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1. 发明授权

US4552864A Gonadoliberin derivatives process for the preparation and pharmaceutical compositions thereof 失效
标题翻译：用于制备其性腺素的衍生物方法及其药物组合物
公开(公告)号：US4552864A
公开(公告)日：1985-11-12
申请号：US608261
申请日：1984-05-04
申请人： Ferenc Antoni , Judit Erchegyi , Aniko Horvath , Gyorgi Keri , Imre Mezo , Karoly Nikolics , Janos Seprodi , Andras Szell , Balazs Szoke , Istvan Teplan
发明人： Ferenc Antoni , Judit Erchegyi , Aniko Horvath , Gyorgi Keri , Imre Mezo , Karoly Nikolics , Janos Seprodi , Andras Szell , Balazs Szoke , Istvan Teplan
IPC分类号： A61K38/00 , C07K7/23 , C07K14/00 , C07K14/575 , A61K37/00
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： The invention relates to new gonadoliberin derivatives of the formula (I)Glp-His-Trp-Ser-Tyr-X-Leu-Arg-Pro-Y, (I)whereinY represents a glycine-amide group or an -NH-alkyl group having 1 to 4 carbon atoms in the alkyl moiety,X stands for a D-thyroxyl, D-thyronyl or D-4-chlorophenylalanyl group,and acid addition salts and metal complexes thereof.The new nona- and decapeptide derivatives have an excellent luteinizing and folliculus stimulating hormone releasing activity, and they can therefore be used as active ingredients in pharmaceutical compositions for human or veterinary application.
摘要翻译： PCT No.PCT / HU83 / 00028 Sec。 371日期1984年1月11日 102（e）日期1984年1月11日PCT提交1983年5月25日PCT公布。出版物WO83 / 04250 1983年12月8日，本发明涉及式（I）Glp-His-Trp-Ser-Tyr-X-Leu-Arg-Pro-Y，（I）的新的性腺激肽衍生物，其中Y代表甘氨酰胺基团或在烷基部分具有1至4个碳原子的-NH-烷基，X表示D-甲醛，D-甲苯甲酰或D-4-氯苯丙氨酰基，以及其酸加成盐和金属络合物。新的非 - 和十肽衍生物具有优异的促黄体激素和促卵泡激素释放活性，因此它们可以用作用于人或兽医应用的药物组合物中的活性成分。

2. 发明授权

US4647553A Gonadoliberin derivatives and process for the preparation thereof 失效
标题翻译： Gonadoliberin衍生物及其制备方法
公开(公告)号：US4647553A
公开(公告)日：1987-03-03
申请号：US684065
申请日：1984-12-20
申请人： Tamas Gulyas , Aniko Horvath , Gyorgy Keri , Karoly Nikolics , Balazs Szoke , Istvan Teplan
发明人： Tamas Gulyas , Aniko Horvath , Gyorgy Keri , Karoly Nikolics , Balazs Szoke , Istvan Teplan
IPC分类号： C07K14/575 , A61K38/00 , A61K38/08 , A61K38/24 , A61P5/00 , C07K7/06 , C07K7/23 , A61K37/43 , C07K7/20
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： The invention relates to gonadoliberin derivatives of the general formula (I)Glp--His--Trp--Ser--Tyr--X.sub.1 --X.sub.2 --X.sub.3 --Pro--X.sub.4whereinX.sub.1 is a glycyl group or a D-isomer of any natural or synthetic amino acid group,X.sub.2 represents an L-amino acid group having 1 to 4 carbon atoms in the side chain, L-phenyl-alanyl or L-tryptophyl group,X.sub.3 represents an L-amino acid group having a C.sub.1-4 alkyl or C.sub.2-4 alkanoyl-amide side chain, andX.sub.4 is a glycine amide or a C.sub.1-4 alkyl amide group,with the proviso that if X.sub.1 stands for a group other than glycyl and X.sub.2 is a tryptophyl group then X.sub.3 may not be leucyl, and the addition salts formed with therapeutically useable acids and complexes thereof. Furthermore the invention relates to a process for preparing these compounds.The new gonadoliberin derivatives can be effectively used for the reproduction process of fish, birds and mammals.
摘要翻译：本发明涉及通式（I）Glp-His-Trp-Ser-Tyr-X1-X2-X3-Pro-X4的性腺蛋白衍生物，其中X1是任何天然或合成氨基酸的甘氨酰基或D-异构体基团，X2表示侧链具有1〜4个碳原子的L-氨基酸基，L-苯丙氨酰或L-色氨酰基，X3表示具有C1-4烷基或C2-4的L-氨基酸烷酰基酰胺侧链，X4为甘氨酸酰胺或C1-4烷基酰胺基，条件是如果X1表示除甘氨酰以外的基团，X2表示色氨酸基，则X3不可以是亮氨酰基，加成与治疗上可用的酸及其复合物形成的盐。此外，本发明涉及一种制备这些化合物的方法。新的促性腺激肽衍生物可以有效地用于鱼，鸟和哺乳动物的繁殖过程。

