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公开(公告)号：KR100893763B1
公开(公告)日：2009-04-20
申请号：KR1020070087036
申请日：2007-08-29
Applicant: 한국화학연구원
IPC: C12P41/00
Abstract: 본 발명은 광학활성 알킬 3-하이드록시부타노에이트 유도체의 제조방법에 관한 것으로, 보다 구체적으로는 캔디다 안타르크티카(
Candida
antarctica ) 유래의 리파제, 슈도모나스 세파시아(
Pseudomonas
cepacia ) 유래의 리파제, 리조무코어 미에헤이(
Rhizomucor
miehei ) 유래의 리파제, 버코올데리아 세파시아(
Burkholderia
cepacia ) 유래의 아마노(Amano) PS 리파제, 아마노 리파제 PS-CI, 아마노 리파제 PS-CII, 또는 아마노 리파제 PS-DI, 리파제-OF 촉매 존재 하에, 라세믹 β-락톤 유도체를 알코올과 반응시켜 입체선택적으로 가알코올분해(alcoholysis) 반응을 수행한 후, 다시 산 존재하에 가알코올분해하여 (S) 및 (R)-형태의 광학활성체로서의 광학활성 알킬 3-하이드록시부타노에이트를 얻는 것을 특징으로 한다.
광학활성 알킬 3-하이드록시부타노에이트, 리파제 촉매, 라세믹 β-락톤-
22.发明公开
公开(公告)号：KR1020080055756A
公开(公告)日：2008-06-19
申请号：KR1020080039550
申请日：2008-04-28
IPC: A61K31/045 , A61K31/435 , A61P35/00
CPC classification number: Y02A50/411
Abstract: A pharmaceutical composition comprising beta-aminoalcohol derivatives is provided to inhibit secretion of TNF-alpha(tumor necrosis factor-alpha), so that the composition is useful for preventing or treating TNF-alpha mediated diseases. A pharmaceutical composition for preventing or treating TNF-alpha mediated diseases comprises beta-aminoalcohol derivatives represented by the formula(1), wherein R^1 is phenyl optionally substituted by halogen; R^2 is pyridinyl optionally substituted by cyano or halogen, pyrimidinyl, indolyl or quinolyl; R^3 is hydrogen or C1-4 alkyl; and daily dosage of the compounds is 0.1-10 mg/kg for parenteral administration or 1-100mg/kg for oral administration.
Abstract translation: 提供包含β-氨基醇衍生物的药物组合物以抑制TNF-α（肿瘤坏死因子-α）的分泌，使得该组合物可用于预防或治疗TNF-α介导的疾病。 用于预防或治疗TNF-α介导的疾病的药物组合物包括由式（1）表示的β-氨基醇衍生物，其中R 1是任选被卤素取代的苯基; R 2是任选被氰基或卤素取代的吡啶基，嘧啶基，吲哚基或喹啉基; R 3是氢或C 1-4烷基; 化合物的日剂量为0.1-10mg / kg用于胃肠外给药或1-100mg / kg口服给药。
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23.发明公开아미노 치환기를 갖는 알파-아릴메톡시아크릴레이트 유도체및 이를 함유하는 대사성 골 질환의 예방 및 치료용 약학조성물 有权具有氨基取代基和药物组合物的ALPHA-ARYLMETHOXYACRYLATE衍生物用于预防和治疗含有其的代谢性骨髓疾病
公开(公告)号：KR1020060134303A
公开(公告)日：2006-12-28
申请号：KR1020050053883
申请日：2005-06-22
IPC: A61K31/44 , A61K31/496 , A61K31/535
CPC classification number: A61K31/5375 , A61K31/136 , A61K31/4439 , A61K31/451
Abstract: A pharmaceutical composition comprising an alpha-arylmethoxyacrylate derivative is provided to be able to excellently inhibit osteoclast formation and absorption activity thereof, thereby being effectively utilized for preventing metabolic bone diseases such as osteoporosis and ossification at a growth period. The pharmaceutical composition for preventing and treating metabolic bone disease comprises an alpha-arylmethoxyacrylate derivative represented by the formula(1), a physiologically acceptable salt thereof or a solvate thereof as an effective ingredient. In the formula(1), A is N or CH, X is H or halogen, Y is H, halogen or CF3, Z is substituted or unsubstituted N-containing heteroaryl or (CH2)n-NR^1R^2(where n is 0, 1 or 2 and each R^1 and R^2 is independently H, C1-8 alkyl, C1-8 haloalkyl, hydroxy, C2-8 alkenyl, C2-4 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkyl C1-4 alkyl, C1-4 alkoxy C1-4 alkyl, C3-8 cycloalkoxy C1-4 alkyl, C1-8 alkylsulfonyl, C2-7 heterocyclyl C1-4 alkyl containing at least one N, O or S, or substituted or unsubstituted aryl, or forms a heterocycle with adjacent N).
