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公开(公告)号：KR100428703B1
公开(公告)日：2004-04-30
申请号：KR1020000005140
申请日：2000-02-02
Applicant: 한국과학기술연구원
IPC: C07D309/04
Abstract: PURPOSE: A novel macrolide compound having an inhibiting activity for the growth of Helicobacter pylori is provided, which is not easily decomposed by gastric acid. CONSTITUTION: The macrolide compound is represented by formula (1), in which R1 is hydrogen, 4-methoxy phenoxy methyl, 2-methoxy phenoxy methyl or methoxy ethoxy methyl; R2 is hydrogen, acyl or lower alkoxy; R3 is the same or different and hydrogen or acyl; and Q and W form oxo together or independently -OR4 and hydrogen, wherein R4 is hydrogen. It has an inhibiting activity for the growth of Helicobacter pylori which causes several stomach diseases.
Abstract translation: 目的：提供一种对幽门螺杆菌生长具有抑制活性的新型大环内酯化合物，其不易被胃酸分解。 构成：大环内酯类化合物由式（1）表示，其中R1为氢，4-甲氧基苯氧基甲基，2-甲氧基苯氧基甲基或甲氧基乙氧基甲基; R2是氢，酰基或低级烷氧基; R3相同或不同，为氢或酰基; 并且Q和W一起或独立地形成氧代-OR 4和氢，其中R 4是氢。 它对幽门螺杆菌的生长具有抑制活性，引起多种胃病。
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公开(公告)号：KR1020010077376A
公开(公告)日：2001-08-17
申请号：KR1020000005140
申请日：2000-02-02
Applicant: 한국과학기술연구원
IPC: C07D309/04
Abstract: PURPOSE: A novel macrolide compound having an inhibiting activity for the growth of Helicobacter pylori is provided, which is not easily decomposed by gastric acid. CONSTITUTION: The macrolide compound is represented by formula (1), in which R1 is hydrogen, 4-methoxy phenoxy methyl, 2-methoxy phenoxy methyl or methoxy ethoxy methyl; R2 is hydrogen, acyl or lower alkoxy; R3 is the same or different and hydrogen or acyl; and Q and W form oxo together or independently -OR4 and hydrogen, wherein R4 is hydrogen. It has an inhibiting activity for the growth of Helicobacter pylori which causes several stomach diseases.
Abstract translation: 目的：提供一种具有幽门螺杆菌生长抑制活性的新型大环内酯类化合物，不易被胃酸分解。 构成：大环内酯类化合物由式（1）表示，其中R1是氢，4-甲氧基苯氧基甲基，2-甲氧基苯氧基甲基或甲氧基乙氧基甲基; R2是氢，酰基或低级烷氧基; R3相同或不同，为氢或酰基; 并且Q和W一起或独立地代表-OR4和氢，其中R4是氢。 它对幽门螺杆菌的生长具有抑制作用，导致多种胃部疾病。
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4.发明公开신규 피리도[2,3-ｄ]피리미딘 카르보알데히드 옥심계ＰＤＥ Ⅳ 효소 저해 화합물 및 이의 제조방법 失效PYRIDO [2,3-D]吡啶二羰基氧化物衍生物作为PDE IV抑制剂及其制备方法有用
公开(公告)号：KR1020030076072A
公开(公告)日：2003-09-26
申请号：KR1020020015728
申请日：2002-03-22
IPC: C07D471/04
Abstract: PURPOSE: Pyrido£2,3-d|pyridine carboaldehyde oxime derivatives useful as PDE IV inhibitor and a preparation method thereof are provided, which compounds are useful for treatment of respiration diseases, and diseases associated with TNF(tumor necrosis factor) formation. CONSTITUTION: Pyrido£2,3-d|pyridine carboaldehyde oxime derivatives represented by formula (I) or pharmaceutically acceptable salts are provided, wherein R1 is C1-3 lower alkyl, C3-7 cycloalkyl, cycloalkyloxy, cycloalkylamino, cycloalkyl lower alkyl, C1-3 lower alkoxy, formyl, hydroxy lower alkyl or carboxyalkyl, or X-substituted phenyl, in which X is methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, cyano, carboxylic acid, carboxymethyl ester, carboxyethyl ester, nitro, fluoro or trifluoromethyl; R2 is hydrogen or methyl; and R3 is hydrogen, methyl, C3-7 lower alkyloxy, allyl, phenyl, benzyl, X-substituted phenyl, methyloxyphenyl or methyloxy Y-substituted phenyl in which X is cyano, halogen, carboxyalkyl, nitro, methyl, trihalogenated methyl or alkyloxy, and Y is methoxy. A method for preparing pyrido£2,3-d|pyridine carboaldehyde oxime derivatives of formula (I) comprises preparing a compound of formula (III) from a compound of formula (II) in the presence of palladium catalyst and base; reacting the compound of formula (III) with hydroxylamine, alkyloxyamine or hydrochloric acid salts thereof.
