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1. 发明授权

KR101636563B1 급성 폐 손상 및 급성 호흡곤란 증후군의 예방 또는 치료용 조성물 有权
标题翻译：用于预防或治疗急性肺损伤和急性呼吸道感染综合征的组合物
公开(公告)号：KR101636563B1
公开(公告)日：2016-07-06
申请号：KR1020150011171
申请日：2015-01-23
申请人： 주식회사 엘지생명과학
发明人： 김순하 , 이용철 , 김소리 , 김형진 , 박희술
IPC分类号： A61K31/404 , A61K31/517
CPC分类号： A61K31/54 , A61K9/0019 , A61K9/145 , A61K9/2059 , A61K9/4866
摘要： 본발명은 (테트라하이드로피란-4-일)-[2-페닐-5-(1,1-디옥소-티오몰포린-4-일)메틸-1H-인돌-7-일]아민을유효성분으로포함하는급성폐 손상및 급성호흡곤란증후군의예방또는치료용조성물에관한것으로, 본발명에따른 (테트라하이드로피란-4-일)-[2-페닐-5-(1,1-디옥소-티오몰포린-4-일)메틸-1H-인돌-7-일]아민은 LPS 유발급성폐 손상마우스의기관지폐포세척액에서전체염증세포수및 대식세포, 림프구및 중성구의수를감소시키며, 폐손상및 염증정도를현저히감소시키고, 혈관투과성및 단백질삼출성을감소시킴으로써, 급성폐 손상및 급성호흡곤란증후군에대한예방또는치료용으로유용하게사용될수 있다.

2. 发明授权

KR101456286B1 ＧＰＲ119 효능제로서의 옥심 유도체 有权
标题翻译： OXIME衍生物作为GPR119激动剂
公开(公告)号：KR101456286B1
公开(公告)日：2014-11-03
申请号：KR1020120015736
申请日：2012-02-16
申请人： 주식회사 엘지생명과학
发明人： 김영관 , 김명열 , 주현우 , 박희술 , 심동섭 , 곽효신 , 이태희 , 최은실
IPC分类号： C07D401/04 , A61K31/496 , A61P3/10
CPC分类号： C07D451/06 , C07D211/46 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/04 , C07D413/14 , C07D417/12 , C07D417/14
摘要： 본 발명은 하기 화학식 1의 옥심 유도체, 이의 제조방법, 이를 포함하는 약제학적 조성물 및 사용 방법에 관한 것이다. 특히, 본 발명에 따른 옥심 유도체는 제2형 당뇨병, 당뇨병의 합병증, 비만, 이상지질혈증(dyslipidemia) 또는 골다공증 치료를 위해 GLP-1의 분비를 촉진시키고 또한 인슐린 분비를 증가시키는 GPR119 효능제로서 작용할 수 있다.
[화학식 1]

상기 식에서 RA, RB, n, Ar, A, B, R1 및 R2 는 명세서 중에 정의된 바와 같다.

3. 发明公开

KR1020090034009A 글라이신 모액을 포함하는 신규한 베타-세크리타제 저해용화합물 无效
标题翻译：具有蛋白质环境的BETA-SECRETASE抑制化合物
公开(公告)号：KR1020090034009A
公开(公告)日：2009-04-07
申请号：KR1020070099130
申请日：2007-10-02
申请人： 주식회사 엘지생명과학
发明人： 박희술 , 곽효신
IPC分类号： C07D295/125 , C07D401/12 , A61K31/4965 , A61K31/497
摘要： A novel peptide-free compound is provided to inhibit beta-secretase, offer superior inhibiting activity a peptide-free compound and to offer superior cerebrum permeability of the compound through oral medication. A novel peptide-free compound for inhibiting beta-secretase includes a compound indicated as a chemical formula I, and salt or an isomer. In the formula 1, Y is N or C; R1 and R2 are independently hydrogen, alkyl, heteroalkyl, cycloalkyl, heterocycle, heteroaryl, aryl, - (CH2) m- aryl, - (CH2) m- heteroaryl, - C (O) - aryl or - C (O) - aryl- acyl; R3 and R5 are independently the hydrogen, the alkyl, the cycloalkyl, the heterocycle, the aryl or - (CH2) m- aryl; and R5 and R6 are independently the hydrogen, the alkyl, the cycloalkyl, the heterocycle, the aryl, the heteroaryl, - C (O) - alkyl, - C (O) - aryl, - C (O) - (CH2) m- aryl or - (CH2) m- aryl. The composition is used for curing Alzheimer disease.
摘要翻译：提供新的无肽化合物以抑制β-分泌酶，提供优异的抑制活性的无肽化合物，并通过口服药物提供优异的大脑通透性。用于抑制β-分泌酶的新型无肽化合物包括化学式I表示的化合物和盐或异构体。在式1中，Y是N或C; R 1和R 2独立地是氢，烷基，杂烷基，环烷基，杂环，杂芳基，芳基， - （CH 2）m - 芳基， - （CH 2）m - 杂芳基，-C（O） - 芳基或-C（O）酰基; R3和R5独立地是氢，烷基，环烷基，杂环，芳基或 - （CH2）m-芳基; 且R 5和R 6独立地为氢，烷基，环烷基，杂环，芳基，杂芳基，-C（O） - 烷基，-C（O） - 芳基，-C（O） - （CH 2）m - 芳基或 - （CH 2）m - 芳基。该组合物用于治疗阿尔茨海默病。

