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    제초성 2,3-디히드로티오펜일시클로헥산-1,3-디온 유도체 및 그 제법
    22.
    发明授权
    제초성 2,3-디히드로티오펜일시클로헥산-1,3-디온 유도체 및 그 제법 失效
    制备2,3-二氢苯并噻唑环己烷-1,3-二酮衍生物的方法

    公开(公告)号：KR1019950006923B1

    公开(公告)日：1995-06-26

    申请号：KR1019920009493

    申请日：1992-06-01

    Applicant: 한국화학연구원

    Inventor： 유응걸 ,  김형래 ,  김경만 ,  송종환 ,  정근희 ,  황인택

    IPC: A01N43/10

    Abstract: A 2,3-dihydrothiophenyl cyclohexane-1,3-dione derivative of formula (I) for using herbicide and plant growth regulating agent is prepd. by reacting the compound of formula (II) and H2NOR3˜HCl in an inert organic solvent. In the formula, R1 is H or C1˜C4 alkyl, R2 is C1˜C6 alkenyl, C2˜C6 alkynyl or C1˜C6 haloalkyl, R3 is H, C1˜C6 alkyl, C2˜C6 alkenyl, C2˜C6 alkynyl, C1˜C6 haloalkyl, C2˜C6 haloalkenyl, C2˜C6 haloalkynyl, C1˜C6 alkoxyalkyl, C1˜C6 alkylthioalkyl, benzyl or haloalkanoyl group.

    Abstract translation: 使用除草剂和植物生长调节剂的式（I）的2,3-二氢噻吩环己烷-1,3-二酮衍生物是制备的。 通过使式（II）化合物和H 2 NOR 3〜HCl在惰性有机溶剂中反应。 在该式中，R 1为H或C 1〜C 4烷基，R 2为C 1〜C 6烯基，C 2〜C 6炔基或C 1 -C 6卤代烷基，R 3为H，C 1〜C 6烷基，C 2〜C 6烯基，C 2〜C 6炔基，C 1 C 6卤代烷基，C 2〜C 6卤代烯基，C 2〜C 6卤代炔基，C 1 -C 6烷氧基烷基，C 1〜C 6烷硫基烷基，苄基或卤代烷酰基。

    신규한 피리딘을 포함하는 알킬로 치환된 인덴 유도체, 이의 약학적으로 허용가능한 염 또는 이의 이성질체, 이의 제조방법 및 이를 포함하는 ＰＡＲ-1 관련 질환의 예방 또는 치료용 약학적 조성물
    26.
    发明公开
    신규한 피리딘을 포함하는 알킬로 치환된 인덴 유도체, 이의 약학적으로 허용가능한 염 또는 이의 이성질체, 이의 제조방법 및 이를 포함하는 ＰＡＲ-1 관련 질환의 예방 또는 치료용 약학적 조성물 有权
    由含有吡啶，含有药用盐或其异构体的烷基取代的新型衍生物，其制备方法和用于预防或治疗含有作为活性成分的PAR-1相关疾病的药物组合物

    公开(公告)号：KR1020120111887A

    公开(公告)日：2012-10-11

    申请号：KR1020110114755

    申请日：2011-11-04

    Applicant: 한국화학연구원

    Inventor： 이선경 ,  박철민 ,  송종환 ,  임동철 ,  조우영

    IPC: C07D405/06 ,  C07D401/06 ,  A61K31/443 ,  A61P9/00

    Abstract: PURPOSE: A pharmaceutical composition containing an alkyl-substituted indene derivative containing novel pyridine, or pharmaceutically acceptable salts or isomers thereof is provided to prevent or treat PAR-1 related diseases, inflammation, or cancer. CONSTITUTION: An alkyl-substituted indene derivative containing pyridine is denoted by chemical formula 1. A pharmaceutical composition for preventing or treating PAR-1 activation-related diseases contains the indene derivative, salts, or isomers as an active ingredient. A pharmaceutical composition for cardiovascular treatment aid is alternately used with cardiovascular drugs such as aspirin, clopidogrel, ticlopidine, abciximab, or tirofiban.

