专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06448247B1 Method for treating an inflammatory disease 失效
标题翻译：治疗炎性疾病的方法
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。

2. 发明授权

US5302621A Azasteroid compounds for the treatment of prostatic hypertrophy, their preparation and use 失效
标题翻译：氮芥类化合物用于治疗前列腺肥大，其制备和使用
公开(公告)号：US5302621A
公开(公告)日：1994-04-12
申请号：US23871
申请日：1993-02-26
申请人： Koichi Kojima , Hitoshi Kurata , Hiroyoshi Horikoshi , Takakazu Hamada
发明人： Koichi Kojima , Hitoshi Kurata , Hiroyoshi Horikoshi , Takakazu Hamada
IPC分类号： A61K31/56 , A61K31/58 , A61P13/02 , A61P15/00 , A61P43/00 , C07J73/00
CPC分类号： C07J73/005
摘要： Compounds of formula (I): ##STR1## (in which: R.sup.1 is a hydrogen atom, an unsubstituted alkyl group, an aryl-substituted alkyl group or a heterocyclic-substituted alkyl group; R.sup.2 is an aryl-substituted alkyl group, a heterocyclic-substituted alkyl group or a diarylamino group; R.sup.3 is a hydrogen atom, an unsubstituted alkyl group, an aryl-substituted alkyl group or an alkenyl group having from 3 to 6 carbon atoms; and each of the bonds represented by .alpha.-.beta. and .gamma.-.delta. is a carbon-carbon single bond or a carbon-carbon double bond;) and pharmaceutically acceptable salts and esters thereof are useful for the treatment and prophylaxis of prostatic hypertrophy. We also provide processes for their preparation.
摘要翻译：式（I）化合物：其中：R1是氢原子，未取代的烷基，芳基取代的烷基或杂环取代的烷基; R2是芳基取代的烷基，杂环取代的烷基或二芳基氨基; R3是氢原子，未取代的烷基，芳基取代的烷基或具有3至6个碳原子的烯基;并且每个由α- β和γ-δ是碳 - 碳单键或碳 - 碳双键;）及其药学上可接受的盐和酯可用于治疗和预防前列腺肥大。我们还提供准备工作。

3. 发明申请

US20070275968A1 Substituted Biphenyl Derivative 审中-公开
标题翻译：取代的联苯衍生物
公开(公告)号：US20070275968A1
公开(公告)日：2007-11-29
申请号：US11574811
申请日：2005-09-05
申请人： Hitoshi Kurata , Toyoki Nishimata , Yukiko Watanabe , Masayuki Ebisawa , Teppei Fujimoto , Hideki Kobayashi
发明人： Hitoshi Kurata , Toyoki Nishimata , Yukiko Watanabe , Masayuki Ebisawa , Teppei Fujimoto , Hideki Kobayashi
IPC分类号： C07D401/02 , A61K31/4436 , A61K31/4439 , A61K31/497 , C07D401/14 , C07D413/14 , C07D413/02 , A61K31/5377 , A61P1/16 , A61P43/00
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D513/04
摘要： The present invention relates to a biaryl derivative or a pharmacologically acceptable salt thereof having an excellent collagen-synthesis inhibition activity. A biaryl derivative having a structure represented by the following General Formula (I) or a pharmacologically acceptable salt thereof: wherein R1 represents a C6-C10 aryl group which is substituted with one to three group(s) each independently selected from the group consisting of a group defined by formula R-L-, a di-(C1-C6 alkyl)amino group, a di-(C1-C6 alkyl)aminosulfonyl group, a hydroxyaminocarbonyl group, and a halogen atom, and so on; R represents a C1-C6 alkyl group, and so on; L represents a sulfonyl group, an aminosulfonyl group, or a sulfonylamino group, and so on; R2 represents a hydrogen atom, and so on; A represents a group defined by formula (II), (III), or (IV); R3 represents a C1-C6 alkyl group, and so on; and R4 represents a C1-C6 alkyl group, and so on.
摘要翻译：本发明涉及具有优异的胶原合成抑制活性的联芳基衍生物或其药理学上可接受的盐。具有由以下通式（I）表示的结构的联芳衍生物或其药理学上可接受的盐：其中R 1表示C 6 -C 10烷基，被一至三个取代基取代的芳基，其各自独立地选自由式RL-定义的基团，二 - （C 1 -C 3）（C 1 -C 6烷基）氨基，二 - （C 1 -C 6烷基）氨基磺酰基，羟基氨基羰基和卤素原子等 ; R表示C 1 -C 6烷基，等等; L表示磺酰基，氨基磺酰基或磺酰基氨基，等等; R 2表示氢原子等等; A表示由式（II），（III）或（IV）定义的基团; R 3表示C 1 -C 6烷基，等等; 和R 4代表C 1 -C 6烷基，等等。