4. 发明公开

KR1020050045928A 멜라노코틴 수용체의 항진제 失效
标题翻译：梅兰康汀受体激动剂
公开(公告)号：KR1020050045928A
公开(公告)日：2005-05-17
申请号：KR1020040092249
申请日：2004-11-12
申请人： 주식회사 엘지생명과학 , 아스텔라스세이야쿠 가부시키가이샤
发明人： 이구 , 박희술 , 안인애 , 유현주 , 김종엽 , 최덕영 , 임현주 , 정경하 , 심동섭 , 이상균 , 콘도유타카 , 히라바야시료지 , 혼다슈고 , 가쿠히데다카 , 시시쿠라준이치 , 이토히로유키 , 쿠라마다케시
IPC分类号： C07D207/14 , C07D403/12 , A61P3/00 , A61P15/10
CPC分类号： C04B35/632 , C07D205/04 , C07D207/14 , C07D211/58 , C07D401/12 , C07D403/12 , C07D405/12
摘要： 본 발명은 멜라노코틴 수용체에 대한 항진활성이 우수한 하기 화학식 1의 화합물, 약제학적으로 허용되는 그의 염, 수화물, 용매화물 또는 이성체, 및 이를 유효성분으로 함유함을 특징으로 하는 멜라노코틴 수용체의 기능항진제 조성물에 관한 것이다:

상기 식에서 R
1 , R
2 , R
3 , R
4 , R
5 , n 및 m은 명세서에 정의한 바와 같다.

5. 发明公开

KR1020030035588A 멜라노코틴 수용체의 항진제 无效
标题翻译： MELANOCORTIN 4 RECEIPTOR（MC4R）AGONIST
公开(公告)号：KR1020030035588A
公开(公告)日：2003-05-09
申请号：KR1020010067701
申请日：2001-10-31
申请人： 주식회사 엘지생명과학
发明人： 이구 , 박희술 , 정원혁 , 안인애 , 유현주 , 최덕영 , 권오환
IPC分类号： C07D403/14
摘要： PURPOSE: A melanocortin 4 receptor(MC4R) agonist is provided, thereby accelerating the function of the melanocortin 4 receiptor(MC4R), and consequently preventing and treating diseases associated with the MC4R such as obesity, penile erection disorder, diabetes and inflammation. CONSTITUTION: Compounds functioning as a melanocortin 4 receptor(MC4R) agonist are represented by formula(1), wherein A is hydrogen, COR1, CO2R1, SO2R1, SO2NHR1, SO2N(R1)2, PO(OR1)2, C1-C8-alkyl, (CH2)n-C5-C10-aryl or (CH2)n-C5-C10-heteroaryl in which R1 is hydrogen, C1-C8-alkyl, (CH2)n-C3-C7-cycloalkyl, (CH2)n-C5-C10-aryl or (CH2)n-C5-C10-heteroaryl, n is an integer of 0 to 7; B and C are independently hydrogen, C1-C8-alkyl, (CH2)n-C3-C7-cycloalkyl, (CH2)n-C5-C10-aryl, (CH2)n-C5-C10-heteroaryl, (CH2)n-C5-C10-heterocycle or (CH2)n-O(CH2)-C5-C10-aryl in which n is an integer of 1 to 7; D is hydrogen, C1-C8-alkyl, (CH2)n-C3-C7-cycloalkyl, (CH2)n-C5-C10-aryl, (CH2)n-C5-C10-heteroaryl, (CH2)n-C5-C10-heterocycle or (CH2)n-O(CH2)-C5-C10-aryl in which n is an integer of 1 to 7; E is C5-C10-alkyl or (CH2)m-C5-C7-cycloalkyl in which m is an integer of 0 to 2; and F is (CH2)m-C5-C10-heteroaryl or (CH2)m-C5-C10-heterocycle in which n is an integer of 0 to 2.
摘要翻译：目的：提供黑皮质素4受体（MC4R）激动剂，从而加速黑皮质素4受体（MC4R）的功能，从而预防和治疗与MC4R相关的疾病，如肥胖，阴茎勃起障碍，糖尿病和炎症。构成：作为黑皮质素4受体（MC4R）激动剂起作用的化合物由式（1）表示，其中A为氢，COR1，CO2R1，SO2R1，SO2NHR1，SO2N（R1）2，PO（OR1）2，C1-C8- 烷基，（CH2）n-C5-C10-芳基或（CH2）n-C5-C10-杂芳基，其中R1是氢，C1-C8-烷基，（CH2）n-C3-C7-环烷基，（CH2）n -C 5 -C 10 - 芳基或（CH 2）n -C 5 -C 10 - 杂芳基，n为0〜7的整数。 B和C独立地是氢，C1-C8-烷基，（CH2）n-C3-C7-环烷基，（CH2）n-C5-C10-芳基，（CH2）n-C5-C10-杂芳基，（CH2）n -C 5 -C 10 - 杂环或（CH 2）n O（CH 2）-C 5 -C 10 - 芳基，其中n为1至7的整数; D是氢，C 1 -C 8 - 烷基，（CH 2）n -C 3 -C 7 - 环烷基，（CH 2）n -C 5 -C 10 - 芳基，（CH 2）n -C 5 -C 10杂芳基，（CH 2）n -C 5 - C10-杂环或（CH2）nO（CH2）-C5-C10-芳基，其中n为1至7的整数; E为C 5 -C 10 - 烷基或（CH 2）m -C 5 -C 7 - 环烷基，其中m为0〜2的整数; 并且F是（CH 2）m -C 5 -C 10 - 杂芳基或（CH 2）m -C 5 -C 10 - 杂环，其中n是0至2的整数。