3. 发明授权

US4647552A Process for obtaining ready for fertilization sexual products from sexually mature fish 失效
标题翻译：从性成熟鱼获得受精性产品的准备过程
公开(公告)号：US4647552A
公开(公告)日：1987-03-03
申请号：US684066
申请日：1984-12-20
申请人： Tamas Gulyas , Aniko Horvath , Gyorgy Keri , Karoly Nikolics , Balazs Szoke , Istvan Teplan
发明人： Tamas Gulyas , Aniko Horvath , Gyorgy Keri , Karoly Nikolics , Balazs Szoke , Istvan Teplan
IPC分类号： A01K61/00 , A61K38/00 , C07K7/06 , C07K7/23 , C07K14/575 , A61K37/24
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： The invention relates to a process for obtaining ready-for-fertilization sexual products from sexually mature fish in a period independent of their natural spawning season, in which actual stage of ripening is determined by probing of sexual products [sperm or eggs], fish not yet ripe for ovulation are separated from ripe fish, compounds of hormonal effect are administered to fish, and after the ovulation sexual products are obtained from the fish or from their environment.In the process according to the invention a nonapeptide-C.sub.1-4 -alkyl-amide or a decapeptide amide of the general formula (I),Glp-His-Trp-Ser-Tyr-X.sub.1 -X.sub.2 -X.sub.3 -Pro-X.sub.4 (I)whereinX.sub.1 is a glycyl group or a D-isomer of any natural or synthetic amino acid group,X.sub.2 represents an L-amino acid group having 1 to 4 carbon atoms in the side chain, L-phenyl-alanyl or L-tryptophyl group,X.sub.3 represents an L-amino acid group having a C.sub.1-4 alkyl or C.sub.2-4 alkyl-amide side chain,X.sub.4 is a glycine-amide or a C.sub.1-4 alkyl-amide group,as well as salts or metal-complexes of these compounds are administered to fish in a dose of 0.1 .mu.g to 5 mg, and to fish not yet ripe for ovulation the above quantities are administered in at least 2 but at most 12 portions, wherein the last dose used is at least the same or advantageously at least 1.5 times higher than the previous one.The process according to the invention makes possible the obtaining of ripe sexual products ready for natural or artificial fertilization from any fish species in any period, independently of the natural spawning season of fish.
摘要翻译：本发明涉及一种独立于自然产卵季节从性成熟鱼获得即食受精性产品的方法，其中成熟的实际阶段是通过探查性产品[精子或卵]，鱼类成熟的排卵与成熟的鱼分离，激素作用的化合物被施用于鱼，并且在排卵之后，从鱼或其环境获得性产物。在根据本发明的方法中，通式（I）的Glc-His-Trp-Ser-Tyr-X1-X2-X3-Pro-X4（I）的非肽-C1-4-烷基酰胺或十肽酰胺）其中X1是任何天然或合成氨基酸基团的甘氨酰基或D-异构体，X2表示侧链中具有1至4个碳原子的L-氨基酸基团，L-苯丙氨酰基或L-色氨酸基团，X3表示具有C1-4烷基或C2-4烷基 - 酰胺侧链的L-氨基酸基，X4是甘氨酸 - 酰胺或C1-4烷基 - 酰胺基，以及盐或金属络合物这些化合物以0.1μg至5mg的剂量施用于鱼，并且为了排卵尚未成熟，上述量以至少2但最多12份施用，其中使用的最后剂量至少相同或有利地比前一个高至少1.5倍。根据本发明的方法使得可以在任何时间段内获得准备好从任何鱼类进行天然或人造受精的成熟性产品，而与鱼的天然产卵季节无关。

