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1.发明公开세라마이드 유도체, 이의 약학적으로 허용 가능한 염, 이의제조방법 및 이를 유효성분으로 함유하는 암 예방 및치료용 약학적 조성물 失效CERAMIDE衍生物，其药学上可接受的盐，用于预防和治疗含有作为活性成分的癌症的制剂方法和药物组合物
公开(公告)号：KR1020080065086A
公开(公告)日：2008-07-11
申请号：KR1020070002038
申请日：2007-01-08
Applicant: 재단법인서울대학교산학협력재단
IPC: C07D249/04 , C07D235/28
Abstract: A ceramide derivative is provided to change equilibrium of sphingolipid metabolites by mimicking the activity of ceramide and controlling related enzymes, thereby being developed as a controlling agent of apoptosis induction or a prophylactic and therapeutic agent of cancer. A ceramide derivative is represented by a formula(1) and is prepared by reacting a compound represented by a formula(2) with an alkyne compound, wherein R1 is C1-35 alkyl which may be substituted or unsubstituted with at least one substitutent selected from the group consisting of halogen, hydroxy, amino, amino substituted with at least one C1-20 alkyl, thiol, cyano, nitro, sulfonyl, phenyl, C1-30 alkoxy, C1-30 alkyl, C1-30 haloalkyl, C1-30 hydroxyalkyl, C1-30 alkoxyalkyl, C5-10 aryl, C5-10 heteroaryl, C5-10 arylalkyl and C5-10 heteroarylalkyl; a bond is a single bond or a double bond; and R2 is hydroxy when the bond is the single bond, and R2 is H when the bond is the double bond. A controlling agent for inducing apoptosis or a pharmaceutical composition for preventing and treating cancer comprises the ceramide derivative or a pharmaceutically acceptable salt thereof as an effective ingredient.
Abstract translation: 提供神经酰胺衍生物，通过模拟神经酰胺的活性和控制相关酶来改变神经鞘脂代谢物的平衡，从而被开发为细胞凋亡诱导的控制剂或癌症的预防和治疗剂。 神经酰胺衍生物由式（1）表示，并且通过使式（2）表示的化合物与炔化合物反应制备，其中R 1为可被取代或未取代的至少一个选自以下的取代基的C1-35烷基 由卤素，羟基，氨基，被至少一个C 1-20烷基取代的氨基，硫醇，氰基，硝基，磺酰基，苯基，C 1-3烷氧基，C 1-30烷基，C 1-30卤代烷基，C 1-30羟基烷基 ，C 1-3烷氧基烷基，C 5-10芳基，C 5-10芳基，C 5-10芳基烷基和C 5-10杂芳基烷基; 债券是单一债券或双重债券; 当键为单键时，R2为羟基，当键为双键时，R2为H。 用于诱导凋亡的控制剂或用于预防和治疗癌症的药物组合物包括神经酰胺衍生物或其药学上可接受的盐作为有效成分。
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2.发明授权
公开(公告)号：KR100796459B1
公开(公告)日：2008-01-21
申请号：KR1020060098619
申请日：2006-10-10
Applicant: 재단법인서울대학교산학협력재단
IPC: C07C69/16
Abstract: A fatty acid glycerol derivative is provided to inhibit the formation of cyclooxygenase-2-dependent prostaglandin D2, to ensure a strong inhibitory activity against phospholipase A2, thereby preventing and treat inflammatory diseases, allergies, and asthma. A method for preparing a compound of the structural formula (B) and a palmitoyl glycerol, stearoyl glycerol, oleoyl glycerol, linoleoyl glycerol, gamma-linolenoyl glycerol, alpha-linolenoyl glycerol, dihomo-gamma-linolenoyl glycerol, eicosapentaenoyl glycerol, adrenoyl glycerol, or docosahexaenoyl glycerol derivative compound includes the steps of: (1) condensing a fatty acid of the formula (I) and a cyclized glycerol of the formula (II) to obtain an ester of the formula (III); purifying the ester compound by chromatography; (3) decyclizing the pured ester with a boric acid as a reducing agent to synthesize fatty acid glycerol of the formula (IV); and (4) purifying the synthesized compound by chromatography.
Abstract translation: 提供脂肪酸甘油衍生物以抑制环氧合酶-2依赖性前列腺素D2的形成，以确保对磷脂酶A2的强抑制活性，从而预防和治疗炎性疾病，过敏反应和哮喘。 制备结构式（B）的化合物和棕榈酰甘油，硬脂酰甘油，油酰甘油，亚油酰甘油，γ-亚麻酰基甘油，α-亚麻酸酰甘油，二高-γ-亚麻油酰甘油，二十碳五烯酰甘油，肾上腺素甘油， 或二十二碳六烯酰基甘油衍生物化合物包括以下步骤：（1）将式（I）的脂肪酸与式（II）的环化甘油缩合得到式（III）的酯; 通过色谱纯化酯化合物; （3）用硼酸作为还原剂使得该酯脱酯，合成式（IV）的脂肪酸甘油; 和（4）通过色谱法纯化合成的化合物。
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公开(公告)号：KR100574392B1
公开(公告)日：2006-05-02
申请号：KR1020030007877
申请日：2003-02-07
Applicant: 재단법인서울대학교산학협력재단 , 최상윤 , 김선여
IPC: C07D307/36
Abstract: 본 발명은 신경보호활성을 갖는 신규 페닐환 유도체 화합물 및 이를 함유하는 약학 조성물을 제공하는 것으로, 본 발명의 페닐환 유도체 화합물이 허혈성 신경계 질환을 유의성있게 차단시키는 효과를 가짐으로서, 중풍 또는 뇌졸중 등의 신경계 질환의 예방 및 치료제로 사용할 수 있다.
