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1. 发明授权

US5719159A 4-azasteroids with side-chain fluoroketones 失效
标题翻译：具有侧链含氟酮的4-azasteroids
公开(公告)号：US5719159A
公开(公告)日：1998-02-17
申请号：US615242
申请日：1996-05-31
申请人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
发明人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
IPC分类号： A61K31/59 , A61P3/00 , C07J3/00 , C07J73/00 , A61K31/58 , C07D221/02
CPC分类号： C07J73/005
摘要： The present invention provides compounds of formula (D wherein the symbol - - - represents a single or a double bond; R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; A is a single bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain; B is a straight or branched C.sub.1 -C.sub.12 alkylene group optionally substituted by one or more aryl groups or fluorine atoms; W is a group R.sub.1 or (a) wherein R.sub.1 is a straight or branched C.sub. -C.sub.6 alkyl group unsubstituted or substituted by one or more fluorine atoms, provided that at least a fluorine atom is present in B or W. The compounds of the invention are useful as testosterone 5.alpha.-reductase inhibitors. ##STR1##
摘要翻译： PCT No.PCT / EP95 / 02649第 371日期：1996年5月31日 102（e）日期1996年5月31日PCT提交1995年7月7日PCT公布。出版物WO96 / 03422 日期：1996年2月8日本发明提供了式（D的化合物，其中符号+ E，不 - + EE表示单键或双键; R是氢原子或C1-C4烷基; A是单键或直链或支链C1-C6亚烷基链; B是任选被一个或多个芳基或氟原子取代的直链或支链C 1 -C 12亚烷基; W是基团R 1或（a）其中R 1是直链或未被取代或被一个或多个氟原子取代的支链C 1 -C 6烷基，条件是至少在B或W中存在氟原子。本发明的化合物可用作睾酮5α-还原酶抑制剂。

2. 发明授权

US5922728A Phenylsubstituted 4-azasteroid fluoroderivatives 失效
标题翻译：苯基取代的4-azasteroid氟代衍生物
公开(公告)号：US5922728A
公开(公告)日：1999-07-13
申请号：US836052
申请日：1997-05-13
申请人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
发明人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
IPC分类号： A61K31/58 , A61P43/00 , C07J73/00 , C07D221/18
CPC分类号： C07J73/005
摘要： Compounds of formula (I), wherein: the symbol represents a single or a double bond; R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; R.sub.f and R'.sub.f, each independently, are C.sub.1 -C.sub.4 alkyl groups substituted by one or more fluorine atoms; and R.sub.1 and R.sub.2, each independently, are selected from: a hydrogen atom; a phenyl group; a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms; a halogen atom; a cyano (CN) group; a group OR.sub.4, wherein R.sub.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; a group SR.sub.5, wherein R.sub.5 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and a group COR.sub.6, wherein R.sub.6 is a group OR.sub.4 in which R.sub.4 is as defined above or a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms. They are useful as testosterone 5a-reductase inhibitors.
摘要翻译： PCT No.PCT / EP96 / 03518 Sec。 371日期1997年5月13日 102（e）日期1997年5月13日PCT提交1996年8月9日PCT公布。第WO97 / 10257号公报日期1997年3月20日式（I）化合物，其中：符号+ Z表示单键或双键; R是氢原子或C 1 -C 4烷基; Rf和R'f各自独立地是被一个或多个氟原子取代的C 1 -C 4烷基; 并且R 1和R 2各自独立地选自：氢原子; 苯基; 未被取代或被一个或多个氟原子取代的C 1 -C 4烷基; 卤素原子; 氰基（CN）基团; OR 4，其中R 4是氢原子或C 1 -C 4烷基; 基团SR5，其中R5是氢原子或C1-C4烷基; 和基团COR6，其中R6是其中R4如上定义的基团OR4或未被取代或被一个或多个氟原子取代的C 1 -C 4烷基。它们可用作睾酮5a还原酶抑制剂。

3. 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.

