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    도파민 Ｄ3 및 Ｄ4 수용체의 선택적 활성을 지닌 신규4,5-디히드로이소옥사졸릴알킬피페라진 유도체와, 이의제조방법
    2.
    发明公开
    도파민 Ｄ3 및 Ｄ4 수용체의 선택적 활성을 지닌 신규4,5-디히드로이소옥사졸릴알킬피페라진 유도체와, 이의제조방법 失效
    在DOPAMINE D3和D4受体上具有选择性生物活性的新的4,5-二羟基甲基丙烯酰胺衍生物及其制备方法

    公开(公告)号：KR1020020043413A

    公开(公告)日：2002-06-10

    申请号：KR1020000073122

    申请日：2000-12-04

    Applicant: 한국과학기술연구원 ,  한국과학기술원 ,  한국화학연구원 ,  학교법인 성신학원

    Inventor： 고훈영 ,  최경일 ,  조용서 ,  배애님 ,  공재양 ,  정대영 ,  정선호 ,  정지영 ,  이희윤

    IPC: C07D413/14

    CPC classification number: C07D413/04 ,  C07D261/08

    Abstract: PURPOSE: Provided are novel 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity to dopamine D3 and D4 receptors, and their preparation method by reductive amination in the presence of reductant. CONSTITUTION: 4,5-dihydroisoxazolylalkylpiperazine derivative is represented by the formula(1), wherein R1, R2, R3, R4 and R5 are identical or different from each other, and represents individually hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 alkoxy group, C2-C6 alkenyl group, hydroxy group , hydroxymethyl group, aryl group, heteroaryl group, amino group, C1-C6 alkyl amino group, carbonyl group, C3-C8 cycloalkyl group, or C3-C8 heterocyclic group; R6 represents hydrogen atom, halogen atom, alkyl group, C1-C6 alkoxy group, aryl group, pyridyl group, heterocyclic group or pyrimidyl group; X represents CH or nitrogen atom; and n is 3 or 4.

    Abstract translation: 目的：提供对多巴胺D3和D4受体具有选择性生物活性的新型4,5-二氢异恶唑烷基哌嗪衍生物及其在还原剂存在下还原胺化的制备方法。 构成：4,5-二氢异恶唑基烷基哌嗪衍生物由式（1）表示，其中R 1，R 2，R 3，R 4和R 5彼此相同或不同，并且表示单独的氢原子，卤素原子，C1-C6烷基， C1-C6烷氧基，C2-C6烯基，羟基，羟甲基，芳基，杂芳基，氨基，C1-C6烷基氨基，羰基，C3-C8环烷基或C3-C8杂环基; R6表示氢原子，卤素原子，烷基，C1-C6烷氧基，芳基，吡啶基，杂环基或嘧啶基; X表示CH或氮原子; n为3或4。

    도파민 Ｄ４ 수용체 길항제로 유용한 피라졸부틸 화합물, 이의 제조방법 및 이를 포함하는 약학적 조성물
    3.
    发明公开
    도파민 Ｄ４ 수용체 길항제로 유용한 피라졸부틸 화합물, 이의 제조방법 및 이를 포함하는 약학적 조성물 有权
    吡咯啉化合物作为多巴胺D4受体拮抗剂，其制备方法和含有其的药物组合物

    公开(公告)号：KR1020120050841A

    公开(公告)日：2012-05-21

    申请号：KR1020100112296

    申请日：2010-11-11

    Applicant: 한국화학연구원

    Inventor： 박우규 ,  공재양 ,  조희영 ,  정대영 ,  최길돈 ,  고훈영 ,  이희윤 ,  정선호 ,  이해황 ,  이정국 ,  서용완