    Abstract translation: 目的：提供含有含有新吡啶的烷基取代茚衍生物或其药学上可接受的盐或异构体的药物组合物，用于预防或治疗PAR-1相关疾病，炎症或癌症。 构成：含有吡啶的烷基取代的茚衍生物由化学式1表示。用于预防或治疗PAR-1活化相关疾病的药物组合物含有茚衍生物，盐或异构体作为活性成分。 用于心血管治疗助剂的药物组合物与心血管药物如阿司匹林，氯吡格雷，噻氯匹定，阿昔单抗或替罗非班交替使用。

    신규한 2,4-피리미딘 유도체 및 이의 용도
    27.
    发明公开
    신규한 2,4-피리미딘 유도체 및 이의 용도 有权
    空值

    公开(公告)号：KR1020110048476A

    公开(公告)日：2011-05-11

    申请号：KR1020100108201

    申请日：2010-11-02

    Applicant: 서울대학교산학협력단 ,  한국화학연구원

    Inventor： 김성훈 ,  한정민 ,  김형래 ,  전동주 ,  송종환 ,  박경은

    IPC: C07D401/12 ,  C07D239/34 ,  A61K31/513 ,  A61P29/00

    CPC classification number: C07D239/60 ,  C07D239/52 ,  C07D401/12

    Abstract: PURPOSE: A composition containing a novel 2,4-pyrimidine derivative is provided to suppress gp96 surface translocation and to prevent and treat SLE(systemic lupus etythematosus). CONSTITUTION: A novel 2,4-pyrimidine derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating SLE contains the 2,4-pyrimidine derivative compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A method for screening a therapeutic agent for SLE comprises: a step of contacting a test agent with AIMP1 and gp96; a step of measuring disintegration activity of AIMP1 and gp96 and selecting an agent which changes AIMP1 and gp96 binding ability; and a step of testing the treatment or relief on SLE by the selected agent.

    Abstract translation: 目的：提供含有新的2,4-嘧啶衍生物的组合物，以抑制gp96表面易位并预防和治疗SLE（系统性红斑狼疮）。 构成：化学式1表示新的2,4-嘧啶衍生物。用于预防和治疗SLE的药物组合物含有化学式1的2,4-嘧啶衍生物化合物或其药学上可接受的盐作为活性成分。 用于筛选SLE治疗剂的方法包括：使测试试剂与AIMP1和gp96接触的步骤; 测量AIMP1和gp96的分解活性并选择改变AIMP1和gp96结合能力的药剂的步骤; 以及由所选代理测试SLE的治疗或救济的步骤。

    7-(3′,4′-디알콕시페닐)-4,5,6,7-테트라히드로피라졸로[1,5-ａ]피리미딘 화합물, 이의 제조방법 및 이를 포함하는천식 및 만성폐쇄성 폐질환을 포함한 염증관련 질환,관절염, 아토피 피부염, 암 및 뇌질환의 치료 및 예방을위한 약제학적 조성물
    28.
    发明授权
    7-(3′,4′-디알콕시페닐)-4,5,6,7-테트라히드로피라졸로[1,5-ａ]피리미딘 화합물, 이의 제조방법 및 이를 포함하는천식 및 만성폐쇄성 폐질환을 포함한 염증관련 질환,관절염, 아토피 피부염, 암 및 뇌질환의 치료 및 예방을위한 약제학적 조성물 失效
    7-（3'，4'-二烷氧基苯基）-4,5,6,7-四氢吡咯并[1,5-A]吡嗪化合物，其制备方法和药物组合物，用于治疗或预防哮喘，慢性阻塞性肺动脉疾病， ARTHRITIS，ATOPIC DERMATITIS，TUMOR AND DEGENERATIVE BRAIN DISEASES COMPATH THE SAME

