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1. 发明授权

US5891916A Aromatic hydroxamix acid compounds, their production and use 失效
标题翻译：芳香族异羟肟酸化合物，其生产和使用
公开(公告)号：US5891916A
公开(公告)日：1999-04-06
申请号：US662240
申请日：1996-06-14
申请人： Kaneyoshi Kato , Yoshihiro Sugiura , Ken-ichi Naruo , Hideki Takahashi
发明人： Kaneyoshi Kato , Yoshihiro Sugiura , Ken-ichi Naruo , Hideki Takahashi
IPC分类号： C07C259/06 , C07C271/60 , C07D277/30 , C07C239/08 , A61K31/19 , C07D277/00
CPC分类号： C07C271/60 , C07C259/06
摘要： A compound represented by the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; Q represents an optionally substituted divalent aliphatic hydrocarbon group optionally containing O or S; R.sup.1 represents H, acyl group, etc.; and X represents an electron-withdrawing group, an optionally substituted aromatic group, a group of the formula: ##STR2## wherein R.sup.2 and R.sup.3 independently represent H, acyl group or an optionally substituted hydrocarbon group, etc., etc.; or salts thereof are useful as an excellent anti-neurodegenerative agent.
摘要翻译：由下式表示的化合物：其中Ar 1和Ar 2独立地表示任选取代的芳基; Q表示任选含有O或S的任选取代的二价脂族烃基; R1代表H，酰基等; X表示吸电子基团，可以具有取代基的芳基，下式的基团：其中R2和R3独立地表示H，酰基或任意取代的烃基等; 或其盐可用作优异的抗神经变性剂。

2. 发明授权

US5804601A Aromatic hydroxamic acid compounds, their production and use 失效
标题翻译：芳香族异羟肟酸化合物，其生产和使用
公开(公告)号：US5804601A
公开(公告)日：1998-09-08
申请号：US629623
申请日：1996-04-09
申请人： Kaneyoshi Kato , Shokyo Miki , Ken-ichi Naruo , Hideki Takahashi
发明人： Kaneyoshi Kato , Shokyo Miki , Ken-ichi Naruo , Hideki Takahashi
IPC分类号： C07C259/06 , C07D215/14 , C07D215/20 , C07D217/14 , C07D235/16 , C07D263/56 , C07D277/64 , C07D513/04 , A61K31/165
CPC分类号： C07D263/56 , C07C259/06 , C07D215/14 , C07D215/20 , C07D217/14 , C07D235/16 , C07D277/64 , C07D513/04
摘要： The present invention relates to a compound of the formula: ##STR1## wherein Ar represents an optionally substituted aromatic group; Q represents a divalent aliphatic hydrocarbon group; R.sub.1 represents hydrogen, cyano, an optionally substituted hydrocarbon group, a group of the formula: ##STR2## wherein R.sup.3 and R.sub.4 independently represent hydrogen, acyl or an optionally substituted hydrocarbon group, or R.sup.3 and R.sup.4 jointly form a ring, or acyl; R.sup.2 represents acyl; ......... represents a single bond or a double bond; m represents 1 or 2 or a salt, a process of producing thereof and an anti-neurodegenerative composition.
摘要翻译：本发明涉及下式的化合物：其中Ar表示任选取代的芳族基团; Q表示二价脂族烃基; R 1表示氢，氰基，任选取代的烃基，下式的基团：其中R 3和R 4独立地表示氢，酰基或任选取代的烃基，或者R 3和R 4共同形成环或酰基; R2代表酰基; + E，ovs ......... + EE表示单键或双键; m表示1或2或其盐，其制备方法和抗神经变性组合物。

