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202.发明授权
公开(公告)号：KR100454767B1
公开(公告)日：2004-11-03
申请号：KR1020010043490
申请日：2001-07-19
IPC: A61K31/426
CPC classification number: A61K31/426 , Y10S514/878
Abstract: 본 발명은 류코트리엔-B
4 (Leukotriene-B
4 ; 이하 "LTB-4"로 약칭한다)의 수용체 길항작용을 갖는 것으로 알려진 하기 화학식 1로 표시되는 4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}-벤즈아미딘 또는 N-히드록시-4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}-벤즈아미딘의 골다공증의 예방 및 치료제로서의 용도에 관한 것이다.
[화학식 1]
상기 식에서 R은 H 또는 OH이다.Abstract translation: 本发明涉及含有下式1表示的4 - [（4-噻唑基）苯氧基]烷氧基 - 苄脒衍生物用于预防和治疗骨质疏松症的药物组合物，更具体地涉及4- {5- [4 - （5-异丙基-2-甲基-1,3-噻唑-4-基）苯氧基]戊氧基} - 苄脒或N-羟基-4- {5- [4-（5-异丙基-2-甲基 - 噻唑-4-基）苯氧基]戊氧基} - 苄脒作为用于预防和治疗骨质疏松症的药物组合物，其已知为白三烯-B4受体的拮抗剂。 [通式1]其中，R是氢原子或羟基。
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公开(公告)号：KR100435085B1
公开(公告)日：2004-08-18
申请号：KR1019960053450
申请日：1996-11-12
IPC: C07D403/12 , A61K31/41
Abstract: PURPOSE: Provided are a novel sulfonyl-imidazolone derivative of the formula(1) and its pharmaceutically acceptable salt, a manufacturing method thereof and an anti-tumor composition containing the same as an active ingredient. CONSTITUTION: The 4-phenyl-1-(indolin-5-sulfonyl)-2-imidazolone derivative is represented by the formula(1), wherein R is chloroacetyl, C1-C5 alkylamino acetyl, C1-C4 alkoxy carbonyl. benzoyl, nitrobenzoyl, aminobenzoyl, ethoxybenzoyl, chlorobenzoyl, chloroacetyl aminobenzoyl, furanoyl, thiophenoyl and C1-C6 alkylcarbamoyl; and R1 is hydrogen or C1-C4 lower alcohol. The compound of the formula(1) is manufactured by reacting a compound of the formula(A) and a compound of the formula(B).
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公开(公告)号：KR100437670B1
公开(公告)日：2004-08-16
申请号：KR1019970019365
申请日：1997-05-19
Applicant: 동화약품주식회사
IPC: C07D403/12 , A61K31/40
Abstract: PURPOSE: (S)-Isomer type indoline sulfonyl urea derivatives, a preparation method thereof and a pharmaceutical composition comprising the same are provided. The derivatives have improved anticancer activity and improved hydrophobic properties so as to be easily absorbed into the human body. CONSTITUTION: The (S)-4-phenyl-1-(N-(4-amino-benzoyl)-indoline-5-sulfonyl)- 4,5-dihydro-2-imidazolone derivatives are represented by the formula (1), wherein R is hydrogen, or an amino acid residue which is linked through an amide bond, and selected from glycine, alanine, valine, leucine, methionine, proline and phenylalanine. The method for preparing a compound of the formula (1a) comprises the steps of: combining a compound of the formula (7) with a compound of the formula (8) to prepare (S)-4-phenyl-1-(indoline-5-sulfonyl)-4,5-dihydro-2-imidazolone of the formula (3); reacting the compound of the formula (3) with 4-nitrobenzoylchloride of the formula (4); and reducing a nitro group of the resulting product. The method for preparing a compound of the formula (1b) comprises the steps of: condensing the compound of the formula (1a) with am amino acid of which amino group is protected with t-butoxycarbonyl; and deprotecting the amino group, wherein R' is an amino acid residue which is linked through an amide bond, and selected from glycine, alanine, valine, leucine, methionine, proline and phenylalanine.
