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1.2015024984PYRAZOLE-AMIDE COMPOUND AND ITS PHARMACEUTICAL USE

JP - 05.02.2015

Int.Class C07D 231/12 Appl.No 2014050964 Applicant JAPAN TOBACCO INC Inventor MOTOMURA TAKANAO

PROBLEM TO BE SOLVED: To provide a pyrazole-amide compound having inhibitory activity against pyruvic acid dehydrogenase kinase, and being useful, when used for pharmaceutical composition, in preventing or treating diabetes (Type 1 diabetes, Type 2 diabetes), insulin resistant syndrome, metabolic syndrome, hyperglycemia, hyperlactacidemia, diabetic complications (diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, cataract), heart failure (acute heart failure, chronic heart failure), cardiomyopathy, myocardial ischemia, myocardial infarction, angina pectoris, dyslipidemia, atherosclerosis, peripheral arterial disease, intermittent claudication, chronic obstructive pulmonary disease, cerebral ischemia, stroke, mitochondrial disorders, mitochondrial encephalomyopathy, cancer, pulmonary hypertension, or Alzheimer's disease and the like.

SOLUTION: The compound represented by formula I, in which n is 1 to 2, or a pharmaceutically acceptable salt thereof is provided.

2.WO/2019/151274NITROGENATED HETEROCYCLIC AMIDE COMPOUND, AND USE THEREOF FOR MEDICAL PURPOSES

WO - 08.08.2019

Int.Class C07D 487/04 Appl.No PCT/JP2019/003052 Applicant JAPAN TOBACCO INC. Inventor MAEBA, Takaki

The present invention provides a compound which has a PDHK-inhibiting activity and is useful for the treatment or prevention of diabetes (type 1 diabetes, type 2 diabetes, etc.), insulin resistance syndrome, metabolic syndrome, hyperglycemia, hyperlactatemia, diabetes complications (diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, cataract, etc.), heart failure (acute heart failure, chronic heart failure), cardiomyopathy, myocardial ischemia, myocardial infarction, angina pectoris, dyslipidemia, atherosclerosis, peripheral arterial disease, intermittent claudication, chronic obstructive pulmonary disease, brain ischemia, stroke, mitochondrial disease, mitochondrial encephalomyopathy, cancer, pulmonary hypertension or Alzheimer's disease. The present invention relates to a compound represented by formula [I-a] or [II] or a pharmaceutically acceptable salt thereof. [In the formulae, each symbol is as defined in the description.]

3.2023071925NITROGEN-CONTAINING HETEROCYCLIC AMIDE COMPOUND AND PHARMACEUTICAL USE THEREOF

JP - 23.05.2023

Int.Class A61P 3/10 Appl.No 2023034806 Applicant JAPAN TOBACCO INC Inventor MAEBA TAKAKI

PROBLEM TO BE SOLVED: To provide a compound having PDHK inhibitory activity and useful for treating or preventing diabetes (type 1 diabetes, type 2 diabetes, etc.), insulin resistance syndrome, metabolic syndrome, hyperglycemia, hyperlacticacidemia, diabetic complications (diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, cataract, etc.), heart failure (acute heart failure, chronic heart failure), cardiomyopathy, myocardial ischemia, myocardial infarction, angina pectoris, dyslipidemia, atherosclerosis, peripheral artery disease, intermittent claudication, chronic obstructive pulmonary disease, cerebral ischemia, stroke, mitochondrial disease, mitochondrial encephalomyopathy, cancer, pulmonary hypertension, or Alzheimer's disease.

SOLUTION: A compound of formula [I-a] or formula [II], or a pharmaceutically acceptable salt thereof is synthesized.

SELECTED DRAWING: None

4.2024116307NITROGEN-CONTAINING HETEROCYCLIC AMIDE COMPOUND AND PHARMACEUTICAL USE THEREOF

JP - 27.08.2024

Int.Class C12N 9/99 Appl.No 2024094812 Applicant JAPAN TOBACCO INC Inventor MAEBA TAKAKI

SOLUTION: A compound of formula [I-a] or formula [II], or a pharmaceutically acceptable salt thereof is synthesized.

SELECTED DRAWING: None

5.2023159268PEPTIDE FOR TREATING AND PREVENTING DIABETES MELLITUS AND RELATED DISORDER

JP - 31.10.2023

Int.Class C07K 7/08 Appl.No 2023133077 Applicant UNIV DE STRASBOURG Inventor VINCENT MARION

PROBLEM TO BE SOLVED: To provide a pharmaceutical composition for treating diabetes mellitus and related disorders.