    IPC: C07D403/06 ,  A61K31/496 ,  A61P25/00

    Abstract: PURPOSE: A pyrazole butyl compound and a pharmaceutical composition containing the same are provided to ensure dopamine D4 receptor affinity and to prevent and treat central nervous system diseases. CONSTITUTION: A pyrazole butyl compound and pharmaceutically acceptable salt thereof are denoted by chemical formula 1. The salt includes inorganic acid salt, organic acid salt, amino acid salt, alkali metal salt, or ammonium salt. A method for preparing the pyrazole butyl compounds comprises: a step of performing reductive amination of pyrazole aldehyde compound of chemical formula 2 with heterocycle compounds of chemical formula 3 under the presence of reducing agent and base. A pharmaceutical composition for treating central nervous system diseases contains 1-(4-chlorophenyl)-4-(4-(1-phenyl-3-propyl-1H-pyrazole-5-yl)butyl)piperazine(compound No. 33) or 1-(4-(1-phenyl-3-propyl-1H-pyrazole-5-yl)butyl)-4-(3-(trifluoromethyl)phenyl)piperazine(compound No. 36).

    Abstract translation: 目的：提供吡唑丁基化合物和含有它们的药物组合物以确保多巴胺D4受体亲和力并预防和治疗中枢神经系统疾病。 构成：吡唑基丁基化合物及其药学上可接受的盐由化学式1表示。盐包括无机酸盐，有机酸盐，氨基酸盐，碱金属盐或铵盐。 制备吡唑丁基化合物的方法包括：在还原剂和碱的存在下，用化学式3的杂环化合物进行化学式2的吡唑醛化合物的还原胺化的步骤。 用于治疗中枢神经系统疾病的药物组合物含有1-（4-氯苯基）-4-（4-（1-苯基-3-丙基-1H-吡唑-5-基）丁基）哌嗪（化合物33）或 1-（4-（1-苯基-3-丙基-1H-吡唑-5-基）丁基）-4-（3-（三氟甲基）苯基）哌嗪（化合物36）。

    도파민 Ｄ3, Ｄ4 수용체 길항제인 신규 3-(메톡시메틸)피라졸 유도체, 이의 제조방법 및 이를 포함하는 약학적 조성물
    4.
    发明公开
    도파민 Ｄ3, Ｄ4 수용체 길항제인 신규 3-(메톡시메틸)피라졸 유도체, 이의 제조방법 및 이를 포함하는 약학적 조성물 失效
    作为DOPAMINE D3和D4受体拮抗剂的3-（甲氧基甲基）吡唑衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：KR1020110024940A

    公开(公告)日：2011-03-09

    申请号：KR1020090083133

    申请日：2009-09-03

    Applicant: 한국화학연구원 ,  인하대학교 산학협력단

    Inventor： 고훈영 ,  김지희 ,  카말키숄포파트로랜지 ,  공재양 ,  박우규 ,  조희영 ,  정대영 ,  최길돈 ,  이희윤

    IPC: C07D403/08 ,  C07D403/06 ,  A61K31/415 ,  A61P25/18

    Abstract: PURPOSE: A pharmaceutical composition containing a novel 3-(methoxymethyl)pyrazole derivative is provided to ensure dopamine D3 and D4 receptor affinity and to suppress psychotic behavior(cage climbing) in a mouse. CONSTITUTION: A novel 3-(methoxymethyl)pyrazole derivative is denoted by chemical formula 1. The compound of chemical formula 1 is prepared by reductive amination of pyrazole aldehyde derivative of chemical formula 2 with piperazine derivative of chemical formula 3 under the presence of reductant and base. A pharmaceutical composition for treating central nervous system diseases contains the compound of chemical formula 1.

