JPH0820594A - Antineoplastic cycloalkaneamine derivative/platinum (iv) complex - Google Patents

Antineoplastic cycloalkaneamine derivative/platinum (iv) complex

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Publication number
JPH0820594A
JPH0820594A JP17764494A JP17764494A JPH0820594A JP H0820594 A JPH0820594 A JP H0820594A JP 17764494 A JP17764494 A JP 17764494A JP 17764494 A JP17764494 A JP 17764494A JP H0820594 A JPH0820594 A JP H0820594A
Authority
JP
Japan
Prior art keywords
platinum
complex
derivative
cycloalkaneamine
represented
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.)
Pending
Application number
JP17764494A
Other languages
Japanese (ja)
Inventor
Junji Onishi
潤治 大西
Yasunobu Komota
安伸 古茂田
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Tanaka Kikinzoku Kogyo KK
Original Assignee
Tanaka Kikinzoku Kogyo KK
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Tanaka Kikinzoku Kogyo KK filed Critical Tanaka Kikinzoku Kogyo KK
Priority to JP17764494A priority Critical patent/JPH0820594A/en
Publication of JPH0820594A publication Critical patent/JPH0820594A/en
Pending legal-status Critical Current

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Abstract

PURPOSE:To obtain the subject new compound derivative platinum (IV) complex being a specific cycloalkaneamine derivative platinum (IV) complex, having high fat-soluble property and higher antineoplastic activity, directing simple oral administration and useful as a carcinostatic agent, etc. CONSTITUTION:This new antineoplastic cycloalkaneamine derivative platinum (IV) complex is expressed by formula I [R is a 5-7C cycloalkane; X is bromine, iodine, fluorine, hydroxy or carboxylate; formula II is a ligand forming a 5 or 6-membered ring at O, Oorientation to chlorine or platinum (IV)] and has higher antineoplastic activity and further, directs simple oral administration and is extremely effective for treatment for various kinds of organ tumors including brain tumor. The complex is obtained by adding dimethylacetamide and 31% H2O2 to a compound, etc., of the formula PtCl2(C6H11NH2)2 and reacting these components at 70 deg.C for 7hr and cooling the reaction system and filtering and collecting the deposited precipitation.

Description

【発明の詳細な説明】Detailed Description of the Invention

【０００１】[0001]

【産業上の利用分野】本発明は、制癌剤として用いられ
る抗腫瘍性シクロアルカンアミン誘導体白金(IV)錯体に
関する。TECHNICAL FIELD The present invention relates to an antitumor cycloalkaneamine derivative platinum (IV) complex used as an anticancer agent.

【０００２】[0002]

【従来の技術】従来、白金制癌剤薬剤としては、シスジ
クロロジアミン白金(II)錯体（一般名シスプラチン）や
カルボプラチンが、卵巣癌、膀胱癌、肺癌、及び頭頸部
癌を中心に使用されている。2. Description of the Related Art Conventionally, cisdichlorodiamineplatinum (II) complex (general name cisplatin) and carboplatin have been used as platinum anticancer drug mainly in ovarian cancer, bladder cancer, lung cancer and head and neck cancer.

【０００３】[0003]

【発明が解決しようとする課題】しかしながら、従来の
白金制癌剤では、静注投与されており、患者への負担が
大きい一方、卵巣や睾丸以外の他の臓器の腫瘍（例えば
脳腫瘍等）にも活性のある白金制癌剤の開発が望まれて
いる。そこで、本発明はより一層の抗腫瘍活性を有し、
更に簡便な経口投与を志向した抗腫瘍性シクロアルカン
アミン誘導体白金(IV)錯体の提供を目的とする。However, while conventional platinum anti-cancer agents are administered intravenously, they impose a heavy burden on patients, while they are also active against tumors of organs other than the ovary and testes (eg brain tumors). It is desired to develop a platinum anticancer drug. Therefore, the present invention has further antitumor activity,
It is another object of the present invention to provide an antitumor cycloalkaneamine derivative platinum (IV) complex intended for simple oral administration.