SOLUTION: A pharmaceutical composition includes peptide, and is used for treating diabetes mellitus and related disorders selected from the group consisting of type I diabetes mellitus, type II diabetes mellitus, insulin resistance, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy, hyperglycemia, obesity, hyperinsulinemia and Bardet-Biedl syndrome, where the peptide can reduce an expression of FATP2 in an adipose tissue, does not simultaneously contain a single methionine, a single proline and a single arginine, adopts a secondary structure being helix, preferably alpha-helix, has the length of 5 to 60 amino acid, and includes a specific sequence.

SELECTED DRAWING: None

6.2006508975ジペプチジルペプチダーゼＩＶを阻害するフッ素化環状アミド

JP - 16.03.2006

Int.Class C07D 207/10 Appl.No 2004552974 Applicant ファイザー・プロダクツ・インク Inventor ベルナード　フリン

本発明は、ジペプチジルペプチダーゼ−IV酵素の治療的に有効で選択的な新規阻害剤、前記化合物を含む医薬組成物、並びにＤＰＰ−IVによる処理を被るタンパク質に関連する疾病、例えばII型真性糖尿病、高血糖症、耐糖能障害、代謝症候群（症候群Ｘ又はインスリン耐性症候群）、糖尿、代謝性アシドーシス、白内障、糖尿病性神経障害、糖尿病性腎症、糖尿病性網膜症、糖尿病性心筋症、Ｉ型糖尿病、肥満症、肥満症によって悪化した状態、高血圧症、高脂血症、アテローム性動脈硬化症、骨粗しょう症、骨減少症、虚弱性、骨損失、骨折、急性冠症候群、多嚢胞性卵巣症候群による不妊症、短腸症候群、不安、うつ病、不眠症、慢性疲労、てんかん、摂食障害、慢性疼痛、アルコール嗜癖、腸運動に関連する疾病、潰瘍、過敏性腸症候群、炎症性腸症候群を治療するための及びII型糖尿病における疾病進行を予防するための前記化合物の使用に関する。また、本発明は、糖尿病用のインスリン分泌促進剤の同定方法にも関する。

7.2009535347糖尿病の治療方法

JP - 01.10.2009

Int.Class A61K 35/12 Appl.No 2009507829 Applicant テュレーン・ユニバーシティ・ヘルス・サイエンシーズ・センター Inventor ダーウィン・ジェイ・プロコップ

多能性間質細胞（ＭＳＣ）を糖尿病マウスに移植すると、血糖が降下し、血中インスリンレベルが上昇し、腎臓病が改善される。よって、本発明は、単離されたＭＳＣを投与することにより、糖尿病を治療または予防するための方法を提供する。本発明はまた、単離されたＭＳＣを移植することにより、糖尿病性腎症を含む糖尿病から起こる合併症を治療または予防するための方法を提供する。

8.WO2004002474糖尿病性合併症の予防又は進展阻止用医薬組成物

JP - 08.01.2004

Int.Class A61K 31/403 Appl.No 2004517287 Applicant キッセイ薬品工業株式会社 Inventor 御子柴　今雄

本発明は、良好な血糖コントロール状態を達成し、食後高血糖や早期空腹時高血糖を是正させることができる医薬組成物を提供する。該医薬組成物は、単回投与量としてミチグリニド若しくはその薬理学的に許容される塩、又はそれらの水和物（例えば、ミチグリニドカルシウム塩水和物）を５〜４５ｍｇ含有する、糖尿病性合併症の予防又は進展阻止のための食前投与用医薬組成物であり、低血糖症状や消化管障害の副作用発現率が低値であるため、例えば、糖尿病性細小血管合併症や動脈硬化性疾患の予防又は進展阻止に極めて有用である。

9.WO/2004/002474DRUG COMPOSITION FOR PREVENTION OR INHIBITION OF ADVANCE OF DIABETIC COMPLICATION

WO - 08.01.2004

Int.Class A61K 31/4035 Appl.No PCT/JP2003/008084 Applicant KISSEI PHARMACEUTICAL CO., LTD. Inventor MIKOSHIBA, Imao

A drug composition capable of attaining a good state of blood sugar control so as to enable correcting postprandial high blood sugar levels or high blood sugar levels at early fasting time. In particular, a drug composition for prevention or inhibition of advance of diabetic complications to be taken before meals, comprising 5 to 45 mg, in terms of one-time dose, of mitiglinide or its pharmacologically acceptable salt or a hydrate thereof (e.g., mitiglinide calcium salt hydrate). The drug composition is highly useful for the prevention or inhibition of advance of, for example, diabetic microangio complications and arteriosclerosis because the ratio of occurrence of side effects, such as low blood sugar level symptom and gastrointestinal tract disorder, is low.

10.WO2007119623Ｇ蛋白質共役型受容体およびそのリガンドの新規用途

JP - 25.10.2007

Int.Class A61K 38/00 Appl.No 2008510903 Applicant 国立研究開発法人理化学研究所 Inventor 東　秀好

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