3. 发明授权

US5607939A Condensed heterocyclic compounds, their production and use 失效
标题翻译：稠合杂环化合物，其生产和使用
公开(公告)号：US5607939A
公开(公告)日：1997-03-04
申请号：US428499
申请日：1995-04-25
申请人： Kaneyoshi Kato , Yoshihiro Sugiura , Koichi Kato , Yasuo Nagai
发明人： Kaneyoshi Kato , Yoshihiro Sugiura , Koichi Kato , Yasuo Nagai
IPC分类号： C07D217/14 , C07D311/76 , C07D401/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/10 , C07D495/10 , C07D521/00 , A61K31/44
CPC分类号： C07D249/08 , C07D217/14 , C07D231/12 , C07D233/56 , C07D311/76 , C07D401/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/10 , C07D495/10
摘要： The compound ##STR1## wherein ring A represents a benzene ring; Ar represents an aromatic group; R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group; m represents an integer of 1 to 6; n represents an integer of 2 to 3; ----- represents a single bond or a double bond; X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where ----- is a single bond or .dbd.N-- where ----- is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.
摘要翻译：化合物＆lt; IMAGE＆gt;其中环A表示苯环; Ar表示芳基; R 1和R 2独立地表示氢，酰基或烃基，或者R 1和R 2与相邻的氮原子一起表示含氮杂环基; m表示1〜6的整数， n表示2〜3的整数， + E，uns ----- + EE表示单键或双键; X代表-O-或-NR3-，其中R3表示氢，酰基或烃基，其中+ E，uns ----- + EE是单键或= N-，其中+ E， + EE是具有优异的GnRH受体拮抗活性，钙拮抗和单胺摄取抑制活性的双键，并且作为性激素依赖性疾病和中枢神经系统疾病的预防/治疗药物。

4. 发明授权

US5654296A Condensed heterocyclic compounds, their production and use 失效
标题翻译：稠合杂环化合物，其生产和使用
公开(公告)号：US5654296A
公开(公告)日：1997-08-05
申请号：US760904
申请日：1996-12-06
申请人： Kaneyoshi Kato , Yoshihiro Sugiura , Koichi Kato , Yasuo Nagai
发明人： Kaneyoshi Kato , Yoshihiro Sugiura , Koichi Kato , Yasuo Nagai
IPC分类号： C07D217/14 , C07D311/76 , C07D401/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/10 , C07D495/10 , C07D521/00 , C07D223/16 , A61K31/55
CPC分类号： C07D249/08 , C07D217/14 , C07D231/12 , C07D233/56 , C07D311/76 , C07D401/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/10 , C07D495/10
摘要： The compound ##STR1## wherein ring A represents a benzene ring;Ar represents an aromatic group;R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group;m represents an integer of 1 to 6;n represents an integer of 2 to 3;- - - - - represents a single bond or a double bond;X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where - - - - - is a single bond or .dbd.N-- where - - - - - is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.
摘要翻译：化合物＆lt; IMAGE＆gt;其中环A表示苯环; Ar表示芳基; R 1和R 2独立地表示氢，酰基或烃基，或者R 1和R 2与相邻的氮原子一起表示含氮杂环基; m表示1〜6的整数， n表示2〜3的整数， + E，非 - - - + EE表示单键或双键; X代表-O-或-NR3-，其中R3代表氢，酰基或烃基，其中+ E，非 - - - + EE是单键或= N-，其中+ E，非 - + EE是具有优异的GnRH受体拮抗活性，钙拮抗和单胺摄取抑制活性的双键，并且作为性激素依赖性疾病和中枢神经系统疾病的预防/治疗药物。

5. 发明授权

US5633248A Amine compounds, their production and use 失效
标题翻译：胺化合物，其生产和使用
公开(公告)号：US5633248A
公开(公告)日：1997-05-27
申请号：US561282
申请日：1995-11-21
申请人： Kaneyoshi Kato , Yoshihiro Sugiura , Koichi Kato
发明人： Kaneyoshi Kato , Yoshihiro Sugiura , Koichi Kato
IPC分类号： C07C233/40 , C07C235/84 , C07C311/18 , C07D209/96 , C07D211/14 , C07D211/22 , C07D213/38 , C07D221/10 , C07D221/20 , C07D223/14 , C07D223/16 , C07D241/38 , C07D265/34 , C07D295/125 , C07D401/12 , C07D405/12 , C07D409/12 , C07D491/10 , C07D221/00 , A61K31/40 , A61K31/41 , A61K31/44 , A61K31/47 , C07D211/00 , C07D241/00 , C07D295/00
CPC分类号： C07D221/20 , C07C233/40 , C07C235/84 , C07C311/18 , C07D209/96 , C07D211/14 , C07D211/22 , C07D213/38 , C07D221/10 , C07D223/14 , C07D223/16 , C07D241/38 , C07D265/34 , C07D295/125 , C07D401/12 , C07D405/12 , C07D409/12 , C07D491/10
摘要： A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.
摘要翻译：下式的化合物：其中Ar 1和Ar 2独立地表示任选取代的芳族基团; P和Q独立地表示在碳链中具有至少2个碳原子并任选具有氧或硫的二价脂族烃基; R1和R3独立地表示-CO-R，-CONH-R（R表示烃基或杂环基）或烃基; R2和R4独立地表示氢或烷基; R2和R4独立地表示氢或烷基; R1和R2或R3和R4与相邻的氮原子一起可以形成含氮杂环基; 并且j表示0或1或其盐具有优异的GnRH受体拮抗活性，并且可用作激素依赖性和其它疾病的预防和治疗剂。