4. 发明授权

US5480870A Tumor growth-inhibiting somatostatin analogues, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：肿瘤生长抑制性生长抑素类似物，含有它们的药物组合物及其制备方法
公开(公告)号：US5480870A
公开(公告)日：1996-01-02
申请号：US233558
申请日：1994-04-26
申请人： Gyorgy Keri , Imre Mezo , Aniko Horvath , Zsolt Vadasz , Istvan Teplan , Agnes Balogh , Orsolya Csuka , Gyongyi Bokonyi , Balas Szoke , Judit Horvath , Miklos Idei , Janos Seprodi
发明人： Gyorgy Keri , Imre Mezo , Aniko Horvath , Zsolt Vadasz , Istvan Teplan , Agnes Balogh , Orsolya Csuka , Gyongyi Bokonyi , Balas Szoke , Judit Horvath , Miklos Idei , Janos Seprodi
IPC分类号： A61K38/04 , A61K38/00 , A61P35/00 , C07K1/04 , C07K1/113 , C07K7/02 , C07K7/06 , C07K14/575 , C07K14/655
CPC分类号： C07K7/02 , C07K14/6555 , A61K38/00
摘要： The invention relates to tumor-inhibiting heptapeptide and octapeptide amide derivatives and to a method of treating mammals, including men, suffering from tumors or from the excessive secretion of insulin, glucagon or growth hormone using these compounds.
摘要翻译：本发明涉及肿瘤抑制七肽和八肽酰胺衍生物以及一种治疗患有肿瘤的哺乳动物或包括男性在内的哺乳动物或使用这些化合物过量分泌胰岛素，胰高血糖素或生长激素的方法。

5. 发明授权

US5023322A Analogs of growth hormone releasing factor (GRF) and a method for the preparation thereof 失效
标题翻译：生长激素释放因子（GRF）的类似物及其制备方法
公开(公告)号：US5023322A
公开(公告)日：1991-06-11
申请号：US400587
申请日：1989-08-30
申请人： Magdolna Kovacs , Judit Horvath , Sandor Vigh , Imre Mezo , Istvan Teplan , Balazs Szoke , Janos Seprodi , Zsolt Vadasz , Edit Hegedus , Gabor Makara , Gyorgy Rappay
发明人： Magdolna Kovacs , Judit Horvath , Sandor Vigh , Imre Mezo , Istvan Teplan , Balazs Szoke , Janos Seprodi , Zsolt Vadasz , Edit Hegedus , Gabor Makara , Gyorgy Rappay
IPC分类号： A61K38/00 , C07K14/60
CPC分类号： C07K14/60 , A61K38/00
摘要： The invention relates to new peptides of the formula ##STR1## wherein R.sup.2 represents Ala or D-Ala,R.sup.11 represents Arg or D-Arg,R.sup.13 represents Val or Ile,R.sup.15 represents Gly, Leu, Phe or a valence bond,R.sup.27 represents Met or Nle,R.sup.28 represents Ser, D-Ser or Asn, andY represents OH or NH.sub.2,and to salts thereof. These compounds stimulate the release of growth hormone and can be used in the therapy as well as for veterinary or animal husbandry purposes.
摘要翻译：本发明涉及式H-Tyr-R2-Asp-Ala-Ile-Phe-Thr-Asn-Ser-（I）-Tyr-R11-Lys-R13-Leu-R15-Gln-Leu-Ser -Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile- + TR -R27-R28-Arg-Gaba-Y，其中R2表示Ala或D-Ala，R11表示Arg或D-Arg，R13表示 Val或Ile，R 15表示Gly，Leu，Phe或价键，R 27表示Met或Nle，R 28表示Ser，D-Ser或Asn，Y表示OH或NH 2，以及其盐。这些化合物刺激生长激素的释放，并可用于治疗以及兽医或畜牧业。

