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公开(公告)号：KR1020030032592A
公开(公告)日：2003-04-26
申请号：KR1020010064474
申请日：2001-10-18
IPC: C07F1/06
CPC classification number: C07C235/84 , A61K31/166
Abstract: PURPOSE: Provided are a preparation method of 1,2-naphthoquinone derivatives of formula(1) and their pharmaceutically acceptable salt which inhibit the activity of protein phosphatase. The compounds are widely used in treatment of type 1 and 2 diabetes, autoimmune diseases, acute and chronic infection and various cancers. CONSTITUTION: The method of preparation of 1,2-naphthoquinone derivatives represented by the formula(1) as defined in the specification and their pharmaceutically acceptable salt comprises the steps of: oxidizing a naphthol compound of formula(2) with selenium oxides and obtaining a compound of formula(3); and substituting B at 4 position of the compound(3) using mixtures selected from (Pb(OAc)2),CeCl3 7H2O and NaIO3 mixture and RMgX and CuCN mixture.
Abstract translation: 目的：提供抑制蛋白磷酸酶活性的式（1）的1,2-萘醌衍生物及其药学上可接受的盐的制备方法。 该化合物广泛用于治疗1型和2型糖尿病，自身免疫性疾病，急性和慢性感染和各种癌症。 构成：由说明书中定义的式（1）表示的1,2-萘醌衍生物及其药学上可接受的盐的制备方法包括以下步骤：用氧化硒氧化式（2）的萘酚化合物，得到 式（3）化合物; 并且使用选自（Pb（OAc）2），CeCl 3·7H 2 O和NaIO 3混合物的混合物和RMgX和CuCN混合物在化合物（3）的4位置取代B。
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公开(公告)号：KR100380520B1
公开(公告)日：2003-04-23
申请号：KR1020000053309
申请日：2000-09-08
Applicant: 한국화학연구원
IPC: C07D213/24
Abstract: PURPOSE: Provided are β-aminoalcohol derivative containing pyridine, its pharmaceutically acceptable salt and its manufacturing method. The β-aminoalcohol derivative has a hypotensive effect and reduces weight, and is thus used as a therapeutic gent in hyperglycemia related diseases or obesity. CONSTITUTION: β-aminoalcohol derivative containing pyridine is represented by the formula(I), wherein A is halogen atom or haloalkyl substituted or unsubstituted phenyl, thiophene, phenyloxymethyl, naphthyloxymethyl, or biphenyloxymethyl group; R is hydrogen or C1-4 alkyl group; Y is methylene or oxygen; and G is at least one substituent selected from the group consisting of hydrogen, halogen atom, C1-3 alkyl, alkoxy, amino, cyano, phenyl substituted urea, phenyl or C1-3 alkyl substituted carboxamide, carboxylester, alkoxy carbonyl methyloxy, alkoxycarbonylalkyl group, alkoxycarbonylacryl and tetrazol group. It is manufactured by condensation reaction with a compound of the formula(II) and a compound of the formula(III) and hydrogenation with organic metal catalyst.
Abstract translation: 用途：提供含有吡啶的β-氨基醇衍生物，其药学上可接受的盐及其制造方法。 β-氨基醇衍生物具有降压作用并减轻体重，因此用作高血糖相关疾病或肥胖症的治疗剂。 构成：含吡啶的β-氨基醇衍生物由式（I）表示，其中A为卤素原子或卤代烷基，取代或未取代的苯基，噻吩，苯氧基甲基，萘氧基甲基或联苯氧基甲基; R为氢或C 1-4烷基; Y是亚甲基或氧; G是至少一个选自氢，卤原子，C1-3烷基，烷氧基，氨基，氰基，苯基取代的脲，苯基或C1-3烷基取代的羧酰胺，羧酸酯，烷氧基羰基甲氧基，烷氧基羰基烷基 ，烷氧基羰基丙烯酰基和四唑基。 它是通过与式（II）化合物和式（III）化合物缩合反应并用有机金属催化剂氢化而制得的。
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公开(公告)号：KR1019960011370B1
