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公开(公告)号：US06362209B1
公开(公告)日：2002-03-26
申请号：US09398997
申请日：1999-09-17
IPC分类号： A61K3142
CPC分类号： C07D413/04 , C07C45/004 , C07C49/567 , C07C49/813 , C07C69/007 , C07C233/31 , C07C233/47 , C07C251/42 , C07C311/16 , C07C311/29 , C07C311/32 , C07C311/37 , C07C317/24 , C07C317/32 , C07C2601/14 , C07D263/32
摘要： A heterocyclic aromatic oxazole compound of the formula (I) wherein Z is an oxygen atom; one of R and R1 is a group of the formula wherein R3 is lower alkyl, amino or lower alkylamino, and R4, R5, R6 and R7 are the same or different and each is hydrogen atom, halogen atom, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy or amino, provided that at least one of R4, R5, R6 and R7 is not hydrogen atom, and the other is an optionally substituted cycloalkyl, an optionally substituted heterocyclic group or an optionally substituted aryl; and R2 is a lower alkyl or a halogenated lower alkyl, and a pharmaceutically acceptable salt thereof. The heterocyclic aromatic oxazole compound and pharmaceutically acceptable salts thereof have antipyretic action, analgesic action, anti-inflammatory action, and particularly, selective inhibitory action on cyclooxygenase-2 (COX-2), and are expected to be useful as anti-inflammatory agents with less side-effects such as digestive tract disorders.
摘要翻译： 式（I）的杂环芳族恶唑化合物，其中Z是氧原子; R和R中的一个是一个基团，其中R 3是低级烷基，氨基或低级烷基氨基，R 4，R 5，R 6和R 7相同或不同，各自为氢原子，卤素原子，低级烷基，低级烷氧基，三氟甲基 ，羟基或氨基，条件是R 4，R 5，R 6和R 7中的至少一个不是氢原子，另一个是任选取代的环烷基，任选取代的杂环基或任选取代的芳基; 和R2是低级烷基或卤代低级烷基，及其药学上可接受的盐。 杂芳基恶唑化合物及其药学上可接受的盐具有解热作用，止痛作用，抗炎作用，特别是对环氧合酶-2（COX-2）的选择性抑制作用，并且预期可用作抗炎剂， 较少的副作用如消化道疾病。
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公开(公告)号：US5994381A
公开(公告)日：1999-11-30
申请号：US693051
申请日：1996-08-19
IPC分类号： C12N9/99 , A61K31/42 , A61K31/421 , A61P25/04 , A61P29/00 , A61P43/00 , C07C45/00 , C07C49/563 , C07C49/567 , C07C49/792 , C07C49/813 , C07C69/007 , C07C233/31 , C07C233/47 , C07C235/74 , C07C251/40 , C07C251/42 , C07C311/16 , C07C311/29 , C07C311/32 , C07C311/37 , C07C317/22 , C07C317/24 , C07C317/32 , C07D263/30 , C07D263/32 , C07D413/02 , C07D413/04
CPC分类号： C07D413/04 , C07C233/31 , C07C233/47 , C07C251/42 , C07C311/16 , C07C311/29 , C07C311/32 , C07C311/37 , C07C317/24 , C07C317/32 , C07C45/004 , C07C49/567 , C07C49/813 , C07C69/007 , C07D263/32 , C07C2101/14
摘要： A heterocyclic aromatic oxazole compound of the formula (I) ##STR1## wherein Z is an oxygen atom; one of R and R.sub.1 is a group of the formula ##STR2## wherein R.sub.3 is lower alkyl, amino or lower alkylamino, and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and each is hydrogen atom, halogen atom, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy or amino, provided that at least one of R.sub.4, R.sub.5, R.sub.6 and R.sub.7 is not hydrogen atom, and the other is an optionally substituted cycloalkyl, an optionally substituted heterocyclic group or an optionally substituted aryl; and R.sub.2 is a lower alkyl or a halogenated lower alkyl, and a pharmaceutically acceptable salt thereof. The heterocyclic aromatic oxazole compound and pharmaceutically acceptable salts thereof have antipyretic action, analgesic action, anti-inflammatory action, and particularly, selective inhibitory action on cyclooxygenase-2 (COX-2), and are expected to be useful as anti-inflammatory agents with less side-effects such as digestive tract disorders.