페닐환 유도체, 허혈성, 중풍, 뇌졸중, 신경계 질환, 약학조성물.-
公开(公告)号：KR100507041B1
公开(公告)日：2005-08-08
申请号：KR1020030056204
申请日：2003-08-13
Applicant: 재단법인서울대학교산학협력재단
IPC: A01N31/06
Abstract: 본 발명은 신규한 항생물질 및 이를 함유하는 항균조성물에 관한 것으로, 상세하게는 주목나무 내피의 식물 내생진균인 페리코니아 미누티시마(
Periconia minutissima ) 진균이 생산하는 항균성 항생물질인 신규 디테르펜계 화합물인 페리코니신(periconicin) A, B 및 이를 함유하는 항균 조성물에 관한 것이다.-
公开(公告)号：KR100773765B1
公开(公告)日：2007-11-12
申请号：KR1020050112928
申请日：2005-11-24
Applicant: 재단법인서울대학교산학협력재단
IPC: C07C213/08
CPC classification number: Y02P20/55
Abstract: 본 발명은 개선된 스핑고신 유사체의 제조 방법에 관한 것으로, 팔라듐으로 촉매된 소노가시라 중합반응을 합성단계 중에 이용하고, 아세토나이드 및 Boc 보호기를 동시에 제거하여 간결하고 효과적으로 고수율의 스핑고신 유사체를 얻을 수 있으므로, 경제적으로 산업적 규모의 대량 생산에 사용될 수 있으며, 다른 유사체들의 대량 반응에도 유용하게 사용될 수 있다.
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Patent Agency Ranking
公开(公告)号：KR1020050017077A
公开(公告)日：2005-02-21
申请号：KR1020030056204
申请日：2003-08-13
Applicant: 재단법인서울대학교산학협력재단
IPC: A01N31/06
Abstract: PURPOSE: Provided is an antibacterial composition which contains novel antibacterial compounds including periconicin A and B produced from Periconia minutissima. Therefore, the composition is useful for treatment of infectious diseases. CONSTITUTION: The novel periconicin derivatives are represented by the formula(I), wherein R1 and R2 are independently methyl group or hydroxy methylene group. The derivatives include periconicin A and B. The antibacterial composition contains the compound of the formula(I) and a pharmaceutically acceptable carrier.
Abstract translation: 目的：提供一种抗菌组合物，其包含由Periconia minutissima产生的包含periconicin A和B的新型抗菌化合物。 因此，该组合物可用于治疗感染性疾病。 构成：新颖的periconicin衍生物由式（I）表示，其中R 1和R 2独立地是甲基或羟基亚甲基。 衍生物包括孔雀绿素A和B.抗菌组合物含有式（I）的化合物和药学上可接受的载体。
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公开(公告)号：KR100809927B1
公开(公告)日：2008-03-06
申请号：KR1020060092901
申请日：2006-09-25
Applicant: 재단법인서울대학교산학협력재단
IPC: C07C215/10 , C07C215/02
CPC classification number: Y02P20/55
Abstract: A method for preparing D-erythro-sphingosine of a natural substance is provided to obtain a sphingosine having trans selectivity and to lower a manufacturing cost by using D-ribo-phytosphingosine. A method for preparing D-erythro-sphingosine comprises the steps of reacting a compound represented by the formula 4 with SOx and oxidizing it, or reacting a compound represented by the formula 4 with SO2X2, thereby preparing a compound represented by the formula 5; cyclic ring opening the compound represented by the formula 5; deprotecting the P2O group of the obtained compound to prepare a compound represented by the formula 3; and deprotecting the compound of the formula 3 to obtain the D-erythro-sphingosine represented by the formula 1, wherein X is a halogen atom; P1 is NH3 or N4; and P2 and P3 are a protecting group.