【０００４】[0004]

【課題を解決するための手段】前記課題を解決するた
め、本発明の抗腫瘍性シクロアルカンアミン誘導体白金
(IV)錯体は、一般式、化１（式中、ＲはＣ5 〜Ｃ7 のシ
クロアルカン、Ｘは臭素、沃素、弗素、ヒドロキシ又は
カルボキシレートより選ばれる１種であり、化２は塩素
又は白金(IV)にＯ，Ｏ−配位の５あるいは６員環を形成
する配位子である。）で表されることを特徴とする。前
記配位子は化３で示されるオキサレート、化４で示され
る１、１−シクロブタンジカルボキシレート、あるいは
化５で示されるマロナート、化６で示されるグリコラー
ト及び各々の誘導体より選ばれる１種であることが好ま
しい。前記誘導体は、化７又は化８においてＲ1 がＣ1
〜Ｃ10の脂肪族環状アルキルを含む脂肪族アルキルある
いは芳香族アルキルで表されるものである。In order to solve the above-mentioned problems, the antitumor cycloalkaneamine derivative platinum of the present invention
The (IV) complex is a compound represented by the general formula 1, wherein R is a C 5 to C 7 cycloalkane, X is one selected from bromine, iodine, fluorine, hydroxy or carboxylate, and the compound 2 is chlorine. Or a ligand that forms an O, O-coordinated 5- or 6-membered ring on platinum (IV).). The ligand is one selected from oxalate represented by Chemical formula 3, 1,1-cyclobutanedicarboxylate represented by Chemical formula 4, malonate represented by Chemical formula 5, glycolate represented by Chemical formula 6, and derivatives thereof. Preferably there is. In the above-mentioned derivative, R 1 is C 1
It is represented by an aliphatic alkyl or an aromatic alkyl including a C 10 aliphatic cyclic alkyl.

【０００５】[0005]

【作用】本発明の抗腫瘍性シクロアルカンアミン誘導体
白金(IV)錯体においては、脂溶性が高く、抗腫瘍作用に
優れている。The antitumor cycloalkaneamine derivative platinum (IV) complex of the present invention has high lipophilicity and excellent antitumor effect.

【０００６】[0006]

【実施例】以下、本発明の実施例について詳細に説明す
る。なお、以下の説明において実施例番号を化合物番号
とする。EXAMPLES Examples of the present invention will be described in detail below. In the following description, the example numbers are compound numbers.

【０００７】[0007]

【実施例１】 ＰｔＣｌ2 （ＯＨ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 の合成。 先ず、ＰｔＣｌ2 （Ｃ6 Ｈ11ＮＨ2 ）2 10.26ｇ（22.1
mmol）にジメチルアセトアミド（ＤＭＡ）と31％Ｈ2 Ｏ
2 80mlを加えて70℃の温度で７時間反応させた。次いで
冷却後にろ取してＰｔＣｌ2 （ＯＨ）2 （Ｃ6 Ｈ11ＮＨ
2 ）2 ・３／２Ｈ2 Ｏ2.62ｇ（収率24％）を得た。Example 1 Synthesis of PtCl 2 (OH) 2 (C 6 H 11 NH 2 ) 2 . First, 10.26 g of PtCl 2 (C 6 H 11 NH 2 ) 2 (22.1
Dimethylacetamide (DMA) and 31% H 2 O
2 80 ml was added and reacted at a temperature of 70 ° C. for 7 hours. Then, after cooling, it is collected by filtration and PtCl 2 (OH) 2 (C 6 H 11 NH
2) to give a 2 · 3 / 2H 2 O2.62g ( 24% yield).