6. 发明授权

US06784314B2 Process for producing amine derivatives 失效
标题翻译：制备胺衍生物的方法
公开(公告)号：US06784314B2
公开(公告)日：2004-08-31
申请号：US10240574
申请日：2002-10-01
申请人： Makoto Yamashita , Kaneyoshi Kato , Hiroyuki Tawada
发明人： Makoto Yamashita , Kaneyoshi Kato , Hiroyuki Tawada
IPC分类号： C07C23305
CPC分类号： C07C235/34 , C07B2200/07 , C07C217/74 , C07C2602/10
摘要： This invention provides a convenient and industrially advantageous process producing amine derivatives having the action of inhibiting the secretion and accumulation of amyloid &bgr; protein. In Compound (I), the ether linkage is selectively cleaved without cleaving the amide linkage present in the same molecule and tertiary amines are not converted into quaternary salts, and thus Amine Derivative (V) with good qualities having the action of inhibiting the secretion and accumulation of amyloid &bgr; protein can be obtained in high yield.
摘要翻译：本发明提供了方便和工业上有利的方法，产生具有抑制淀粉样蛋白β蛋白分泌和积累作用的胺衍生物。在化合物（I）中，醚键被选择性地切割而不裂解同一分子中存在的酰胺键和叔胺不会转化为季盐，因此可以高产率获得具有抑制淀粉样β蛋白分泌和积累作用的具有良好品质的胺衍生物（V）。

7. 发明授权

US07115750B1 Melanin concentrating hormone antagonist 失效
标题翻译：黑色素浓缩激素拮抗剂
公开(公告)号：US07115750B1
公开(公告)日：2006-10-03
申请号：US10088771
申请日：2000-09-19
申请人： Kaneyoshi Kato , Jun Terauchi , Masaaki Mori , Nobuhiro Suzuki , Yukio Shimomura , Shiro Takekawa , Yuji Ishihara
发明人： Kaneyoshi Kato , Jun Terauchi , Masaaki Mori , Nobuhiro Suzuki , Yukio Shimomura , Shiro Takekawa , Yuji Ishihara
IPC分类号： C09B5/00 , A61K3/41 , C07D209/56 , C07D487/00 , C07D491/00
CPC分类号： C07D207/277 , C07C217/74 , C07C219/28 , C07C233/29 , C07C233/44 , C07C233/80 , C07C235/42 , C07C235/50 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C271/28 , C07C275/42 , C07C311/21 , C07C2602/10 , C07C2602/12 , C07D209/18 , C07D209/22 , C07D209/42 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/32 , C07D211/52 , C07D211/62 , C07D211/70 , C07D213/56 , C07D213/81 , C07D213/82 , C07D215/14 , C07D215/38 , C07D233/24 , C07D239/28 , C07D239/30 , C07D261/18 , C07D263/14 , C07D263/34 , C07D265/28 , C07D271/06 , C07D295/096 , C07D295/13 , C07D295/185 , C07D307/68 , C07D307/81 , C07D311/58 , C07D317/60 , C07D319/20 , C07D333/24 , C07D333/28 , C07D333/38 , C07D335/16 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/12 , C07D493/04
摘要： A melanin-concentrating hormone antagonist which comprises a compound of the formula: wherein Ar1 is a cyclic group which may have substituents; X is a spacer having a main chain of 1 to 6 atoms; Y is a bond or a spacer having a main chain of 1 to 6 atoms; Ar is a monocyclic aromatic ring which may be condensed with a 4 to 8 membered non-aromatic ring, and may have further substituents; R1 and R2 are independently hydrogen atom or a hydrocarbon group which may have substituents; R1 and R2, together with the adjacent nitrogen atom, may form a nitrogen-containing hetero ring which may have substituents; R2 may form a spiro ring together with Ar; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing hetero ring which may have substituents; or a salt thereof; which is useful as an agent for preventing or treating obesity, etc.
摘要翻译：一种黑色素浓缩激素拮抗剂，其包含下式化合物：其中Ar 1是可以具有取代基的环状基团; X是具有1至6个原子的主链的间隔物; Y是具有1至6个原子的主链的键或间隔基; Ar是可以与4至8元非芳族环稠合的单环芳环，并且可以具有其它取代基; R 1和R 2独立地是氢原子或可以具有取代基的烃基; R 1和R 2与相邻的氮原子一起可以形成可以具有取代基的含氮杂环; R 2可以与Ar一起形成螺环; 或R 2连同相邻的氮原子和Y可以形成可具有取代基的含氮杂环; 或其盐; 其可用作预防或治疗肥胖症等的药剂。

