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。

公开(公告)号：US5418238A

公开(公告)日：1995-05-23

申请号：US98935

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 ,  C07J73/00 ,  C12N9/99

CPC分类号： C07J73/005

摘要： A compound of formula (I): ##STR1## wherein 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;R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sub.2 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.7 cycloalkyl or a C.sub.6 -C.sub.10 cycloalkylalkyl group, aryl or a C.sub.7 -C.sub.10 arylalkyl group, or a C.sub.6 -C.sub.10 heterocyclylalkyl group;R.sub.3 is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aryl or a C.sub.7 -C.sub.10 arylalkyl group;Z is a C.sub.1 -C.sub.6 alkyl group, an --OR.sub.5 group wherein R.sub.5 is a C.sub.1 -C.sub.6 alkyl group, ##STR2## group wherein each of R.sub.6 and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl or R.sub.6 and R.sub.7 taken together with the nitrogen to which they are linked form a pentatomic or hexatomic saturated heteromonocyclic ring; and the symbol represents a single or a double bond, is a testosterone 68 5.alpha.-reductase inhibitor and is therapeutically useful in benign prostatic hyperplasia, prostatic and breast cancers, seborrhoea, female hirsutism and male pattern baldness.

摘要翻译： 式（I）的化合物：其中R是氢原子或C 1 -C 4烷基; A是单键或直链或支链C1-C6亚烷基链; R1是氢原子或C1-C6烷基; R2是C1-C6烷基，C5-C7环烷基或C6-C10环烷基烷基，芳基或C7-C10芳基烷基或C6-C10杂环基烷基; R3是氢，C1-C4烷基或芳基或C7-C10芳烷基; Z是C1-C6烷基，其中R5是C1-C6烷基的-OR5基团，其中R6和R7各自是氢，C1-C6烷基，C5-C7环烷基，苯基或R6和 R7与它们所连接的氮一起形成五原子或六原子饱和杂单环; 符号表示单键或双键，是睾酮685α-还原酶抑制剂，可用于良性前列腺增生，前列腺和乳腺癌，皮脂溢，女性多毛症和男性型秃发。

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。

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.

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。

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。

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。

公开(公告)号：US4626597A

公开(公告)日：1986-12-02

申请号：US643014

申请日：1984-08-22

申请人： Franco Faustini ,  Roberto d'Alessio ,  Achille Panzeri ,  Enrico di Salle

发明人： Franco Faustini ,  Roberto d'Alessio ,  Achille Panzeri ,  Enrico di Salle

IPC分类号： A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/557 ,  A61K31/5575 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D207/32 ,  C07D207/333 ,  C07D207/337 ,  C07D213/30 ,  C07D213/55 ,  C07D241/12 ,  C07D261/08 ,  C07D307/42 ,  C07D307/54 ,  C07D309/12 ,  C07D333/24 ,  C07C177/00

CPC分类号： C07D207/337 ,  C07C405/00 ,  C07C405/0033 ,  C07C405/0041 ,  C07D213/55 ,  C07D241/12 ,  C07D261/08 ,  C07D307/54 ,  C07D333/24

摘要： 16-Fluoro-16,17-didehydro prostanoids, processes for their preparation, compositions containing them and methods of using them are disclosed. The compounds and compositions have pharmaceutical utility including, for example, luteolytic activity.

摘要翻译： 公开了16-氟-16,17-二氢前列腺素类，其制备方法，含有它们的组合物及其使用方法。 化合物和组合物具有药物效用，包括例如溶血活性。

公开(公告)号：US4585791A

公开(公告)日：1986-04-29

申请号：US667367

申请日：1984-11-01

申请人： Franco Faustini ,  Achille Panzeri ,  Fabrizio Orzi ,  Enrico di Salle ,  Roberto Ceserani

发明人： Franco Faustini ,  Achille Panzeri ,  Fabrizio Orzi ,  Enrico di Salle ,  Roberto Ceserani

IPC分类号： C07D307/38 ,  A61K31/557 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07D307/54 ,  C07D307/935 ,  A61K31/34