【０００８】[0008]

【実施例２】 ＰｔＣｌ2 （ＯＨ）2 （Ｃ6 Ｈ9 ＮＨ2 ）2 の合成。 先ず、ＰｔＣｌ2 （Ｃ5 Ｈ9 ＮＨ2 ）2 1.0ｇ（2.29ｇ
mmol）に31％Ｈ2 Ｏ220mlを加えた。次いで、実施例１
と同様にしてＰｔＣｌ2 （ＯＨ）2 （Ｃ5 Ｈ9 ＮＨ2 ）
2 ・Ｈ2 Ｏ 420mg（収率39％）を得た。Example 2 Synthesis of PtCl 2 (OH) 2 (C 6 H 9 NH 2 ) 2 . First, PtCl 2 (C 5 H 9 NH 2 ) 2 1.0 g (2.29 g
mmol) with 20% of 31% H 2 O 2 was added. Then, Example 1
In the same manner as in PtCl 2 (OH) 2 (C 5 H 9 NH 2 ).
420 mg of 2 · H 2 O (yield 39%) was obtained.

【０００９】[0009]

【実施例３】 ＰｔＣｌ2 （ＯＨ）2 （Ｃ7 Ｈ13ＮＨ2 ）2 の合成。 先ず、ＰｔＣｌ2 （Ｃ7 Ｈ13ＮＨ2 ）2 750mg（1.52mm
ol）にＤＭＡ20mlとＨ2 Ｏ2 10mlを加えた。次いで、実
施例１と同様にしてＰｔＣｌ2 （ＯＨ）2 （Ｃ7 Ｈ13Ｎ
Ｈ2 ）2 ・１／２Ｈ2 Ｏ 430mg（収率54％）を得た。Example 3 Synthesis of PtCl 2 (OH) 2 (C 7 H 13 NH 2 ) 2 . First, PtCl 2 (C 7 H 13 NH 2 ) 2 750 mg (1.52 mm
20 ml of DMA and 10 ml of H 2 O 2 were added to ol). Then, in the same manner as in Example 1, PtCl 2 (OH) 2 (C 7 H 13 N
430 mg (yield 54%) of H 2 ) 2 · 1 / 2H 2 O was obtained.

【００１０】[0010]

【実施例４】 ＰｔＣｌ2 Ｂｒ2 （Ｃ6 Ｈ11ＮＨ2 ）2 の合成。 先ず、ＰｔＣｌ2 （Ｃ6 Ｈ11ＮＨ2 ）1.00ｇ（2.15mmo
l）にＢｒ2 0.35ｇ（2.19mmol）と水20mlを加え一昼夜
反応させた。次いで生じた沈殿をろ取してＰｔＣｌ
2 （Ｃ6 Ｈ11ＮＨ2 ）2 270mg（収率20％）を得た。Example 4 Synthesis of PtCl 2 Br 2 (C 6 H 11 NH 2 ) 2 . First, PtCl 2 (C 6 H 11 NH 2 ) 1.00 g (2.15 mmo
It was reacted overnight added Br 2 0.35g (2.19mmol) and 20ml of water to l). Then, the resulting precipitate is collected by filtration and PtCl
2 (C 6 H 11 NH 2 ) 2 270 mg (yield 20%) was obtained.

【００１１】[0011]

【実施例５】 ＰｔＣｌ2 Ｂｒ2 （Ｃ7 Ｈ13ＮＨ2 ）2 の合成。 先ず、ＰｔＣｌ2 （Ｃ7 Ｈ13ＮＨ2 ）2 1.00ｇ（2.03mm
ol）にＭｅＯＨ20mlとＢｒ2 0.33ｇ（2.06mmol）を加え
て１時間撹拌した後、ＨＢｒ２mlを加えて30分間反応さ
せた。次いで、生じた沈殿をろ取してＰｔＣｌ2 Ｂｒ2
（Ｃ7 Ｈ13ＮＨ2 ）2 0.42ｇ（収率32％）を得た。Example 5 Synthesis of PtCl 2 Br 2 (C 7 H 13 NH 2 ) 2 . First, 1.00 g (2.03 mm) of PtCl 2 (C 7 H 13 NH 2 ) 2
ol), 20 ml of MeOH and 0.33 g (2.06 mmol) of Br 2 were added and stirred for 1 hour, and then 2 ml of HBr was added and reacted for 30 minutes. Then, the formed precipitate is collected by filtration and PtCl 2 Br 2
0.42 g (yield 32%) of (C 7 H 13 NH 2 ) 2 was obtained.