6. 发明授权

US4751215A Process for increasing the sexual activity of birds and useful domestic mammals and for preparing spermatozoa suitable to their propagation 失效
标题翻译：增加鸟类和有用的家养哺乳动物的性活动和准备适合其繁殖的精子的过程
公开(公告)号：US4751215A
公开(公告)日：1988-06-14
申请号：US852217
申请日：1986-04-15
申请人： Janos Seprodi , Zsolt Vadasz , Peter Peczely , Istvan Teplan , Judit Erchegyi , Tibor Muray , Istvan Gyorvari
发明人： Janos Seprodi , Zsolt Vadasz , Peter Peczely , Istvan Teplan , Judit Erchegyi , Tibor Muray , Istvan Gyorvari
IPC分类号： A61K38/04 , A61D19/00 , A61K38/00 , A61K38/22 , A61P15/00 , C07K7/23 , A61K37/24
CPC分类号： C07K7/23 , A61D19/00 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： The invention relates to a process for increasing the sexual activity of birds and useful domestic mammals and for preparing spermatozoa suitable to their propagation. The process of the invention comprises treating sexually mature male birds or useful domestic mammals at least twice and at most four times with 0.1 to 5 .mu.g/kg of body weight of a compound of the general formula (I),Glp-His-Trp-Ser-Tyr-X.sub.1 -Leu-Arg-Pro-X.sub.4 (I)whereinX.sub.1 stands for a glycyl group, a natural or synthetic aminoacid or aminoacid derivative of D configuration, an -Asp-Q group of L configuration, wherein Q is attached to the .alpha.-carbonyl moiety of the aspartyl group and represents a C.sub.1-5 alkylamide, an arylamide, a C.sub.1-4 alkoxy or a benzyloxy group; andX.sub.4 stands for a glycylamide or a C.sub.1-4 alkylamide group,while keeping a pause of at least 30 hours and at most 72 hours between the consecutive treatments.The process of the invention can mainly be used in such large-scale breedings, where artificial insemination is employed but it can be used also for any domestic bird or cought wild-fowl and ornamental bird as well as useful domestic mammal under the conditions of the natural reproduction or artificial insemination.
摘要翻译：本发明涉及增加鸟类和有用的家养哺乳动物的性活性以及制备适于其繁殖的精子的方法。本发明的方法包括用0.1至5μg/ kg体重的通式（I）的化合物，Glp-His-Trp，将性成熟的雄性鸟类或有用的家用哺乳动物处理至少两次，最多四次 -Ser-Tyr-X1-Leu-Arg-Pro-X4（I）其中X1表示甘氨酰基，D构型的天然或合成氨基酸或氨基酸衍生物，L构型的-Asp-Q基团，其中Q为连接到天冬氨酰基的α-羰基部分，并且表示C1-5烷基酰胺，芳基酰胺，C1-4烷氧基或苄氧基; 并且X 4代表甘氨酰酰胺或C 1-4烷基酰胺基团，同时在连续处理之间保持至少30小时和至多72小时的停顿。本发明的方法主要用于大规模种植，其中人工授精使用，但也可用于任何家禽或被驯养的野禽和观赏鸟以及有用的国内哺乳动物自然繁殖或人工授精。

