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11.发明申请Method and intermediates for preparing 2-alkoxy and 2-aryloxy estrogen compounds 审中-公开制备2-烷氧基和2-芳氧基雌激素化合物的方法和中间体公开(公告)号：US20110130581A1
公开(公告)日：2011-06-02
申请号：US12929644
申请日：2011-02-07
申请人： Paolo Lombardi , Franco Buzzetti
发明人： Paolo Lombardi , Franco Buzzetti
CPC分类号： C07J1/0059 , C07J1/007 , C07J41/0005
摘要： The present invention relates to 2-alkoxy and 2-aryloxyestrogen compounds, and the intermediate compounds prepared during the preparation thereof, which intermediate compounds are useful intermediates in the preparation of certain physiologically active compounds.
摘要翻译： 本发明涉及2-烷氧基和2-芳氧基雌激素化合物及其在制备过程中制备的中间体化合物，该中间体化合物是制备某些生理活性化合物的有用中间体。
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12.发明申请Process for the synthesis of distamycin and derivatives thereof using 1-methyl-4-formylamino-2-pyrrolecarbonyl chloride iteratively as an intermediate 有权使用1-甲基-4-甲酰氨基-2-吡咯羰酰氯作为中间体反复合成霉素及其衍生物的方法公开(公告)号：US20070060523A1
公开(公告)日：2007-03-15
申请号：US10557424
申请日：2004-05-28
申请人： Paolo Lombardi
发明人： Paolo Lombardi
IPC分类号： A61K38/10 , A61K38/08 , A61K38/05 , A61K38/06 , A61K31/4025 , C07D403/14
CPC分类号： C07D207/34
摘要： A process for the total synthesis of Distamycin, and synthetic poly-(4aminopyrrole-2-carboxamide) congeners thereof, using 1-methyl-4-forinylamino-2-pyrrolecarbonyl chloride iteratively as an intermediate, is provided. The process finds application for both in solution and solid support synthetic technologies.
摘要翻译： 提供了使用1-甲基-4-戊酰氨基-2-吡咯烷酰氯作为中间体的方法来全面合成雷霉霉素及其合成的聚（4-氨基吡咯-2-甲酰胺）同系物。 该过程在解决方案和固体支持合成技术中都得到应用。
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公开(公告)号：US5130472A
公开(公告)日：1992-07-14
申请号：US608505
申请日：1990-11-02
申请人： Franco Buzzetti , Angelo Crugnola , Paolo Lombardi
发明人： Franco Buzzetti , Angelo Crugnola , Paolo Lombardi
IPC分类号： A61K31/165 , A61P43/00 , C07C231/12 , C07C231/24 , C07C233/18
CPC分类号： C07C233/18 , C07C231/12
摘要： The present invention relates to a new process for the preparation of Erbstatin and Erbstatin analogs, which can be represented by the following formula (I) ##STR1## wherein R is hydrogen, a lower alkyl or a lower alkanoyl group;n is an integer of 1 to 3;A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --;R.sub.1 is hydrogen or a lower alkyl group, andR.sub.2 is a hydrogen or halogen atom.
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公开(公告)号：US4904650A
公开(公告)日：1990-02-27
申请号：US225674
申请日：1988-07-26
IPC分类号： A61K31/565 , A61P13/02 , A61P15/00 , A61P35/00 , C07J1/00
CPC分类号： C07J1/0011
摘要： The invention relates to 6-alkylidenadrosta-1,4-diene-3,17-dione derivatives, having the following general formula ##STR1## wherein each of R and R.sub.2, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl, which are useful in therapy, in particular in the treatment of hormone-dependent cancers.
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15.发明申请Method and intermediates for preparing 2-alkoxy and 2-aryloxy estrogen compounds 有权制备2-烷氧基和2-芳氧基雌激素化合物的方法和中间体公开(公告)号：US20100099141A1
公开(公告)日：2010-04-22
申请号：US12285901
申请日：2008-10-16
申请人： Paolo Lombardi , Franco Buzzetti
发明人： Paolo Lombardi , Franco Buzzetti
CPC分类号： C07J1/0059 , C07J1/007 , C07J41/0005
摘要： The present invention relates to a method for preparing 2-alkoxy and 2-aryloxyestrogen compounds, and the intermediate compounds prepared during the use of this method, which intermediate compounds are useful intermediates in the preparation of certain physiologically active compounds.
