KR970704682A - 테크네튬-술폰아미드 착물, 이들의 용도, 이들을 함유하는 약제, 및 상기 착물 및 약제의 제조 방법(Technetium-Sulphonamide Complexes, Their Use, Pharmaceutical Agents Containing Them, and Process for Producing the Complexes and Agents) - Google Patents
테크네튬-술폰아미드 착물, 이들의 용도, 이들을 함유하는 약제, 및 상기 착물 및 약제의 제조 방법(Technetium-Sulphonamide Complexes, Their Use, Pharmaceutical Agents Containing Them, and Process for Producing the Complexes and Agents) Download PDFInfo
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- 239000003814 drug Substances 0.000 title claims abstract 5
- 229940079593 drug Drugs 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 239000003795 chemical substances by application Substances 0.000 title 1
- 239000008177 pharmaceutical agent Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 11
- 108090000765 processed proteins & peptides Proteins 0.000 claims abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 10
- 229910021645 metal ion Inorganic materials 0.000 claims 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 230000002285 radioactive effect Effects 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 150000001413 amino acids Chemical class 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- -1 imino, phenylene Chemical group 0.000 claims 3
- 102000040430 polynucleotide Human genes 0.000 claims 3
- 108091033319 polynucleotide Proteins 0.000 claims 3
- 239000002157 polynucleotide Substances 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 239000011593 sulfur Substances 0.000 claims 3
- ZMZDMBWJUHKJPS-UHFFFAOYSA-M thiocyanate group Chemical group [S-]C#N ZMZDMBWJUHKJPS-UHFFFAOYSA-M 0.000 claims 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical compound ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 150000004696 coordination complex Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- ZMZDMBWJUHKJPS-UHFFFAOYSA-N hydrogen thiocyanate Natural products SC#N ZMZDMBWJUHKJPS-UHFFFAOYSA-N 0.000 claims 2
- 229910052751 metal Inorganic materials 0.000 claims 2
- 239000002184 metal Substances 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 238000001959 radiotherapy Methods 0.000 claims 2
- 150000003431 steroids Chemical class 0.000 claims 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 claims 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 150000001447 alkali salts Chemical class 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 239000012736 aqueous medium Substances 0.000 claims 1
- 150000001491 aromatic compounds Chemical class 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 125000002843 carboxylic acid group Chemical group 0.000 claims 1
- 239000003638 chemical reducing agent Substances 0.000 claims 1
- 239000008139 complexing agent Substances 0.000 claims 1
- KZNICNPSHKQLFF-UHFFFAOYSA-N dihydromaleimide Natural products O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 125000000350 glycoloyl group Chemical group O=C([*])C([H])([H])O[H] 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- 229910044991 metal oxide Inorganic materials 0.000 claims 1