6. 发明公开

KR1020120113886A 잔틴 옥시다아제 저해제로서 효과적인 신규 화합물 및 그를 함유한 약제학적 조성물 无效
标题翻译：新化合物作为XANTHINE氧化酶抑制剂和含有其的药物组合物
公开(公告)号：KR1020120113886A
公开(公告)日：2012-10-16
申请号：KR1020110031558
申请日：2011-04-06
申请人： 주식회사 엘지생명과학
发明人： 박희술 , 김근태 , 송정욱 , 김태훈 , 이주연 , 백승엽 , 곽효신
IPC分类号： C07D417/04 , C07D209/14 , A61K31/427 , A61P9/04
摘要： PURPOSE: A novel compound and a pharmaceutical composition containing the same are provided to prevent and/or treat diseases related to xanthine oxidase. CONSTITUTION: An indole compound is denoted by chemical formula 1. A pharmaceutical composition which suppresses xanthine oxidase contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof. The composition is used for preventing or treating xanthine oxidase related diseases including cardiac insufficiency or cardiovascular diseases, hypertension, inflammatory diseases, inflammatory bowel diseases, joint diseases, or renal diseases.
摘要翻译：目的：提供新型化合物和含有该化合物的药物组合物，以预防和/或治疗与黄嘌呤氧化酶相关的疾病。构成：吲哚化合物由化学式1表示。抑制黄嘌呤氧化酶的药物组合物含有化学式1的化合物或其药学上可接受的盐。该组合物用于预防或治疗黄嘌呤氧化酶相关疾病，包括心功能不全或心血管疾病，高血压，炎性疾病，炎性肠病，关节疾病或肾脏疾病。

