JPH04506057A - 黒色腫の診断および治療薬 - Google Patents
黒色腫の診断および治療薬Info
- Publication number
- JPH04506057A JPH04506057A JP2504230A JP50423090A JPH04506057A JP H04506057 A JPH04506057 A JP H04506057A JP 2504230 A JP2504230 A JP 2504230A JP 50423090 A JP50423090 A JP 50423090A JP H04506057 A JPH04506057 A JP H04506057A
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- JP
- Japan
- Prior art keywords
- formula
- tables
- formulas
- compound
- mathematical
- 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.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
- C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/18—Sulfonamides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0404—Lipids, e.g. triglycerides; Polycationic carriers
- A61K51/0406—Amines, polyamines, e.g. spermine, spermidine, amino acids, (bis)guanidines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
- C07C233/77—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
- C07C233/78—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Physics & Mathematics (AREA)
- Optics & Photonics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
Claims (11)
- 1.悪性黒色腫を診断および治療するための薬剤であって、次の一般式Iの化合 物: ▲数式、化学式、表等があります▼I 〔上式中、 Xは水素またはハロゲン原子を表し、 YはZ−CONH−,Z−O−,Z−S(O)n1−(n1=0,1,2または 3),Z−SO2−NH−またはZ−NHCO−基を表し、ここでZは結合、− CH2−または▲数式、化学式、表等があります▼であり、nは2〜4の整数で あり、そして R1およびR2は各々、水素原子、C1−C6アルキル、アリールまたはC6− C12アラルキル基を表し、それらの化合物は、123I,125I,131I ,75Br,77Br,18Fもしくは11Cから選択された放射性同位体、ま たは13Cもしくは19Fから選択された安定な同位体により標識されている〕 並びにそれらと医薬上許容される酸との付加塩であって、ただしYがZ−CON H−を表し、Zが結合であり、そしてXがオルト、メタもしくはバラ位のF,C l,Brまたはオルトもしくはメタ位のIを表す式Iの化合物、YがZ−SO2 −NH−を表し、Zが結合であり、そしてXがパラ位のClを表す式Iの化合物 、およびYがZ−CONH−を表し、Zが結合であり、Xがパラ位のヨウ素原子 を表し、そしてR1とR2がエチル基を表す式Iの化合物を除く前記薬剤。
- 2.Xが123I,125Iまたは131Iを表し、YがZ−CONH−または Z−SO2−NH−を表し、Zが結合、−CH2−または▲数式、化学式、表等 があります▼であり、 R2およびR2が各々、水素原子またはC1−C6アルキル基を表す式Iに相当 する、請求項1に記載の薬剤。
- 3.次の一般式IIの化合物: ▲数式、化学式、表等があります▼II〔上式中、 X1はハロゲン原子またはそれの放射性同位体の1つであり、Y1はCOまたは SO2基を表し、 nは2〜4の整数であり、そして R1およびR2は各々、水素原子またはC1−C6アルキル基を表す〕並びにそ れらと医薬上許容される酸との付加塩でって、ただしY1がCOを表し、X1が オルト、メタもしくはパラ位のF,C1,Brまたはオルトもしくはメタ位のI を表す式IIの化合物、Y1がSO2を表し、X1がバラ位のC1を表す式II の化合物、およびY1がCOを表し、X1がパラ位のヨウ素原子を表し、そして R1およびR2がエチル基を表す式IIの化合物を除く化合物。
- 4.次の式: ▲数式、化学式、表等があります▼ (上式中、*Iは125I,123I,131Iである)に相当する化合物。
- 5.請求項3に記載の化合物の調製方法であって、式IIIのハロゲノ安息香酸 クロリドまたはハロゲノベンゼンスルホン酸クロリド: ▲数式、化学式、表等があります▼III(上式中、X1とY1は式IIのもの と同じ意味を有する)を式IVのジアミン: NH2−(CH2)n−NR1R2IV(上式中、n,R1およびR2は式II のものと同じ意味を有する)と縮合せしめ、次いで所望により、得られた構造体 (II)をハロゲンX1の放射性同位体で標識することを含んで成る方法。
- 6.Y1=COである請求項3に記載の式IIの化合物の調製方法であって、式 IIIのハロゲノ安息香酸クロリド:▲数式、化学式、表等があります▼III (上式中、X1とY1は式IIIのものと同じ意味を有する)をバラニトロフェ ノールと縮合させて式Vのエステル:▲数式、化学式、表等があります▼V を生成せしめ、次いで化合物Vを式IVのジアミン:NH2−(CH2)n−N R1R2IV(上式中、n,R1およびR2は式IIのものと同じ意味を有する )と反応させ、次いで所望により得られた構造体をX1の放射性同位体で標識す ることを含んで成る方法。
- 7.核磁気共鳴画像診断において使用される19Fまたは13Cで標識された請 求項1に記載の薬剤。
- 8.悪性黒色腫の診断および/または治療薬の調製のための、次の一般式I: ▲数式、化学式、表等があります▼I 〔上式中、 Xは水素またはハロゲン原子を表し、 YはZ−CONH−,Z−O−,Z−S(O)n1−(n1=0,1,2または 3),Z−SO2−NH−またはZ−NHCO−基を表し、ここでZは結合、− CH2−または▲数式、化学式、表等があります▼であり、nは2〜4の整数で あり、そして R1およびR2は各々、水素原子、C1−C6アルキル、アリールまたはC6− C12アラルキル基を表し、それらの化合物は、123I,125I,131I ,75Br,77Br,18Fもしくは11Cから選択された放射性同位体、ま たは13Cもしくは19Fから選択された安定な同位体により標識されている〕 並びにそれらと医薬上許容される酸との付加塩の用途。
