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    신경세포 사멸을 억제하는2,2'-알킬치환-3,4-디하이드로-6-알킬아미노 벤조피란유도체
    2.
    发明授权
    신경세포 사멸을 억제하는2,2'-알킬치환-3,4-디하이드로-6-알킬아미노 벤조피란유도체 失效
    作为胚胎细胞死亡的保护剂的2,2'-烷基-3,4-脱水-6-烷基亚苄基衍生物

    公开(公告)号：KR100769732B1

    公开(公告)日：2007-10-23

    申请号：KR1020060068562

    申请日：2006-07-21

    Applicant: 한국화학연구원 ,  한국생명공학연구원

    Inventor： 공영대 ,  권기선 ,  서해영 ,  전문국 ,  유성은 ,  박성섭 ,  서현우 ,  유승완

    IPC: A61K31/352 ,  A61P25/28

    Abstract: A 2,2'-alkylsubstitued-3,4-dehydro-6-alkylamino benzopyran derivative is provided to secure the activity of controlling neuronal death by controlling the activity of a glutamate receptor, thereby being useful as a prophylactic and therapeutic agent of stroke, epilepsy, amyotrophic lateral sclerosis, Parkinson's diseases, Huntington's disease and Alzheimer's disease. A pharmaceutical composition comprises a 2,2'-double substituted-7,8-double substituted-6-alkylamino benzopyran derivative represented by the formula(1) or a pharmaceutically acceptable salt thereof. In the formula(1), R^1 is C1-10 alkyl, benzyl, or substituted benzyl, phenethyl, 2-pyrimidylmethyl, thiophene, 2-methylthiophenemethyl, 5-methyl-2-thiophenemethyl, 3-thiophenemethyl, indolylmethyl, benzo dioxiranylmethyl, naphthalenylmethyl, or furanylmethyl, each R^2 and R^3 is H, C1-6 alkyl, halogen, or phenyl and substituted phenyl, R^4 is C1-10 alkyl, phenyl or substituted phenyl, or a hetero-cyclic group selected from the group consisting of thiophene and furan(wherein the benzyl, phenyl or the heterocyclic group is able to be substituted by 1-4 substituents selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, nitro, cyano and C1-6 alkoxy), and n is an integer from 1 to 5.

    Abstract translation: 提供了一种2,2'-烷基苯基-3,4-脱氢-6-烷基氨基苯并吡喃衍生物，以通过控制谷氨酸受体的活性来确保控制神经元死亡的活性，从而可用作中风的预防和治疗剂， 癫痫，肌萎缩性侧索硬化，帕金森病，亨廷顿病和阿尔茨海默病。 药物组合物包含由式（1）表示的2,2'-双取代-7,8-双取代-6-烷基氨基苯并吡喃衍生物或其药学上可接受的盐。 在式（1）中，R 1是C 1-10烷基，苄基或取代的苄基，苯乙基，2-嘧啶基甲基，噻吩，2-甲基噻吩甲基，5-甲基-2-噻吩甲基，3-噻吩甲基，吲哚基甲基，苯并二氧杂环丙基甲基 ，萘基甲基或呋喃基甲基，每个R 2和R 3是H，C 1-6烷基，卤素或苯基和取代的苯基，R 4是C 1-10烷基，苯基或取代的苯基或杂环基 选自噻吩和呋喃（其中苄基，苯基或杂环基团能够被1-4个选自C1-6烷基，C1-6卤代烷基，硝基，氰基和C1的取代基取代） -6烷氧基），n为1〜5的整数。

    Ｎ-페닐아마이드 유도체를 함유하는 허혈성 질환의 예방또는 치료용 조성물
    3.
    发明授权
    Ｎ-페닐아마이드 유도체를 함유하는 허혈성 질환의 예방또는 치료용 조성물 失效
    用于预防或治疗含有N-苯甲酰胺衍生物的化学物质的组合物