7. 发明公开

KR1020120094859A ＧＰＲ119 효능제로서의 옥심 유도체 有权
标题翻译： OXIME衍生物作为GPR119激动剂
公开(公告)号：KR1020120094859A
公开(公告)日：2012-08-27
申请号：KR1020120015736
申请日：2012-02-16
申请人： 주식회사 엘지생명과학
发明人： 김영관 , 김명열 , 주현우 , 박희술 , 심동섭 , 곽효신 , 이태희 , 최은실
IPC分类号： C07D401/04 , A61K31/496 , A61P3/10
CPC分类号： C07D451/06 , C07D211/46 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/04 , C07D413/14 , C07D417/12 , C07D417/14
摘要： PURPOSE: An oxime derivative as a GPR119 effector, a manufacturing method thereof, a pharmaceutical composition including the same are provided to act as a GPR119 effector which increases insulin secretion and promotes GLP-1 secretion. CONSTITUTION: An oxime derivative as a GPR119 effector is represented by chemical formula 1. The GPR119 effector includes an oxime derivative represented by the chemical formula 1, a pharmaceutically allowed carrier, pharmaceutically allowed salt or isomer as an active component. A pharmaceutical composition for preventing or treating diabetes, complication of the diabetes, obesity, and dyslipidemia contains the oxime derivative represented by the chemical formula 1, pharmaceutically allowed salt or the isomer and the pharmaceutically allowed carrier as an active component. The diabetes is type 2 diabetes. A composition for decreasing the blood glucose contains the oxime derivative represented by the chemical formula 1, pharmaceutically allowed salt or the isomer and the pharmaceutically allowed carrier as an active component. A manufacturing method of composition for preventing or treating diabetes complication of the diabetes, obesity, dyslipidemia or osteoporosis comprises the following step: mixing the pharmaceutically allowed carrier with the pharmaceutically allowed compound represented by the chemical formula 1, the pharmaceutically allowed salt or isomer.
摘要翻译：目的：提供作为GPR119效应子的肟衍生物及其制备方法，包含其的药物组合物作为增加胰岛素分泌并促进GLP-1分泌的GPR119效应子。构成：作为GPR119效应子的肟衍生物由化学式1表示.GPR119效应子包括由化学式1表示的肟衍生物，药学上允许的载体，药学上允许的盐或异构体作为活性成分。用于预防或治疗糖尿病，糖尿病并发症，肥胖症和血脂异常的药物组合物含有由化学式1表示的肟衍生物，药学上允许的盐或异构体和药学上允许的载体作为活性成分。糖尿病是2型糖尿病。用于降低血糖的组合物含有由化学式1表示的肟衍生物，药学上允许的盐或异构体和药学上允许的载体作为活性成分。用于预防或治疗糖尿病，肥胖，血脂异常或骨质疏松症的糖尿病并发症的组合物的制备方法包括以下步骤：将药学上允许的载体与由化学式1表示的药学上允许的化合物，药学上允许的盐或异构体混合。

8. 发明公开

KR1020090075638A 세포, 조직 및 장기 보존 효과를 갖는 인돌 및 인다졸 유도체 有权
标题翻译：具有细胞，组织和组织保护作用的内毒素和吲哚美辛化合物
公开(公告)号：KR1020090075638A
公开(公告)日：2009-07-08
申请号：KR1020090000363
申请日：2009-01-05
申请人： 주식회사 엘지생명과학
发明人： 김형진 , 김순하 , 정철웅 , 박희술 , 곽효신 , 박진구 , 김성호
IPC分类号： A61K31/404 , A61P39/06
CPC分类号： C07D417/04 , C07D209/08 , C07D231/54 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14
摘要： An indole and indazole derivative which has preservative effect of cell, tissue and organ is provided to prevent reperfusion injury generated after transplantation or preservation at low temperature. A preservative composition of cell, tissue, and organ comprises a compound of the chemical formula (1) and its pharmaceutically allowable salt or isomer as active ingredients. The compound of the chemical formula (1) comprises an indole or indazole structure of the chemical formula (1a) or (1b). The cell is hypatocyte, skin cell, mucosal cell, langerhans cell, nerve cell, chondrocyte, endothelial cell, epithelial cell, osteocyte or muscle cell. The cell is zooblast, or sperm, egg or fertilized egg of cattle or fishes. The compound of the chemical formula (1), its pharmaceutically allowable salt or isomer, and carrier is produced as the composition for preserving a cell, tissue, or organ of animal.
摘要翻译：提供具有细胞，组织和器官的防腐作用的吲哚和吲唑衍生物，以防止在低温下移植或保存后产生的再灌注损伤。细胞，组织和器官的防腐组合物包含化学式（1）的化合物及其药学上可允许的盐或异构体作为活性成分。化学式（1）的化合物包含化学式（1a）或（1b）的吲哚或吲唑结构。细胞是细胞细胞，皮肤细胞，粘膜细胞，朗格汉斯细胞，神经细胞，软骨细胞，内皮细胞，上皮细胞，骨细胞或肌肉细胞。细胞是动物，或精子，卵或受精卵的牛或鱼。制备化学式（1）的化合物，其药学上允许的盐或异构体和载体作为用于保存动物的细胞，组织或器官的组合物。