【００１２】[0012]

【実施例６】 ＰｔＣｌ2 （ＯＣＯＥｔ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 の合
成。 先ず、ＰｔＣｌ2 （ＯＨ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 1.00
ｇ（2.01mmol）にＯ（ＣＯＥｔ）2 ６ml（ 46.56mmol）
を加えて70℃の温度で 4.5時間反応させた。次いで、ヘ
キサンを加え、生じた沈殿をろ取してＰｔＣｌ2 （ＯＣ
ＯＥｔ）2（Ｃ6 Ｈ11ＮＨ2 ）2 700mg（収率57％）を
得た。Example 6 Synthesis of PtCl 2 (OCOEt) 2 (C 6 H 11 NH 2 ) 2 . First, PtCl 2 (OH) 2 (C 6 H 11 NH 2 ) 2 1.00
6 g (46.56 mmol) of O (COEt) 2 in g (2.01 mmol)
Was added and reacted at a temperature of 70 ° C. for 4.5 hours. Next, hexane was added, the resulting precipitate was collected by filtration, and PtCl 2 (OC
OEt) 2 (C 6 H 11 NH 2 ) 2 700 mg (yield 57%) was obtained.

【００１３】[0013]

【実施例７】 ＰｔＣｌ2 （ＯＣＯＰｒ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 の合
成。 先ず、ＰｔＣｌ2 （ＯＨ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 0.80
ｇ（1.61mmol）にＯ（ＣＯＰｒ）2 ３ml（18.4mmol）を
加えた。次いで、実施例６と同様にしてＰｔＣｌ2 （Ｏ
ＣＯＰｒ）2 （Ｃ6 Ｈ11ＮＨ2）2 ・１／２Ｈ2 Ｏ 600m
g（収率58％）を得た。Example 7 Synthesis of PtCl 2 (OCOPr) 2 (C 6 H 11 NH 2 ) 2 . First, PtCl 2 (OH) 2 (C 6 H 11 NH 2 ) 2 0.80
3 g (18.4 mmol) of O (COPr) 2 was added to g (1.61 mmol). Then, in the same manner as in Example 6, PtCl 2 (O
COPr) 2 (C 6 H 11 NH 2 ) 2 · 1 / 2H 2 O 600m
g (yield 58%) was obtained.

【００１４】[0014]

【実施例８】 ＰｔＣｌ2 （ＯＣＯＢｕ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 の合
成。 先ず、ＰｔＣｌ2 （ＯＨ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 0.80
ｇ（1.61mmol）にＯ（ＣＯＢｕ）2 ３ml（15.3mmol）を
加えた。次いで、実施例６と同様にしてＰｔＣｌ2 （Ｏ
ＣＯＢｕ）2 （Ｃ6 Ｈ11ＮＨ2）2 ・１／２Ｈ2 Ｏ 360m
g（収率34％）を得た。Example 8 Synthesis of PtCl 2 (OCOBu) 2 (C 6 H 11 NH 2 ) 2 . First, PtCl 2 (OH) 2 (C 6 H 11 NH 2 ) 2 0.80
3 g (15.3 mmol) of O (COBu) 2 was added to g (1.61 mmol). Then, in the same manner as in Example 6, PtCl 2 (O
COBu) 2 (C 6 H 11 NH 2 ) 2 · 1 / 2H 2 O 360m
g (34% yield) was obtained.

【００１５】[0015]

【実施例９】 ＰｔＣｌ2 〔ＯＣＯ（ＣＨ2 ）4 ＣＨ3 〕2 （Ｃ6 Ｈ11
ＮＨ2 ）2 の合成。 ＰｔＣｌ2 （ＯＨ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 0.27ｇ（0.
54mmol）にＯ〔ＣＯ（ＣＨ2 ）4 ＣＨ3 〕2 1.5ml（
6.5mmol）を加えた。次いで、実施例６と同様にしてＰ
ｔＣｌ2 〔ＣＯ（ＣＨ2 ）4 ＣＨ3 〕2 （Ｃ6 Ｈ11ＮＨ
2 ）2 180mg（収率48％）を得た。Example 9 PtCl 2 [OCO (CH 2 ) 4 CH 3 ] 2 (C 6 H 11
Synthesis of NH 2 ) 2 . PtCl 2 (OH) 2 (C 6 H 11 NH 2 ) 2 0.27 g (0.
54 mmol) of O [CO (CH 2 ) 4 CH 3 ] 2 1.5 ml (
6.5 mmol) was added. Then, in the same manner as in Example 6, P
tCl 2 [CO (CH 2 ) 4 CH 3 ] 2 (C 6 H 11 NH
2 ) 2 180 mg (yield 48%) was obtained.