Abstract translation: 提供了制备天然物质的D-赤式 - 鞘氨醇的方法，以获得具有反式选择性的鞘氨醇，并通过使用D-核糖 - 鞘氨醇作为降低制造成本。 制备D-赤式 - 鞘氨醇的方法包括以下步骤：将式4化合物与SOx反应并使其氧化，或使由式4表示的化合物与SO 2 X 2反应，从而制备由式5表示的化合物; 环式开环由式5表示的化合物; 使所得化合物的P2O基脱保护，制备式3表示的化合物; 并使式3的化合物脱保护，得到式1所示的D-赤式 - 鞘氨醇，其中X为卤素原子; P1是NH3或N4; P2和P3是保护基。
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8.发明授权
公开(公告)号：KR100796458B1
公开(公告)日：2008-01-21
申请号：KR1020060098291
申请日：2006-10-10
Applicant: 재단법인서울대학교산학협력재단
Abstract: An octadecatetraenoyl glycerol compound or a pharmaceutically acceptable derivative thereof is provided to prevent and treat inflammatory diseases, allergies, and asthma by inhibiting an activity of 5-lipoxygenase and showing a strong inhibitory activity against phospholipase A2. An octadecatetraenoyl glycerol compound or a pharmaceutically acceptable derivative thereof has a structure represented by the formula (A). A method for separating the octadecatetraenoyl glycerol compound includes the steps of: (1) extracting Sargassum sagamianum with water or methanol to obtain a crude extract; (2) evaporating a solvent of the crude extract under reduced pressure to obtain a residue, and obtaining fractions from the residue according to polarities thereof; and (3) evaporating a solvent of the fractions to obtain an organic concentrate, and then purifying and isolating the organic concentrate by chromatography.
Abstract translation: 提供十八四烯酰甘油化合物或其药学上可接受的衍生物，通过抑制5-脂氧合酶的活性并显示出对磷脂酶A2的强抑制活性来预防和治疗炎性疾病，过敏和哮喘。 十八四烯酰基甘油化合物或其药学上可接受的衍生物具有由式（A）表示的结构。 分离十八四烯酰甘油化合物的方法包括以下步骤：（1）用水或甲醇萃取马齿苋，得到粗提物; （2）减压蒸发粗提取物的溶剂，得到残渣，根据其极性从残渣中得到馏分; 和（3）蒸发馏分的溶剂，得到有机浓缩物，然后通过色谱法纯化和分离有机浓缩物。
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公开(公告)号：KR1020070054863A
公开(公告)日：2007-05-30
申请号：KR1020050112928
申请日：2005-11-24
Applicant: 재단법인서울대학교산학협력재단
IPC: C07C213/08
CPC classification number: Y02P20/55
Abstract: 본 발명은 개선된 스핑고신 유사체의 제조 방법에 관한 것으로, 팔라듐으로 촉매된 소노가시라 중합반응을 합성단계 중에 이용하고, 아세토나이드 및 Boc 보호기를 동시에 제거하여 간결하고 효과적으로 고수율의 스핑고신 유사체를 얻을 수 있으므로, 경제적으로 산업적 규모의 대량 생산에 사용될 수 있으며, 다른 유사체들의 대량 반응에도 유용하게 사용될 수 있다.
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公开(公告)号：KR1020090056584A
公开(公告)日：2009-06-03
申请号：KR1020070123798
申请日：2007-11-30
Applicant: (주)아모레퍼시픽 , 재단법인서울대학교산학협력재단
CPC classification number: A61K31/16
Abstract: A pharmaceutical composition regulating the activity of sphingosylphosphorylcholine(SPC) is provided to regulate cell proliferation, inflammation and pruritus and treat inflammmatin or pruritus of dermatitis such as atopic dermatitis. A pharmaceutical composition which regulates the activity of sphingosylphosphorylcholine(SPC) comprises a compound of the chemical formula 1 or its pharmaceutically allowable salt. In the chemical formula 1, X is O or S, Y is CH2 or carbonyl. R1 is hydrogen or C1-10 alkyl, R2 is hydrogen or methyl, but when X is O, either R1 or R2 cannot be hydrogen, R3 is C1-4 alkyl. A method for manufacturing a compound of the chemical formula 1a comprises: a step of reacting a compound of the chemical formula 2 and a compound of the chemical formula 3 under the presence of base to obtain a compound of the chemical formula 4; a step of stirring the compound of the chemical formula 4 under the presence of base to obtain a compound of the chemical formula 5; and a step of performing the peptide bond between the compound of the chemical formula 5 and a compound of the chemical formula 6 to obtain the compound of the chemical formula 1a.
Abstract translation: 提供调节肌动蛋白磷酰胆碱（SPC）活性的药物组合物，用于调节细胞增殖，炎症和瘙痒，并治疗诸如特应性皮炎等炎性炎症或皮炎瘙痒症。 调节鞘糖基磷酰胆碱（SPC）活性的药物组合物包含化学式1的化合物或其药学上可允许的盐。 在化学式1中，X为O或S，Y为CH 2或羰基。 R1是氢或C1-10烷基，R2是氢或甲基，但当X是O时，R1或R2不能是氢，R3是C1-4烷基。 制备化学式1a化合物的方法包括：使化学式2的化合物与化学式3化合物在碱存在下反应得到化学式4的化合物的步骤; 在碱的存在下搅拌化学式4的化合物以获得化学式5的化合物的步骤; 在化学式5的化合物与化学式6的化合物之间进行肽键的步骤，得到化学式1a的化合物。
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