Abstract translation: 目的：提供用作PDE IV抑制剂的吡啶2,3-d-吡啶甲醛肟衍生物及其制备方法，该化合物可用于治疗呼吸疾病和与TNF（肿瘤坏死因子）形成相关的疾病。 构成：提供由式（I）表示的吡啶2,3-d-吡啶甲醛肟衍生物或其药学上可接受的盐，其中R 1为C 1-3低级烷基，C 3-7环烷基，环烷氧基，环烷基氨基，环烷基低级烷基，C 1 -3低级烷氧基，甲酰基，羟基低级烷基或羧基烷基或X取代的苯基，其中X是甲基，乙基，丙基，异丙基，甲氧基，乙氧基，丙氧基，异丙氧基，氰基，羧酸，羧甲基酯，羧乙基酯， 硝基，氟或三氟甲基; R2是氢或甲基; R 3为氢，甲基，C 3-7低级烷氧基，烯丙基，苯基，苄基，X取代苯基，甲氧基苯基或甲氧基Y取代苯基，其中X为氰基，卤素，羧基烷基，硝基，甲基，三卤代甲基或烷氧基， Y为甲氧基。 制备式（I）的吡啶并[2,3-d]吡啶甲醛肟衍生物的方法包括在钯催化剂和碱的存在下由式（II）化合物制备式（III）化合物; 使式（III）的化合物与羟胺，烷氧基胺或其盐酸盐反应。
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公开(公告)号：KR100393523B1
公开(公告)日：2003-08-06
申请号：KR1020000002382
申请日：2000-01-19
Applicant: 한국과학기술연구원
IPC: C07D501/16
CPC classification number: Y02P20/55
Abstract: PURPOSE: A pyrazolopyridine substituted cephalosporin compound is provided, which have the wide antimicrobial activity for gram positive and gram negative bacteria. And a producing method thereof is also provided. CONSTITUTION: The pyrazolopyridine substituted cephalosporin compound is represented by formula (1), in which R1 is hydrogen, C1 to C3 alkyl, C1 to C3 alkyl containing hydroxy, C1 to C3 alkyl containing amine; and R2 is hydrogen, amino, amino protected by amine protecting groups, carboxy or its inorganic salts, carbarmoyl, C1 to C3 alkyl substituted carbarmoyl, C1 to C3 alkyl containing hydroxy, and C1 to C3 alkyl esterified carboxy. The method for producing the pyrazolopyridine substituted cephalosporin compounds comprises the steps of: reacting the compounds of formula (2) and (3); and deprotecting R3 and R4, in which R3 is amine protecting groups, R4 is carboxylic acid protecting groups; and Y is halogen or acetoxy.