    公开(公告)号：KR100838692B1

    公开(公告)日：2008-06-16

    申请号：KR1020070069765

    申请日：2007-07-11

    Applicant: 한국화학연구원

    Inventor： 전동주 ,  송종환 ,  이계형 ,  김익연

    IPC: C07D487/04 ,  A61K31/52 ,  A61P29/00

    Abstract: A novel 7-(3',4'-dialkoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine compound is provided to show excellent inhibitory activity and high enzyme selectivity on PDE-4 enzyme, thereby being used in order to prevent and treat inflammation related diseases, arthritis, atopic dermatitis, tumor, and brain diseases. A 7-(3',4'-dialkoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine compound is represented by a formula(1), wherein each R1 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl, linear or branched saturated or unsaturated C1-7 alkyl including O, N or S, C3-7 cycloalkyl, C3-7 cycloalkyl including O, N or S, (C3-7)cycloalkyl(C1-7)alkyl, 3 to 7-membered saturated or unsaturated heterocycloalkyl including O, N or S in a hetero-ring, phenyl or benzyl, or R1 and R2 may be linked to each other by C1-3 alkylene or C1-3 alkylene including halogen; each R3 and R4 is independently H, formyl, halogen, linear or branched saturated or unsaturated C1-7 alkyl. C1-7 alkoxy, C3-7 cycloalkyl, (C1-7)alkoxy(C1-7)alkyl, C1-7 alkyl ketone, hydroxy(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, C1-7 alkyl carboxyl, carboxy(C1-10)alkylester, carboxyl(C1-10)alkylamide, amino, mono or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, (C3-7)cycloalkylamino, morpholine, morpholine oxide, thio- morpholine, piperidine, piperazine, piperazine oxide, piperidine, piperidine oxide, pyrrolidine, cyano, nitro, carboxyl, guanidine, urea, phenoxy, benzyloxy or aryl represented by Ar; and R5 is H, linear or branched saturated or unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C1-7)alkoxy(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, mono or di(C1-7)alkylamino, carbonyl, cyano, C1-7 alkoxycarbonyl, aminocarbonyl, C1-7 alkylcarbonyl, (C6-10)ar(C1-7)alkylcarbonyl or C6-10 arylcarbonyl. A method for preparing the compound of the formula(1) comprises the steps of: (a) after reacting a 3-amino-5-substituted pyrazole compound represented by a formula(4) with a 3-(dimethylamino)-1-(3,4-dialkoxyphenyl)prophenone compound represented by a formula(5) or a 3-(3,4-dialkoxyphenyl)cinnamic aldehyde compound represented by a formula(6) in the presence of an acetic acid, reducing a reaction producing with NaBH4 to prepare a compound represented by the formula(1); and (b) subjecting the compound of a formula(10) to nucleophilic substitution. A pharmaceutical composition for treating or preventing asthma, chronic obstructive pulmonary disease, arthritis, atopic dermatitis, tumor and degenerative brain diseases comprises the compound of the formula(1) or a pharmaceutically acceptable salt thereof.

