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1. 发明授权

US07176240B2 Pentanoic acid derivatives 失效
公开(公告)号：US07176240B2
公开(公告)日：2007-02-13
申请号：US10194247
申请日：2002-07-15
申请人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
发明人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
IPC分类号： A01N37/00 , A61K31/20 , A61K31/19 , A61K31/231 , C07C63/04
CPC分类号： C07D213/75 , A61K31/19 , C07C53/21 , C07C69/612 , C07C69/63 , C07C69/708 , C07C233/05 , C07C233/11 , C07C233/25 , C07C233/47 , C07C233/54 , C07C323/52 , C07D295/185
摘要： The compound of the formula (I): wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together a saturated heterocyclic ring or amino acid residues; and non-toxic salts thereof and acid addition salts thereof. The compounds of the present invention of the formula (I) and the compounds of the formula (X): wherein n is 0 or 1, R11 is hydrogen and chlorine, R5 is R7—CH2— or R8, or R5 and R11, taken together is alkylidene; R6 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR9R10, in which R9, R10 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl-substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R9 and R10, taken together a saturated heterocyclic ring or amino acid residues, R7 is (i) F—(CH2)m— or F3C—CH2—, (ii) alkyl substituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R8 is alkyl, alkenyl, alkoxy, alkylthio, cycloalkyl, phenyl, phenoxy; non-toxic salts and acid addition salts thereof are useful for prevention and/or treatment for neurodegenerarive disease (Alzheimer's disease etc.) and neuronal dysfunction by stroke or traumic injury (Multiple sclerosis etc.) etc.

2. 发明授权

US07569609B2 Pentanoic acid derivatives 失效
标题翻译：戊酸衍生物
公开(公告)号：US07569609B2
公开(公告)日：2009-08-04
申请号：US11192004
申请日：2005-07-29
申请人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
发明人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
IPC分类号： A61K31/19 , A61K31/192 , A61K31/20
CPC分类号： C07D213/75 , A61K31/19 , C07C53/21 , C07C69/612 , C07C69/63 , C07C69/708 , C07C233/05 , C07C233/11 , C07C233/25 , C07C233/47 , C07C233/54 , C07C323/52 , C07D295/185
摘要： Formula (I) compounds: wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl subsituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof. Also, Formula (X) compounds: wherein n is 0 or 1, R11 is hydrogen and chlorine, R5 is R7—CH2— or R8, or R5 and R11, taken together is alkylidene; R6 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR9R10, in which R9, R10 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl-substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R9 and R10, taken together is a saturated heterocyclic ring or amino acid residue, R7 is (i) F—(CH2)m- or F3C—CH2—, (ii) alkyl substituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R8 is alkyl, alkenyl, alkoxy, alkylthio, cycloalkyl, phenyl, phenoxy. Non-toxic and acid addition salts thereof are useful to prevent and/or treat neurodegenerative disease (e.g., Alzheimer's) and neuronal dysfunction by stroke or traumatic injury (e.g., Multiple sclerosis).
摘要翻译：式（I）化合物：其中R1是被氟取代的烷基; R2是羟基，烷氧基，被苯基取代的烷氧基，NR3R4，其中R3，R4是（i）氢，（ii）烷基，（iii）苯基，（iv）被烷氧基或羧基取代的苯基，（v）氮原子，（vi）被苯基取代的烷基，被烷氧基或羧基取代的苯基，含有氮原子的杂环，（vii）与R3和R4键合的氮原子一起是饱和杂环或氨基酸残基; 及其无毒盐及其酸加成盐。另外，式（X）化合物：其中n为0或1，R11为氢和氯，R5为R7-CH2-或R8，或R5和R11为亚烷基; R6是羟基，烷氧基，被苯基取代的烷氧基，NR9R10，其中R9，R10是（i）氢，（ii）烷基，（iii）苯基，（iv）被烷氧基或羧基取代的苯基，（v）氮原子，（vi）被苯基取代的烷基，被烷氧基或羧基取代的苯基，含氮原子的杂环，（vii）与R 9和R 10结合的氮一起是饱和的杂环或氨基酸残基，R7是（ⅰ）F-（CH2）m-或F3C-CH2-，（ⅱ）被氯取代的烷基，（ⅲ）被烷氧基，环烷基，苯基，苯氧基取代的烷基; R8是烷基，烯基，烷氧基，烷硫基，环烷基，苯基，苯氧基。其无毒和酸加成盐可用于预防和/或治疗神经变性疾病（例如阿尔茨海默氏症）和神经元功能障碍（卒中或创伤性损伤（例如多发性硬化））。