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Patent Agency Ranking
公开(公告)号：KR1020030062139A
公开(公告)日：2003-07-23
申请号：KR1020020002577
申请日：2002-01-16
Applicant: 동화약품주식회사
IPC: A61K9/24
Abstract: PURPOSE: A film applicable to the oral mucosa comprising two layers such as a protective layer and an adhesive layer which contain a drug is provided to effectively delivery the drug without changing the formulation. The film causes no foreign body sensation when applied to oral mucosa and has excellent convenience and efficiency in the preparation process. CONSTITUTION: An oral mucoadhesive film comprises: an adhesion layer containing 5 to 80% by weight of each of a polyacrylic acid-based polymer and a cellulose-based polymer, 5 to 70% by weight of poloxamer, 0.05 to 20% by weight of a drug absorbable through the oral mucosa and 0.1 to 10% by weight of a plasticizer; and a protective layer containing 5 to 50% by weight of a water-insoluble, water-impermeable polymer and 0.1 to 10% by weight of a plasticizer. The film has a thickness of 50 to 300 microns.
Abstract translation: 目的：提供适用于包含两层如口服粘膜的保护层和含有药物的粘合剂层的膜，以有效地输送药物而不改变制剂。 当应用于口腔粘膜时，该膜不引起异物感，并且在制备过程中具有极好的便利性和效率。 构成：口腔粘膜粘附膜包括：含有5〜80重量％的聚丙烯酸类聚合物和纤维素系聚合物的粘合层，5〜70重量％的泊洛沙姆，0.05〜20重量％ 通过口腔粘膜吸收的药物和0.1〜10重量％的增塑剂; 和含有5〜50重量％水不溶性水不渗透性聚合物和0.1〜10重量％增塑剂的保护层。 该膜具有50至300微米的厚度。
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公开(公告)号：KR100385364B1
公开(公告)日：2003-05-27
申请号：KR1020020052421
申请日：2002-09-02
IPC: C07D265/22
Abstract: PURPOSE: Provided are azetidinone compound of the formula(I) as an intermediate useful for the manufacture of carbapenem antibiotics and a process for the preparation thereof. CONSTITUTION: The azetidine compound is represented by the formula(I). It is useful as an intermediate for the manufacture of beta-methylcarbapenem antibiotics and manufactured by reacting 4-acetoxy-azetidine compound of the formula(II) and alpha-halo propionic acid amide compound of the formula(III).
Abstract translation: 目的：提供式（I）的氮杂环丁酮化合物作为可用于制备碳青霉烯类抗生素的中间体及其制备方法。 构成：氮杂环丁烷化合物由式（I）表示。 它可用作制备β-甲基碳青霉烯类抗生素的中间体，并通过使式（II）的4-乙酰氧基 - 氮杂环丁烷化合物与式（III）的α-卤代丙酰胺化合物反应制备。
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公开(公告)号：KR1020030002377A
公开(公告)日：2003-01-09
申请号：KR1020010037947
申请日：2001-06-29
Applicant: 동화약품주식회사
IPC: A61K36/8962 , A61P3/14
Abstract: PURPOSE: A pharmaceutical composition for prophylaxis and treatment of osteoporosis containing an extract of onion or kale, quercetin or rutin as an effective ingredient is provided. The quercetin or rutin has the excellent function of inhibiting differentiation of osteoclast, is low in cost and has no adverse effect, it can be thus effectively used in the prevention and treatment of osteoporosis. CONSTITUTION: The pharmaceutical composition for prophylaxis and treatment of osteoporosis contains an extract obtained by extracting one of onion and kale in methanol, quercetin represented by formula(1) or rutin represented by formula(2). For an example, onion and kale are extracted in methanol at 80deg.C for 3hr, filtered and washed two times after cooling. The extract is cultured with 200μl osteoclast solution at 37deg.C under 5% CO2 for 1 to 2 day and shows a high inhibition rate of osteoclast.