摘要翻译： 本发明涉及一种制备2-烷氧基和2-芳氧基雌激素化合物的方法，以及在该方法的使用中制备的中间体化合物，该中间体化合物是制备某些生理活性化合物的有用中间体。
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16.发明授权6- or 7-methylenandrosta-1,4-diene-3,17-dione derivatives and process for their preparation 失效6-或7-亚甲基雄甾-1,4-二烯-3,17-二酮衍生物及其制备方法
公开(公告)号：US4824830A
公开(公告)日：1989-04-25
申请号：US070685
申请日：1987-07-07
CPC分类号： C07J21/008 , C07J1/0011 , C07J71/001
摘要： The invention relates to new 6- or 7-methylenandrosta-1,4-diene-3,17-diones of the following formula ##STR1## wherein R is hydrogen or fluorine; R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or halogen; one of R.sub.3 and R.sub.4 is .dbd.CH.sub.2 and the other is hydrogen or C.sub.1 -C.sub.4 alkyl, and when R.sub.3 is .dbd.CH.sub.2, at least one of R and R.sub.4 is other than hydrogen; and the symbol ##STR2## represents a double bond and the symbol ##STR3## represents a single bond when R.sub.3 is .dbd.CH.sub.2 or the symbol ##STR4## represents a single bond and the symbol ##STR5## represents a double bond when R.sub.4 is .dbd.CH.sub.2, which are useful in therapy, in particular as anti-cancer agents.
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17.发明授权6-Alkylidene 10 .beta.-alkynylestrene derivatives and pharmaceutical methods for their use 失效6-亚烷基10β-炔雌醇衍生物及其使用的药物方法
公开(公告)号：US4808578A
公开(公告)日：1989-02-28
申请号：US941348
申请日：1986-12-15
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00 , C07J21/00 , C07J41/00 , C07J71/00 , C10L1/32 , A61K31/56
CPC分类号： C07J1/0011 , C07J1/0022 , C07J21/006 , C07J41/0011 , C07J41/0027 , C07J71/001
摘要： The invention relates to 6-substituted 10.beta.-alkynylestrene derivatives wherein the 6 substituent is amino, azido, halogen or an alkylidene group and to corresponding 6,7-dihalo analogs.The invention provides also a process for the preparation of the above compounds and pharmaceutical compositions containing same.The compounds of the invention are useful aromatase inhibitors and can be used, e.g., in the treatment of hormone-dependent tumors and prostatic hyperplasia.
摘要翻译： 本发明涉及6-取代的10β-炔雌醇衍生物，其中6个取代基是氨基，叠氮基，卤素或亚烷基，以及相应的6,7-二卤代类似物。 本发明还提供了制备上述化合物的方法和含有它们的药物组合物。 本发明的化合物是有用的芳香酶抑制剂，可用于例如激素依赖性肿瘤和前列腺增生的治疗。
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18.发明申请Use of poly-amminopyrrolecarboxamides alone or in combination with a cyclodextrin in the prophylaxis and treatment of animal parasitosis 审中-公开单独或与环糊精组合使用聚琥珀酰亚胺酰胺在预防和治疗动物寄生虫病公开(公告)号：US20060069033A1
公开(公告)日：2006-03-30
申请号：US10538838
申请日：2004-05-13
申请人： Paolo Lombardi
发明人： Paolo Lombardi
IPC分类号： A61K38/06 , A61K38/05 , A61K38/04 , A61K31/4025
CPC分类号： A61K9/0095 , A61K31/4025 , A61K38/06 , A61K47/40 , Y02A50/491
摘要： Use of distamycin, analogues and/or derivatives thereof in the manufacture of a pharmaceutical composition having activity against endoparasitosis in animals.
摘要翻译： 在用于制造具有抗动物内寄生虫病活性的药物组合物中使用雷霉素，其类似物和/或衍生物。
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公开(公告)号：US4970327A
公开(公告)日：1990-11-13
申请号：US294016
申请日：1989-01-06
申请人： Antonio Longo , Paolo Lombardi
发明人： Antonio Longo , Paolo Lombardi
摘要： The invention relates to a new process for the preparation of know aromatase inhibitors of the following formula (I) ##STR1## wherein each of R.sub.1 R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; andR.sub.4 is hydrogen or fluorine;the process comprising submitting to Mannich reaction a compound of formula (II) ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined above and R is a lower alkyl group, and then dehydrogenating the respective 6-methylene-3-oxo-.DELTA..sup.4 -steroid derivative thus obtained, by methods known per se.
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20.发明授权Process for the preparation of methylene derivatives of androsta-1,4-diene-3,17-dione 失效雄甾-1,4-二烯-3,17-二酮的亚甲基衍生物的制备方法
公开(公告)号：US4876045A
公开(公告)日：1989-10-24
申请号：US242854
申请日：1988-09-12
申请人： Antonio Longo , Paolo Lombardi
发明人： Antonio Longo , Paolo Lombardi
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00
CPC分类号： C07J1/0011 , C07J1/0022
摘要： The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula ##STR1## wherein each of R.sub.1 and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl andR.sub.4 is hydrogen or fluorine; the process comprising subjecting to Mannich reaction a compound of formula ##STR2## wherein R.sub.1,R.sub.2,R.sub.3 and R.sub.4 are as defined above, and then oxidizing the respective 6-methylene derivative thus obtained by methods known per se.
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