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公开(公告)号：US5981521A
公开(公告)日：1999-11-09
申请号：US191511
申请日：1998-11-13
申请人： Fortuna Haviv , Wesley J. Dwight , Bradley W. Crawford , Rolf E. Swenson , Milan Bruncko , Michele A. Kaminski , Lisa M. Frey , John DeMattei , Jonathan Greer
发明人： Fortuna Haviv , Wesley J. Dwight , Bradley W. Crawford , Rolf E. Swenson , Milan Bruncko , Michele A. Kaminski , Lisa M. Frey , John DeMattei , Jonathan Greer
IPC分类号： C07D217/06 , A61K31/472 , A61K31/4725 , A61K31/4741 , A61K31/55 , A61P13/08 , A61P15/00 , A61P35/00 , C07D217/04 , C07D217/14 , C07D217/16 , C07D217/18 , C07D217/20 , C07D217/22 , C07D217/26 , C07D223/16 , C07D401/06 , C07D401/08 , C07D401/12 , C07D491/04 , C07D491/056 , A61K31/47
CPC分类号： C07D401/06 , C07D217/04 , C07D217/16 , C07D217/18 , C07D217/20 , C07D217/22 , C07D401/12 , C07D491/04
摘要： Tetrahydroisoquinoline derivatives of the formula: ##STR1## or a pharmaceutically acceptable salt, ester, or prodrug thereof, having activity as an LHRH antagonist, as well as pharmaceutical compositions containing the same, and methods for their use and preparation.
摘要翻译： 具有作为LHRH拮抗剂的活性的下式的四氢异喹啉衍生物，或其药学上可接受的盐，酯或前药，以及含有它们的药物组合物及其使用和制备方法。
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公开(公告)号：US5300492A
公开(公告)日：1994-04-05
申请号：US784204
申请日：1991-10-28
申请人： Fortuna Haviv , Jonathan Greer
发明人： Fortuna Haviv , Jonathan Greer
摘要： The present invention relates to novel "pseudo" nonapeptide and decapeptide derivatives of LHRH. More particularly the present invention relates to derivatives of LHRH wherein the nitrogen atom of at least one of the amide bonds has been alkylated.
摘要翻译： 本发明涉及LHRH的新型“假”十肽和十肽衍生物。 更具体地，本发明涉及LHRH的衍生物，其中至少一个酰胺键的氮原子已被烷基化。
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公开(公告)号：US5972898A
公开(公告)日：1999-10-26
申请号：US49458
申请日：1998-03-27
申请人： Daryl R. Sauer , Fortuna Haviv , John Randolph , Nicholas A. Mort , Christopher R. Dalton , Milan Bruncko , Michele A. Kaminski , Bradley W. Crawford , Lisa Marie Frey , Jonathan Greer
发明人： Daryl R. Sauer , Fortuna Haviv , John Randolph , Nicholas A. Mort , Christopher R. Dalton , Milan Bruncko , Michele A. Kaminski , Bradley W. Crawford , Lisa Marie Frey , Jonathan Greer
IPC分类号： A61K31/7042 , A61K31/7048 , A61P5/00 , A61P15/00 , A61P43/00 , C07H17/08 , A61K31/70 , C07H1/00
CPC分类号： C07H17/08
摘要： Disclosed are 3',3'-N-bisdesmethyl-3',3'-N-bis-substituted-6-O-methyl-11-deoxy-11,12-cyclic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.
摘要翻译： 公开了3'，3'-N-双甲基-3'，3'-N-双取代-6-O-甲基-11-脱氧-11,12-环氨基甲酸酯红霉素A衍生物，其是促黄体激素 - 释放激素（LHRH）。 还公开了包含该化合物的药物组合物，使用该化合物的方法及其制备方法。
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公开(公告)号：US6020521A
公开(公告)日：2000-02-01
申请号：US140805
申请日：1998-08-26
申请人： John T. Randolph , Fortuna Haviv , Daryl Sauer , Philip Waid , Charles J. Nichols , Nicholas A. Mort , Christopher R. Dalton , Jonathan Greer
发明人： John T. Randolph , Fortuna Haviv , Daryl Sauer , Philip Waid , Charles J. Nichols , Nicholas A. Mort , Christopher R. Dalton , Jonathan Greer
CPC分类号： A61K31/7048 , C07H17/08
摘要： Disclosed are 3'-N-desmethyl-3'-N-susbstituted-6-O-methyl-11-deoxy-11,12-cyclic carbamate erythrolide A derivatives which are antagonists of luteinizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.
摘要翻译： 公开了作为促黄体激素释放激素（LHRH）的拮抗剂的3'-N-去甲基-3'-N-疑似取代的-6-O-甲基-11-脱氧-11,12-环状氨基甲酸酯类红景天素A衍生物。 还公开了包含该化合物的药物组合物，使用该化合物的方法及其制备方法。
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公开(公告)号：US5955440A
公开(公告)日：1999-09-21
申请号：US49963
申请日：1998-03-27
申请人： Daryl R. Sauer , Fortuna Haviv , John Randolph , Nicholas A. Mort , Christopher R. Dalton , Milan Bruncko , Michele A. Kaminski , Bradley W. Crawford , Lisa Marie Frey , Jonathan Greer
发明人： Daryl R. Sauer , Fortuna Haviv , John Randolph , Nicholas A. Mort , Christopher R. Dalton , Milan Bruncko , Michele A. Kaminski , Bradley W. Crawford , Lisa Marie Frey , Jonathan Greer
IPC分类号： A61K31/7042 , A61K31/7048 , A61K31/7056 , A61P5/24 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00 , C07H17/08 , A61K31/70 , C07H1/00
CPC分类号： C07H17/08
摘要： Disclosed are 3'-N-desmethyl-3'-N-substituted-6-O-methyl-11-deoxy-11,12-cyclic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also disclosed are pharmaceutical compositions comprising the compounds, to methods of using the compounds and to the process of making the same.