    公开(公告)号：KR100832750B1

    公开(公告)日：2008-05-27

    申请号：KR1020060124581

    申请日：2006-12-08

    Applicant: 한국화학연구원

    Inventor： 서지희 ,  유성은 ,  김낙정 ,  김은희 ,  정용삼 ,  이윤숙 ,  서해영

    IPC: A61K31/166 ,  A61P9/10

    Abstract: A composition is provided to decrease ischemic apoptosis significantly, thereby being usefully utilized as a prophylactic or therapeutic agent of ischemic diseases mediated by the ischemic apoptosis, or an organ protecting agent. A composition for preventing or treating an ischemic disease selected from the group consisting of cerebral ischemia, cardiac ischemia, diabetic cardiovascular diseases, cardiac failure, hypertrophy, retinal ischemia, ischemic colitis, ischemic acute cardiac failure, stroke, traumatic brain injury, Alzheimer's disease, Parkinson's disease, newborn hypoxia, glaucoma and diabetic neurosis mediated by ischemic apoptosis comprises an N-phenyl amide derivative represented by a formula(1) or a pharmaceutically acceptable salt thereof as an effective ingredient, wherein the ischemic apoptosis is induced under low oxygen condition. In the formula(1), R^1 is H, -CO2R^5, -CH2OR^5, -CONR^5R^5, or a structural formula(1)(wherein each R^5 and R^6 is independently H or methyl); each R^2, R^3 and R^4 is independently H, C1-3 alkyl or alkoxy, or halogen; B is H or phenyl; n is 0 or 1; Y is S; Z is H, halogen or C1-3 alkoxy; and A is CH or N.

    Abstract translation: 提供了显着降低缺血性凋亡的组合物，从而有效地用作由缺血性细胞凋亡介导的缺血性疾病或器官保护剂的预防或治疗剂。 用于预防或治疗缺血性疾病的组合物，其选自脑缺血，心脏缺血，糖尿病心血管疾病，心力衰竭，肥大，视网膜缺血，缺血性结肠炎，缺血性急性心力衰竭，中风，创伤性脑损伤，阿尔茨海默氏病， 由缺血性细胞凋亡介导的帕金森病，新生儿缺氧，青光眼和糖尿病性神经症包括由式（1）表示的N-苯基酰胺衍生物或其药学上可接受的盐作为有效成分，其中在低氧条件下诱导缺血性凋亡。 在式（1）中，R 1是H，-CO 2 R 5，-CH 2 OR 5，-CONR 5 R 5或结构式（1）（其中每个R 5和R 6独立地是H 或甲基）; 每个R 2，R 3和R 4独立地是H，C 1-3烷基或烷氧基或卤素; B是H或苯基; n为0或1; Y是S; Z是H，卤素或C 1-3烷氧基; A是CH或N.

    아마이드로 치환된 벤조퓨란 및 벤조싸이오펜 유도체, 이의제조 방법 및 이를 포함하는 약학적 조성물
    6.
    发明公开
    아마이드로 치환된 벤조퓨란 및 벤조싸이오펜 유도체, 이의제조 방법 및 이를 포함하는 약학적 조성물 失效
    酰胺取代的苯并呋喃衍生物及其制备方法以及含有它们的药物组合物

    公开(公告)号：KR1020090037744A

    公开(公告)日：2009-04-16

    申请号：KR1020070103244

    申请日：2007-10-12

    Applicant: 한국화학연구원

    Inventor： 서지희 ,  유성은 ,  이규양 ,  김낙정 ,  김은희 ,  정용삼 ,  이윤숙 ,  서해영

    IPC: C07D307/85 ,  C07D405/12 ,  C07D491/048 ,  C07D413/04

    CPC classification number: C07D307/85 ,  C07D333/70 ,  C07D401/12 ,  C07D409/12 ,  C07D413/04 ,  C07D491/048 ,  C07D495/04