- 9.Xが123I,125Iまたは131Iを表し、YがZ−CONH−または Z−SO2−NH−を表し、Zが結合、−CH2−または▲数式、化学式、表等 があります▼であり、 そしてR1およびR2が各々、水素原子またはC1−C6アルキル基を表す式I に相当する化合物の、請求項8に記載の用途。
- 10.次の式: ▲数式、化学式、表等があります▼ (上式中、*Iは125I,123I.131Iである)に相当する悪性黒色腫 を診断および治療するための放射性医薬品の用途。
- 11.悪性黒色腫の診断および/または治療薬の調製のための、一般式II: ▲数式、化学式、表等があります▼II〔上式中、 X1はハロゲン原子またはそれの放射性同位体の1つを表し、Y1はCOまたは SO2基を表し、 nは2〜4の整数であり、そして R1およびR2は各々、水素原子またはC1−C6アルキル基を表す〕に相当す る化合物並びにそれらと医薬上許容される酸との付加塩の用途。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR89/01898 | 1989-02-14 | ||
FR898901898A FR2642972B1 (fr) | 1989-02-14 | 1989-02-14 | Agents pour le diagnostic et le traitement des melanomes, derives halogenes aromatiques utilisables comme de tels agents et leur preparation |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH04506057A true JPH04506057A (ja) | 1992-10-22 |
JP2846459B2 JP2846459B2 (ja) | 1999-01-13 |
Family
ID=9378769
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2504230A Expired - Lifetime JP2846459B2 (ja) | 1989-02-14 | 1990-02-14 | 黒色腫の診断および治療薬 |
Country Status (7)
Country | Link |
---|---|
US (1) | US5190741A (ja) |
EP (1) | EP0458886B1 (ja) |
JP (1) | JP2846459B2 (ja) |
AU (1) | AU5191390A (ja) |
DE (1) | DE69003937T2 (ja) |
FR (1) | FR2642972B1 (ja) |
WO (1) | WO1990009170A2 (ja) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPWO2014156196A1 (ja) * | 2013-03-29 | 2017-02-16 | 国立大学法人 熊本大学 | 2型糖尿病治療剤 |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5045303A (en) * | 1985-05-17 | 1991-09-03 | Neorx Corporation | Radiohalogenated small molecules for protein labeling |
US6517811B2 (en) | 1993-05-06 | 2003-02-11 | Research Corporation Technologies, Inc. | Compounds for cancer imaging and therapy |
EP0650372A4 (en) * | 1993-05-06 | 1996-07-03 | Christy S John | COMPOUNDS FOR CANCER VISUALIZATION AND THERAPY. |
US5911970A (en) * | 1993-05-06 | 1999-06-15 | Research Corporation Technologies, Inc. | Methods for cancer imaging and therapy using benzamine compounds |
US5993777A (en) * | 1993-05-06 | 1999-11-30 | Research Corporation Technologies, Inc. | Benzamide compounds for cancer imaging and therapy |
DE19519508C2 (de) * | 1995-05-31 | 1997-05-28 | Michael Prof Dr Eisenhut | Radiohalogenierte Verbindungen und deren Verwendung zur Diagnose und Behandlung von Tumoren, insbesondere Melanomen |
US5919934A (en) * | 1997-02-19 | 1999-07-06 | The George Washington University | Compounds, compositions, and methods for cancer imaging and therapy |
DE19952146A1 (de) | 1999-10-29 | 2001-06-07 | Boehringer Ingelheim Pharma | Arylalkane, Arylalkene und Aryl-azaalkane, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
US20060235035A1 (en) * | 2002-04-09 | 2006-10-19 | 7Tm Pharma A/S | Novel methoxybenzamibe compounds for use in mch receptor related disorders |
DE102004011720B4 (de) * | 2004-03-10 | 2008-04-03 | Bayer Schering Pharma Aktiengesellschaft | Radiohalogenierte Benzamidderivate und deren Verwendung in der Tumordiagnostik und Tumortherapie |
FR2904317A1 (fr) * | 2006-07-27 | 2008-02-01 | Inst Nat Sante Rech Med | Analogues d'halogenobenzamides marques a titre de radiopharmaceutiques |
EP2085390A1 (en) * | 2008-01-31 | 2009-08-05 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Labelled analogues of halobenzamides as multimodal radiopharmaceuticals and their precursors |