摘要翻译： PCT No.PCT / JP95 / 02600 Sec。 371日期：1996年8月19日 102（e）日期1996年8月19日PCT提交1995年12月18日PCT公布。 WO96 / 19463 PCT出版物 日期：1995年6月27日一种其中Z为氧原子的式（I）的杂芳基恶唑化合物; R和R 1中的一个是下式的基团，其中R 3是低级烷基，氨基或低级烷基氨基，R 4，R 5，R 6和R 7相同或不同，各自为氢原子，卤素原子，低级烷基，低级烷氧基， 三氟甲基，羟基或氨基，条件是R 4，R 5，R 6和R 7中的至少一个不是氢原子，另一个是任选取代的环烷基，任选取代的杂环基或任选取代的芳基; 和R2是低级烷基或卤代低级烷基，及其药学上可接受的盐。 杂环芳族恶唑化合物及其药学上可接受的盐具有解热作用，止痛作用，抗炎作用，特别是对环氧合酶-2（COX-2）的选择性抑制作用，并且预期可用作抗炎剂， 较少的副作用如消化道疾病。
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公开(公告)号：US6002014A
公开(公告)日：1999-12-14
申请号：US302498
申请日：1999-04-30
IPC分类号： C12N9/99 , A61K31/42 , A61K31/421 , A61K31/422 , A61P25/04 , A61P29/00 , A61P43/00 , C07C45/00 , C07C49/567 , C07C49/813 , C07C69/007 , C07C233/31 , C07C233/47 , C07C251/42 , C07C311/16 , C07C311/29 , C07C311/32 , C07C311/37 , C07C317/24 , C07C317/32 , C07D263/32 , C07D413/04
CPC分类号： C07D413/04 , C07C233/31 , C07C233/47 , C07C251/42 , C07C311/16 , C07C311/29 , C07C311/32 , C07C311/37 , C07C317/24 , C07C317/32 , C07C45/004 , C07C49/567 , C07C49/813 , C07C69/007 , C07D263/32 , C07C2101/14
摘要： Oxazole derivatives of the formula (I) ##STR1## wherein one of R and R.sub.1 is a methylsulfonylphenyl, an aminosulfonylphenyl or an alkylaminosulfonylphenyl, and the other is a cycloalkyl having 5 to 7 carbon atoms which is optionally substituted by lower alkyl, a thienyl optionally substituted by lower alkyl or halogen atom or a furanyl optionally substituted by lower alkyl or halogen atom, and R.sub.2 is a lower alkyl, and pharmaceutically acceptable salts thereof. The oxazole derivatives and pharmaceutically acceptable salts thereof have superior antipyretic action, analgesic action, anti-inflammatory action, and particularly, selective inhibitory action on cyclooxygenase-2 (COX-2), and are expected to be useful as an antipyretic agent, an analgesic agent and an anti-inflammatory agent with less side-effects such as disorders in the digestive tract.