4. 发明授权

US06329405B1 Cyclobutene derivatives, their preparation and their therapeutic uses 失效
标题翻译：环丁烯衍生物，其制备及其治疗用途
公开(公告)号：US06329405B1
公开(公告)日：2001-12-11
申请号：US09620741
申请日：2000-07-20
申请人： Hitoshi Kurata , Takafumi Kohama , Keita Kono , Ken Kitayama
发明人： Hitoshi Kurata , Takafumi Kohama , Keita Kono , Ken Kitayama
IPC分类号： C07D21302
CPC分类号： C07C309/14 , C07B2200/07 , C07C225/20 , C07C229/16 , C07C233/40 , C07C233/44 , C07C233/78 , C07C239/16 , C07C251/48 , C07C323/32 , C07C2601/04 , C07C2601/14 , C07D209/14 , C07D213/38 , C07D333/20
摘要： Compounds of formula (I): {wherein: R1 and R2 each represents a variety of organic groups; R3 and R4 each represents hydrogen or a variety of organic groups; A represents a group of formula (A-1): [wherein: R5 represents hydrogen, hydroxy or alkyl, R6 represents hydroxy, alkoxy, alkylthio or an amine residue, X and Y each represents oxygen or sulfur, and Z represents a direct single bond between the nitrogen atom shown and the benzene ring shown in formula (I), or an alkylene group], G represents a single bond, alkylene or substituted alkylene; the broken line represents a single or double bond; when the broken line represents a double bond, D represents a carbon atom; and E represents an ═N—O— group; when the broken line represents a single bond, D represents a CH group or a nitrogen atom, and E represents an oxygen atom, a sulfur atom, an —NH— group or a —CO— group}; and pharmaceutically acceptable salts, esters or other derivatives thereof have the ability to inhibit an ileal bile transporter and so may be used to treat or prevent hypercholesterolemia.
摘要翻译：式（I）化合物：其中：R 1和R 2各自表示各种有机基团; R3和R4各自表示氢或各种有机基团; A表示式（A-1）基团：其中：R5表示氢，羟基或烷基，R6表示羟基，烷氧基，烷硫基或胺残基，X和Y各自表示氧或硫，Z表示直接单所示的氮原子和式（I）所示的苯环之间的键或亚烷基]，G表示单键，亚烷基或取代的亚烷基; 虚线表示单键或双键; 当虚线代表双键时，D表示碳原子; E表示= N-O-基; 当虚线表示单键时，D表示CH基或氮原子，E表示氧原子，硫原子，-NH-基或-CO-基}。其药学上可接受的盐，酯或其它衍生物具有抑制回肠胆汁转运蛋白的能力，因此可用于治疗或预防高胆固醇血症。

5. 发明授权

US5536714A Steroid derivatives for the treatment of prostatic hypertrophy their preparation and uses 失效
标题翻译：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
申请人： Koichi Kojima , Hitoshi Kurata , Koki Ishibashi , Hiroyoshi Horikoshi , Takakazu Hamada
发明人： Koichi Kojima , Hitoshi Kurata , Koki Ishibashi , Hiroyoshi Horikoshi , Takakazu Hamada
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。