3. 发明申请

US20050267168A1 Pentanoic acid derivatives 审中-公开
公开(公告)号：US20050267168A1
公开(公告)日：2005-12-01
申请号：US11192003
申请日：2005-07-29
申请人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
发明人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
IPC分类号： A61K31/20 , A61K31/00 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/197 , A61K31/22 , A61K31/23 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P25/00 , A61P25/04 , A61P25/28 , A61P43/00 , C07B61/00 , C07C51/06 , C07C51/36 , C07C53/126 , C07C53/128 , C07C53/134 , C07C53/19 , C07C53/21 , C07C53/23 , C07C57/03 , C07C57/30 , C07C59/125 , C07C59/135 , C07C59/68 , C07C67/303 , C07C69/02 , C07C69/22 , C07C69/24 , C07C69/34 , C07C69/533 , C07C69/612 , C07C69/63 , C07C69/708 , C07C231/12 , C07C233/05 , C07C233/07 , C07C233/11 , C07C233/12 , C07C233/22 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/54 , C07C323/52 , C07D213/40 , C07D213/72 , C07D213/75 , C07D295/18 , C07D295/185
CPC分类号： C07D213/75 , A61K31/19 , C07C53/21 , C07C69/612 , C07C69/63 , C07C69/708 , C07C233/05 , C07C233/11 , C07C233/25 , C07C233/47 , C07C233/54 , C07C323/52 , C07D295/185
摘要： Formula (I) compounds: wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl subsituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof. Also, Formula (X) compounds: wherein n is 0 or 1, R11 is hydrogen and chlorine, R5 is R7—CH2— or R8, or R5 and R11, taken together is alkylidene; R6 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR9R10, in which R9, R10 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl-substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R9 and R10, taken together is a saturated heterocyclic ring or amino acid residue, R7 is (i) F—(CH2)m— or F3C—CH2—, (ii) alkyl subsstituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R8 is alkyl, alkenyl, alkoxy, alkylthio, cycloalkyl, phenyl, phenoxy. Non-toxic and acid addition salts thereof are useful to prevent and/or treat neurodegenerative disease (e.g., Alzheimer's) and neuronal dysfunction by stroke or traumatic injury (e.g., Multiple sclerosis).

4. 发明申请

US20050261371A1 Pentanoic acid derivatives 失效
公开(公告)号：US20050261371A1
公开(公告)日：2005-11-24
申请号：US11192004
申请日：2005-07-29
申请人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
发明人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
IPC分类号： A61K31/20 , A61K31/00 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/197 , A61K31/22 , A61K31/23 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P25/00 , A61P25/04 , A61P25/28 , A61P43/00 , C07B61/00 , C07C51/06 , C07C51/36 , C07C53/126 , C07C53/128 , C07C53/134 , C07C53/19 , C07C53/21 , C07C53/23 , C07C57/03 , C07C57/30 , C07C59/125 , C07C59/135 , C07C59/68 , C07C67/303 , C07C69/02 , C07C69/22 , C07C69/24 , C07C69/34 , C07C69/533 , C07C69/612 , C07C69/63 , C07C69/708 , C07C231/12 , C07C233/05 , C07C233/07 , C07C233/11 , C07C233/12 , C07C233/22 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/54 , C07C323/52 , C07D213/40 , C07D213/72 , C07D213/75 , C07D295/18 , C07D295/185
CPC分类号： C07D213/75 , A61K31/19 , C07C53/21 , C07C69/612 , C07C69/63 , C07C69/708 , C07C233/05 , C07C233/11 , C07C233/25 , C07C233/47 , C07C233/54 , C07C323/52 , C07D295/185
摘要： Formula (I) compounds: wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl subsituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof. Also, Formula (X) compounds: wherein n is 0 or 1, R11 is hydrogen and chlorine, R5 is R7—CH2— or R8, or R5 and R11, taken together is alkylidene; R6 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR9R10, in which R9, R10 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl-substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R9 and R10, taken together is a saturated heterocyclic ring or amino acid residue, R7 is (i) F—(CH2)m- or F3C—CH2—, (ii) alkyl substituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R8 is alkyl, alkenyl, alkoxy, alkylthio, cycloalkyl, phenyl, phenoxy. Non-toxic and acid addition salts thereof are useful to prevent and/or treat neurodegenerative disease (e.g., Alzheimer's) and neuronal dysfunction by stroke or traumatic injury (e.g., Multiple sclerosis).