4. 发明授权

US6114345A Phenylsubstituted 4-azasteroid fluoroderivatives 失效
标题翻译：苯基取代的4-azasteroid氟代衍生物
公开(公告)号：US6114345A
公开(公告)日：2000-09-05
申请号：US300454
申请日：1999-04-28
申请人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
发明人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
IPC分类号： A61K31/58 , A61P43/00 , C07J73/00
CPC分类号： C07J73/005
摘要： Compounds of formula (I), wherein: the symbol ---- represents a single or a double bond; R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; R.sub.f and R'.sub.f, each independently, are C.sub.1 -C.sub.4 alkyl groups substituted by one or more fluorine atoms; and R.sub.1 and R.sub.2, each independently, are selected from: a hydrogen atom; a phenyl group; a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms; a halogen atom; a cyano (CN) group; a group OR.sub.4, wherein R.sub.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; a group SR.sub.5, wherein R.sub.5 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and a group COR.sub.6, wherein R.sub.6 is a group OR.sub.4 in which R.sub.4 is as defined above or a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms. They are useful as testosterone 5a-reductase inhibitors.
摘要翻译：式（I）的化合物，其中：符号+ E，uns ---- + EE表示单键或双键; R是氢原子或C 1 -C 4烷基; Rf和R'f各自独立地是被一个或多个氟原子取代的C 1 -C 4烷基; 并且R 1和R 2各自独立地选自：氢原子; 苯基; 未被取代或被一个或多个氟原子取代的C 1 -C 4烷基; 卤素原子; 氰基（CN）基团; OR 4，其中R 4是氢原子或C 1 -C 4烷基; 基团SR5，其中R5是氢原子或C1-C4烷基; 和基团COR6，其中R6是其中R4如上定义的基团OR4或未被取代或被一个或多个氟原子取代的C 1 -C 4烷基。它们可用作睾酮5a还原酶抑制剂。

5. 发明授权

US5407939A Fluorinated 17 .beta.-substituted 4-aza-5 .alpha.-androstan-3-one derivatives 失效
标题翻译：氟化17β-取代的4-氮杂-5α-雄甾烷-3-酮衍生物
公开(公告)号：US5407939A
公开(公告)日：1995-04-18
申请号：US98729
申请日：1993-07-29
申请人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
发明人： Achille Panzeri , Marcella Nesi , Enrico Di Salle
IPC分类号： A61K31/58 , A61P5/28 , A61P17/00 , A61P17/08 , A61P17/14 , A61P35/00 , C07J73/00 , C12N9/99 , A61K31/47
CPC分类号： C07J73/005
摘要： Compounds of formula (I) ##STR1## wherein: the symbol represents a single or a double bond;B is a bond or a straight or branched C.sub.1 -C.sub.6 alkylene chain;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl;R.sub.2 isa) hydrogen, fluorine, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl or C.sub.6 -C.sub.9 cycloalkylalkyl; orb) aryl or C.sub.7 -C.sub.10 arylalkyl;R.sub.3 isa) hydrogen, fluorine or C.sub.1 -C.sub.4 alkyl; orb) aryl or C.sub.7 -C.sub.10 arylalkyl;R.sub.4 is hydrogen, fluorine, or is absent when Y is a double bond;R.sub.5 is hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; and when Y is a single bond, A is hydrogen, fluorine or ##STR2## wherein each of R.sub.6, R.sub.7 and R.sub.8 independently is hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; and when Y is a double bond, A is a ##STR3## wherein each of R.sub.6 and R.sub.7 is independently hydrogen, fluorine or C.sub.1 -C.sub.6 alkyl; with the proviso that at least one of the groups R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 or A contains at least one fluorine atom.
摘要翻译：式（I）化合物其中：符号表示单键或双键; B是键或直链或支链C1-C6亚烷基链; R是氢或C 1 -C 4烷基; R1是氢，C1-C6烷基或苄基; R2是a）氢，氟，C1-C6烷基，C5-C7环烷基或C6-C9环烷基烷基; 或b）芳基或C7-C10芳基烷基; R3是a）氢，氟或C1-C4烷基; 或b）芳基或C7-C10芳基烷基; R4是氢，氟，或当Y是双键时不存在; R5是氢，氟或C1-C6烷基; 当Y是单键时，A是氢，氟或者其中R6，R7和R8各自独立地是氢，氟或C1-C6烷基; 当Y是双键时，A是一个，其中R6和R7各自独立地是氢，氟或C1-C6烷基; 条件是基团R，R 1，R 2，R 3，R 4，R 5或A中的至少一个含有至少一个氟原子。