Abstract translation: 目的：提供吡唑并吡啶取代的头孢菌素化合物，其对革兰氏阳性和革兰氏阴性细菌具有广泛的抗微生物活性。 并且还提供了其制造方法。 组成：取代的头孢菌素化合物的吡唑并吡啶是由式（1）表示，其中R1是氢，C1-C3烷基，C1至C3烷基含羟基，C1至含胺C3烷基; 和R2是氢，氨基，被胺保护基团保护的氨基，羧基或其无机盐，氨基甲酰基，C1-C3烷基取代的氨基甲酰基，含有C1-C3烷基的羟基和C1-C3烷基酯化的羧基。 生产吡唑并吡啶取代的头孢菌素化合物的方法包括以下步骤：使式（2）和（3）的化合物反应; 并将R3和R4去保护，其中R3是胺保护基，R4是羧酸保护基; Y是卤素或乙酰氧基。
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Patent Agency Ranking
公开(公告)号：KR100393160B1
公开(公告)日：2003-07-31
申请号：KR1020010033382
申请日：2001-06-14
Applicant: 한국과학기술연구원
IPC: C07D487/04
CPC classification number: C07D487/04
Abstract: Novel pyrazolopyrimidinethione compounds of formula 1: wherein R1 and R2 are independently each hydrogen atom, a C1-C6 alkyl group, or a C3-C6 cycloalkyl group, R3 is a C1-C6 alkyl group. C3-C6 cycloalkyl group or C3-C6 alkenyl group which is substituted or unsubstituted, X is O or NR4, and R4 is hydrogen atom, or a C1-C6 alkyl group, a C3-C6 cycloalkyl group or a C3-C6 alkenyl group which is unsubstituted or substituted with OH or an alkoxy group, pharmacologically acceptable salts or hydrates thereof, and preparation methods thereof are disclosed. Pharmaceutical compositions comprising the compounds are effectively used for the treatment of erectile dysfunction.
Abstract translation: 式1的新型吡唑并嘧啶硫酮化合物：其中R 1和R 2各自独立地为氢原子，C 1 -C 6烷基或C 3 -C 6环烷基，R 3为C 1 -C 6烷基。 C 3 -C 6环烷基或被取代或未被取代的C 3 -C 6烯基，X是O或NR 4，并且R 4是氢原子或C 1 -C 6烷基，C 3 -C 6环烷基或C 3 -C 6烯基 其未被取代或被OH或烷氧基取代，其药理学上可接受的盐或水合物及其制备方法。 包含这些化合物的药物组合物有效地用于治疗勃起功能障碍。
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公开(公告)号：KR1020000067306A
公开(公告)日：2000-11-15
申请号：KR1019990015016
申请日：1999-04-27
Applicant: 한국과학기술연구원
IPC: C07D413/14 , A61K31/42
Abstract: PURPOSE: Quinolone substituted oxazolidinone capable of exhibiting an excellent antibacterial activity against resistant bacteria as a characteristic of an oxazolidinone antibacterial agent as well as maintaining a wide range of antibacterial activities of quinolone antibacterial agent, process for producing the same and their use as an antibacterial agent are provided which can be effectively used in the treatment of infectious diseases such as various bacterial infections. CONSTITUTION: Quinolone substituted oxazolidinone of formula 1 and pharmaceutically acceptable salts thereof, which has strong antibacterial activity against existing betalactam, quinolone, vancomycin as well as having a wide range of antibacterial activities against gram-positive and gram-negative bacteria and Pseudomonas bacteria are described. In formula, R1, R2, R4, R5, X and Y are defined in the description.
Abstract translation: 目的：喹诺酮取代的恶唑烷酮能够表现出对抗性细菌的优良抗菌活性，作为恶唑烷酮抗菌剂的特征，以及维持喹诺酮抗菌剂的广泛抗菌活性，其制备方法及其作为抗菌剂的用途 可以有效地用于治疗感染性疾病如各种细菌感染。 描述：描述了式1的喹诺酮取代的恶唑烷酮及其药学上可接受的盐，其对现有的β-内酰胺，喹诺酮，万古霉素以及对革兰氏阳性和革兰氏阴性菌和假单胞菌具有广泛的抗菌活性具有很强的抗菌活性 。 在式中，R1，R2，R4，R5，X和Y在说明书中定义。
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公开(公告)号：KR100355345B1
公开(公告)日：2002-10-12
申请号：KR1020000002868
申请日：2000-01-21
Applicant: 한국과학기술연구원
IPC: C07D413/08
Abstract: 본 발명은 하기 화학식 1로 표시되는 신규한 옥사졸리디논 유도체 또는 그의 약학적으로 허용가능한 염 및 수화물을 제공한다.