9. 发明公开

KR1020090031331A 옥소 디하이드로 피라졸을 포함하는 신규한 베타 세크리타제 저해용 화합물 无效
标题翻译：具有氧 - 二 - 吡唑环的BETA-分泌酶抑制化合物
公开(公告)号：KR1020090031331A
公开(公告)日：2009-03-25
申请号：KR1020080092487
申请日：2008-09-22
申请人： 주식회사 엘지생명과학
发明人： 박희술 , 최덕영 , 곽효신 , 정혜진 , 민경식 , 임동철 , 최재웅 , 박미정 , 박현정
IPC分类号： C07D231/20 , C07D231/14 , C07D401/12 , C07D471/04
CPC分类号： C07D403/12 , C07D231/22 , C07D401/04 , C07D413/12 , C07D487/04
摘要： A pharmaceutical composition including a compound for inhibiting beta-secretase is provided to treat an Alzheimer disease and a neurodegenerative disease. A pharmaceutical composition comprises a compound, which is used for inhibiting beta-secretase, represented by the formula 1. In the formula 1, r is 1 to 3; R1 is selected from the group consisting of hydrogen, alkyl, alkene and - (CH) p-A-R7; and R2 is selected from the group consisting of hydrogen, alkyl, alkoxy and - (CR8R9) p-R10. With regard to the R1, p is 0~2 and R7 is selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, - NHC(O)alkyl and aryloxy.
摘要翻译：提供包含用于抑制β-分泌酶的化合物的药物组合物以治疗阿尔茨海默病和神经变性疾病。药物组合物包含用于抑制由式1表示的β-分泌酶的化合物。在式1中，r为1至3; R1选自氢，烷基，烯烃和 - （CH）p-A-R7; 并且R 2选自氢，烷基，烷氧基和 - （CR 8 R 9）p -R 10。关于R 1，p为0〜2，R 7选自氢，卤素，烷基，烷氧基，-NHC（O）烷基和芳氧基。

10. 发明公开

KR1020020038401A 멜라노코틴 수용체에 작용하는 트리펩타이드형 화합물 无效
标题翻译：三肽类化合物操作梅毒素受体
公开(公告)号：KR1020020038401A
公开(公告)日：2002-05-23
申请号：KR1020000068620
申请日：2000-11-17
申请人： 주식회사 엘지생명과학
发明人： 안인애 , 노성구 , 윤혜성 , 추승호 , 박희동 , 박미정 , 임현주 , 박희술 , 신동규 , 김태훈 , 전영호 , 한희정
IPC分类号： C07K5/08
CPC分类号： C07K5/08 , A61K8/64 , A61K38/06 , A61Q19/02
摘要： PURPOSE: A tri-peptide type compound operating a melanocortin receptor is provided, which compound is useful as an accelerator or antagonist for a melanocortin receptor. CONSTITUTION: The tri-peptide type compound operating a melanocortin receptor is represented by formula(1) or (2), wherein a is 0 or 1, provided that a is 0 when b is 1 and a is 1 when b is 0; W is C1-10 alkyl; E1 is amino acid or its derivative represented by formula(3) or (4) wherein A1 and A2 is the same or different alkyl, and A3 and A4 are the same or different alkyl; E2 is amino acid or its derivative represented by formula(5) or (6) wherein n is 0, 1 or 2, A5 and A6 are linked together, each is C1-3 alkyl, and A7 and A8 is the same or different alkyl; E3 is amino acid or its derivative represented by formula(7) wherein A9 and A10 are any one of hydrogen and the other of C1-5 alkyl; and E4 is amino acid or its derivative represented by formula(8) or (9) wherein A11 and A12 are any one of hydrogen and the other of C1-3 alkyl.
摘要翻译：目的：提供一种操作黑皮质素受体的三肽型化合物，该化合物可用作黑皮质素受体的促进剂或拮抗剂。构成：操作黑皮质素受体的三肽型化合物由式（1）或（2）表示，其中a为0或1，条件是当b为1时a为0，当b为0时a为1; W是C1-10烷基; E1是由式（3）或（4）表示的氨基酸或其衍生物，其中A1和A2是相同或不同的烷基，A3和A4是相同或不同的烷基; E2是由式（5）或（6）表示的氨基酸或其衍生物，其中n是0,1或2，A5和A6连接在一起，各自是C 1-3烷基，A 7和A 8是相同或不同的烷基 ; E3是由式（7）表示的氨基酸或其衍生物，其中A9和A10是氢和C1-5烷基中的另一个; 和E4是由式（8）或（9）表示的氨基酸或其衍生物，其中A11和A12是氢和C1-3烷基中的另一个。

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