8. 发明授权

US06613805B2 Amine compounds, their production and use 有权
标题翻译：胺化合物，其生产和使用
公开(公告)号：US06613805B2
公开(公告)日：2003-09-02
申请号：US09931140
申请日：2001-08-16
申请人： Kaneyoshi Kato , Jun Terauchi , Hiroaki Fukumoto , Mitsuru Kakihana
发明人： Kaneyoshi Kato , Jun Terauchi , Hiroaki Fukumoto , Mitsuru Kakihana
IPC分类号： A61K31137
CPC分类号： C07D213/30 , C07B2200/07 , C07C217/74 , C07C255/54 , C07C2602/10 , C07D215/14 , C07D215/20 , C07D215/58 , C07D271/06 , C07D277/64 , C07D295/096 , C07D307/80 , C07D317/54 , C07D333/16
摘要： A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc., (iv) —CO—O— or (v) —(CH2)p-X1—, —(CH2)p-X1-(CH2)q-, —(CH2)r-CO-X1-, —SO2—NR8— or —(CH2)r-SO2—NR8— wherein X1 is O or NR8, R8 is H, a hydrocarbon group which may be substituted or an acyl, p is 0 to 5, q is 1 to 5, p+q is 1 to 5, and r is 1 to 4; Y is a divalent C1-6 aliphatic hydrocarbon group optionally containing O or S, which may be substituted; R1 and R2 each is H or a lower alkyl which may be substituted, or R1 and R2 form a N-containing heterocyclic ring which may be substituted; Ring A is a benzene ring which may be further substituted; and Ring B is a 4- to 8-membered ring which may be further substituted, or a salt thereof has the effect of inhibiting amyloid-&bgr; protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.
摘要翻译：下式的化合物：其中Ar是可被取代的芳环组合基团或可被取代的稠合芳基; X是（i）键，（ii）-S-，-SO-或-SO 2 - ，（iii）C 1-6亚烷基，C 2-6亚烯基或C 2-6亚炔基等，（iv）-CO- O-或（V） - （CH 2）p -X 1 - ， - （CH 2）p -X 1 - （CH 2）q - ， - （CH 2）r -CO-X 1 - ，-SO 2 -NR 8 - 或 - （CH 2） r-SO 2 -NR 8 - ，其中X 1为O或NR 8，R 8为H，可被取代的烃基或酰基，p为0至5，q为1至5，p + q为1至5，r 是1到4; Y是任选地含有O或S的二价C 1-6脂族烃基，其可被取代; R 1和R 2各自为H或可被取代的低级烷基，或R 1和R 2形成可被取代的含氮杂环; 环A是可以被进一步取代的苯环; 环B为可进一步取代的4-至8-元环，或其盐具有抑制淀粉样蛋白β蛋白产生和/或分泌的作用，并且可用作预防和/或治疗神经变性疾病等

