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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
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.
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公开(公告)号：KR1020080037911A
公开(公告)日：2008-05-02
申请号：KR1020060105183
申请日：2006-10-27
Applicant: 한국화학연구원
IPC: C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12
CPC classification number: C07D231/38 , C07D231/40 , C07D401/12 , C07D413/04 , C07D413/12
Abstract: Aminopyrazole derivatives are provided to reduce ischemic apoptosis significantly and protect internal organs, so that the derivatives are useful for preventing or treating ischemic diseases mediated by ischemic apoptosis. The aminopyrazole derivatives represented by the formula(1) or pharmaceutically acceptable salts are provided in order to prevent or treat ischemic diseases, wherein R^1 is -CO2R^3, -CH2OR^3, -CONR^3R^4 or a structural formula in which R^3 and R^4 are each independently H or C1-C6 linear, branched or cyclic alkyl; R^2 is -(CH2)m Ar or C1-C6 linear, branched or cyclic alkyl in which m is an integer from 1 to 3 and Ar is phenyl or C1-C3 alkyl or halogen substituted phenyl; B is H, phenyl or C1-C3 alkyl or halogen substituted phenyl; n is an integer from 0 to 2; Y is S, O, C, SO, SO2 or NR^3R^4; Z is H, halogen, OCH3, NO2, NH2 or C1-C3 linear or branched alkyl; and A is CH or N.
Abstract translation: 提供氨吡唑衍生物以显着减少缺血性凋亡并保护内脏，使得该衍生物可用于预防或治疗缺血性细胞凋亡介导的缺血性疾病。 提供由式（1）表示的氨基吡唑衍生物或其药学上可接受的盐，以便预防或治疗缺血性疾病，其中R 1是-CO 2 R 3，-CH 2 OR 3，-CONR 3 3R 4或结构式 其中R 3和R 4各自独立地为H或C 1 -C 6直链，支链或环状烷基; R 2是 - （CH 2）m Ar或C 1 -C 6直链，支链或环状烷基，其中m是1至3的整数，Ar是苯基或C 1 -C 3烷基或卤素取代的苯基; B是H，苯基或C 1 -C 3烷基或卤素取代的苯基; n为0〜2的整数; Y是S，O，C，SO，SO 2或NR 3 3R 4; Z是H，卤素，OCH 3，NO 2，NH 2或C 1 -C 3直链或支链烷基; A是CH或N.
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公开(公告)号：KR100832747B1
公开(公告)日：2008-05-27
申请号：KR1020060105183
申请日：2006-10-27
Applicant: 한국화학연구원
IPC: C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12
CPC classification number: C07D231/38 , C07D231/40 , C07D401/12 , C07D413/04 , C07D413/12
Abstract: 본 발명은 아미노피라졸 유도체, 이의 제조 방법 및 이를 유효성분으로 포함하는 허혈성 질환의 예방 또는 치료용 조성물에 관한 것으로서, 본 발명의 아미노피라졸 유도체는 허혈성 세포사를 현저히 감소시킬 수 있으므로, 이를 유효성분으로 함유하는 조성물은 허혈성 세포사에 의해 매개되는 허혈성 질환의 예방 및 치료제 또는 장기 보호제로 유용하게 활용될 수 있다.
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Patent Agency Ranking
公开(公告)号：KR100818752B1
公开(公告)日：2008-04-01
申请号：KR1020060095742
申请日：2006-09-29
Applicant: 한국화학연구원
CPC classification number: A61K38/1761 , C07K14/4747
Abstract: A human FAF1 protein inhibitor is provided to inhibit expression or function of an FAF1 protein effectively and inhibit ischemic cell death effectively by acting on a caspase non-dependent cell death passage during the ischemic cell death, and generation of reactive oxygen species, activation of PARP-1, and a nucleus movement passage of AIF, thereby being used as a pharmaceutical composition for treating or preventing ischemic diseases. A composition for treating or preventing ischemic diseases comprises a human FAF1(Fas-associated factor 1) inhibitor as an effective ingredient, which is selected from the group consisting of a double stranded siRNA consisting of a forward single stranded siRNA having a sequence of SEQ ID : NO. 3 and a reverse single stranded siRNA having a sequence of SEQ ID : NO. 4, a double stranded siRNA consisting of a forward single stranded siRNA having a sequence of SEQ ID : NO. 5 and a reverse single stranded siRNA having a sequence of SEQ ID : NO. 6, and a protein having an amino acid sequence of SEQ ID : NO. 7, wherein the ischemic diseases is cerebral ischemia, cardiac ischemia, diabetic cardiovascular diseases, heart failure, myocardial hypertrophy, retinal ischemia, ischemic colitis, and ischemic acute renal failure mediated by ischemic cell death.
Abstract translation: 提供人FAF1蛋白抑制剂以有效抑制FAF1蛋白的表达或功能，并通过在缺血性细胞死亡期间作用于胱天蛋白酶非依赖性细胞死亡通道并产生活性氧，有效激活PARP，有效抑制缺血性细胞死亡 -1和AIF的核运动通道，因此用作治疗或预防缺血性疾病的药物组合物。 用于治疗或预防缺血性疾病的组合物包含作为有效成分的人FAF1（Fas相关因子1）抑制剂，其选自由具有SEQ ID NO：1的序列的正向单链siRNA组成的组 ：否 3和具有SEQ ID NO：3的序列的反向单链siRNA。 4，由具有SEQ ID NO：1的序列的正向单链siRNA组成的双链siRNA。 5和具有SEQ ID NO：5的序列的反向单链siRNA。 6，以及具有SEQ ID NO：6的氨基酸序列的蛋白质。 7，其中缺血性疾病是脑缺血，心脏缺血，糖尿病心血管疾病，心力衰竭，心肌肥大，视网膜缺血，缺血性结肠炎和由缺血性细胞死亡介导的缺血性急性肾衰竭。
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公开(公告)号：KR100937134B1
公开(公告)日：2010-01-15
申请号：KR1020070103244
申请日：2007-10-12
Applicant: 한국화학연구원
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: 본 발명은 하기 화학식 1의 아마이드로 치환된 벤조퓨란 및 벤조싸이오펜 유도체, 이의 제조 방법 및 이를 포함하는 약학적 조성물에 관한 것으로, 본 발명의 아마이드로 치환된 벤조퓨란 및 벤조싸이오펜 유도체는 허혈성 세포사를 현저히 감소시킬 수 있으므로, 이를 유효성분으로 함유하는 조성물은 허혈성 세포사에 의해 매개되는 허혈성 질환의 예방 및 치료제 또는 장기 보호제로 유용하게 활용될 수 있다.
상기 식에서,
R
1 ,
B, n, Y, Z, X, W 및 A는 명세서 중에 정의한 바와 같다.-
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
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。
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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
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。
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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
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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