摘要翻译： 式（I）的恶唑衍生物，其中R和R 1中的一个是甲基磺酰基苯基，氨基磺酰基苯基或烷基氨基磺酰基苯基，另一个是任选被低级烷基取代的碳原子数5〜7的环烷基， 烷基或卤素原子或任选被低级烷基或卤原子取代的呋喃基，R2是低级烷基，及其药学上可接受的盐。 恶唑衍生物及其药学上可接受的盐具有优异的解热作用，止痛作用，抗炎作用，特别是对环氧合酶-2（COX-2）的选择性抑制作用，并且预期可用作解热剂，止痛剂 药剂和消炎剂等副作用减轻的消炎剂。
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公开(公告)号：US5945539A
公开(公告)日：1999-08-31
申请号：US849879
申请日：1997-06-18
IPC分类号： C12N9/99 , A61K31/42 , A61K31/421 , A61K31/422 , A61P25/04 , A61P29/00 , A61P43/00 , C07C45/00 , C07C49/567 , C07C49/813 , C07C69/007 , C07C233/31 , C07C233/47 , C07C251/42 , C07C311/16 , C07C311/29 , C07C311/32 , C07C311/37 , C07C317/24 , C07C317/32 , C07D263/32 , C07D413/04 , C07D263/30
CPC分类号： C07D413/04 , C07C233/31 , C07C233/47 , C07C251/42 , C07C311/16 , C07C311/29 , C07C311/32 , C07C311/37 , C07C317/24 , C07C317/32 , C07C45/004 , C07C49/567 , C07C49/813 , C07C69/007 , C07D263/32 , C07C2101/14
摘要： Oxazole derivatives of the formula (I) ##STR1## wherein one of R and R.sub.1 is a methylsulfonylphenyl, an aminosulfonyl-phenyl or an alkylaminosulfonylphenyl, and the other is a cycloalkyl having 5 to 7 carbon atoms which is optionally substituted by lower alkyl, a thienyl optionally substituted by lower alkyl or halogen atom or a furanyl optionally substituted by lower alkyl or halogen atom, and R.sub.2 is a lower alkyl, and pharmaceutically acceptable salts thereof. The oxazole derivatives and pharmaceutically acceptable salts thereof have superior antipyretic action, analgesic action, anti-inflammatory action, and particularly, selective inhibitory action on cyclooxygenase-2 (COX-2), and are expected to be useful as an antipyretic agent, an analgesic agent and an anti-inflammatory agent with less side-effects such as disorders in the digestive tract.
摘要翻译： PCT No.PCT / JP95 / 02588 Sec。 371日期：1997年6月18日 102（e）日期1997年6月18日PCT提交1995年12月15日PCT公布。 WO96 / 19462 PCT出版物 日期：1996年6月27日，式（I）的化合物，其中R和R 1中的一个为甲基磺酰基苯基，氨基磺酰基 - 苯基或烷基氨基磺酰基苯基，另一个为碳原子数5〜7的环烷基， 任选被低级烷基或卤素原子取代的噻吩基，或被低级烷基或卤原子任意取代的呋喃基，R 2为低级烷基，及其药学上可接受的盐。 恶唑衍生物及其药学上可接受的盐具有优异的解热作用，止痛作用，抗炎作用，特别是对环氧合酶-2（COX-2）的选择性抑制作用，并且预期可用作解热剂，止痛剂 药剂和消炎剂等副作用减轻的消炎剂。
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公开(公告)号：US5151497A
公开(公告)日：1992-09-29
申请号：US729415
申请日：1991-07-12
申请人： Itsuo Uchida , Akira Saito , Akihiro Yasuda , Kunio Iwata , Hiroaki Hari , Katsuyoshi Hara , Mutsuyoshi Matsushita , Koretake Anami , Junichi Haruta , Noboru Furukawa
发明人： Itsuo Uchida , Akira Saito , Akihiro Yasuda , Kunio Iwata , Hiroaki Hari , Katsuyoshi Hara , Mutsuyoshi Matsushita , Koretake Anami , Junichi Haruta , Noboru Furukawa
CPC分类号： C07K5/06147 , C07K5/06043 , C07K5/0606 , C07K5/06069 , C07K5/06078 , C07K5/06095 , C07K5/06113 , C07K5/0821 , A61K38/00
摘要： Novel peptide derivatives of the following formula ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable acid addition salts thereof and analogous copounds thereof.Since the derivatives and their pharmaceutically acceptable acid addition salts of the present invention possess stronger actions on central nervous system (e.g. antagonistic action against hypothermia, locomotor stimulant action, signal reflex stimulant action), they are of use as a therapeutic medicament for central nervous disorders such as impaired consciousness, depression, hypomnesia, the like in association association with schizophrenia, melancholia, senile dementia, sequelae of cerebrovascular disorders, head trauma, epilepsy and spinocerebellar degeneracy.