    Abstract translation: 提供了一种新型的7-（3'，4'-二烷氧基苯基）-4,5,6,7-四氢吡唑并[1,5-a]嘧啶化合物，以显示优异的抑制活性和对PDE-4酶的高酶选择性 用于预防和治疗炎症相关疾病，关节炎，特应性皮炎，肿瘤和脑疾病。 7-（3'，4'-二烷氧基苯基）-4,5,6,7-四氢吡唑并[1,5-a]嘧啶化合物由式（1）表示，其中每个R 1和R 2独立地为H，线性 或支链饱和或不饱和C 1-7烷基，包括O，N或S，C 3-7环烷基的直链或支链饱和或不饱和C 1-7烷基，包括O，N或S的C 3-7环烷基，（C 3-7）环烷基（ C 1-7烷基，含有杂环中O，N或S的3至7元饱和或不饱和杂环烷基，苯基或苄基，或R 1和R 2可以通过C 1-3亚烷基或C 1-3 包括卤素的亚烷基; 每个R 3和R 4独立地是H，甲酰基，卤素，直链或支链饱和或不饱和的C 1-7烷基。 C 1-7烷氧基，C 3-7环烷基，（C 1-7）烷氧基（C 1-7）烷基，C 1-7烷基酮，羟基（C 1-7）烷基，（C 3-7）环烷基（C 1-7）烷基， （C 3-7）环烷基（C 1-7）烷氧基，C 1-7烷基羧基，羧基（C 1-10）烷基酯，羧基（C 1-10）烷基酰胺，氨基，单或二（C 1-7）烷基氨基，单或二 （C 1-7）烷基氨基羰基，（C 3-7）环烷基氨基，吗啉，吗啉氧化物，硫代吗啉，哌啶，哌嗪，哌嗪氧化物，哌啶，哌啶氧化物，吡咯烷，氰基，硝基，羧基，胍，脲，苯氧基， 或由Ar表示的芳基; 并且R 5为H，直链或支链饱和或不饱和的C 1-7烷基，C 3-7环烷基，（C 1-7）烷氧基（C 1-7）烷基，（C 3-7）环烷基（C 1-7） 7）环烷基（C 1-7）烷氧基，一或二（C 1-7）烷基氨基，羰基，氰基，C 1-7烷氧基羰基，氨基羰基，C 1-7烷基羰基，（C 6-10）芳（C 1-7）烷基羰基或C 6 -10芳基羰基。 制备式（1）化合物的方法包括以下步骤：（a）使由式（4）表示的3-氨基-5-取代的吡唑化合物与3-（二甲基氨基）-1-（ （5）表示的丙烯酮化合物或由式（6）表示的3-（3,4-二烷氧基苯基）肉桂醛化合物在乙酸存在下还原产生的反应 以制备由式（1）表示的化合物; 和（b）使式（10）的化合物进行亲核取代。 用于治疗或预防哮喘，慢性阻塞性肺病，关节炎，特应性皮炎，肿瘤和退行性脑疾病的药物组合物包含式（1）化合物或其药学上可接受的盐。

    제초활성을 갖는9-(5-이속사졸메톡시페닐)이미노-8-치아-1,6-디아자비시클로[4.3.0]노난-7-온 유도체
    30.
    发明授权
    제초활성을 갖는9-(5-이속사졸메톡시페닐)이미노-8-치아-1,6-디아자비시클로[4.3.0]노난-7-온 유도체 失效
    除草9-5-异恶唑甲氧基苯基亚氨基-8-硫杂-1,6-二氮杂双环[4.3.0]壬-7-酮衍生物

    公开(公告)号：KR100477892B1

    公开(公告)日：2005-03-18

    申请号：KR1020030026416

    申请日：2003-04-25

    Applicant: 한국화학연구원

    Inventor： 전동주 ,  김형래 ,  송종환 ,  박관용 ,  정순민 ,  황인택

    IPC: A01N43/90

    Abstract: 본 발명은 다음 화학식 1로 표시되는 신규의 9-(5-이속사졸메톡시페닐)이미노-8-치아-1,6-디아자비시클로[4.3.0]노난-7-온 유도체와 이들을 유효성분으로 포함하는 제초제에 관한 것이다.

    상기 화학식 1에서, R은 C
    1 ∼C
    5 의 알킬기, 페닐기 또는 치환된 페닐기이고, 이때 치환된 페닐기는 C
    1 ∼C
    3 의 알킬기, C
    1 ∼C
    3 의 알콕시기, 할로겐 원자, 시아노기, 니트로기, 카르복실기 및 카르복실산 에스테르기 중에서 선택된 치환기가 1 ∼ 3개 단일 혹은 복합적으로 치환된 페닐기이다.

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