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1.发明授权Steroid derivatives for the treatment of prostatic hypertrophy their preparation and uses 失效类固醇衍生物用于治疗前列腺肥大其制备和用途
公开(公告)号：US5536714A
公开(公告)日：1996-07-16
申请号：US375264
申请日：1995-01-19
IPC分类号： C07J1/00 , A61K20060101 , A61K31/56 , A61K31/568 , A61K31/575 , A61P5/00 , A61P13/02 , A61P15/00 , C07J20060101 , C07J41/00 , C07J43/00 , C07J3/00 , A61K31/58
CPC分类号： C07J41/0066 , C07J41/0094 , C07J43/003 , Y02P20/55
摘要： The invention includes compounds of formula (I): ##STR1## in which R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl; and pharmaceutically acceptable salts and esters of the compounds. The compounds have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydro-testosterone.
摘要翻译： 本发明包括式（I）的化合物：其中R 1是氢，烷基，芳基取代的烷基或芳族杂环取代的烷基; R2是芳基取代的烷基，芳族杂环取代的烷基或二芳基氨基; 并且R 3是羧基或式-CONHSO 2 R 4基团，其中R 4是烷基; 和化合物的药学上可接受的盐和酯。 这些化合物具有有价值的5α-还原酶抑制活性，因此可用于治疗和预防尤其是前列腺肥大以及由过量水平的5α-二氢睾酮引起的其它障碍。
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2.发明授权Steroid derivatives for the treatment of prostatic hypertrophy, their preparation and uses 失效类固醇衍生物用于治疗前列腺肥大，其制备和用途
公开(公告)号：US5760025A
公开(公告)日：1998-06-02
申请号：US414909
申请日：1995-03-31
IPC分类号： C07J1/00 , A61K20060101 , A61K31/56 , A61K31/568 , A61K31/575 , A61P5/00 , A61P13/02 , A61P15/00 , C07J20060101 , C07J41/00 , C07J43/00 , A61K58/00 , A61K56/00
CPC分类号： C07J41/0066 , C07J41/0094 , C07J43/003 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## �wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.
摘要翻译： 式（I）化合物：其中：R 1为氢，烷基，芳基取代的烷基或芳族杂环取代的烷基; R2是：芳基取代的烷基，芳族杂环取代的烷基或二芳基氨基; 并且R 3是羧基或式-CONHSO 2 R 4的基团，其中R 4是烷基]; 其药学上可接受的盐和酯具有有价值的5α-还原酶抑制活性，因此可用于治疗和预防尤其是前列腺肥大以及由过量水平的5α-二氢睾酮引起的其它障碍。
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3.发明授权Method of making steroid derivatives for the treatment of prostatic hypertrophy 失效制备类固醇衍生物治疗前列腺肥大的方法
公开(公告)号：US5717088A
公开(公告)日：1998-02-10
申请号：US618850
申请日：1996-03-20
IPC分类号： C07J1/00 , A61K20060101 , A61K31/56 , A61K31/568 , A61K31/575 , A61P5/00 , A61P13/02 , A61P15/00 , C07J20060101 , C07J41/00 , C07J43/00 , C07J3/00 , C07J17/00
CPC分类号： C07J41/0066 , C07J41/0094 , C07J43/003 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## �wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.
摘要翻译： 式（I）化合物：其中：R 1是氢，烷基，芳基取代的烷基或芳族杂环取代的烷基; R2是：芳基取代的烷基，芳族杂环取代的烷基或二芳基氨基; 并且R 3是羧基或式-CONHSO 2 R 4的基团，其中R 4是烷基]; 其药学上可接受的盐和酯具有有价值的5α-还原酶抑制活性，因此可用于治疗和预防尤其是前列腺肥大以及由过量水平的5α-二氢睾酮引起的其它障碍。
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公开(公告)号：US5698720A
公开(公告)日：1997-12-16
申请号：US631809
申请日：1996-04-12
CPC分类号： C07J43/003 , C07J41/0066 , C07J41/0094
摘要： The invented compound ##STR1## is useful for the production of steroidal-17-amides that have 5.alpha.-reductase inhibitory activity.
摘要翻译： 本发明化合物
可用于生产具有5种α-还原酶抑制活性的甾体-17-酰胺。 -
公开(公告)号：US06448247B1
公开(公告)日：2002-09-10
申请号：US09533061
申请日：2000-03-22
申请人： Takahide Nishi , Koki Ishibashi , Katsuyoshi Nakajima , Tetsuya Fukazawa , Hitoshi Kurata , Takeshi Yamaguchi , Kazuhiro Ito
发明人： Takahide Nishi , Koki Ishibashi , Katsuyoshi Nakajima , Tetsuya Fukazawa , Hitoshi Kurata , Takeshi Yamaguchi , Kazuhiro Ito
IPC分类号： A61K315375
CPC分类号： C07D263/04 , C07D413/06 , C07D413/14 , C07D471/10 , C07D491/10 , C07D495/10
摘要： Compounds of the formula and quaternary ammonium ions thereof, wherein R1 and R2 are the same or different and are carbocyclic aryl or aromatic heterocyclic; A is methylene, carbonyl or sulfonyl; B is a single bond, C1-C4 alkylene or C2-C4 alkenylene; D is oxygen or sulfur; E is C2-C6 alkylene, C1-C6 haloalkylene, C3-C6 cycloalkane-1,1-diyl or C3-C6-cycloalkane-1,1-diylmethyl; G is C1-C4 alkylene or C2-C4 alkenylene; and L is —NR3 or —C(R4)(R5), wherein R3 is a carbocyclic aryl or an aromatic heterocyclic; R4 is hydrogen, carbocyclic aryl or aromatic heterocyclic; R5 is —COR6, C1-C6 alkyl, C1-C6 alkoxy, amino, or acylamino, wherein R6 is C1-C6 alkyl or C1-C6 alkoxy, or R4 and R5 together with the carbon atom to which they are attached represent a C5-C10 cycloalkyl or a C5-C10 heterocyclic. The compounds have tachykinin receptor antagonist activity and exhibit an activity against both the NK1 and NK2 receptors.