6. 发明授权

US5155107A 17.beta.-substituted-4-aza-5.alpha.-androstan-3-one derivatives and process for their preparation 失效
标题翻译： 17（BETA）-SUBSTITUTED-4-AZA-5（ALPHA）-ANDROSTAN-3-ONE衍生物及其制备方法
公开(公告)号：US5155107A
公开(公告)日：1992-10-13
申请号：US650970
申请日：1991-02-05
申请人： Achille Panzeri , Enrico Di Salle , Marcella Nesi
发明人： Achille Panzeri , Enrico Di Salle , Marcella Nesi
IPC分类号： A61K31/56 , A61K31/58 , A61P35/00 , C07J20060101 , C07J73/00
CPC分类号： C07J73/005
摘要： The present invention concerns steroidic 5.alpha.-reductase inhibitors having the formula: ##STR1## As a result of their 5.alpha.-reductase inhibiting activity, these compounds are useful in the treatment of androgen dependent conditions and diseases.
摘要翻译：本发明涉及具有下式的类固醇5α-还原酶抑制剂：作为其5α-还原酶抑制活性的结果，这些化合物可用于治疗雄激素依赖性病症和疾病。

7. 发明授权

US5502044A Fluorinated 4-aminoandrostadienone derivatives and process for their preparation 失效
标题翻译：氟化4-氨基雄二烯酮衍生物及其制备方法
公开(公告)号：US5502044A
公开(公告)日：1996-03-26
申请号：US195205
申请日：1994-02-14
申请人： Franco Buzzetti , Antonio Longo , Enrico Di Salle
发明人： Franco Buzzetti , Antonio Longo , Enrico Di Salle
IPC分类号： A61K31/565 , C07J1/00 , C07J41/00 , C07J71/00 , A61K31/56
CPC分类号： C07J41/0005 , C07J1/0011 , C07J41/0011 , C07J41/0027 , C07J71/001
摘要： The present invention relates to a compound of formula (I) ##STR1## wherein (x) and (y) are single or double bonds; A is a ##STR2## R and R.sup.3 are hydrogen or acyl; R.sup.1 is hydrogen or fluorine;and wherein:when (y) is a single bond, R.sup.2 is hydrogen, fluorine methyl, trifluoromethyl;when (y) is a double bond, R.sup.2 is methylene provided that when one of (x) or (y) is a double bond the other is a single bond and at least one of R.sub.1 and R.sub.2 is fluorine or trifluoromethyl or a pharmaceutically acceptable salt thereof. The compounds of formula (I) are useful as aromatase inhibitors.
摘要翻译：本发明涉及式（I）化合物，其中（x）和（y）是单键或双键; A是R 1和R 3是氢或酰基; R1是氢或氟; 并且其中：当（y）为单键时，R 2为氢，氟甲基，三氟甲基; 当（y）是双键时，R2是亚甲基，条件是当（x）或（y）中的一个是双键时，另一个是单键，并且R 1和R 2中的至少一个是氟或三氟甲基或药学上可接受的的盐。式（I）化合物可用作芳香酶抑制剂。

8. 发明授权

US5457097A Androst-4-eno[4,5-b]pyrrole derivatives 失效
标题翻译：雄甾-4-烯[4,5-b]吡咯衍生物
公开(公告)号：US5457097A
公开(公告)日：1995-10-10
申请号：US92789
申请日：1993-07-19
申请人： Franco Buzzetti , Antonio Longo , Enrico Di Salle
发明人： Franco Buzzetti , Antonio Longo , Enrico Di Salle
IPC分类号： C12N9/99 , A61K31/58 , A61P43/00 , C07J7/00 , C07J51/00 , C07J71/00 , C07J1/00 , A61K31/56
CPC分类号： C07J71/0042 , C07J7/0085
摘要： This invention refers to compounds of formula (I) ##STR1## wherein x, y, z represent single or double bonds;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 is hydrogen or an acyl group;R.sub.2 is hydrogen; C.sub.1 -C.sub.4 alkyl unsubstituted or substituted by phenyl; phenyl unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; andA is a >C.dbd.O, >CH OH or >CH OR.sub.3 group, in which R.sub.3 is an acyl group provided that one of z and y is a double bond and the other is a single bond.The compounds are useful as aromatase inhibitors.
摘要翻译：本发明涉及式（I）的化合物：其中x，y，z表示单键或双键; R是氢或C 1 -C 4烷基; R1是氢或酰基; R2是氢; 未被取代或被苯基取代的C 1 -C 4烷基; 未被取代或被C 1 -C 4烷基或C 1 -C 4烷氧基取代的苯基; 并且A是> C = O，> CH OH或> CH OR 3基团，其中R 3是酰基，条件是z和y之一是双键，而另一个是单键。该化合物可用作芳香酶抑制剂。