    Abstract translation: 目的：提供含有新的3-（甲氧基甲基）吡唑衍生物的药物组合物，以确保多巴胺D3和D4受体的亲和力，并抑制小鼠的精神病性行为（笼养）。 组成：化学式1表示新的3-（甲氧基甲基）吡唑衍生物。化学式1的化合物通过化学式2的吡唑醛衍生物与化学式3的哌嗪衍生物在还原剂的存在下还原胺化而制备， 基础。 用于治疗中枢神经系统疾病的药物组合物含有化学式1的化合物。

    도파민 Ｄ4 수용체 길항제인 신규 피페라지닐프로필피라졸유도체, 이의 제조방법 및 이를 포함하는 약학적 조성물
    8.
    发明公开
    도파민 Ｄ4 수용체 길항제인 신규 피페라지닐프로필피라졸유도체, 이의 제조방법 및 이를 포함하는 약학적 조성물 有权
    作为多巴胺D4受体拮抗剂的哌嗪衍生物和含有它们的药物组合物

    公开(公告)号：KR1020080082250A

    公开(公告)日：2008-09-11

    申请号：KR1020070022845

    申请日：2007-03-08

    Applicant: 한국화학연구원

    Inventor： 공재양 ,  박우규 ,  조희영 ,  정대영 ,  최길돈 ,  고훈영 ,  배애님 ,  조용서 ,  차주환 ,  추현아 ,  채상은 ,  김상희 ,  이희윤

    IPC: C07D401/06 ,  A61K31/437

    CPC classification number: C07D403/06

    Abstract: A piperazinyl-propyl-pyrazole derivative is provided to show excellent dopamine D4 affinity, inhibit the psychotic action of a mouse induced by apomorphine and exhibit relatively weak side effect at a mouse rotarod test, thereby being effectively used as a therapeutic and prophylactic agent of central nervous system diseases. A piperazinyl-propyl-pyrazole derivative is represented by a formula(1). In the formula(1), R^1 is C1-10 alkyl, or substituted or unsubstituted aryl or heteroaryl; one of R^2 or R^3 is H, and the other one of R^2 or and R^3 is C1-10 alkyl, benzyl, or substituted or unsubstituted aryl or heteroaryl; each R^4, R^5, R^6, and R^7 is independently H or C1-10 alkyl; each R^8, R^9, R^10, R^11 and R^12 is independently H, halogen, C1-10 alkyl, C1-C10 alkoxy, bis(substituted or unsubstituted aryl)alkylene, benzyl, nitro, hydroxy, cyano, amino, mono- or di-alkylamino, alkylcarbonylamino, aminosulfonyl, mono- or di-alkylaminosulfonyl, alkylcarbonyl, or alkyloxycarbonyl; and a dotted line is a single-bonded line or a double bond, wherein the aromaticity of a pyrazole-ring should be maintained, the aryl is phenyl, the heteroaryl is thiophenyl or pyridyl, and the substituted aryl or heteroaryl is an aryl or a heteroaryl substituted with one to three substituent(s) selected from the group consisting of halogen, nitro, C1-10 alkyl, C1-10 alkoxy, C1-10 haloalkyl, and C1-10 haloalkoxy. A method for preparing the piperazinyl-propyl-pyrazole derivative comprises a step of subjecting a pyrazole aldehyde derivative represented by a formula(2) and a piperazine derivative represented by a formula(3) to a reductive amination reaction. A pharmaceutical composition for treating central nervous system diseases comprise the compound of the formula(1).

    Abstract translation: 提供哌嗪基 - 丙基 - 吡唑衍生物以显示出优异的多巴胺D4亲和力，抑制阿扑吗啡诱导的小鼠的精神病作用，并且在小鼠旋转试验中显示相对较弱的副作用，从而有效地用作中枢的治疗和预防剂 神经系统疾病 哌嗪基 - 丙基 - 吡唑衍生物由式（1）表示。 在式（1）中，R 1是C 1-10烷基或取代或未取代的芳基或杂芳基; R 2或R 9中​​的一个为H，R 2和R 3中的另一个为C 1-10烷基，苄基或取代或未取代的芳基或杂芳基; 每个R 4，R 5，R 6和R 9独立地是H或C 1-10烷基; 每个R 8，R 9，R 10，R 11和R 12独立地是H，卤素，C 1-10烷基，C 1 -C 10烷氧基，双（取代或未取代的芳基）亚烷基，苄基，硝基，羟基 氰基，氨基，一或二烷基氨基，烷基羰基氨基，氨基磺酰基，一或二烷基氨基磺酰基，烷基羰基或烷氧基羰基; 并且虚线是单键或双键，其中应保持吡唑环的芳香性，芳基为苯基，杂芳基为噻吩基或吡啶基，取代的芳基或杂芳基为芳基或 被一至三个选自卤素，硝基，C 1-10烷基，C 1-10烷氧基，C 1-10卤代烷基和C 1-10卤代烷氧基的取代基取代的杂芳基。 制备哌嗪基 - 丙基 - 吡唑衍生物的方法包括将由式（2）表示的吡唑醛衍生物和由式（3）表示的哌嗪衍生物进行还原胺化反应的步骤。 用于治疗中枢神经系统疾病的药物组合物包含式（1）的化合物。