公开(公告)日：1996-08-22
申请号：KR1019910025885
申请日：1991-12-31
Applicant: 한국화학연구원
IPC: C07D209/12
CPC classification number: C07D221/20 , C07D209/54 , Y02P20/55
Abstract: Spiroalkylamine derivatives and their salts have a general formula (I), wherein R1 is hydrogen, substituted or unsubstituted C1-C20 alkyl, substituted or unsubstituted benzyl, formyl, substituted or unsubstituted C1-C5 alkylcarbonyl, substituted or unsubstituted benzoyl, substituted or unsubstituted C1-C5 alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl, substituted or unsubstituted C1-C5 alkylsulfonyl, or substituted or unsubstituted benzenesulfonyl; R2 is hydrogen or methyl substituted at the position of 4 or 6; R3 is hydroxy, hydroxymethyl, carboxy, C1-C4 alkoxy, C2-C5 alkoxymethyl, C2-C5 acyloxy, C3-C6 acyloxymethyl, methanesulfonyloxy, methanesulfonyloxymethyl, p-toluenesulfonyloxy, p-toluenesulfonyloxymethyl, cyanato, C2-C6 alkoxycarbonyl, azidocarbonyl, C1-C8 alkyl, C1-C5 alkoxycarbonyl, aminocarbonyl substituted or unsubstituted benzyl or -(CH2)m-NR4R5, where m is 0 or 1; R4 is hydrogen, C1-C4 alkanoyl or benzoyl; and R5 is hydrogen, C1-C4 -alkyl, nitrogen protective group degradable in a living body, n is 1 or 2, diastereomers may be (1,3)-R,S, (1,3)-R,R, (1,3)-S,S or (1,3)-S,R.
Abstract translation: 螺烷基胺衍生物及其盐具有通式（I），其中R1是氢，取代或未取代的C1-C20烷基，取代或未取代的苄基，甲酰基，取代或未取代的C1-C5烷基羰基，取代或未取代的苯甲酰基，取代或未取代的C1 C 5烷氧基羰基，取代或未取代的苄氧基羰基，取代或未取代的C 1 -C 5烷基磺酰基，或取代或未取代的苯磺酰基; R2为4或6位的氢或甲基取代; R3是羟基，羟甲基，羧基，C1-C4烷氧基，C2-C5烷氧基甲基，C2-C5酰氧基，C3-C6酰氧基甲基，甲磺酰氧基，甲磺酰氧基甲基，对甲苯磺酰氧基，对甲苯磺酰氧基甲基，氰基，C2-C6烷氧羰基，叠氮羰基，C1 C 1-8烷基，C 1 -C 5烷氧基羰基，氨基羰基取代或未取代的苄基或 - （CH 2）m -NR 4 R 5，其中m为0或1; R4是氢，C1-C4烷酰基或苯甲酰基; R5为氢，C1-C4烷基，可在生物体中降解的氮保护基，n为1或2，非对映异构体可为（1,3）-R，S，（1,3）-R，R（（ 1,3）-S，S或（1,3）-S，R。
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公开(公告)号：KR1019950018001A
公开(公告)日：1995-07-22
申请号：KR1019930026941
申请日：1993-12-08
Applicant: 한국화학연구원 , 스미스크라인 비참 리미티드
IPC: C07D471/04
Abstract: 본 발명은 다음 일반식(I)로 표시되는 퀴놀론계 유도체와 약제학적으로 허용가능한 그의 산 부가염에 관한 것이다.
윗 식에서, R
1 은 탄소 원자수가 1-3인 사슬형 또는 고리형 저급알킬기, 할로겐이 치환된 탄소원자수가 1-3인 사슬형 또는 고리형 저급알킬기, 페닐기 또는 1-2개의 할로겐이 치환된 페닐기이고; R
2 는 수소 원자, 저급알킬기 또는 아미노기이며; R
3 는 할로겐 원자 또는 치환되거나 치환되지 않은, 헤테로 원자로 고리내에 적어도 1개의 질소 원자를 포함하는 헤테로 고리 화합물로서 다음의 일반식(A):
(윗 식에서 R
6 ,R
7 ,R
8 및 R
9 는 각각 수소 원자이거나 저급 알킬기이며, 이들 중 둘은 서로 결합을 형성할 수 있고, m 및 n은 0 내지 1이며 Ca-Cb는 결합을 형성하지 않거나 단일 결합 또는 이중 결합을 나타낸다.)로 표시되거나, 또는 다음의 일반식(B):
(윗 식에서, R
10 은 수소 원자이거나, 또는 메틸, 에틸 또는 부톡시카르보닐 같은 저급알킬기 또는 아미노보호기이고, R
11 ,R
12 ,R
13 및 R
14 은 같거나 다르며, 각각 수소, 또는 아미노기, 히드록시기 또는 할로겐으로 임의 치환된, 메틸 또는 에틸과 같은 저급알킬기이다.)로 표시되며; X는 질소 원자 또는 CR
4 (여기서 R
4 는 수소원자, 할로겐원자, 저급알킬기 또는 저급 알콕시기를 나타낸다.)를 나타내며; R
4 와 R
1 은 함께 고리를 형성하여 -CH
2 CH
2 CH
2 -,-CH
2 CH
2 CH(CH
3 )-,OCH
2 CH
2 ,-OCH
2 CH(CH
3 )-,-SCH
2 CH
2 - 또는 -SCH
2 CH(CH
3 )-일 수 있으며; Y는 산성 프로톤[p＜α＜14]을 갖는 5 내지 7원의 카르복실 또는 헤테로시클릭 고리의 잔기이다.