摘要翻译： 下式的新型肽衍生物
其中每个符号如说明书中所定义，其药学上可接受的酸加成盐及其类似物。 由于本发明的衍生物及其药学上可接受的酸加成盐对中枢神经系统具有较强的作用（例如抗低温，运动兴奋剂作用，信号反射兴奋剂作用的拮抗作用），因此它们可用作中枢神经障碍的治疗药物 诸如与精神分裂症，忧郁症，老年性痴呆，脑血管疾病后遗症，头部创伤，癫痫和脊髓小脑退化有关的意识障碍，抑郁症，hypomnesia等。 -
公开(公告)号：US5191074A
公开(公告)日：1993-03-02
申请号：US746083
申请日：1991-08-12
申请人： Yasumitsu Tamura , Junichi Haruta , Nishi Koichi
发明人： Yasumitsu Tamura , Junichi Haruta , Nishi Koichi
IPC分类号： C07D205/08 , C07F7/08 , C07F7/18
CPC分类号： C07D205/08 , C07F7/0812 , C07F7/186
摘要： A process for producing a .beta.-lactam compound of the formula ##STR1## wherein OR.sup.1 is a protected or unprotected hydroxyl group; R.sup.2 is a C.sub.1 to C.sub.7 alkyl or aryl group; from an azetidinone compound of the formula ##STR2## wherein X is an electronegative group removable through the reaction in three steps in which the second step subjects the .beta.-lactam compound obtained in the first step to silylation to convert the R.sup.2 group to the beta form.
摘要翻译： 制备式“IMAGE”的β-内酰胺化合物的方法，其中OR1是被保护或未被保护的羟基; R2是C1-C7烷基或芳基; 其中X是通过三个步骤可以通过反应除去的电负性基团，其中第二步骤将第一步中获得的β-内酰胺化合物甲硅烷基化以将R2基团转化为β形式 。
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公开(公告)号：US06420561B1
公开(公告)日：2002-07-16
申请号：US09714435
申请日：2000-11-17
IPC分类号： C07C23728
CPC分类号： C07D213/75 , A61K31/166 , C07C235/60 , C07C235/84 , C07C237/22 , C07C237/44 , C07C259/06 , C07C279/08 , C07C323/62 , C07C327/22 , C07C2601/14 , C07C2603/74 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/62 , C07D263/58 , C07D271/06 , C07D295/088 , C07D295/15 , Y02P20/55
摘要： An amide compound of the formula (I): wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-&agr;, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.
摘要翻译： 式（I）的酰胺化合物：其中R是氨基等，A是亚烷基等，X是O，S等，M是亚芳基等，R 1，R 2，R 3和R 4是H ，羟基等，R5为H，烷基等，m为0-6的整数，R6为任意取代的芳基等，R7为H，可以具有取代基的烷基等，药学上可接受的 其加成盐和含有它们作为活性成分的药物。 酰胺化合物对直接或间接参与炎症的细胞因子如IL-8，IL-1，IL-6，TNF-α，GM-CSF等表现出优异的抑制作用，并且可用于预防和治疗 风湿性疾病，由痛风引起的关节炎等。
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公开(公告)号：US5329042A
公开(公告)日：1994-07-12
申请号：US955757
申请日：1992-12-24
IPC分类号： C07C61/22 , C07C62/24 , C07C62/34 , C07C62/36 , C07C62/38 , C07C67/317 , C07C67/333 , C07C69/757 , C07D307/88 , C07C205/00
CPC分类号： C07D307/88 , C07C61/22 , C07C62/24 , C07C62/34 , C07C62/36 , C07C62/38 , C07C67/317 , C07C67/333 , C07C69/757
摘要： Provided is a novel (1R, 2S)-1-acyl-2-carboxycyclohex-4-ene derivative represented by the following general formula [I], and its producing method, ##STR1## (where R.sup.1 represents a hydrogen atom, a lower alkyl group, or substituted or unsubstituted aryl group, and R.sup.2 represents a hydrogen atom, or a lower alkyl group). Also provided is a method of producing a (3S, 4R)-4-substituted-3-carboxycyclopentanone derivative represented by the following general formula [A], ##STR2## (where R.sup.1 and R.sup.2 are the same as those mentioned above).