7. 发明授权

US4948873A Gonadoliberine analogues of high activity 失效
标题翻译：活性高甘露醇类似物
公开(公告)号：US4948873A
公开(公告)日：1990-08-14
申请号：US921770
申请日：1986-10-21
申请人： Janos Seprodi , Istvan Teplan , Istvan Schon , Judit Erchegyi , Zsolt Vadasz , Olga N. nee Kuprina , Tamas Szirtes , Andras Selmezci , Bela Kanyicska
发明人： Janos Seprodi , Istvan Teplan , Istvan Schon , Judit Erchegyi , Zsolt Vadasz , Olga N. nee Kuprina , Tamas Szirtes , Andras Selmezci , Bela Kanyicska
IPC分类号： A61K38/22 , A61K38/00 , A61K38/04 , A61P5/00 , C07K7/23 , C07K14/575
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80
摘要： The present invention relates to novel gonadoliberine analogues of formula IGlp-His-Trp-Ser-X-W-Leu-Arg-Pro-Y (I)whereinX is Phe-, Tyr (3,5-.sup.3 H) or 3,5-dibromo-tyrosyl,W is Asu or Asp OR, wherein R is alkyl having 1 to 6 carbon atoms or phenyl or phenyl (alkyl having 1 to 4 carbon atoms), which latter two groups may optionally be substituted by nitro or one or more halogen atoms, andY is glycinamide, aza-glycinamide or alkylamino having 1 to 4 carbon atoms,and acid-addition salts thereof, processes for preparing the same and pharmaceutical compositions comprising the same.The novel compounds have an influence on the sexual processes.
摘要翻译：本发明涉及式I Glp-His-Trp-Ser-XW-Leu-Arg-Pro-Y（I）的新型性腺素类似物，其中X为Phe-，Tyr（3,5-3H）或3,5- 二溴 - 酪氨酰基，W是Asu或Asp OR，其中R是具有1至6个碳原子的烷基，或苯基或苯基（具有1至4个碳原子的烷基），后两个基团可任选地被硝基或一个或多个卤素原子，Y是甘氨酰胺，氮杂 - 甘氨酰胺或具有1至4个碳原子的烷基氨基，及其酸加成盐，其制备方法以及含有它们的药物组合物。新化合物对性过程有影响。

8. 发明授权

US4600705A Gonadoliberin derivatives containing a .beta.-aspartyl group, a process for the preparation thereof and pharmaceutical preparations containing them 失效
标题翻译：含有β-天冬氨酰基的生殖霉素衍生物，其制备方法和含有它们的药物制剂
公开(公告)号：US4600705A
公开(公告)日：1986-07-15
申请号：US594880
申请日：1984-03-29
申请人： Janos Seprodi , Istvan Teplan , Imre Mezo , Judit rchegyi
发明人： Janos Seprodi , Istvan Teplan , Imre Mezo , Judit rchegyi
IPC分类号： C07K14/575 , A61K38/00 , A61K38/04 , A61P5/00 , C07K5/02 , C07K7/02 , C07K7/06 , C07K7/23 , A61K37/02
CPC分类号： C07K7/02 , C07K5/0215 , C07K7/23 , A61K38/00 , Y10S930/13
摘要： The invention relates to novel gonadoliberine derivatives of the general formula (I) ##STR1## wherein X represents an --O--R group wherein R is a benzyl group or a C.sub.1-4 alkyl group, an ##STR2## group wherein R1 and R2 independently stand for hydrogen, a C.sub.1-5 alkyl, aryl, aryl-C.sub.1-2 -alkyl, morpholino, 1-indolinyl or 1-pyrrolidinyl group,Y is a glycine amide or a C.sub.1-4 -alkyl-amide group,the addition salts thereof formed with acids used in therapy and complexes thereof as well as pharmaceutical compositions containing them, furthermore to a process for the preparation of the above compounds.The reproductive processes of vertebrates can be advantageously influenced with the compounds of general formula (I).
摘要翻译：本发明涉及通式（I）的新颖的性那诺贝因衍生物，其中X代表-OR基团，其中R是苄基或C1-4烷基，其中R1和R2 独立地代表氢，C 1-5烷基，芳基，芳基-C 1-2 - 烷基，吗啉代，1-二氢吲哚基或1-吡咯烷基，Y是甘氨酰胺或C1-4烷基 - 酰胺基，其与治疗中使用的酸形成的盐及其复合物以及含有它们的药物组合物，以及制备上述化合物的方法。脊椎动物的繁殖过程可以有利于通式（I）的化合物的影响。