9. 发明授权

US06586475B1 &bgr;-amyloid protein production/secretion inhibitors 失效
标题翻译： β-淀粉样蛋白生成/分泌抑制剂
公开(公告)号：US06586475B1
公开(公告)日：2003-07-01
申请号：US09856317
申请日：2001-06-05
申请人： Kaneyoshi Kato , Jun Terauchi , Hiroaki Fukumoto , Mitsuru Kakihana
发明人： Kaneyoshi Kato , Jun Terauchi , Hiroaki Fukumoto , Mitsuru Kakihana
IPC分类号： A61K31165
CPC分类号： C07D213/82 , C07C217/60 , C07C235/34 , C07C235/50 , C07C237/22 , C07C237/42 , C07C237/44 , C07C311/21 , C07D295/088 , C07D295/13
摘要： A compound of the formula: wherein Ar is an aromatic group; X and Y are a bivalent group selected from —O—, —S—, —CO—, —SO2—, —NR8—, —CONR8—, SO2NR8 and —COO— (wherein R8 is H, a hydrocarbon group or acyl), or a bivalent C1-6 aliphatic hydrocarbon group which may contain one or two above bivalent groups; R1 and R2 are H or C1-6 alkyl, or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring; and ring A is a monocyclic aromatic ring, or a salt thereof or a prodrug thereof exhibits an excellent inhibitory activity of the production and/or the secretion of amyloid-&bgr; protein.
摘要翻译：下式的化合物：其中Ar是芳族基团; X和Y是选自-O - ， - S - ， - CO - ， - SO 2 - ， - NR 8 - ， - CONR 8 - ，SO 2 NR 8和-COO-（其中R 8是H，烃基或酰基），或可以含有一个或两个上述二价基团的二价C 1-6脂族烃基; R1和R2是H或C1-6烷基，或R1和R2可以与相邻的氮原子一起形成含氮杂环; 环A是单环芳环，或其盐或其前药对淀粉样蛋白-β蛋白的产生和/或分泌具有优异的抑制活性。

10. 发明授权

US06310107B1 Amine compounds, their production and use as amyloid-&bgr; production inhibitors 有权
标题翻译：胺化合物，其生产和用作淀粉样蛋白-β生产抑制剂
公开(公告)号：US06310107B1
公开(公告)日：2001-10-30
申请号：US09331460
申请日：1999-06-21
申请人： Kaneyoshi Kato , Jun Terauchi , Hiroaki Fukumoto , Mitsuru Kakihana
发明人： Kaneyoshi Kato , Jun Terauchi , Hiroaki Fukumoto , Mitsuru Kakihana
IPC分类号： A61K31137
CPC分类号： C07D213/30 , C07B2200/07 , C07C217/74 , C07C255/54 , C07C2602/10 , C07D215/14 , C07D215/20 , C07D215/58 , C07D271/06 , C07D277/64 , C07D295/096 , C07D307/80 , C07D317/54 , C07D333/16
摘要： A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc., (iv) —CO—O— or (v) —(CH2)p-X1—, —(CH2)p-X1— (CH2)q-, —(CH2)r-CO—X1—, —SO2—NR8— or —(CH2)r-SO2—NR8— wherein X1 is O or NR8, R8 is H, a hydrocarbon group which may be substituted or an acyl, p is 0 to 5, q is 1 to 5, p+q is 1 to 5, and r is 1 to 4; Y is a divalent C1-6 aliphatic hydrocarbon group optionally containing O or S, which may be substituted; R1 and R2 each is H or a lower alkyl which may be substituted, or R1 and R2 form a N-containing heterocyclic ring which may be substituted; Ring A is a benzene ring which may be further substituted; and Ring B is a 4- to 8-membered ring which may be further substituted, or a salt thereof has the effect of inhibiting amyloid-&bgr; protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.
摘要翻译：下式的化合物：其中Ar是可被取代的芳环组合基团或可被取代的稠合芳基; X是（i）键，（ii）-S-，-SO-或-SO 2 - ，（iii）C 1-6亚烷基，C 2-6亚烯基或C 2-6亚炔基等，（iv）-CO- O-或（V） - （CH 2）p -X 1 - ， - （CH 2）p -X 1 - （CH 2）q - ， - （CH 2）r -CO-X 1 - ，-SO 2 -NR 8 - 或 - （CH 2） r-SO 2 -NR 8 - ，其中X 1为O或NR 8，R 8为H，可被取代的烃基或酰基，p为0至5，q为1至5，p + q为1至5，r 是1到4; Y是任选地含有O或S的二价C 1-6脂族烃基，其可被取代; R 1和R 2各自为H或可被取代的低级烷基，或R 1和R 2形成可被取代的含氮杂环; 环A是可以被进一步取代的苯环; 环B为可进一步取代的4-至8-元环，或其盐具有抑制淀粉样蛋白β蛋白产生和/或分泌的作用，并且可用作预防和/或治疗神经变性疾病等

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