Abstract translation: 提供包含α-芳基甲氧基丙烯酸酯衍生物的药物组合物，以能够极好地抑制破骨细胞形成和吸收活性，从而有效地用于预防生长期骨质疏松和骨化等代谢骨疾病。 用于预防和治疗代谢性骨病的药物组合物包含由式（1）表示的α-芳基甲氧基丙烯酸酯衍生物，其生理学上可接受的盐或其溶剂合物作为有效成分。 在式（1）中，A是N或CH，X是H或卤素，Y是H，卤素或CF 3，Z是取代或未取代的含N杂芳基或（CH 2）n -NR 4 R 12（其中n 每个R 1和R 2独立地为H，C 1-8烷基，C 1-8卤代烷基，羟基，C 2-8烯基，C 2-4炔基，C 3-8环烷基，C 3-8环烷基 C 1-4烷基，C 1-4烷氧基C 1-4烷基，C 3-8环烷氧基C 1-4烷基，C 1-8烷基磺酰基，含有至少一个N，O或S的C 2-7杂环基C 1-4烷基，或取代或未取代的 芳基，或与相邻的N形成杂环）。
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24.发明授权
公开(公告)号：KR100575479B1
公开(公告)日：2006-05-10
申请号：KR1020050056454
申请日：2005-06-28
CPC classification number: A61K31/34 , A23L33/10 , A23L33/15 , A23L33/16 , A61K31/341 , C07D307/68
Abstract: 본 발명은 퓨란 유도체 및 그의 약학적으로 허용가능한 염을 함유하는 골다공증 예방 및 치료용 식품 조성물에 관한 것으로, 더욱 구체적으로 하기 화학식 1로 표시되는 퓨란 유도체는 종래 골다공증 치료제에 비해 골 증식 효과가 우수할 뿐만 아니라 부작용이 적어 골질환 예방 및 치료를 위한 의약품 또는 기능성 식품으로 사용할 수 있다.
화학식 1
(상기 식에서, X 및 Y는 하기 명세서에서 정의한 바와 같다.)-
25.发明公开
公开(公告)号：KR1020050002109A
公开(公告)日：2005-01-07
申请号：KR1020030043425
申请日：2003-06-30
IPC: A61K31/15
CPC classification number: A61K31/15 , A23L29/055 , A61K9/20 , A61K9/48
Abstract: PURPOSE: Provided is a composition comprising a methoxyacrylate-based compound. The composition inhibits osteoclast generation and bone absorption strongly without cytotoxicity to prevent or treat osteoporosis easily and effectively. CONSTITUTION: The pharmaceutical composition for prevention and treatment of osteoporosis is characterized by containing as an active ingredient, a methoxyacrylate-based compound represented by the formula(1) and pharmaceutically acceptable carriers. In the formula, X is CH or N; Y is O or S; Z is O or NHR1 and R2 are independently H; C1-4 alkyl; C1-4 alkyl having at least one of halogen substituents; phenyl having at least one substituent selected from halogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, phenoxy and methylenedioxy; or naphthyl.
Abstract translation: 目的：提供包含甲氧基丙烯酸酯类化合物的组合物。 该组合物强烈地抑制破骨细胞产生和骨吸收而不具有细胞毒性以便容易且有效地预防或治疗骨质疏松症。 构成：用于预防和治疗骨质疏松症的药物组合物的特征在于含有式（1）表示的基于甲氧基丙烯酸酯的化合物和药学上可接受的载体作为活性成分。 在该式中，X是CH或N; Y为O或S; Z是O或NHR1，R2独立地是H; C 1-4烷基; 具有至少一个卤素取代基的C 1-4烷基; 具有至少一个选自卤素，C 1-4烷基，C 1-4卤代烷基，C 1-4烷氧基，苯氧基和亚甲二氧基的取代基的苯基; 或萘基。
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Patent Agency Ranking
公开(公告)号：KR1020030032301A
公开(公告)日：2003-04-26
申请号：KR1020010064008
申请日：2001-10-17
Applicant: 에스케이바이오랜드 주식회사 , 한국화학연구원
IPC: C07C67/313
CPC classification number: C07C67/08 , C07C67/14 , C07C68/02 , C07C69/017 , C07C69/96 , C07C69/16 , C07C69/78
Abstract: PURPOSE: A monocarbonylation method of benzenediol is provided, to prepare the monocarbonyl benzenediol with a high production yield without using a base. CONSTITUTION: The method comprises the step of reacting the benzenediol represented by the formula II with an acid anhydride or a carbonyl halide represented by the formula III in the absence of an organic or inorganic base to prepare the monocarbonyl benzenediol represented by the formula I, wherein R is H, an alkyl group of C1-C14, a cycloalkyl group, an aryl group, an alkoxy group, an aryloxy group, a dialkylamino group, an alkylarylamino group or a diarylamino group; and X is a common leaving group comprising Cl or an acetoxy group. The unreacted benzenediol of the formula II is recovered by using a nonpolar solvent, and the nonpolar solvent is at least one selected from the group consisting of benzene, toluene, xylene, ether, hexane, petroleum ether, methylene chloride and chloride.