R
1 은 페닐기 또는 할로겐, 알콕시기가 치환된 페닐기이며: R
2 는 탄소수 1-4의 포화 알킬기 또는 1개의 수소가 페닐기로 치환된 탄소수 1-3의 알킬기, 탄소수 3-8의 시클로알킬기, 아릴기에 탄소수 1-3의 알킬기가 치환된 벤질기이고; R
3 는 수소 또는 불소이다.-
9.发明公开
公开(公告)号：KR1020010076509A
公开(公告)日：2001-08-16
申请号：KR1020000003695
申请日：2000-01-26
Applicant: 한국과학기술연구원
IPC: C07D501/16
Abstract: PURPOSE: Provided is a novel cephalosporin which has an amino thiazole derivative at the position number 7 and N-methyl-N-(3-methyl-1,3-thiazolium-2-yl)amino group at position number 3, and shows antibacterial activity against various gram positive bacteria and gram negative bacteria. CONSTITUTION: The cephalosporin is characterized by having an amino thiazole derivative at the position number 7 and N-methyl-N-(3-methyl-1,3-thiazolium-2-yl)amino group at the position number 3 and represented by formula (1). In formula (1), R represents a saturated alkyl group of C1-3 and an unsaturated alkene group of C3-5; R1 is hydrogen, or a saturated alkyl group of C1-3; and R2 represents hydrogen, carboxyl group(or the inorganic cation thereof), carbamoyl group, carbamoyl group of which one or two hydrogen are substituted with an alkyl group of C1-3, or carboxyl group esterified with alkyl group of C1-3. Also, R1 and R2 represent a ring structure linked with 3 to 5 methylene groups.
Abstract translation: 目的：提供一种新型头孢菌素，其在位置7具有氨基噻唑衍生物，在位置3具有N-甲基-N-（3-甲基-1,3-噻唑鎓-2-基）氨基，并显示抗菌剂 针对各种革兰氏阳性菌和革兰氏阴性细菌的活性。 构成：头孢菌素的特征在于具有位置7的氨基噻唑衍生物和位置3处的N-甲基-N-（3-甲基-1,3-噻唑鎓-2-基）氨基，由式 （1）。 在式（1）中，R表示C 1-3的饱和烷基和C3-5的不饱和烯基; R1是氢或C1-3的饱和烷基; R2代表氢，羧基（或其无机阳离子），氨基甲酰基，其中一个或两个氢被C1-3烷基取代的氨基甲酰基，或被C1-3烷基酯化的羧基。 此外，R 1和R 2表示与3至5个亚甲基连接的环结构。
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10.发明授权아미노메틸계 피리도[2,3-ｄ]피리미딘-2,4-디온 ＰＤＥ Ⅳ효소 억제 화합물 및 이의 제조방법 失效新颖的吡啶[2,3-α]吡嗪-2,4-二酮的氨基甲酸酯衍生物有效为A ？ 抑制剂及其制备方法
公开(公告)号：KR100522533B1
公开(公告)日：2005-10-20
申请号：KR1020020015729
申请日：2002-03-22
IPC: C07D471/04
Abstract: 본 발명에 따르면 다음의 일반식 (I)로 표시되는 신규한 아미노메틸계 피리도[2,3-d]피리미딘 2,4-디온 화합물, 이의 제조방법 및 이의 선택적 포스포디에스테라아제 IV (PDE IV)효소 활성 억제 효과에 의한 약리학적 적용에 관한 것이다.
(I)
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