EP2657213A1 (en) | 2012-04-24 | 2013-10-30 | Institut National de la Santé et de la Recherche Medicale | Labelled quinoxaline derivatives as multimodal radiopharmaceuticals and their precursors |
CN109721533A (zh) * | 2017-10-27 | 2019-05-07 | 华中科技大学同济医学院附属协和医院 | 靶向黑色素瘤的显像剂及其制备方法与应用 |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR1514517A (fr) * | 1967-03-08 | 1968-02-23 | Ile De France | Procédé de préparation de dérivés de n-substitués benzamides |
GB1184047A (en) * | 1967-03-17 | 1970-03-11 | Ile De France | Process for Preparing Derivatives of N-substituted Benzamides |
DD107262A1 (ja) * | 1972-09-27 | 1974-07-20 | ||
JPS522882B2 (ja) * | 1973-11-30 | 1977-01-25 | ||
DE2616486A1 (de) * | 1976-04-14 | 1977-11-03 | Basf Ag | Farbstoffe der perylentetracarbonsaeurediimidreihe |
FR2424253A1 (fr) * | 1978-04-27 | 1979-11-23 | Brun Lab Sa Le | Nouveaux derives de peptides analogues des enkephalines, leur procede de preparation et leur application therapeutique |
US4279887A (en) * | 1978-11-29 | 1981-07-21 | Medi-Physics, Inc. | Amides useful as brain imaging agents |
DE3200258A1 (de) * | 1982-01-07 | 1983-07-21 | Lentia GmbH Chem. u. pharm. Erzeugnisse - Industriebedarf, 8000 München | Substituierte 1-benzoyl-2-phenylimino-imidazolidine, deren saeureadditionssalze, verfahren zu deren herstellung und diese enthaltende arzneimittel |
CH653670A5 (de) * | 1983-03-03 | 1986-01-15 | Hoffmann La Roche | Benzamid-derivate. |
EP0199042A1 (en) * | 1985-03-26 | 1986-10-29 | Abbott Laboratories | Procainamide assay, tracers, immunogens and antibodies |
DE3515278A1 (de) * | 1985-04-27 | 1986-10-30 | Grünenthal GmbH, 5190 Stolberg | Neue benzoesaeurederivate, diese enthaltende arzneimittel und verfahren zur herstellung dieser verbindungen und arzneimittel |
US4804662A (en) * | 1987-05-05 | 1989-02-14 | Schering A.G. | Substituted 4-(1H-imidazol-1-yl)benzamides as antiarrhythmic agents |
-
1989
- 1989-02-14 FR FR898901898A patent/FR2642972B1/fr not_active Expired - Fee Related
-
1990
- 1990-02-14 DE DE90903857T patent/DE69003937T2/de not_active Expired - Lifetime
- 1990-02-14 JP JP2504230A patent/JP2846459B2/ja not_active Expired - Lifetime
- 1990-02-14 EP EP90903857A patent/EP0458886B1/fr not_active Expired - Lifetime
- 1990-02-14 WO PCT/FR1990/000107 patent/WO1990009170A2/fr active IP Right Grant
- 1990-02-14 AU AU51913/90A patent/AU5191390A/en not_active Abandoned
- 1990-02-14 US US07/741,481 patent/US5190741A/en not_active Expired - Fee Related
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPWO2014156196A1 (ja) * | 2013-03-29 | 2017-02-16 | 国立大学法人 熊本大学 | 2型糖尿病治療剤 |
Also Published As
Publication number | Publication date |
---|---|
WO1990009170A2 (fr) | 1990-08-23 |
DE69003937D1 (de) | 1993-11-18 |
AU5191390A (en) | 1990-09-05 |
JP2846459B2 (ja) | 1999-01-13 |
EP0458886B1 (fr) | 1993-10-13 |
FR2642972A1 (fr) | 1990-08-17 |
US5190741A (en) | 1993-03-02 |
FR2642972B1 (fr) | 1994-08-05 |
WO1990009170A3 (fr) | 1990-11-01 |
EP0458886A1 (fr) | 1991-12-04 |
DE69003937T2 (de) | 1994-05-05 |
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