Abstract translation: 目的：提供苯二酚的单羰基化方法，以无需使用碱就可以高产率地制备单羰基苯二酚。 方案：该方法包括在不存在有机或无机碱的情况下使由式II表示的苯二酚与式III表示的酸酐或羰基卤反应以制备由式I表示的单羰基苯二酚，其中 R是H，C1-C14的烷基，环烷基，芳基，烷氧基，芳氧基，二烷基氨基，烷基芳基氨基或二芳基氨基; 并且X是包含Cl或乙酰氧基的常见离去基团。 通过使用非极性溶剂回收式II的未反应的苯二酚，非极性溶剂为选自苯，甲苯，二甲苯，醚，己烷，石油醚，二氯甲烷和氯化物中的至少一种。
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27.发明授权
公开(公告)号：KR100379761B1
公开(公告)日：2003-04-11
申请号：KR1020000070103
申请日：2000-11-23
Applicant: 한국화학연구원
IPC: C07C211/37
Abstract: PURPOSE: Provided are novel propanoic ester and amide derivatives having an oxime group as a branched chain, which are excellent in disinfecting activity, a preparation thereof, and a disinfectant composition containing the propanoic ester and amide derivatives. CONSTITUTION: The propaonic ester and amide derivatives represented by the formula 1 are produced by a process comprising the steps of: reacting a bromine compound represented by the formula 2 and 2,3-butanedione monoxime represented by the formula 3 in the presence of a base to produce an oxime-based ketone compound; reducing the oxime-based ketone compound or condensing the oxime-based ketone compound with a hydroxyl amine to produce an oxime-based alcohol compound or a dioxime-based compound; reacting the oxime-based alcohol compound or the dioxime-based compound with a propanyl fluoride compound in the presence of a base. In the formula, R1 is trifluoromethyl, R2 is a phenyl group, X is CH or N, and Y is O or NH.
Abstract translation: 目的：提供具有肟基作为支链的新型丙酸酯和酰胺衍生物，其消毒活性极好，其制备和含有丙酸酯和酰胺衍生物的消毒剂组合物。 构成：由式1代表的丙酸酯和酰胺衍生物通过包括以下步骤的方法制备：使式2代表的溴化合物和式3代表的2,3-丁二酮单肟在碱存在下反应 制造肟类酮化合物; 还原所述肟类酮化合物或使所述肟类酮化合物与羟基胺缩合以制备肟类醇类化合物或二肟类化合物; 使肟基醇化合物或二肟基化合物与丙基氟化物在碱存在下反应。 在该式中，R1是三氟甲基，R2是苯基，X是CH或N，并且Y是O或NH。
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28.发明公开옥심기를 가교로 하는, 불소화 비닐기가 치환된 프로페노익 에스테르 및 아미드 화합물, 이의 제조방법 및 이를 포함하는 살균제 조성물 有权由氟族基团交联并由氟化乙烯基团取代的新型丙烯酸酯和酰胺化合物，其制备方法和包括其的双酚A的组合物
公开(公告)号：KR1020010017960A
公开(公告)日：2001-03-05
申请号：KR1019990033722
申请日：1999-08-16
Applicant: 한국화학연구원
IPC: C07C207/00
Abstract: PURPOSE: Provided is a novel propenoic ester and amide compound being cross-linked by an oxime group and substituted by a fluorinated vinyl group. The novel compound has excellent sterilizability and a broad antibacterial activity. Also, its preparation method and a bactericide composition including these are provided. CONSTITUTION: A novel propenoic ester compound being cross-linked by an oxime group and substituted by a fluorinated vinyl group is represented by the formula (1), wherein X is CH or N ; Y is O or NH ; R1 is hydrogen, C1-4 alkyl or C1-4 alkyl substituted with halogen ; and R2 is phenyl, C1-4 alkyl,, C1-4 alkyl substituted with halogen, C1-4 alkoxy, methylenedioxy, phenyl in which more than one group is substituted with halogen or naphthalene. The novel propenoic ester compound is prepared by reacting a brominated compound of the formula (2) and an oxime compound of the formula (3) in the presence of a base, to obtain compound of the formula (4); debenzylating the resultant compound, to obtain phenolic ester compound of the formula (5); and reacting the resultant compound with a fluorinated vinyl compound of the formula (6) in the presence of a base.
