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    도파민 Ｄ4 수용체 길항제인 신규 피페라지닐프로필피라졸유도체, 이의 제조방법 및 이를 포함하는 약학적 조성물
    21.
    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。

    1,2,5,6/1,2,3,6-테트라히드로피리디닐테트라히드로사이클로펜타/-헥사이속사졸 유도체 및 그 제조방법
    23.
    发明公开
    1,2,5,6/1,2,3,6-테트라히드로피리디닐테트라히드로사이클로펜타/-헥사이속사졸 유도체 및 그 제조방법 无效
    1,2,5,6 / 1,2,3,6-四氢吡啶并吡咯并环庚酮衍生物及其制备方法

    公开(公告)号：KR1020040021992A

    公开(公告)日：2004-03-11

    申请号：KR1020020053796

    申请日：2002-09-06

    Applicant: 주식회사 코오롱 ,  한국화학연구원

    Inventor： 정명희 ,  안미자 ,  박정미 ,  최일영 ,  정대영 ,  정용준 ,  김윤철 ,  박호진

    IPC: C07D413/04

    Abstract: PURPOSE: 1,2,5,6/1,2,3,6- Tetrahydropyridinyltetrahydrocyclopenta/-hexaisoxazole derivatives and a method for preparing the same are provided. The compounds are useful for treatment of dementia and brain disease as muscarinic receptor agonist and operated as tetrahydropyridine bioisostere. CONSTITUTION: 1,2,5,6/1,2,3,6- Tetrahydropyridinyltetrahydrocyclopenta/ -hexaisoxazole derivatives are represented by the formula(1), wherein X is CH2, O or S; n is an integer of 1 or 2; HA is inorganic or organic salt selected from HCl, oxalic acid, p-toluenesulfonic acid, tartaric acid and fumaric acid. A method for preparing the 1,2,5,6/1,2,3,6- Tetrahydropyridinyltetrahydrocyclopenta/-hexaisoxazole derivatives comprises the steps of: (a) adding NaOCl to 3/4-pyridinealdoxime of the formula(2) and cyclopentene/-hexene derivatives in a solvent and cyclizing them to prepare a compound of the formula(4); (b) reacting the compound of the formula(4) with CH3I to prepare 3/4-substituent isomer of the formula(5); and (c) reducing the compound of the formula(5) and adding inorganic and organic acids into the reduced compound.

    Abstract translation: 目的：提供1,2,5,6 / 1,2,3,6-四氢吡啶基四氢环戊二烯并 - 己烯恶唑衍生物及其制备方法。 该化合物可用于治疗痴呆和脑疾病作为毒蕈碱受体激动剂，并作为四氢吡啶生物电子等离子体操作。 构成：1,2,5,6 / 1,2,3,6-四氢吡啶基四氢环戊酯/ - 己烯恶唑衍生物由式（1）表示，其中X为CH 2，O或S; n为1或2的整数; HA是选自HCl，草酸，对甲苯磺酸，酒石酸和富马酸的无机或有机盐。 制备1,2,5,6 / 1,2,3,6-四氢吡啶基四氢环戊二烯并 - 六氢异恶唑衍生物的方法包括以下步骤：（a）将NaOCl加入式（2）的3 / 4-吡啶醛肟和环戊烯 己烯衍生物在溶剂中并使其环化以制备式（4）的化合物; （b）使式（4）的化合物与CH 3 I反应制备式（5）的3 / 4-取代基异构体; 和（c）还原式（5）的化合物，并向还原的化合物中加入无机和有机酸。

    도파민 Ｄ3 및 Ｄ4 수용체의 선택적 활성을 지닌 신규이소옥사졸릴알킬피페라진 유도체와, 이의 제조방법
    25.
    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。

    1,2,3,4-테트라하이드로피리미딘 유도체와 이의 제조방법
    26.
    发明授权
    1,2,3,4-테트라하이드로피리미딘 유도체와 이의 제조방법 失效
    1,2,3,4-四氢嘧啶衍生物及其制备方法