- 150000004706 metal oxides Chemical class 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000012217 radiopharmaceutical Substances 0.000 claims 1
- 229940121896 radiopharmaceutical Drugs 0.000 claims 1
- 230000002799 radiopharmaceutical effect Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229960002317 succinimide Drugs 0.000 claims 1
- 229910052713 technetium Inorganic materials 0.000 claims 1
- 238000003745 diagnosis Methods 0.000 abstract 1
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 125000000565 sulfonamide group Chemical group 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
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Abstract
본 발명은 화학식 (Ⅰ) (여기에서 n,m,p,V1,V2,V3.V4,X1,X2,X3,R1,R2,R3및 R4는 상이한 의미를 갖는다)의, 술폰아미드기를 함유하는 신규의 킬레이트 형성체 및 이들의 금속성 킬레이트, 이들 화합물을 함유하는 약제, 이들의 X-선 진단법 및 치료에서의 용도, 이들 화합물 및 약제의 제조 방법, 및 질병 상태의 조직에서 그들 자신의 선택적으로 농축하는 물질, 특히 펩티드와 상기 화합물과의 콘쥬게이트에 관한 것이다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (12)
- 하기 화학식 (Ⅰ)의 화합물.상기 식에서 V1, V2, V3및 V4는 각각 독립적으로 카르보닐, 카르보닐, CH(COOH) 또는 -CH2기이고, X1은 수소원자이거나, 카르복실, 아미노 또는 티오시아네이트기에 의해 임의로 치환된 C1-12알킬 라디칼이거나, 또는 원자 번호 43, 45, 46, 75, 82 또는 83의 원소의 방사성 금속 이온의 금속 이온 등가물이고, X2, 및 X3은 각각 독립적으로 수소 원자 또는 상기 언급한 원자 번호의 원소의 방사성 금속 이온의 금속 이온 등가물이고, n, m 및 p는 수 0 또는 1이고, 여기에서 m+n은 1이고, R1은 수소 원자, 카르복실기 또는 기-U-Z이고, 여기에서 U는 직접 결합이거나, 직쇄 또는 분지된 포화 또는 불포화 C1-20알킬렌 라디칼이고, 이것은 말레이미드 라디칼, 숙신이미드 라디칼, 또는 1 내지 5개의 불소원자, 아미노 또는 니트로기, 1 또는 2종의 이미노, 페닐렌, 페닐렌옥시, 페닐렌아미노, 아미드, 히드라지드, 카르보닐, 우레이도, 티오우레이도, 티오아미드, 에스테르기(들), 1 내지 2종의 산소, 황 및(또는) 질소 원자(들) 및 임의로는 1 내지 5종의 히드록시, 메르캅토, 옥소, 티옥소, 카르복시, 알킬카르복실산, 에스테르, 티오시아네이트 및(또는) 아미노기에 의해 임의로 치환된 페닐 라디칼을 임의로 함유하고, Z는 수소 원자이거나, 아미노산, 펩티드, 폴리뉴클레오티드 또는 스테로이드의 라디칼이거나, 또는 아미노산, 펩티드, 폴리튜클레오티드 또는 스테로이드의 라디칼이 임의로 결합된 관능기이고, R2는 직쇄 또는 분지된 C1-10알킬 라디칼이고, 이것은 -COOH기, C7-12아르알킬 라디칼 또는 방향족 화합물을 임의로 함유하고, 염소 또는 브롬 원자, 티오시아네이트, 메틸, 에틸, 카르복식 및 (또는)메톡시기에 의해 임의로 치환되고, R4는 수소 원자 또는 카르복실기이거나, 또는 R1이 수소 원자 또는 카르복실기인 경우, 또한 기-U-Z이고, 여기에서 U 및 Z는 상기 언급한 의미를 갖고, R3은 수소 원자, 상기 언급한 원자 번호의 원소의 금속 이온 등가물, 트리풀루오로아세테이트, 아세테이트, 벤조에이트, C1-6아실, 벤조일, 히드록시아세틸, 아세트아미도메틸 라디칼이거나, 염소 또는 브롬 원자, 메틸, 에틸, 카르복실 및 (또는) 메톡시기에 의해 임의로 치환된 벤조산 라디칼, p-메톡시벤질 라디칼, 에톡시에틸 라디칼, SH 보호기,라디말이거나, 또는 X2및 X3수소이고 X1이 수소 원자 또는 임의로 치환된 C1-12알킬 라디칼인 경우, 화학식 (Ⅱ)의 라디칼이고, 여기에서, V1,V2,V3,V4,X1,X2,X3,n,m,p,R1,R2및 R4는 상기 언급한 의미를 갖고, 이에 의해 V1,V2,V3및 V4중 1개 이상 내지 2개 이하의 라디칼은 카르보닐기이다.
- 라디칼 X1,X2,X3또는 R3중 2개 이상의 원자 번호 43,45,46,75,82 또는 83의 방사성 금속 동위 원송의 금속 이온 등가물임을 특징으로 하는 화학식(Ⅰ)의 화합물.
- 제1항 또는 제2항에 있어서, Z가 아미노산 또는 펩티드인 화합물.
- 제1항 내지 제3항 중 어느 한 항에 있어서, Z가 폴리뉴클레오티드인 화합물.
- 제1항 내지 제4항 중 어느 한 항에 있어서, V1및 V4가 각각 카르보닐기이고, V2및 V3이 각각 -CH2기이고, p가 수 0인 화합물.
- 제1항 내지 제5항 중 어느 한 항에 있어서, 99m-테크네튬을 방사성 금속 이온으로서 함유한 화합물.
- 제1항 내지 제6항중 어느 한 항에 있어서, R4가 수소 또는 카르복실산기인 화합물.
- 제1항 내지 제7항 중 어느 한 항에 있어서, R2가 p-CH3-C6H4라디칼인 화합물.
- 제1항에 있어서, X1,X2및 X3이 수소 원자이고 R3이 화학식 (Ⅱ)의 라디칼인 화합물.
- 라디칼 X1,X2,X3및(또는) R3중 2개 이상이 금속 이온 등가물인 화학식(Ⅰ)의 금속 착물을 1개 이상 함유하는 약제.
- 제1항에 따른 금속 착물의 방사선 진단법 또는 방사선 요법에서의 용도.