摘要翻译： 其中式和季铵离子的化合物，其中R 1和R 2相同或不同，为碳环芳基或芳族杂环; A是亚甲基，羰基或磺酰基; B是单键，C1-C4亚烷基或C2-C4亚烯基; D是氧或硫; E为C2-C6亚烷基，C1-C6卤代亚烷基，C3-C6环烷烃-1,1-二基或C3-C6-环烷烃-1,1-二基甲基; G是C 1 -C 4亚烷基或C 2 -C 4亚烯基; 并且L是-NR 3或-C（R 4）（R 5），其中R 3是碳环芳基或芳族杂环; R4是氢，碳环芳基或芳族杂环; R 5是-COR 6，C 1 -C 6烷基，C 1 -C 6烷氧基，氨基或酰氨基，其中R 6是C 1 -C 6烷基或C 1 -C 6烷氧基，或者R 4和R 5与它们所连接的碳原子一起代表C5 -C 10环烷基或C 5 -C 10杂环。 该化合物具有速激肽受体拮抗剂活性，并表现出对NK1和NK2受体的活性。
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6.发明授权Heterocyclic compounds having tachykinin receptor antagonist activity their preparation and their use 失效具有速激肽受体拮抗剂活性的杂环化合物的制备及其用途
公开(公告)号：US6159967A
公开(公告)日：2000-12-12
申请号：US758421
申请日：1996-12-02
申请人： Takahide Nishi , Koki Ishibashi , Katsuyoshi Nakajima , Tetsuya Fukazawa , Hitoshi Kurata , Takeshi Yamaguchi , Kazuhiro Ito
发明人： Takahide Nishi , Koki Ishibashi , Katsuyoshi Nakajima , Tetsuya Fukazawa , Hitoshi Kurata , Takeshi Yamaguchi , Kazuhiro Ito
IPC分类号： A61K31/44 , A61K31/4523 , A61K31/4709 , A61K31/495 , A61K31/535 , A61K31/5377 , A61K31/55 , A61K31/553 , A61P17/00 , A61P19/00 , A61P25/00 , C07D263/04 , C07D413/06 , C07D413/14 , C07D417/06 , C07D471/10 , C07D487/10 , C07D491/10 , C07D495/10 , C07D498/10 , C07D265/00 , C07D265/30 , C07D295/00
CPC分类号： C07D263/04 , C07D413/06 , C07D413/14 , C07D471/10 , C07D491/10 , C07D495/10
摘要： Compounds of the formula and quaternary ammonium ions thereof, wherein R.sup.1 and R.sup.2 are the same or different and are carbocyclic aryl or aromatic heterocyclic; A is methylene, carbonyl or sulfonyl; B is a single bond, C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4, alkenylene; D is oxygen; E is C.sub.2 alkylene; G is C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene; and L is --C(R.sup.4)(R.sup.5), wherein R.sup.4 and R.sup.5 together with the carbon atom to which they are attached represent a C.sub.5 -C.sub.10 cycloalkyl or a C.sub.5 -C.sub.10 heterocyclic. Especially preferred are compounds wherein L represents ##STR1## wherein J is a C.sub.1 -C.sub.6 alkylene; Ar is a ring carbocyclic or aromatic heterocyclic and S*.fwdarw.O is a sulfoxide in which the sulfur atom is in the 5-configuration. The compounds have tachykinin receptor antagonist activity and exhibit an activity against both the NK.sub.1 and NK.sub.2 receptors.
摘要翻译： 式及其季铵离子的化合物，其中R 1和R 2相同或不同，为碳环芳基或芳族杂环; A是亚甲基，羰基或磺酰基; B是单键，C 1 -C 4亚烷基或C 2 -C 4亚烯基; D是氧; E为C2亚烷基; G是C 1 -C 4亚烷基或C 2 -C 4亚烯基; 并且L是-C（R 4）（R 5），其中R 4和R 5与它们所连接的碳原子一起代表C5-C10环烷基或C5-C10杂环。 特别优选的是其中L表示其中J为C1-C6亚烷基的化合物; Ar是环碳环或芳族杂环，并且S * - > O是其中硫原子为5构型的亚砜。 该化合物具有速激肽受体拮抗剂活性，并表现出对NK1和NK2受体的活性。
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