    Abstract: Benzofuran and bezothiophene derivatives substituted with amide, a preparation process thereof, and a pharmaceutical composition containing the same are provided to prevent and treat ischemic diseases such as cerebral ischemia mediated by ischemic cell death. Benzofuran and bezothiophene derivatives substituted with amide are represented by the chemical formula 1. The benzofuran and bezothiophene derivatives substituted with amide of the chemical formula 1 is obtained by reacting a compound of the chemical formula 2 and a compound of the chemical formula 3. The benzofuran and bezothiophene derivatives substituted with amide or their pharmaceutically acceptable salts is contained as an active ingredient of a pharmaceutical composition for preventing and treating ischemic diseases.

    Abstract translation: 提供了被酰胺取代的苯并呋喃和噻唑并噻吩衍生物及其制备方法和含有它们的药物组合物，以预防和治疗缺血性疾病如缺血性细胞死亡介导的脑缺血。 由酰胺取代的苯并呋喃和噻唑并噻吩衍生物由化学式1表示。化学式1的被酰胺取代的苯并呋喃和异噻吩衍生物是通过使化学式2的化合物与化学式3的化合物反应得到的。苯并呋喃 作为预防和治疗缺血性疾病的药物组合物的活性成分，含有被酰胺取代的噻唑并噻吩衍生物或其药学上可接受的盐。

    아미노싸이오펜 유도체를 함유하는 허혈성 질환의 예방또는 치료용 조성물
    7.
    发明授权
    아미노싸이오펜 유도체를 함유하는 허혈성 질환의 예방또는 치료용 조성물 失效
    用于预防或治疗含有氨基胆碱衍生物的化学疾病的组合物

    公开(公告)号：KR100860539B1

    公开(公告)日：2008-09-26

    申请号：KR1020070045992

    申请日：2007-05-11

    Applicant: 한국화학연구원

    Inventor： 서지희 ,  유성은 ,  이규양 ,  김낙정 ,  김은희 ,  정용삼 ,  이윤숙 ,  서해영

    IPC: A61K31/381 ,  A61P9/10

    CPC classification number: A61K31/381

    Abstract: An aminothiophene derivative is provided to decrease ischemic apoptosis, thereby being used as a composition for preventing and treating ischemic diseases mediated by the ischemic apoptosis or for protecting organs. A composition for preventing or treating ischemic diseases comprises an aminothiophene derivative represented by a formula(1) or (2), or a pharmaceutically acceptable salt thereof as an effective ingredient, wherein the ischemic disease is cerebral ischemia, cardiac ischemia, diabetic cardiovascular diseases, cardiac failure, cardiac hypertrophy, retinal ischemia, ischemic colitis, ischemic acute renal failure, stroke, cerebral wound, Alzheimer's disease, Parkinson's disease, hypoxia in newborn, glaucoma and diabetic neuropathy. In the formulae, R^1 is H, CO2R^2, CH2OR^2, CONR^2R^3, or a group(1); each R^2 and R^3 is independently H, or C1-6 linear or branched alkyl, or halogen or hydroxy substituted alkyl; B is H, phenyl, or C1-3 alkyl or halogen substituted phenyl; n is an integer from 0 to 2; Y is S, O, SO or SO2; Z is H, halogen, NO2, NH2, C1-3 linear or branched alkyl or OR^4; R^4 is H or C1-3 linear or branched alkyl; and A is CH, N or N-O. Further, the ischemic diseases are selected from cerebral ischemic damage, Ischemic Heart Failure, cardiac failure, retinal ischemia or Alzheimer's disease.

