JPH072633B2 - Antitumor agent containing acetic acid derivative - Google Patents
Antitumor agent containing acetic acid derivativeInfo
- Publication number
- JPH072633B2 JPH072633B2 JP5895393A JP5895393A JPH072633B2 JP H072633 B2 JPH072633 B2 JP H072633B2 JP 5895393 A JP5895393 A JP 5895393A JP 5895393 A JP5895393 A JP 5895393A JP H072633 B2 JPH072633 B2 JP H072633B2
- Authority
- JP
- Japan
- Prior art keywords
- antitumor agent
- acetic acid
- acid derivative
- agent containing
- substance
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 239000002246 antineoplastic agent Substances 0.000 title claims description 10
- 150000001242 acetic acid derivatives Chemical class 0.000 title claims description 3
- 239000004480 active ingredient Substances 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 3
- 229910052739 hydrogen Inorganic materials 0.000 claims description 3
- 239000001257 hydrogen Substances 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims description 3
- 239000000126 substance Substances 0.000 description 17
- 206010028980 Neoplasm Diseases 0.000 description 6
- 241001465754 Metazoa Species 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 239000002775 capsule Substances 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 208000006268 Sarcoma 180 Diseases 0.000 description 2
- 239000000872 buffer Substances 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 230000009036 growth inhibition Effects 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 238000002054 transplantation Methods 0.000 description 2
- 239000004606 Fillers/Extenders Substances 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 241000269908 Platichthys flesus Species 0.000 description 1
- 239000003708 ampul Substances 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 210000001099 axilla Anatomy 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000007940 sugar coated tablet Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000723 toxicological property Toxicity 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
【０００１】本発明は抗腫瘍剤に関する。The present invention relates to antitumor agents.
【０００２】本発明は、下記一般式（１）で表わされる
酢酸誘導体又はその塩および該化合物又はその塩を活性
成分として含有する抗腫瘍剤に関する。The present invention relates to an acetic acid derivative represented by the following general formula (1) or a salt thereof and an antitumor agent containing the compound or a salt thereof as an active ingredient.
【０００３】[0003]
【化６】 [Chemical 6]
【０００４】（式中、Ｒ1 は(Where R 1 is
【０００５】[0005]
【化７】 [Chemical 7]
【０００６】であり、Ｒ2 は水素又はメチルである）な
お、上記一般式（１）で表わされる本発明物質の中に
は、医薬品要覧 総合新版、薬業時報社（１９７７
年）；医療薬 日本医薬品集 第７版、４５〜４６頁，
４０１〜４０２頁，５６５〜５６６頁，５７２〜５７３
頁，７０４〜７０５頁，７０５〜７０６頁，７６７〜７
６８頁（１９８３年）、薬業時報社；最近の新薬 ３１
集，２０４頁（１９８０年）、３２集，２１９頁，２２
０頁（１９８１年）、３３集，２４６頁，２５３頁（１
９８２年）、３４集，１２５〜１２６頁，１３５〜１３
６頁，２８７頁（１９８３年）等に、抗炎症作用を有す
る物質として記載されている公知物質も含まれる。(Wherein R 2 is hydrogen or methyl) Note that among the substances of the present invention represented by the above general formula (1), there are new editions of the Handbook of Pharmaceuticals, Yakuhin Jikhosha (1977).
); Medical drug Japan Pharmaceutical Collection, 7th edition, pages 45-46,
401-402, 565-566, 572-573
Pages, pages 704-705, pages 705-706, 767-7
Page 68 (1983), Yakuhin Jikhosha; Recent New Drugs 31
Vol. 204, p. 1980, Vol. 32, p. 219, 22
0 pages (1981), 33 collections, 246 pages, 253 pages (1
982), 34, 125-126, 135-13
Known substances described as substances having an anti-inflammatory effect on pages 6 and 287 (1983) are also included.
【０００７】本物質の物理化学的並びに毒物学的特性を
第１表に示す。The physicochemical and toxicological properties of this substance are shown in Table 1.
【０００８】[0008]
【表１】 [Table 1]
【０００９】本物質は、動物又はヒトの腫瘍における腫
瘍細胞数の減少、延命、腫瘍増殖抑制等の効果を有し、
抗腫瘍剤として有用である。This substance has the effects of reducing the number of tumor cells in animal or human tumors, prolonging life, suppressing tumor growth, etc.
It is useful as an antitumor agent.
