A61P15/00 , A61P17/00 , A61P17/02 , A61P17/14 , A61P35/00 , A61P43/00 , C07J20060101 , C07J41/00 , C07J43/00
CPC分类号： C07J43/003 , C07J41/0066
摘要： The present invention concerns steroidic 5.alpha.-reductase inhibitors having the following formula (I) ##STR1## wherein Y is oxygen or sulphur;R is a group;a) --OR.sub.4, wherein R.sub.4 is hydrogen or a C.sub.1 -C.sub.6 alkyl group;b) ##STR2## wherein each of R.sub.5 and R.sub.6, independently, is hydrogen or a C.sub.1 -C.sub.6 alkyl group;c) ##STR3## wherein R.sub.7 is hydrogen or a C.sub.1 -C.sub.6 alkyl group and W is a group:(i) ##STR4## wherein R.sub.8 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.6 cycloalky group, a C.sub.6 -C.sub.6 cycloalkylalkyl group, a phenyl group or a benzyl group; or(ii) ##STR5## wherein R.sub.9 is a C.sub.1 -C.sub.6 alkyl group or a C.sub.5 -C.sub.6 cycloalkyl group; or(iii) ##STR6## wherein R.sub.5 and R.sub.6 are as defined above; d) ##STR7## wherein each of R.sub.10 and R.sub.11 is, independently, hydrogen or a C.sub.1 -C.sub.6 alkyl group or taken together with the nitrogen atom to which they are linked form a pentatomic or hexatomic saturated heteromonocyclic ring, optionally containing at least one additional heteroatom selected from oxygen and nitrogen, and n is an integer of 2 to 4;R.sub.1 is hydrogen, a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.6 cycloalkyl group, a C.sub.6 -C.sub.9 cycloalkyalkyl group or an aryl group;each of R.sub.2 and R.sub.3 is, independently, selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl, C.sub.6 -C.sub.9 cycloalkylalkyl and aryl or R.sub.2 and R.sub.3, taken together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic saturated heteromonocyclic ring, optionally containing at least one additional heteroatom selected from oxygen and nitrogen; and the symbol ( ) represents a single or a double bond provided that when it is a double bond the hydrogen in the 5.alpha. position doesn't exist and the pharmaceutically acceptable salts thereof.In view of their 5-.alpha. reductase inhibiting activity the compounds of the invention can be useful for the treatment of androgen dependent conditions.

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