본 발명은 또한 상기 일반식(I)의 화합물의 유효성분으로 함유하는 항균제에 관한 것이다.-
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Patent Agency Ranking
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公开(公告)号：KR1019940002955B1
公开(公告)日：1994-04-09
申请号：KR1019910006363
申请日：1991-04-20
Applicant: 한국화학연구원
IPC: C07D487/04
Abstract: The quinolone cpd. or its salts of formula (I) are prepd. by heating and reacting the cpd. (II) with the cpd. (III) or (IIIa) in presence of the base. In the formulas, R1 is opt. substd. C1-7 lower alkyl, opt. substd. C3-7 cycloalkyl, opt. substd. lower alkenyl, opt. substd. phenyl; R2 is H, protecting gp. of carboxyl gp. or pharmaceutically usuable metalic or organic cation; R3 is H or C1-4 lower alkyl, C2-4 hydroxy alkyl, C3-7 cycloalkyl or biodegradable N-protecting gp.; X is Cl or Br; Z is methyl; n is 1-3; n is 1 or 2; A is Cl or Br; L is halogen, ethane sulfonyl or paratoluene sulfonyl. The compound is antibacterial.
Abstract translation: 喹诺酮cpd 或其式（I）的盐是制备的。 通过加热和反应cpd。 （II）与cpd。 （III）或（IIIa）。 在公式中，R1是opt。 substd。 C1-7低级烷基，选择。 substd。 C3-7环烷基， substd。 低级链烯基 substd。 苯基; R2是H，保护gp。 的羧基gp。 或药学上可用的金属或有机阳离子; R3是H或C1-4低级烷基，C2-4羟基烷基，C3-7环烷基或可生物降解的N-保护性gp。 X是Cl或Br; Z是甲基; n为1-3; n为1或2; A是Cl或Br; L是卤素，乙磺酰基或对甲苯磺酰基。 该化合物是抗菌的。
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公开(公告)号：KR1019920005745B1
公开(公告)日：1992-07-18
申请号：KR1019900004181
申请日：1990-03-28
Applicant: 한국화학연구원
IPC: C07D498/04 , C07D498/06
Abstract: Benzoxazine derivs. of formula (I) and their pharmaceutically acceptable acid addn. salts are new. In (I), R1 and R2 each = H or lower alkyl; n = 1 or 2. Also clainned is the prepn. of (I) which comprises reacting a benzoxazine carboxylic acid deriv. of formula (II) with a cpd. of formula (III) at room temp. -200 deg.C for 1- 10 hr(s). In (II), X= halogen. The cpds. (I) have a good antibacterial activity, a broad spectrum activity, low toxicity and high bioavailability.
Abstract translation: 苯并恶嗪衍生物。 的式（I）化合物及其药学上可接受的酸加成。 盐是新的。 在（I）中，R 1和R 2各自为H或低级烷基; n = 1或2.也是准备工作。 的（I），其包括使苯并恶嗪羧酸衍生物反应。 的式（II）与cpd。 的式（III）。 -200℃，持续1-10小时（s）。 在（II）中，X =卤素。 cpds。 （I）具有良好的抗菌活性，广谱活性，低毒性和高生物利用度。
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公开(公告)号：KR1019920008051A
公开(公告)日：1992-05-27
申请号：KR1019900016941
申请日：1990-10-23
Applicant: 한국화학연구원
IPC: C07D501/24
Abstract: 내용 없음
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