【００１６】[0016]

【実施例10】 ＰｔＣｌ2 〔ＯＣＯ（ＣＨ2 ）5 ＣＨ3 〕2 （Ｃ6 Ｈ11
ＮＨ2 ）2 の合成。 先ず、ＰｔＣｌ2 （ＯＨ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 0.50
ｇ（1.00mmol）にＯ〔ＣＯ（ＣＨ2 ）5 ＣＨ3 〕2 ２ml
（7.59mmol）を加えた。次いで、実施例６と同様にして
ＰｔＣｌ2 〔ＯＣＯ（ＣＨ2 ）5 ＣＨ3 〕2 （Ｃ6 Ｈ11
ＮＨ2 ）2 ・１／２Ｈ2 Ｏ 210mg（収率29％）を得た。Example 10 PtCl 2 [OCO (CH 2 ) 5 CH 3 ] 2 (C 6 H 11
Synthesis of NH 2 ) 2 . First, PtCl 2 (OH) 2 (C 6 H 11 NH 2 ) 2 0.50
2 ml of O [CO (CH 2 ) 5 CH 3 ] 2 to g (1.00 mmol)
(7.59 mmol) was added. Then, PtCl 2 [OCO (CH 2 ) 5 CH 3 ] 2 (C 6 H 11
210 mg of NH 2 ) 2 · 1 / 2H 2 O (yield 29%) was obtained.

【００１７】[0017]

【実施例11】 ＰｔＣｌ2 〔ＯＣＯ（ＣＨ2 ）6 ＣＨ3 〕2 （Ｃ6 Ｈ11
ＮＨ2 ）2 の合成。 先ず、ＰｔＣｌ2 （ＯＨ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 0.50
ｇ（1.00mmol）にＯ〔ＣＯ（ＣＨ2 ）6 ＣＨ3 〕2 ２ml
（6.73mmol）を加えた。次いで、実施例６と同様にして
ＰｔＣｌ2 〔ＯＣＯ（ＣＨ2 ）6 ＣＨ3 〕2 （Ｃ6 Ｈ11
ＮＨ2 ）2 ・１／２Ｈ2 Ｏ 250mg（収率33％）を得た。Example 11 PtCl 2 [OCO (CH 2 ) 6 CH 3 ] 2 (C 6 H 11
Synthesis of NH 2 ) 2 . First, PtCl 2 (OH) 2 (C 6 H 11 NH 2 ) 2 0.50
2 ml of O [CO (CH 2 ) 6 CH 3 ] 2 to g (1.00 mmol)
(6.73 mmol) was added. Then, in the same manner as in Example 6, PtCl 2 [OCO (CH 2 ) 6 CH 3 ] 2 (C 6 H 11
250 mg (yield 33%) of NH 2 ) 2 · 1 / 2H 2 O was obtained.

【００１８】[0018]

【実施例12】 ＰｔＣｌ2 （ＯＣＯＰｈ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 の合
成。 先ず、ＰｔＣｌ2 （ＯＨ）2 （Ｃ6 Ｈ11ＮＨ2 ）2 0.50
ｇ（1.00mmol）にＯ（ＣＯＰｈ）2 2.00ｇ（8.84mmol）
を加えた。次いで、実施例６と同様にしてＰｔＣｌ
2 （ＯＣＯＰｈ）2 （Ｃ6 Ｈ11ＮＨ2）2 200mg（収率2
8％）を得た。Example 12 Synthesis of PtCl 2 (OCOPh) 2 (C 6 H 11 NH 2 ) 2 . First, PtCl 2 (OH) 2 (C 6 H 11 NH 2 ) 2 0.50
2.00 g (8.84 mmol) of O (COPh) 2 in g (1.00 mmol)
Was added. Then, in the same manner as in Example 6, PtCl
2 (OCOPh) 2 (C 6 H 11 NH 2 ) 2 200 mg (yield 2
8%).