【００１０】本物質を抗腫瘍剤として用いる場合、症状
に応じて薬効を得るのに十分な量の有効成分が含有され
た投薬単位形で提供することができる。その形態として
は経口用として散剤、細粒剤、顆粒剤、錠剤、緩衝錠
剤、糖衣錠剤、カプセル剤、シロップ剤、丸剤、懸濁
剤、液剤、乳剤などの形態をとり得る。非経口用として
注射液としてのアンプル、ビンなどの形態をとり得る。
座剤、軟膏の形態でもよい。When this substance is used as an antitumor agent, it can be provided in a dosage unit form containing an effective amount of an active ingredient sufficient to obtain a drug effect depending on the symptoms. As an oral form, it may be in the form of powder, fine granules, granules, tablets, buffer tablets, sugar-coated tablets, capsules, syrups, pills, suspensions, solutions, emulsions and the like. For parenteral use, it may be in the form of an ampoule, a bottle, etc. as an injection solution.
It may be in the form of suppositories or ointments.
【００１１】本物質は単独又は製薬上許容し得る希釈剤
及び他の薬剤と混合して用いてもよく、希釈剤として固
体、液体、半固体の賦形剤、増量剤、結合剤、湿潤化
剤、崩壊剤、表面活性剤、滑沢剤、分散剤、緩衝剤、香
料、保存料、溶解補助剤、溶剤等が使用され得る。The substance may be used alone or in admixture with pharmaceutically acceptable diluents and other agents, which may be used as diluents such as solid, liquid, semisolid excipients, extenders, binders, wetting agents. Agents, disintegrants, surfactants, lubricants, dispersants, buffers, fragrances, preservatives, solubilizing agents, solvents and the like can be used.
【００１２】本物質を製剤の形で用いる場合、製剤中に
活性成分は一般に０．０１〜１００重量％、好ましくは
０．０５〜８０重量％含まれる。When the substance is used in the form of a preparation, the active ingredient is generally contained in the preparation in an amount of 0.01 to 100% by weight, preferably 0.05 to 80% by weight.
【００１３】本物質は人間及び動物に経口的または非経
口的に投与される。経口的投与は舌下投与を包含する。
非経口的投与は注射投与（例えば皮下、筋肉、静脈注
射、点滴）、直腸投与などを含む。塗布してもよい。The substance is administered to humans and animals orally or parenterally. Oral administration includes sublingual administration.
Parenteral administration includes injection administration (eg subcutaneous, intramuscular, intravenous injection, infusion), rectal administration and the like. You may apply.
【００１４】本物質の投与量は動物か人間により、また
年齢、個人差、病状などに影響されるので場合によって
は下記範囲外量を投与する場合もあるが、一般に人間を
対象とする場合、本物質の投与量は１日当り０．１〜１
０００mg／kg、好ましくは０．５〜５００mg／kgであ
る。１日２〜４回に分けて投与してもよい。Since the dose of this substance is influenced by animals or humans, age, individual difference, medical condition, etc., the dose outside the following range may be administered depending on the case. Generally, in humans, The dose of this substance is 0.1 to 1 per day
It is 000 mg / kg, preferably 0.5 to 500 mg / kg. It may be administered in 2 to 4 divided doses per day.
【００１５】以下、実施例により本発明をさらに説明す
る。The present invention will be further described below with reference to examples.
【００１６】[0016]
【実施例】実施例１ 本物質のＳａｒｃｏｍａ−１８０に対する抗腫瘍効果 Ｓａｒｃｏｍａ−１８０細胞１×１０6 個をＩＣＲ−Ｊ
ＣＬマウスの腋下部皮下に移植し、移植２４時間後より
隔日に１０回、０．５％ＣＭＣ溶液中に溶解もしくは懸
濁させた所定量の本物質を経口投与した。一方、対照群
にはＣＭＣ溶液のみを経口投与した。 Example 1 Antitumor effect of this substance on Sarcoma-180 1 × 10 6 Sarcoma-180 cells were treated with ICR-J.
CL mice were subcutaneously transplanted under the axilla, and a predetermined amount of this substance dissolved or suspended in a 0.5% CMC solution was orally administered 10 times every other day 24 hours after the transplantation. On the other hand, the control group was orally administered with only the CMC solution.
【００１７】移植後２５日目に腫瘍結節を摘出し、次式
に従って各群１０匹の腫瘍重量の平均値から増殖抑制率
（Ｉ．Ｒ．）を算出した。Tumor nodules were excised on the 25th day after the transplantation, and the growth inhibition rate (IR) was calculated from the average value of the tumor weights of 10 animals in each group according to the following formula.