9. 发明授权

US06297216B1 Compounds for reversing drug resistance 失效
标题翻译：用于逆转耐药性的化合物
公开(公告)号：US06297216B1
公开(公告)日：2001-10-02
申请号：US08737255
申请日：1997-02-19
申请人： Balazs Sarkadi , Janos Seprodi , Orsolya Csuka , Maria Magocsi , Imre Mezo , Istvan Palyi , Istvan Teplan , Zsolt Vadasz , Borbala Vincze
发明人： Balazs Sarkadi , Janos Seprodi , Orsolya Csuka , Maria Magocsi , Imre Mezo , Istvan Palyi , Istvan Teplan , Zsolt Vadasz , Borbala Vincze
IPC分类号： A61K3804
CPC分类号： C07K5/06113 , A61K38/00 , C07K5/0215 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06104
摘要： The invention features novel peptide derivatives called Reversins, and provides for their use in a method of reducing the activity of the multi-drug transporter protein MDR1 in order to overcome multidrug resistance in a mammal. The peptide derivatives are of the formula (I) X1n-X2-X3(X4)n-X5, wherein n is 0 or 1, and each n is the same or different; X1 is BOC, BOC-Asu, Z-Asu, benzyloxycarbonyl, Glu(OBzl)-OBzl, Trp-OMe, Trp-Phe-OMe, Phe-Trp-OMe, Phe-Phe-OtBu, Trp-Trp-OtBu, indoloacetyl, benzoyl, an alkylanine of 1-4 carbons, dibenzylamide, tryptamide, 1-amino-adamantine, aminomethylcyclohexane, indoline, phenylethylamide or dicyclohexylamide; X2 is Glu(OBzl), Asp(OBzl), succinyl, O,O-dibenzoyltartaroyl, diphenoyl, muconyl, Thx, Cpa, Asu, Nal, Pen, Phg, Dbt, Lys(BOC), Lys(Z), Cys(Bzl), Thr(Bzl), Glu(OtBu), tert.-Leu, Leu, Nle, Pro, Phe, Tyr(Bzl), or Ser(Bal); X3 is Asp, Asu, Lys, Glu, Trp, Thx, Cpa, Nal, Pen, Phg, Dbt, Glu(OtBu), tert.-Leu, Leu, Nle, Pro, Tyr, Phe, or Tyr(Bzl); X4 is BOC-Glu(OBzl), Glu(OBzl), Asu, OBzl, Bzl, BOC, BOC-Lys(BOC), Z-Glu(OtBu), Asp(OBzl), Asp(OBz)-OBzl, benzyloxycarbonyl, O-(cyclo-hexyl), fluorenylmethyl ester, Glu(OtBu), Glu(OtBu)-OBzl, 1-amino-adamantine, aminomethylcyclohexane, indoline, phenylethylarnide, or dicyclohexylamide; and X5 is OMe, OBzl, OtBu, Phe-OMe, -O-(cyclohexyl), Trp-OMe, (chlorophenyl)-isobutylamide, fluorenylmethyl ester, ONp, 1-aminoadamantane, aminomethylcyclohexane, indoline, phenylethylamide, or dicyclohexylamide.
摘要翻译：本发明的特征在于新颖的肽衍生物，称为Reversins，并且它们用于降低多药物转运蛋白MDR1活性的方法，以克服哺乳动物的多药耐药性。肽衍生物具有式（I）X1n-X2-X3（X4）n-X5，其中n为0或1，并且各个n相同或不同; X1是BOC，BOC-Asu，Z-Asu，苄氧基羰基，Glu（OBzl）-OBz1，Trp-OMe，Trp-Phe-OMe，Phe-Trp-OMe，Phe-Phe-OtBu，Trp-Trp-OtBu，吲哚乙酰，苯甲酰基，1-4个碳的烷基烷基，二苄酰胺，胰蛋白酶，1-氨基 - 金刚烷，氨基甲基环己烷，二氢吲哚，苯乙酰胺或二环己基酰胺; X2是Glu（OBzl），Asp（OBzl），琥珀酰基，O，O-二苯甲酰基联苯酰基，二苯甲酰基，粘蛋白，Thx，Cpa，Asu，Nal，Pen，Phg，Dbt，Lys（BOC），Lys（Z） Bzl），Thr（Bzl），Glu（OtBu），叔-Leu，Leu，Nle，Pro，Phe，Tyr（Bzl）或Ser（Bal） X3是Asp，Asu，Lys，Glu，Trp，Thx，Cpa，Nal，Pen，Phg，Dbt，Glu（OtBu），叔-Leu，Leu，Nle，Pro，Tyr，Phe或Tyr（Bzl）; X4是BOC-Glu（OBzl），Glu（OBz1），Asu，OBz1，Bzl，BOC，BOC-Lys（BOC），Z-Glu（OtBu），Asp（OBzl），Asp（OBz） O-（环己基），芴基甲基酯，Glu（OtBu），Glu（OtBu）-OBzl，1-氨基 - 金刚烷，氨基甲基环己烷，二氢吲哚，苯乙基胺或二环己基酰胺; 和X5是OMe，OBz1，OtBu，Phe-OMe，-O-（环己基），Trp-OMe，（氯苯基） - 异丁基酰胺，芴甲基酯，ONp，1-氨基金刚烷，氨基甲基环己烷，二氢吲哚，苯乙酰胺或二环己基酰胺。