- X2및 X3이 수소 원자이고 X1이 수소 또는 임의로 치환된 C1-12알킬 라디칼인 화학식 (Ⅰ)의 화합물 및 환원제를 생약에서 통상적으로 사용하는 첨가제를 첨가하면서 및 있어서, 임의로는 전이제 리간드를 첨가하면서 수성 매질 중에서 용해시키고, 목적하는 금속 이온의 금속 염 또는 금속 산화막과 반응시키고, 임의로는 약물학적 허용 가능한 방사선학적 부형제와 혼합하고, 과량의 착물화제를, 임의로는 그것의 알칼리 염의 형태로 첨가하는, 제10항에 따른 약제의 제조 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DEP4425781.3 | 1994-07-14 | ||
| DE4425781A DE4425781A1 (de) | 1994-07-14 | 1994-07-14 | Technetium-Sulfonamid-Komplexe, deren Verwendung, diese enthaltende pharmazeutische Mittel, sowie Verfahren zur Herstellung der Komplexe und Mittel |
| PCT/EP1995/002404 WO1996002500A1 (de) | 1994-07-14 | 1995-06-22 | Technetium-sulfonamid-komplexe, deren verwendung, diese enthaltende pharmazeutische mittel, sowie verfahren zur herstellung der komplexe und mittel |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR970704682A true KR970704682A (ko) | 1997-09-06 |
Family
ID=6523740
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019970700193A KR970704682A (ko) | 1994-07-14 | 1995-06-22 | 테크네튬-술폰아미드 착물, 이들의 용도, 이들을 함유하는 약제, 및 상기 착물 및 약제의 제조 방법(Technetium-Sulphonamide Complexes, Their Use, Pharmaceutical Agents Containing Them, and Process for Producing the Complexes and Agents) |
Country Status (11)
| Country | Link |
|---|---|
| EP (1) | EP0770063A1 (ko) |
| JP (1) | JPH10502648A (ko) |
| KR (1) | KR970704682A (ko) |
| CN (1) | CN1152914A (ko) |
| AU (1) | AU698824B2 (ko) |
| CA (1) | CA2194561A1 (ko) |
| DE (1) | DE4425781A1 (ko) |
| HU (1) | HUT76806A (ko) |
| NO (1) | NO970140L (ko) |
| WO (1) | WO1996002500A1 (ko) |
| ZA (1) | ZA955896B (ko) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100445971B1 (ko) * | 2002-04-15 | 2004-08-25 | 한국원자력연구소 | 수소화붕소 교환수지를 이용한 테크네튬 또는 레늄의표지방법 |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5028422A (en) * | 1986-05-27 | 1991-07-02 | Schering Corporation | Treatment of basal cell carcinoma intralesionally with recombinant human alpha interferon |
| AU7818801A (en) * | 2000-07-06 | 2002-01-21 | Array Biopharma Inc | Preparation of phosphatase inhibitors |
| CN100528241C (zh) * | 2002-05-06 | 2009-08-19 | 恩多塞特公司 | 维生素-定向的显象剂 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4980147A (en) * | 1984-06-25 | 1990-12-25 | University Of Utah Research Foundation | Radiolabeled technetium chelates for use in renal function determinations |
| DE3762624D1 (de) * | 1986-05-28 | 1990-06-13 | Mallinckrodt Inc | Technetiumchelate fuer die bestimmung der nierenfunktion. |
-
1994
- 1994-07-14 DE DE4425781A patent/DE4425781A1/de not_active Withdrawn
-
1995
- 1995-06-22 CA CA002194561A patent/CA2194561A1/en not_active Abandoned
- 1995-06-22 HU HU9700101A patent/HUT76806A/hu unknown
- 1995-06-22 WO PCT/EP1995/002404 patent/WO1996002500A1/de not_active Application Discontinuation
- 1995-06-22 JP JP8504625A patent/JPH10502648A/ja active Pending
- 1995-06-22 CN CN95194028A patent/CN1152914A/zh active Pending
- 1995-06-22 KR KR1019970700193A patent/KR970704682A/ko not_active Application Discontinuation
- 1995-06-22 AU AU28865/95A patent/AU698824B2/en not_active Ceased
- 1995-06-22 EP EP95924304A patent/EP0770063A1/de not_active Withdrawn
- 1995-07-14 ZA ZA955896A patent/ZA955896B/xx unknown
-
1997
- 1997-01-13 NO NO970140A patent/NO970140L/no unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100445971B1 (ko) * | 2002-04-15 | 2004-08-25 | 한국원자력연구소 | 수소화붕소 교환수지를 이용한 테크네튬 또는 레늄의표지방법 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1152914A (zh) | 1997-06-25 |
| CA2194561A1 (en) | 1996-02-01 |
| AU2886595A (en) | 1996-02-16 |
| NO970140L (no) | 1997-03-13 |
| EP0770063A1 (de) | 1997-05-02 |
| HUT76806A (en) | 1997-11-28 |
| ZA955896B (en) | 1996-02-19 |
| JPH10502648A (ja) | 1998-03-10 |
| WO1996002500A1 (de) | 1996-02-01 |
| NO970140D0 (no) | 1997-01-13 |
| AU698824B2 (en) | 1998-11-05 |
| DE4425781A1 (de) | 1996-01-18 |
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