5. 发明授权

US06201021B1 Pentanoic acid derivatives 失效
标题翻译：戊酸衍生物
公开(公告)号：US06201021B1
公开(公告)日：2001-03-13
申请号：US08681482
申请日：1996-07-23
申请人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
发明人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
IPC分类号： A61K3119
CPC分类号： C07D213/75 , A61K31/19 , C07C53/21 , C07C69/612 , C07C69/63 , C07C69/708 , C07C233/05 , C07C233/11 , C07C233/25 , C07C233/47 , C07C233/54 , C07C323/52 , C07D295/185
摘要： Formula (I) compounds: wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl subsituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof. Also, Formula (X) compounds: wherein n is 0 or 1, R11 is hydrogen and chlorine, R5 is R7—CH2— or R8, or R5 and R11, taken together is alkylidene; R6 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR9R10, in which R9, R10 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl-substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R9 and R10, taken together is a saturated heterocyclic ring or amino acid residue, R7 is (i) F—(CH2)m— or F3C—CH2—, (ii) alkyl subsstituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R8 is alkyl, alkenyl, alkoxy, alkylthio, cycloalkyl, phenyl, phenoxy. Non-toxic and acid addition salts thereof are useful to prevent and/or treat neurodegenerative disease (e.g., Alzheimer's) and neuronal dysfunction by stroke or traumatic injury (e.g., Multiple sclerosis).
摘要翻译：式（I）化合物：其中R1是被氟取代的烷基; R2是羟基，烷氧基，被苯基取代的烷氧基，NR3R4，其中R3，R4是（i）氢，（ii）烷基，（iii）苯基，（iv）被烷氧基或羧基取代的苯基，（v）氮原子，（vi）被苯基取代的烷基，被烷氧基或羧基取代的苯基，含有氮原子的杂环，（vii）与R3和R4键合的氮原子一起是饱和杂环或氨基酸残基; 及其无毒盐及其酸加成盐。另外，式（X）化合物：其中n为0或1，R11为氢和氯，R5为R7-CH2-或R8，或R5和R11为亚烷基; R6是羟基，烷氧基，被苯基取代的烷氧基，NR9R10，其中R9，R10是（i）氢，（ii）烷基，（iii）苯基，（iv）被烷氧基或羧基取代的苯基，（v）氮原子，（vi）被苯基取代的烷基，被烷氧基或羧基取代的苯基，含氮原子的杂环，（vii）与R 9和R 10结合的氮一起是饱和的杂环或氨基酸残基，R7是（ⅰ）F-（CH2）m-或F3C-CH2-，（ⅱ）由氯取代的烷基，（ⅲ）被烷氧基，环烷基，苯基，苯氧基取代的烷基; R8是烷基，烯基，烷氧基，烷硫基，环烷基，苯基，苯氧基。其无毒和酸加成盐可用于预防和/或治疗神经变性疾病（例如阿尔茨海默氏症）和神经元功能障碍（卒中或创伤性损伤（例如多发性硬化））。