Abstract translation: 目的：提供一种新的丙烯酸酯和酰胺化合物，通过肟基交联并被氟化乙烯基取代。 该新型化合物具有优异的灭菌性和广泛的抗菌活性。 此外，还提供了其制备方法和包括这些的杀菌剂组合物。 构成：通过肟基交联并被氟代乙烯基取代的新型丙烯酸酯化合物由式（1）表示，其中X为CH或N; Y是O或NH; R1是氢，C1-4烷基或被卤素取代的C1-4烷基; 和R 2是苯基，C 1-4烷基，被卤素取代的C 1-4烷基，C 1-4烷氧基，亚甲二氧基，其中多于一个基团被卤素或萘取代的苯基。 通过使式（2）的溴化化合物与式（3）的肟化合物在碱的存在下反应制备新的丙烯酸酯化合物，得到式（4）的化合物; 将所得化合物脱苄化，得到式（5）的酚酯化合物; 并使所得化合物与式（6）的氟化乙烯基化合物在碱的存在下反应。
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公开(公告)号：KR100123414B1
公开(公告)日：1997-11-12
申请号：KR1019940015476
申请日：1994-06-30
Applicant: 한국화학연구원
IPC: C07C57/26
Abstract: This invention relates to fluoride substituted abscisic acid derivatives of formula (I) wherein R is alkyl group of C1-C2, X is H2 or O, and Y is H or OH. A fluoride replaced abscisic acid derivative is produced by witting reaction of triethyl 2-fluorophosphonoacetate with alpha-ionone. Fluoride replaced abscisic acid (ABA) derivatives are more stable than natural ABA and have strong physiological activity, so they can be used as a active ingredient of plant growth regulators such as herbicides or dwarfing chemicals.
Abstract translation: 本发明涉及式（I）的氟化物取代的脱落酸衍生物，其中R是C1-C2的烷基，X是H2或O，Y是H或OH。 通过使2-氟膦酰基乙酸三乙酯与α-紫罗兰酮的反应产生氟化物替代的脱落酸衍生物。 氟化物替代脱落酸（ABA）衍生物比天然ABA更稳定，具有很强的生理活性，因此可用作植物生长调节剂如除草剂或矮化剂的有效成分。
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公开(公告)号：KR1019950032108A
公开(公告)日：1995-12-20
申请号：KR1019940010019
申请日：1994-05-07
Applicant: 한국화학연구원
IPC: C07C321/24 , C07C317/14
Abstract: 본 발명은 신규한 비닐술파이드 및 술폰계 화합물에 관한 것이다. 좀 더 구체적으로, 본 발명은 하기 일반식(I) 및 (Ⅱ)로 표시되는 신규한 비닐 술파이드 및 술폰계 화합물과 그의 제조방법 및, 살균제로서의 용도에 관한 것이다.
상기식에서, n은 O 또는 2의 정수이며; 및 R
1 은 탄소수 1 내지 6개의 1, 2, 3급의 알콕시기; 탄소수 1 내지 6개의 1, 2, 3차 아민기; 수소, 할로겐, 메틸, 니트로가 치환된 페녹시기; 수소, 할로겐, 메틸, 니트로가 치환된 페닐티오기; 2, 2. 2-트리플루오로에톡시기; 에틸티오기; 패닐티오기; 에틸술포닐기 ; 페닐술포닐기; ω-히드록시가 치환된 메틸렌이 2 내지 8개인 옥시 또는 티오옥시기 ; ω-히드록시가 치환된 메틸렌이 2 내지 8개인 술폰기; 또는, 에틸렌디아민기이다.
본 발명에 의해 제조된 비닐 술파이드 및 술폰계 화합물은 그 자체로서 살균활성을 갖는 농약의 활성성분으로 이용될 수 있으며, 농약 및 의약의 유효성분을 합성하는 중간체로서도 유용할 것으로 밝혀졌다.
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