【００１８】（１−Ｔ／Ｃ）×１００＝Ｉ．Ｒ．（％） Ｔ：投与群の平均腫瘍重量 Ｃ：対照群の平均腫瘍重量 結果を第２表に示す。この結果から明らかな如く、本物
質は腫瘍縮小効果を有し、抗腫瘍剤として有効であるこ
とが確認された。(1−T / C) × 100 = I. R. (%) T: average tumor weight of administration group C: average tumor weight of control group The results are shown in Table 2. As is clear from these results, it was confirmed that this substance has a tumor-reducing effect and is effective as an antitumor agent.
【００１９】[0019]
【表２】 第 ２ 表 本物質（化合物 No.） 投与量（mg／kg・回） 増殖抑制率（％） １ ３５０ ４８．３ ２ １５０ ５５．３ ３ ２５０ ４３．５製剤化例１ 本物質２５０mgをカプセルに入れてカプセル剤とした。Table 2 Table 2 present compound (Compound No.) dose (mg / kg · times) Growth inhibition rate (%) 1 350 48.3 2 150 55.3 3 250 43.5 Formulation flounder one substance 250 mg was put into a capsule to make a capsule.
───────────────────────────────────────────────────── フロントページの続き (72)発明者 古荘 孝雄 東京都町田市旭町１−６−13 (72)発明者 吉汲 親雄 東京都国立市東２−19−46 ─────────────────────────────────────────────────── ─── Continuation of the front page (72) Inventor Takao Furuso 1-6-13 Asahimachi, Machida-shi, Tokyo (72) Inventor Chikao Yoshikumi 2-19-46 East, Kunitachi, Tokyo
Claims (4)
誘導体又はその塩を活性成分として含有する抗腫瘍剤。1. A general formula: (In the formula, R 1 is And R 2 is hydrogen or methyl), which is an antitumor agent containing an acetic acid derivative or a salt thereof as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP5895393A JPH072633B2 (en) | 1993-03-18 | 1993-03-18 | Antitumor agent containing acetic acid derivative |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP5895393A JPH072633B2 (en) | 1993-03-18 | 1993-03-18 | Antitumor agent containing acetic acid derivative |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP25318584A Division JPH0649648B2 (en) | 1984-11-30 | 1984-11-30 | Antitumor agent containing acetic acid derivative |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH0616544A JPH0616544A (en) | 1994-01-25 |
| JPH072633B2 true JPH072633B2 (en) | 1995-01-18 |
Family
ID=13099206
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP5895393A Expired - Lifetime JPH072633B2 (en) | 1993-03-18 | 1993-03-18 | Antitumor agent containing acetic acid derivative |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH072633B2 (en) |
-
1993
- 1993-03-18 JP JP5895393A patent/JPH072633B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0616544A (en) | 1994-01-25 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR100643553B1 (en) | Pharmaceutical composition for enhancing leukocyte count | |
| JPH0430924B2 (en) | ||
| JPH072633B2 (en) | Antitumor agent containing acetic acid derivative | |
| JPH0735329B2 (en) | Antitumor agent containing acetic acid derivative | |
| JPH072634B2 (en) | Antitumor agent containing acetic acid derivative | |
| JPH0649648B2 (en) | Antitumor agent containing acetic acid derivative | |
| HUP0203790A2 (en) | Use of compositions containing 6-methoxy-2-naphthylacetic acid prodrugs for treating inflammation | |
| JPH0324446B2 (en) | ||
| JPH0548207B2 (en) | ||
| JPH0559892B2 (en) | ||
| JPH0442368B2 (en) | ||
| JPH0528687B2 (en) | ||
| JPH0425933B2 (en) | ||
| JP5061352B2 (en) | Liver disease therapeutic agent and liver function improving agent | |
| EP0005074A1 (en) | A material and composition for reducing blood pressure | |
| JP4287523B2 (en) | Antitumor agent | |
| JPH0329766B2 (en) | ||
| JPH0528704B2 (en) | ||
| JPH0528690B2 (en) | ||
| WO2007132280A1 (en) | Isatin and its derivatives for use as a medicament | |
| JPS61130224A (en) | Antitumor agent | |
| US7115604B2 (en) | Method for treating erectile dysfunction | |
| JPH0344049B2 (en) | ||
| TW202408499A (en) | Agent for reducing blood myostatin level | |
| JPH0616561A (en) | Antiretroviral agent |