6. 发明申请

US20070249620A1 Urea Derivative 审中-公开
标题翻译：尿素衍生物
公开(公告)号：US20070249620A1
公开(公告)日：2007-10-25
申请号：US11631179
申请日：2005-07-01
申请人： Hitoshi Kurata , Yoshikazu Uto , Yuko Fujibayashi , Takafumi Kohama , Tatsuo Tanimoto , Hiroshi Karasawa
发明人： Hitoshi Kurata , Yoshikazu Uto , Yuko Fujibayashi , Takafumi Kohama , Tatsuo Tanimoto , Hiroshi Karasawa
IPC分类号： A61K31/44 , A61K31/445 , A61K31/47 , A61K31/497 , A61P3/04 , C07D211/30 , C07D211/70 , C07D215/38 , C07D241/04 , C07D401/04
CPC分类号： C07D295/205 , C07D211/26 , C07D213/75 , C07D217/22 , C07D217/24 , C07D217/26 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to a urea derivative or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect. A urea derivative having the formula: [wherein R1 is a C6-C10 aryl group which may be independently mono- to pentasubstituted by a group selected from Substituent Group a or others; R is a C6-C10 aryl group which may be independently mono- to pentasubstituted by a group selected from Substituent Group a or others; E is a group having the formula (II) or the formula (III) (wherein R3 is a hydrogen atom or others; R4 and R5, which are the same or different, are a hydrogen atom or others; X and U, which are the same or different, are a group represented by the formula CH or others; m and n, which are the same or different, are I or another number) or others; and A is a group represented by the formula —NH—C(═O)— or others], or a pharmacologically acceptable salt thereof.
摘要翻译：本发明涉及具有优异DGAT抑制作用的尿素衍生物或其药理学上可接受的盐。具有下式的脲衍生物：其中R 1是C 6 -C 10芳基，其可以独立地被单价五价取代的C 6 -C 10芳基选自取代基组a或其他组的组; R是可以被选自取代基组a或其它基团的基团独立地单 - 五取代的C 6 -C 10 - 芳基; E是具有式（II）或式（III）的基团（其中R 3是氢原子或其它; R 4和R 5，相同或不同的氢原子或其它基团; X和U相同或不同，为由式CH或其它基团表示的基团; m和n相同或不同是我还是其他人）或其他人; A为由式-NH-C（-O） - 或其它]表示的基团，或其药理学上可接受的盐。

7. 发明授权

US6159967A Heterocyclic compounds having tachykinin receptor antagonist activity their preparation and their use 失效
标题翻译：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。

8. 发明授权

US5760025A Steroid derivatives for the treatment of prostatic hypertrophy, their preparation and uses 失效
标题翻译：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
申请人： Koichi Kojima , Hitoshi Kurata , Koki Ishibashi , Hiroyoshi Horikoshi , Takakazu Hamada
发明人： Koichi Kojima , Hitoshi Kurata , Koki Ishibashi , Hiroyoshi Horikoshi , Takakazu Hamada
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。

9. 发明授权

US5717088A Method of making steroid derivatives for the treatment of prostatic hypertrophy 失效
标题翻译：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
申请人： Koichi Kojima , Hitoshi Kurata , Koki Ishibashi , Hiroyoshi Horikoshi , Takakazu Hamada
发明人： Koichi Kojima , Hitoshi Kurata , Koki Ishibashi , Hiroyoshi Horikoshi , Takakazu Hamada
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。

10. 发明授权

US5698720A Steroid derivatives 失效
标题翻译：类固醇衍生物
公开(公告)号：US5698720A
公开(公告)日：1997-12-16
申请号：US631809
申请日：1996-04-12
申请人： Koichi Kojima , Hitoshi Kurata , Koki Ishibashi , Hiroyoshi Horikoshi , Takakazu Hamada
发明人： Koichi Kojima , Hitoshi Kurata , Koki Ishibashi , Hiroyoshi Horikoshi , Takakazu Hamada
IPC分类号： C07J41/00 , C07J43/00 , C07J3/00
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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式