    公开(公告)号：KR100297804B1

    公开(公告)日：2001-09-22

    申请号：KR1019990012805

    申请日：1999-04-12

    Applicant: 한국화학연구원

    Inventor： 정명희 ,  박준규 ,  조귀웅 ,  오정숙 ,  천혜경 ,  정대영

    IPC: C07D239/06 ,  A61K31/505

    Abstract: PURPOSE: Provided are a 1,2,3,4-tetrahydropyrimidine derivative represented by the formula(1), which is useful as a muscarinic receptor agonist in treating imbecility, a pharmaceutically acceptable salt and method for preparation thereof. CONSTITUTION: The 1,2,3,4-tetrahydropyrimidine derivative is represented by the formula(1), wherein R is H, -CH3, -CH2CH3, -CH2(CH2)3CH3, -CH2CH=CH2, CH2C≡CH, C6H5CH2, P-CH2C6H4CH3, P-CH2C6H4-Cl. It is prepared by the following steps of: (a) condensing 5-pyrimidinecarboxylaldehyde represented by the formula(2) and hydroxylamine, to produce compound represented by the formula(3), wherein R1 is -H or -CH3; (b) condensing a compound represented by the formula(3), wherein R1 is H and a compound represented by R2-X, to produce compound represented by the formula(4), wherein R2 is -CH2CH3, -CH2(CH2)3CH3, -CH2CH=CH2, CH2C≡CH, C6H5CH2, P-CH2C6H4CH3, P-CH2C6H4-Cl and X is halogen; (c) methylating a compound represented by the formula(3) or a compound represented by the formula(4) and CH3I, to produce a compound represented by the formula(5), wherein R is H, -CH3, -CH2CH3, -CH2(CH2)3CH3, -CH2CH=CH2, CH2C≡CH, C6H5CH2, P-CH2C6H4CH3, P-CH2C6H4-Cl; and (d) reducing a compound represented by the formula(5) and NaBH4, to produce 1,2,3,4-tetrahydropyrimidine derivative represented by the formula(1), wherein R is H, -CH3, -CH2CH3, -CH2(CH2)3CH3, -CH2CH=CH2, CH2C≡CH, C6H5CH2, P-CH2C6H4CH3, P-CH2C6H4-Cl.

    피리미도 옥사진 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 PI3 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물
    27.
    发明公开
    피리미도 옥사진 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 PI3 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물 有权
    嘧啶并恶嗪衍生物或其药学上可接受的盐，其制备方法和用于疾病包括作为活性成分的本PI3-激酶相关的预防性或治疗性药物组合物

    公开(公告)号：KR1020170074381A

    公开(公告)日：2017-06-30

    申请号：KR1020150183563

    申请日：2015-12-22

    Applicant: 한국화학연구원

    Inventor： 이계형 ,  임희종 ,  조희영 ,  박우규 ,  정대영

    IPC: C07D487/04 ,  C07D498/04 ,  C07D401/12 ,  C07D403/14 ,  A61K31/519 ,  A61K31/47 ,  A61K31/53 ,  A23L1/30

    Abstract: 본발명은피리미도옥사진유도체또는이의약학적으로허용가능한염, 이의제조방법및 이를유효성분으로포함하는 PI3 키나아제관련질환의예방또는치료용약학적조성물에관한것이다. 본발명에따른피리미도옥사진유도체는 PI3 키나아제에대하여선택적으로억제하는효과가우수하므로혈액암, 난소암, 자궁경부암, 유방암, 대장암, 간암, 위암, 췌장암, 결장암, 복막전이암, 피부암, 방광암, 전립선암, 폐암, 골육종, 섬유성종양, 뇌종양등과같은암, 류머티스성관절염, 전신홍반성루푸스, 다발성경화증, 제1형당뇨병, 갑상선기능항진증, 근무력증, 크론병, 강직성척추염, 건선, 자가면역성악성빈혈, 쇼그렌증후군등과같은자가면역질환, 만성폐쇄성폐질환(COPD), 비염, 천식, 만성기관지염, 만성폐 염증성질환, 규폐증, 폐형사르코이드증, 흉막염, 폐포염, 혈관염, 기종, 폐렴, 기관지확장증등과같은호흡기질환등의 PI3 키나아제관련질환을예방또는치료하는데유용하게사용할수 있다.

    Abstract translation: 本发明涉及嘧啶并 - 恶嗪衍生物或其uiyakhak上可接受的盐，它们的制备和药物组合物包含其作为活性成分的PI3激酶相关的疾病的预防或治疗物质。 由于根据本发明的嘧啶并 - 恶嗪衍生物是具有优异的效果，以选择性地抑制相对于PI3激酶血癌，卵巢癌，子宫颈癌，乳腺癌，结肠癌，肝癌，胃癌，胰腺癌，结肠直肠癌，腹膜转移，皮肤癌， 膀胱癌，前列腺癌，肺癌，骨肉瘤，纤维瘤，癌症，如脑肿瘤，类风湿性关节炎，jeonsinhong红斑狼疮，多发性硬化症，1型糖尿病，甲状腺功能亢进症，重症肌无力，克罗恩病，强直性脊柱炎，牛皮癣，自身免疫性 恶性贫血，自身免疫性疾病如斯耶格伦氏综合征，慢性阻塞性肺疾病（COPD），鼻炎，哮喘，慢性支气管炎，慢性肺部炎性疾病，矽肺，结节病pyehyeong，胸膜炎，肺泡炎，脉管炎，肺气肿，肺炎，支气管 所述呼吸系统疾病的PI3激酶相关的疾病，如如支气管扩张可以是用于预防或治疗是有用的。

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