Abstract translation: 目的：提供一种用于预防和治疗含有洋葱或羽衣甘蓝，槲皮素或芦丁提取物作为有效成分的骨质疏松症的药物组合物。 槲皮素或芦丁具有抑制破骨细胞分化的优异功能，成本低，无副作用，可有效用于预防和治疗骨质疏松症。 构成：用于预防和治疗骨质疏松症的药物组合物含有通过在甲醇中提取洋葱和羽衣甘蓝而获得的提取物，由式（1）表示的槲皮素或由式（2）表示的芦丁。 例如，洋葱和羽衣甘蓝在80℃的甲醇中萃取3小时，冷却后过滤并洗涤两次。 提取物在37℃，5％CO 2下，用200μl破骨细胞溶液培养1〜2天，破骨细胞抑制率高。
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公开(公告)号：KR100321275B1
公开(公告)日：2002-05-13
申请号：KR1019980040708
申请日：1998-09-30
Applicant: 동화약품주식회사 , 학교법인 포항공과대학교
IPC: C07K7/08
Abstract: 본 발명은 세포 수용체인 CD4와 인간 면역 결핍 바이러스-1 (human immunodeficiency virus type 1, 이하 "HIV-1"로 약칭함)의 외막 단백질인 gp120과의 상호작용을 저해하는 펩타이드, 그의 용도 및 이 펩타이드의 선별방법에 관한 것으로, 구체적으로는 12개의 아미노산으로 이루어지고 아미노 말단으로부터 4번 아미노산은 프롤린 (proline), 6번 아미노산은 페닐알라닌 (phenylalanine)이고 나머지는 임의의 아미노산인 펩타이드로서 세포 수용체인 CD4와 HIV-1의 외막 단백질인 gp120과의 상호작용을 저해하는 본 발명의 펩타이드는 그 크기가 화학적 합성이 가능한 수준으로 작으면서도 기존의 후천성 면역 결핍증 (acquired immunodeficiency syndrome, 이하 "AIDS"로 약칭함) 치료제의 작용 단계와는 전혀 다른 단계인 HIV-1 바이러스의 감염 초기 단계에 작용하여 세포 수용체인 CD4와 HIV-1의 � ��막 단백질인 gp120과의 상호작용을 특이적으로 저해하므로 새로운 AIDS 치료제로 개발될 수 있을 뿐만 아니라, 다른 AIDS 치료제와 병용되는 복합 치료 방법을 통하여 AIDS 치료에 효과적으로 사용될 수 있는 펩타이드이다. 또한, 본 발명에서는 아가로스 비드 (agarose bead)를 사용하는 특징적인 패닝방법을 사용하여 상기 펩타이드을 효과적으로 선별할 수 있다.
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公开(公告)号：KR1020010111346A
公开(公告)日：2001-12-17
申请号：KR1020000031926
申请日：2000-06-10
Applicant: 동화약품주식회사
IPC: C07D401/12
Abstract: 본 발명은 항바이러스제로 유용한 신규의 6-메틸니코틴아미드 유도체, 그의 제조방법 및 그를 포함하는 약학적 조성물에 관한 것으로서, 구체적으로 비핵산계 화합물인 하기 화학식 1로 표시되는 6-메틸니코틴아미드 유도체는 HBV (Hepatitis B Virus) 및 HCV (Hepatitis C virus)의 증식 뿐만 아니라 HIV (Human Immunodeficiency Virus) 증식을 억제하는 효과도 나타내므로 B형 간염과 C형 간염 및 후천성 면역 결핍증의 치료제 및 예방제로 유용하게 사용될 수 있다.
상기 화학식 1에서, R 및 n은 명세서에 기재된 바와 같다.
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