6. 发明授权

US07569608B2 Pentanoic acid derivatives 失效
标题翻译：戊酸衍生物
公开(公告)号：US07569608B2
公开(公告)日：2009-08-04
申请号：US11192002
申请日：2005-07-29
申请人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
发明人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
IPC分类号： A61K31/19 , A61K31/192 , A61K31/20
CPC分类号： C07D213/75 , A61K31/19 , C07C53/21 , C07C69/612 , C07C69/63 , C07C69/708 , C07C233/05 , C07C233/11 , C07C233/25 , C07C233/47 , C07C233/54 , C07C323/52 , C07D295/185
摘要： Formula (I) compounds: wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof. Also, Formula (X) compounds: wherein n is 0 or 1, R11 is hydrogen and chlorine, R5 is R7—CH2— or R8, or R5 and R11, taken together is alkylidene; R6 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR9R10, in which R9, R10 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl-substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R9 and R10, taken together is a saturated heterocyclic ring or amino acid residue, R7 is (i) F—(CH2)m- or F3C—CH2—, (ii) alkyl substituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R8 is alkyl, alkenyl, alkoxy, alkylthio, cycloalkyl, phenyl, phenoxy. Non-toxic and acid addition salts thereof are useful to prevent and/or treat neurodegenerative disease (e.g., Alzheimer's) and neuronal dysfunction by stroke or traumatic injury (e.g., Multiple sclerosis).
摘要翻译：式（I）化合物：其中R1是被氟取代的烷基; R2是羟基，烷氧基，被苯基取代的烷氧基，NR3R4，其中R3，R4是（i）氢，（ii）烷基，（iii）苯基，（iv）被烷氧基或羧基取代的苯基，（v）氮原子，（vi）被苯基取代的烷基，被烷氧基或羧基取代的苯基，含氮原子的杂环，（vii）与R3和R4键合的氮原子一起是饱和杂环或氨基酸残基; 及其无毒盐及其酸加成盐。另外，式（X）化合物：其中n为0或1，R11为氢和氯，R5为R7-CH2-或R8，或R5和R11为亚烷基; R6是羟基，烷氧基，被苯基取代的烷氧基，NR9R10，其中R9，R10是（i）氢，（ii）烷基，（iii）苯基，（iv）被烷氧基或羧基取代的苯基，（v）氮原子，（vi）被苯基取代的烷基，被烷氧基或羧基取代的苯基，含氮原子的杂环，（vii）与R 9和R 10结合的氮一起是饱和的杂环或氨基酸残基，R7是（ⅰ）F-（CH2）m-或F3C-CH2-，（ⅱ）被氯取代的烷基，（ⅲ）被烷氧基，环烷基，苯基，苯氧基取代的烷基; R8是烷基，烯基，烷氧基，烷硫基，环烷基，苯基，苯氧基。其无毒和酸加成盐可用于预防和/或治疗神经变性疾病（例如阿尔茨海默氏症）和神经元功能障碍（卒中或创伤性损伤（例如多发性硬化））。

7. 发明申请

US20050267167A1 Pentanoic acid derivatives 失效
公开(公告)号：US20050267167A1
公开(公告)日：2005-12-01
申请号：US11192002
申请日：2005-07-29
申请人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
发明人： Shuichi Ohuchida , Kazuo Kishimoto , Narito Tateishi , Hiroyuki Ohno
IPC分类号： A61K31/20 , A61K31/00 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/197 , A61K31/22 , A61K31/23 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P25/00 , A61P25/04 , A61P25/28 , A61P43/00 , C07B61/00 , C07C51/06 , C07C51/36 , C07C53/126 , C07C53/128 , C07C53/134 , C07C53/19 , C07C53/21 , C07C53/23 , C07C57/03 , C07C57/30 , C07C59/125 , C07C59/135 , C07C59/68 , C07C67/303 , C07C69/02 , C07C69/22 , C07C69/24 , C07C69/34 , C07C69/533 , C07C69/612 , C07C69/63 , C07C69/708 , C07C231/12 , C07C233/05 , C07C233/07 , C07C233/11 , C07C233/12 , C07C233/22 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/54 , C07C323/52 , C07D213/40 , C07D213/72 , C07D213/75 , C07D295/18 , C07D295/185
CPC分类号： C07D213/75 , A61K31/19 , C07C53/21 , C07C69/612 , C07C69/63 , C07C69/708 , C07C233/05 , C07C233/11 , C07C233/25 , C07C233/47 , C07C233/54 , C07C323/52 , C07D295/185
摘要： Formula (I) compounds: wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl subsituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof. Also, Formula (X) compounds: wherein n is 0 or 1, R11 is hydrogen and chlorine, R5 is R7—CH2— or R8, or R5 and R11, taken together is alkylidene; R6 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR9R10, in which R9, R10 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl-substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R9 and R10, taken together is a saturated heterocyclic ring or amino acid residue, R7 is (i) F—(CH2)m— or F3C—CH2—, (ii) alkyl subsstituted by chlorine, (iii) alkyl substituted by alkoxy, cycloalkyl, phenyl, phenoxy; R8 is alkyl, alkenyl, alkoxy, alkylthio, cycloalkyl, phenyl, phenoxy. Non-toxic and acid addition salts thereof are useful to prevent and/or treat neurodegenerative disease (e.g., Alzheimer's) and neuronal dysfunction by stroke or traumatic injury (e.g., Multiple sclerosis).