    도파민 Ｄ3 및 Ｄ4 수용체의 선택적 활성을 지닌 신규이소옥사졸릴알킬피페라진 유도체와, 이의 제조방법
    10.
    发明公开
    도파민 Ｄ3 및 Ｄ4 수용체의 선택적 활성을 지닌 신규이소옥사졸릴알킬피페라진 유도체와, 이의 제조방법 失效
    具有多巴胺D3和D4受体的选择性活性的新型异丙唑胺基哌嗪衍生物及其制备方法

    公开(公告)号：KR1020020043918A

    公开(公告)日：2002-06-12

    申请号：KR1020000073121

    申请日：2000-12-04

    Applicant: 한국과학기술연구원 ,  한국과학기술원 ,  한국화학연구원

    Inventor： 고훈영 ,  최경일 ,  조용서 ,  배애님 ,  강경호 ,  차미영 ,  공재양 ,  정대영 ,  이희윤

    IPC: C07D413/14

    CPC classification number: C07D413/04 ,  C07D261/08 ,  C07D413/14

    Abstract: PURPOSE: Provided are novel isoxazolylalkylpiperazine derivatives having selective activity for dopamine D3 and D4 receptor represented by the formula(1) and their manufacturing method by reductive amination in the presence of a reductant. The derivatives and their pharmaceutically acceptable salts are useful in the treatment of mental illness. CONSTITUTION: The novel isoxazolylalkylpiperazine derivative of the formula(1) is prepared by reacting amine compound represented by the chemical formula(2) with aldehyde compound shown in the chemical formula(3) in the presence of a reductant selected from NaBH(OAc)3, NaBH3CN and NaBH4 in a reductive amination reaction. In the formulae, R1,R2,R3,R4, and R5 are same or different each other and are hydrogen atom, halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, hydroxy, hydroxymethyl, aryl, heteroaryl, amino group, C1-C6 alkylamino, carbonyl, C3-C8 cycloalkyl, or C3-C8 heterocyclic group; R6 is hydrogen atom, halogen atom, alkyl, C1-C6 alkoxy, aryl, pyridyl, heterocyclic, pyrimidyl group; X is CH or nitrogen atom; and n is 3 or 4.

    Abstract translation: 目的：提供具有式（1）表示的多巴胺D3和D4受体选择性活性的新型异恶唑基烷基哌嗪衍生物及其制备方法，在还原胺存在下还原胺化。 衍生物及其药学上可接受的盐可用于治疗精神疾病。 构成：式（1）的新型异恶唑基烷基哌嗪衍生物通过使化学式（2）表示的胺化合物与化学式（3）所示的醛化合物在选自NaBH（OAc）3的还原剂存在下反应来制备 ，NaBH 3 CN和NaBH 4在还原胺化反应中。 在式中，R 1，R 2，R 3，R 4和R 5相同或不同，为氢原子，卤原子，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6烯基，羟基，羟甲基，芳基，杂芳基 ，氨基，C1-C6烷基氨基，羰基，C3-C8环烷基或C3-C8杂环基; R6是氢原子，卤素原子，烷基，C1-C6烷氧基，芳基，吡啶基，杂环基，嘧啶基; X是CH或氮原子; n为3或4。

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