CPC分类号： C07D307/935 ,  C07D307/54

摘要： The present invention relates to new furyl derivatives of 16-substituted prostaglandins, to a process for their preparation and to pharmaceutical and veterinary compositions containing them.The new compounds of the invention are optically active or racemic prostaglandins of the following formula (I) ##STR1## wherein R is(1) --OH or --OR' wherein R' is C.sub.1 -C.sub.6 alkyl optionally substituted by phenyl or by a monocycloalkyl group or by a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N;(2) ##STR2## wherein each of R" and R"', is independently, hydrogen; C.sub.1 -C.sub.6 alkyl; phenyl; or a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N; or R" and R"', together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic heteromonocyclic ring optionally containing a further heteroatom chosen from O, S and N;(3) --W--(CH.sub.2).sub.n --X wherein W is --O-- or --NH--, n is an integer of 1 to 4 and X represents a group --OR' or a group ##STR3## wherein R', R" and R"' are as defined above;one of R.sub.1 and R.sub.2 is hydrogen and the other is hydroxy orR.sub.1 and R.sub.2, taken together, form an oxo group;one of R.sub.3 and R.sub.4 is hydrogen and the other is hydroxy;one of R.sub.5 and R.sub.6 is hydroxy and the other 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;one of R.sub.7 and R.sub.8 is hydrogen and the other is a C.sub.1 -C.sub.4 alkyl or tri-halo-C.sub.1 -C.sub.4 alkyl group;m is an integer of 1 to 3;R.sub.9 is a 2-furyl or 3-furyl group, optionally substituted by one or more substituents chosen from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, tri-halo-C.sub.1 -C.sub.4 alkyl and halogen; and the symbol represents a single bond or a cis double bond.

摘要翻译： 本发明涉及16-取代的前列腺素的新呋喃衍生物，其制备方法和含有它们的药物和兽药组合物。 本发明的新化合物是下式（I）的光学活性或外消旋前列腺素其中R是（1）-OH或-OR'，其中R'是任选被苯基取代的C 1 -C 6烷基或 通过单环烷基或含有至少一个选自O，S和N的杂原子的五原子或六原子杂单环; （2）其中R“和R”'各自独立地为氢; C1-C6烷基; 苯基; 或含有至少一个选自O，S和N的杂原子的五原子或六原子杂单环; 或R“和R”'与它们所连接的氮原子一起形成任选地含有选自O，S和N的另外的杂原子的五原子或六原子异单环; （3）-W-（CH2）nX其中W是-O-或-NH-，n是1至4的整数，X表示基团-OR'或基团，其中R'，R“ 和R“'如上所定义; R 1和R 2之一是氢，另一个是羟基或R 1和R 2一起形成氧代基; R3和R4之一是氢，另一个是羟基; R 5和R 6之一是羟基，另一个是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或苯基; R 7和R 8中的一个是氢，另一个是C 1 -C 4烷基或三卤代-C 1 -C 4烷基; m为1〜3的整数。 R9是2-呋喃基或3-呋喃基，任选被一个或多个选自C 1 -C 4烷基，C 1 -C 4烷氧基，三卤代-C 1 -C 4烷基和卤素的取代基取代; 符号表示单键或顺式双键。

公开(公告)号：US6121449A

公开(公告)日：2000-09-19

申请号：US367847

申请日：1999-08-27

申请人： Achille Panzeri ,  Matteo D'Anello ,  Antonio Longo ,  Marcella Nesi

发明人： Achille Panzeri ,  Matteo D'Anello ,  Antonio Longo ,  Marcella Nesi

IPC分类号： A61P5/24 ,  A61K31/58 ,  A61P43/00 ,  C07J41/00 ,  C07J71/00 ,  C07J73/00 ,  C07D221/02

CPC分类号： C07J73/005

摘要： A process for producing a compound of formula (I): ##STR1## wherein the dotted lines - - - independently represent a single or double bond and R, R.sub.1, R.sub.2 and R.sub.3 are each hydrogen or an organic radical, comprises treating the corresponding 17.beta.-carbonylimidazole intermediates with anhydrous acids in the presence of an amine and, optionally, hydrogenating the resulting compound.

摘要翻译： PCT No.PCT / EP98 / 08527 Sec。 371日期1999年8月27日第 102（e）1999年8月27日PCT 1998年12月17日PCT PCT。 公开号WO99 /​​ 35161 日期1999年7月15日制备式（I）化合物的方法：其中虚线 - - - 独立地表示单键或双键，并且R，R 1，R 2和R 3各自为氢或有机基团， 在胺的存在下与无水酸反应，并任选地将所得化合物氢化，得到相应的17β-羰基咪唑中间体。