8. 发明授权

US5411974A Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US5411974A
公开(公告)日：1995-05-02
申请号：US265734
申请日：1994-06-27
申请人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
发明人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
IPC分类号： C07D207/08 , C07D277/04 , C07D405/04 , C07D417/06 , A61K31/425
CPC分类号： C07D207/08 , C07D277/04 , C07D405/04 , C07D417/06
摘要： Heterocyclic compounds of the general formula: ##STR1## wherein, Z represents methylene group or sulfur atom, R represents a general formula:G--E--D--B--A--.
摘要翻译：具有以下通式的杂环化合物：其中Z表示亚甲基或硫原子，R表示通式：G-E-D-B-A-。

9. 发明授权

US5340832A Prolinal derivatives useful for treating amnesia 失效
标题翻译：用于治疗遗忘症的脯氨酸衍生物
公开(公告)号：US5340832A
公开(公告)日：1994-08-23
申请号：US107314
申请日：1993-08-17
申请人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
发明人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
IPC分类号： A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P25/28 , C07D207/08 , C07D401/12 , C07D405/12 , C07D409/12 , A61K31/52
CPC分类号： C07D207/08 , C07D405/12
摘要： A novel prolinal derivative of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms, R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.
摘要翻译：一种新颖的通式如下的流延衍生物：其中A表示1至8个碳原子的亚烷基或亚烯基或3至7个碳原子的饱和烃环，R表示氢原子苯基，苄基，1〜8个碳原子的烷基或3〜7个碳原子的环烷基，B表示1〜8个未被取代或被苯基取代或被苯基取代的亚烷基，苄基或单键，D表示未被取代或被1至3个卤素原子，1至4个碳原子的烷基或烷氧基，硝基或三氟甲基取代的碳环或杂环。]具有抑制性对脯氨酰内肽酶的活性，因此可用于治疗和/或预防药物作为遗忘。

10. 发明授权

US5254550A Prolinal derivatives and pharmaceutical compositions thereof 失效
标题翻译：脯氨酸衍生物及其药物组合物
公开(公告)号：US5254550A
公开(公告)日：1993-10-19
申请号：US803421
申请日：1991-12-06
申请人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
发明人： Masaaki Toda , Shuichi Ohuchida , Hiroyuki Ohno
IPC分类号： C07D207/08 , C07D405/12 , A61K31/495 , C07D401/12
CPC分类号： C07D207/08 , C07D405/12
摘要： A novel prolinal derivative of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms,R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group]posses inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent for amnesia.
摘要翻译：一种新颖的通式如下的流延衍生物：其中A表示1至8个碳原子的亚烷基或亚烯基或3至7个碳原子的饱和烃环，R表示氢原子苯基，苄基，1〜8个碳原子的烷基或3〜7个碳原子的环烷基，B表示1〜8个未被取代或被苯基取代或被苯基取代的亚烷基，苄基或单键，D表示未被取代或被1至3个卤素原子，1至4个碳原子的烷基或烷氧基，硝基或三氟甲基取代的碳环或杂环]具有抑制活性在脯氨酰内肽酶上，因此可用于治疗和/或预防健忘症药物。

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