【００１９】実施例１〜12で合成した各化合物の分析デ
ータを表１、２に示す。The analytical data of each compound synthesized in Examples 1 to 12 are shown in Tables 1 and 2.

【００２０】[0020]

【表１】 [Table 1]

【００２１】[0021]

【表２】 [Table 2]

【００２２】ここで、実施例１〜12で合成した化合物に
ついて、マウスの実験腫瘍、Ｌ1210に対する抗腫瘍性を
調べた。ＣＤＦ、マウスにＬ1210（移植細胞数はマウス
当り105 個）を腹腔内に移植した後、翌日より第１日
目、第５日目及び第９日目に、上記各化合物を薬剤とし
て表３に示す投与量で腹腔内に投与した。効果判定は、
平均生存期間Ｔ／Ｃ（％）（薬剤投与群の平均生存日数
／対照群の平均生存日数×100 ）でみた。Ｌ1210では平
均生存期間Ｔ／Ｃ 125％以上を有効とし、その結果を表
３に示す。一群は、６匹である。The compounds synthesized in Examples 1 to 12 were examined for their antitumor activity against L1210, an experimental tumor of mice. CD12 and L1210 (the number of transplanted cells per mouse was 10 5 per mouse) were intraperitoneally transplanted to CDF, and then from the next day to the 1st, 5th and 9th days, each of the above compounds was used as a drug. It was intraperitoneally administered at the dose shown in. The effect judgment is
The average survival time T / C (%) was calculated (average survival time of drug administration group / average survival time of control group × 100). With L1210, the mean survival time T / C of 125% or more was effective, and the results are shown in Table 3. A group consists of 6 animals.

【００２３】[0023]

【表３】 [Table 3]

【００２４】表３から、各化合物が抗腫瘍性を示すこと
が判る。From Table 3, it can be seen that each compound exhibits antitumor properties.

【００２５】[0025]

【発明の効果】以上説明したように、本発明の抗腫瘍性
シクロアルカンアミン誘導体白金(IV)錯体によれば、抗
腫瘍作用に優れ、又脂溶性が高いので、脳腫瘍をはじめ
とする各種の臓器腫瘍の治療に大変有効である。As described above, according to the antitumor cycloalkaneamine derivative platinum (IV) complex of the present invention, it has excellent antitumor activity and high lipophilicity, and therefore it can be used in various types of tumors including brain tumors. It is very effective in treating organ tumors.

Claims (6)