摘要翻译： PCT No.PCT / JP92 / 00537 Sec。 一九九二年十二月二十四日 102（e）日期1992年12月24日PCT提交1992年4月24日PCT公布。 第WO92 / 19582号公报 日期：1992年11月12日。提供了由以下通式[I]表示的新型（1R，2S）-1-酰基-2-羧基环己-4-烯衍生物及其制备方法， （其中R1表示氢原子，低级烷基或取代或未取代的芳基，R2表示氢原子或低级烷基）。 还提供了制备由以下通式[A]表示的（3S，4R）-4-取代-3-羧基环戊酮衍生物，其中R1和R2与上述相同的方法 ）。
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公开(公告)号：USRE39088E1
公开(公告)日：2006-05-02
申请号：US10342189
申请日：1996-08-15
IPC分类号： A61K31/66 , C07C237/28 , C07C237/32 , C07C237/34
CPC分类号： C07D213/75 , A61K31/166 , C07C235/60 , C07C235/84 , C07C237/22 , C07C237/44 , C07C259/06 , C07C279/08 , C07C323/62 , C07C327/22 , C07C2601/14 , C07C2603/74 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/62 , C07D263/58 , C07D271/06 , C07D295/088 , C07D295/15 , Y02P20/55
摘要： An amide compound of the formula (I): wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-α, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.
摘要翻译： 式（I）的酰胺化合物：其中R是氨基等，A是亚烷基等，X是O，S等，M是亚芳基等，R 1， R 2，R 3和R 4是H，羟基等，R 5是H， 烷基等，m为0-6的整数，R 6为任选取代的芳基等，R 7为H，任意取代的烷基和 其药学上可接受的酸加成盐和含有它们作为活性成分的药物。 酰胺化合物对直接或间接参与炎症的细胞因子如IL-8，IL-1，IL-6，TNF-α，GM-CSF等表现出优异的抑制作用，并且可用于预防和治疗 风湿性疾病，由痛风引起的关节炎等。
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公开(公告)号：US06174887B1
公开(公告)日：2001-01-16
申请号：US09011983
申请日：1998-02-20
IPC分类号： A61K31166
CPC分类号： C07D213/75 , A61K31/166 , C07C235/60 , C07C235/84 , C07C237/22 , C07C237/44 , C07C259/06 , C07C279/08 , C07C323/62 , C07C327/22 , C07C2601/14 , C07C2603/74 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/62 , C07D263/58 , C07D271/06 , C07D295/088 , C07D295/15 , Y02P20/55
摘要： An amide compound of the formula (I): wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-&agr;, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.
摘要翻译： 式（I）的酰胺化合物：其中R是氨基等，A是亚烷基等，X是O，S等，M是亚芳基等，R 1，R 2，R 3和R 4是H ，羟基等，R5为H，烷基等，m为0-6的整数，R6为任意取代的芳基等，R7为H，可以具有取代基的烷基等，药学上可接受的 其加成盐和含有它们作为活性成分的药物。 酰胺化合物对直接或间接参与炎症的细胞因子如IL-8，IL-1，IL-6，TNF-α，GM-CSF等表现出优异的抑制作用，并且可用于预防和治疗 风湿性疾病，由痛风引起的关节炎等。
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