摘要翻译： 公开了作为促黄体激素释放激素（LHRH）的拮抗剂的3'-N-去甲基-3'-N-取代-6-O-甲基-11-脱氧-11,12-环状氨基甲酸酯红霉素A衍生物。 还公开了包含该化合物的药物组合物，使用该化合物的方法及其制备方法。
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公开(公告)号：US5140009A
公开(公告)日：1992-08-18
申请号：US548511
申请日：1990-07-10
摘要： The present invention relates to novel LHRH analogs. The LHRH analogs include "pseudo" hexapeptide, heptapeptide, octapeptide and nonapeptide analogs of LHRH, wherein all or some of the amino acids, 1, 2 and 3 have been eliminated and the remaining (2-9), (2-10), (3-9), (3-10), (4-9) or (4-10) peptide is linked to various carboxylic acids which take the place of amino acids 1, 2 or 3 in LHRH.
摘要翻译： 本发明涉及新的LHRH类似物。 LHRH类似物包括LHRH的“假”六肽，七肽，八肽和非肽类似物，其中所有或一些氨基酸1,2和3已被消除，剩余的（2-9），（2-10）， （3-9），（3-10），（4-9）或（4-10）肽与代替LHRH中的氨基酸1,2或3的各种羧酸连接。
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公开(公告)号：US5110904A
公开(公告)日：1992-05-05
申请号：US548512
申请日：1990-07-10
申请人： Fortuna Haviv , Jonathan Greer
发明人： Fortuna Haviv , Jonathan Greer
摘要： The present invention relates to novel "pseudo" nonapeptide and decapeptide derivatives of LHRH. More particularly the present invention relates to derivatives of LHRH wherein the nitrogen atom of at least one of the amide bonds has been alkylated.
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公开(公告)号：US06191115B1
公开(公告)日：2001-02-20
申请号：US09232425
申请日：1999-01-15
IPC分类号： A61K3800
摘要： The present invention relates to a class of heptapeptide analogs of LHRH. These compounds are useful in the treatment of disease conditions which are mediated by reproductive hormones, including benign prostate hyperplasia, prostate tumors, breast and ovaries tumors, cryptorchidism, hirsuitism, gastric motility disorders, dysmenorrhea, and endometriosis.
摘要翻译： 本发明涉及一类LHRH的七肽类似物。 这些化合物可用于治疗由生殖激素介导的疾病状况，包括良性前列腺增生，前列腺肿瘤，乳腺和卵巢肿瘤，隐睾症，多发性，胃动力障碍，痛经和子宫内膜异位症。
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公开(公告)号：US5698522A
公开(公告)日：1997-12-16
申请号：US446809
申请日：1995-06-01
申请人： Fortuna Haviv , Timothy D. Fitzpatrick , Rolf E. Swenson , Charles J. Nichols , Nicholas A. Mort , Jonathan Greer
发明人： Fortuna Haviv , Timothy D. Fitzpatrick , Rolf E. Swenson , Charles J. Nichols , Nicholas A. Mort , Jonathan Greer
摘要： The present invention provides a class of decapeptide compounds which are potent antagonists of LHRH activity and which have the structure A.sup.1 -D.sup.2 -E.sup.3 -G.sup.4 -J.sup.5 -L.sup.6 -M.sup.7 -Q.sup.8 -R.sup.9 -T.sup.10. The compounds of the percent invention are characterized by having an .OMEGA.-amino-functionalized side chain on the D-aminoacyl residue at position 6. The .OMEGA.-amino group of this side chain is further derivatized by the attachment of an extending group which likewise has a terminal amino group which is capped by an acyl group.
摘要翻译： PCT No.PCT / US93 / 11628 Sec。 371日期：1995年6月1日 102（e）1995年6月1日PCT 1993年11月30日PCT公布。 公开号WO94 / 133132 日期：1994年6月23日本发明提供一类作为LHRH活性的有效拮抗剂的十肽化合物，其具有结构A1-D2-E3-G4-J5-L6-M7-Q8-R9-T10。 本发明百分比的化合物的特征在于在第6位的D-氨基酰基残基上具有OMEGA-氨基官能化侧链。该侧链的OMEGA-氨基通过连接一个延伸基团 被酰基封端的末端氨基。
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公开(公告)号：US06297354B1
公开(公告)日：2001-10-02
申请号：US09373180
申请日：1999-08-12
申请人： Fortuna Haviv , Wesley Dwight , Jonathan Greer
发明人： Fortuna Haviv , Wesley Dwight , Jonathan Greer
IPC分类号： C07K1600
摘要： The present invention relates to a class of pentapeptide analogs of LHRH. These compounds are useful in the treatment of disease conditions which are mediated by reproductive hormones, including benign prostate hyperplasia, prostate tumors, breast and ovaries tumors, cryptorchidism, hirsuitism, gastric motility disorders, dysmenorrhea, and endometriosis.
摘要翻译： 本发明涉及一类LHRH的五肽类似物。 这些化合物可用于治疗由生殖激素介导的疾病状况，包括良性前列腺增生，前列腺肿瘤，乳腺和卵巢肿瘤，隐睾症，多毛症，胃动力障碍，痛经和子宫内膜异位症。
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