【特許請求の範囲】[Claims] 【請求項１】 一般式化１（式中、ＲはＣ5 〜Ｃ7 のシ
クロアルカン、Ｘは臭素、沃素、弗素、ヒドロキシ又は
カルボキシレートより選ばれる１種であり、化２は塩素
又は白金(IV)にＯ、Ｏ−配位の５あるいは６員環を形成
する配位子である。）で表されることを特徴とする抗腫
瘍性シクロアルカンアミン誘導体白金(IV)錯体。 【化１】 【化２】 1. A compound represented by the general formula 1 (wherein R is a C 5 -C 7 cycloalkane, X is one selected from bromine, iodine, fluorine, hydroxy or carboxylate, and Chemical formula 2 is chlorine or platinum). (IV) is a ligand forming an O, O-coordinated 5- or 6-membered ring.) An antitumor cycloalkaneamine derivative platinum (IV) complex. Embedded image Embedded image 【請求項２】 前記配位子が化３で示されるオキサレー
ト、化４で示される１、１−シクロブタンジカルボキシ
レート、あるいは化５で示されるマロナート、化６で示
されるグリコラート及び各々の誘導体より選ばれる１種
であることを特徴とする請求項１記載の抗腫瘍性シクロ
アルカンアミン誘導体白金(IV)錯体。 【化３】 【化４】 【化５】 【化６】 2. The oxalate represented by Chemical Formula 3, the 1,1-cyclobutanedicarboxylate represented by Chemical Formula 4, or the malonate represented by Chemical Formula 5, the glycolate represented by Chemical Formula 6, and a derivative of each of the ligands. The antitumor cycloalkaneamine derivative platinum (IV) complex according to claim 1, wherein the platinum (IV) complex is one selected. Embedded image [Chemical 4] Embedded image [Chemical 6] 【請求項３】 前記誘導体が、化７又は化８においてＲ
1 がＣ1 〜Ｃ10の脂肪族環状アルキルを含む脂肪族アル
キルあるいは芳香族アルキルで表されることを特徴とす
る請求項２記載の抗腫瘍性シクロアルカンアミン誘導体
白金(IV)錯体。 【化７】 【化８】 3. The compound according to claim 7 or 8
Antitumor cycloalkane derivative of platinum (IV) complex according to claim 2, characterized by being represented by aliphatic alkyl or aromatic alkyl containing 1 aliphatic cyclic alkyl of C 1 -C 10. [Chemical 7] Embedded image 【請求項４】 前記配位子が化３で示されるオキサレー
トであることを特徴とする請求項１又は３記載の抗腫瘍
性シクロアルカンアミン誘導体白金(IV)錯体。4. The antitumor cycloalkaneamine derivative platinum (IV) complex according to claim 1 or 3, wherein the ligand is an oxalate represented by Chemical formula 3. 【請求項５】 前記配位子が化４で示される１、１−シ
クロブタンジカルボキシレートであることを特徴とする
請求項１又は３記載の抗腫瘍性シクロアルカンアミン誘
導体白金(IV)錯体。5. The antitumor cycloalkaneamine derivative platinum (IV) complex according to claim 1 or 3, wherein the ligand is 1,1-cyclobutanedicarboxylate represented by Chemical formula 4. 【請求項６】 前記配位子が化５で示されるマロナート
であることを特徴とする請求項１又は３記載の抗腫瘍性
シクロアルカンアミン誘導体白金(IV)錯体。6. The antitumor cycloalkaneamine derivative platinum (IV) complex according to claim 1, wherein the ligand is a malonate represented by Chemical formula 5.
JP17764494A 1994-07-06 1994-07-06 Antineoplastic cycloalkaneamine derivative/platinum (iv) complex Pending JPH0820594A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP17764494A JPH0820594A (en) 1994-07-06 1994-07-06 Antineoplastic cycloalkaneamine derivative/platinum (iv) complex

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP17764494A JPH0820594A (en) 1994-07-06 1994-07-06 Antineoplastic cycloalkaneamine derivative/platinum (iv) complex

Publications (1)

Publication Number Publication Date
JPH0820594A true JPH0820594A (en) 1996-01-23

Family

ID=16034603

Family Applications (1)

Application Number Title Priority Date Filing Date
JP17764494A Pending JPH0820594A (en) 1994-07-06 1994-07-06 Antineoplastic cycloalkaneamine derivative/platinum (iv) complex

Country Status (1)

Country Link
JP (1) JPH0820594A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001064696A1 (en) * 2000-03-03 2001-09-07 Xuqing Yang Dicarboxylato diammine platinum derivatives and compositions comprising them as anti-tumor agents
US8293274B2 (en) 2005-04-06 2012-10-23 Kabushiki Kaisha Sangi Intestinal absorptive anti-tumor agent

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001064696A1 (en) * 2000-03-03 2001-09-07 Xuqing Yang Dicarboxylato diammine platinum derivatives and compositions comprising them as anti-tumor agents
US6699901B1 (en) 2000-03-03 2004-03-02 Xuqing Yang Dicarboxylato diammine platinum derivatives and compositions comprising them as anti-tumor agents
US8293274B2 (en) 2005-04-06 2012-10-23 Kabushiki Kaisha Sangi Intestinal absorptive anti-tumor agent

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