9. 发明授权

US4543353A Ester and amide derivatives of 13,14-didehydro prostaglandins 失效
标题翻译： 13,14-二脱氢前列腺素的酯和酰胺衍生物
公开(公告)号：US4543353A
公开(公告)日：1985-09-24
申请号：US436419
申请日：1982-10-25
申请人： Franco Faustini , Vittoria Villa , Carmelo Gandolfi , Enrico Di Salle
发明人： Franco Faustini , Vittoria Villa , Carmelo Gandolfi , Enrico Di Salle
IPC分类号： A61K31/557 , A61K31/5575 , A61P13/02 , A61P15/00 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D231/12 , C07D233/02 , C07D295/18 , C07C177/00
CPC分类号： C07C405/0041 , C07C405/00
摘要： Esters of 13,14-didehydro prostaglandins have been prepared.
摘要翻译：已经制备了13,14-didehydro前列腺素的酯。

10. 发明授权

US4196288A Ergoline derivatives and a process for their preparation 失效
标题翻译：艾尔莫林衍生物及其制备方法
公开(公告)号：US4196288A
公开(公告)日：1980-04-01
申请号：US856536
申请日：1977-12-01
申请人： Enzo Beacco , Luigi Bernardi , Enrico Di Salle , Giovanni Falconi , Bianca Patelli
发明人： Enzo Beacco , Luigi Bernardi , Enrico Di Salle , Giovanni Falconi , Bianca Patelli
IPC分类号： A61K31/48 , A61K31/495 , A61K31/505 , C07D457/02
CPC分类号： C07D457/02
摘要： New ergoline derivatives are disclosed which are compounds of formula (I) having the structure: ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or methyl; andX is hydroxy, R.sub.3 COO, S--R.sub.4 or NR.sub.5 R.sub.6 in which R.sub.3 is a straight or branched alkyl having from 1 to 6 carbon atoms, unsubstituted- or substituted-phenyl, the substituents being selected from the class consisting of chlorine, bromine, alkyl or alkoxy having from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, or a heterocycle;R.sub.4 is phenyl or a heterocycle, andR.sub.5 and R.sub.6 are alkyl having from 1 to 4 carbon atoms, or together with the N atom to which they are attached, forming a heterocycle. The heterocycle may be a 5- or 6-membered ring which contains from 1 to 3 hetero atoms selected from the class consisting of nitrogen, oxygen and sulphur, and may be saturated or unsaturated, and unsubstituted or substituted by halogen, alkyl having from 1 to 3 carbon atoms, hydroxy, nitro, amino, CONHNH.sub.2 and COOH.
摘要翻译：公开了新的麦角灵衍生物，其是具有以下结构的式（I）的化合物：其中R 1是氢或甲氧基; R2是氢或甲基; 并且X是羟基，R 3 COO，S-R 4或NR 5 R 6，其中R 3是具有1至6个碳原子的直链或支链烷基，未取代或取代的苯基，所述取代基选自氯，溴，烷基或具有1至4个碳原子的烷氧基，含3至6个碳原子的环烷基或杂环; R 4是苯基或杂环，R 5和R 6是具有1至4个碳原子的烷基，或与它们相连的N原子一起形成杂环。杂环可以是含有1至3个选自氮，氧和硫的杂原子的5或6元环，并且可以是饱和或不饱和的，未取代的或被卤素取代的烷基，具有1个至3个碳原子，羟基，硝基，氨基，CONHNH 2和COOH。

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