    Abstract translation: 提供氨基噻吩衍生物以减少缺血性细胞凋亡，从而用作预防和治疗由缺血性细胞凋亡或保护器官介导的缺血性疾病的组合物。 用于预防或治疗缺血性疾病的组合物包含由式（1）或（2）表示的氨基噻吩衍生物或其药学上可接受的盐作为有效成分，其中缺血性疾病是脑缺血，心脏缺血，糖尿病心血管疾病， 心脏衰竭，心脏肥大，视网膜缺血，缺血性结肠炎，缺血性急性肾衰竭，中风，脑伤，阿尔茨海默病，帕金森病，新生儿缺氧，青光眼和糖尿病性神经病变。 在式中，R 1是H，CO 2 R 2，CH 2 OR 2，CONR 2 R 3，或基团（1）; 每个R 2和R 3独立地是H或C 1-6直链或支链烷基，或卤素或羟基取代的烷基; B是H，苯基或C 1-3烷基或卤素取代的苯基; n为0〜2的整数; Y是S，O，SO或SO2; Z是H，卤素，NO 2，NH 2，C 1-3直链或支链烷基或OR 4; R 4是H或C 1-3直链或支链烷基; A是CH，N或N-O。 此外，缺血性疾病选自脑缺血性损伤，缺血性心力衰竭，心力衰竭，视网膜缺血或阿尔茨海默病。

    Ｎ-페닐아마이드 유도체 및 이의 제조방법
    8.
    发明授权
    Ｎ-페닐아마이드 유도체 및 이의 제조방법 失效
    N-苯甲酰胺衍生物及其制备方法

    公开(公告)号：KR100832751B1

    公开(公告)日：2008-05-27

    申请号：KR1020060124590

    申请日：2006-12-08

    Applicant: 한국화학연구원

    Inventor： 서지희 ,  유성은 ,  이규양 ,  김낙정 ,  김은희 ,  정용삼 ,  이윤숙 ,  서해영

    IPC: C07D213/70 ,  C07D213/63 ,  C07D413/12

    Abstract: An N-phenylamide derivative is provided to decrease ischemic apoptosis significantly, thereby being used for preventing and treating ischemic diseases. An N-phenylamide derivative is represented by a formula(1), wherein R^1 is H, -CO2R^5, -CH2OR^5, -CONR^5R^5, or a structural formula(1)(wherein each R^5 and R^6 is independently H or methyl); each R^2, R^3 and R^4 is independently H, C1-3 alkyl or alkoxy, or halogen; B is H or phenyl; n is 0 or 1; Y is S; Z is H, halogen or C1-3 alkoxy; and A is CH or N, provided that B is phenyl or phenyl substituted by C1-3 alkyl or halogen when n is 0, and A is N when n is 1. A method for preparing the compound of the formula(1) comprises a step of subjecting a compound represented by a formula(2) with a compound represented by a formula(3) to nucleophilic substitution in the presence of an organic solvent and a base, wherein R^1, R^2, R^3, R^4, B, n, Z, Y and A are same as defined above and L is a leaving group such as halide, mesylate, or tosylate.

    Abstract translation: 提供的N苯基酰胺衍生物显著减少缺血性细胞凋亡，从而被用于预防和治疗缺血性疾病。 的N-苯基酰胺衍生物由式（1），其中R ^ 1是H，-CO 2 R ^ 5表示-CH 2 OR ^ 5，-CONR ^ 5R ^ 5，或结构式（1）（其中各R ^ 5和R 6独立地是H或甲基）; 每个R ^ 2，R ^ 3和R ^ 4独立地是H，C 1-3烷基或烷氧基，或卤素; B是H或苯基; n为0或1; Y是S; Z是H，卤素或C 1-3烷氧基; A为CH或N，条件是当n为0时，B为苯基或被C 1-3烷基或卤素取代的苯基。当n为1时，A为N。制备式（1）化合物的方法包括： 在有机溶剂和碱的存在下，将由式（2）表示的化合物与式（3）表示的化合物进行亲核取代的步骤，其中R 1，R 2，R 3，R ^ 4，B，n，Z，Y和A与上述相同，L是离去基团如卤化物，甲磺酸酯或甲苯磺酸酯。

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