10. 发明申请

US20060189539A1 Novel GnRH analogues with antitumour effects and pharmaceutical compositions thereof 审中-公开
标题翻译：具有抗肿瘤作用的新型GnRH类似物及其药物组合物
公开(公告)号：US20060189539A1
公开(公告)日：2006-08-24
申请号：US10695382
申请日：2003-10-28
申请人： Sandor Lovas , Richard Murphy , Geza Toth , Adrienn Kalnay , Dezso Gaal , Istvan Palyi , Gizella Turi , Borbala Vincze , Imre Mezom , Henrietta Tanai , Zsolt Vadasz , Istvan Teplan , Janos Seprodi , Edit Szabo , Janos Pato , Melinda Mora
发明人： Sandor Lovas , Richard Murphy , Geza Toth , Adrienn Kalnay , Dezso Gaal , Istvan Palyi , Gizella Turi , Borbala Vincze , Imre Mezom , Henrietta Tanai , Zsolt Vadasz , Istvan Teplan , Janos Seprodi , Edit Szabo , Janos Pato , Melinda Mora
IPC分类号： A61K38/09
CPC分类号： C07K7/23
摘要： The present invention provides peptides and pharmacologically active compounds including gonadotropin-releasing hormone (GnRH) analogues according to formulas of the invention, wherein the compounds show an antitumour effect. The invention additionally provides compositions including these peptides and compounds.
摘要翻译：本发明提供了包括根据本发明的配方的促性腺激素释放激素（GnRH）类似物的肽和药理活性化合物，其中化合物显示出抗肿瘤作用。本发明另外提供包括这些肽和化合物的组合物。

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