JO1734B1 - New isosteric peptides - Google Patents
New isosteric peptidesInfo
- Publication number
- JO1734B1 JO1734B1 JO19931734A JOP19931734A JO1734B1 JO 1734 B1 JO1734 B1 JO 1734B1 JO 19931734 A JO19931734 A JO 19931734A JO P19931734 A JOP19931734 A JO P19931734A JO 1734 B1 JO1734 B1 JO 1734B1
- Authority
- JO
- Jordan
- Prior art keywords
- phenyl
- group
- methyl
- carbon atoms
- straight
- Prior art date
Links
- 102000004196 processed proteins & peptides Human genes 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- -1 5-(1H)-tetrazolyl Chemical group 0.000 abstract 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 abstract 1
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 abstract 1
- 239000005977 Ethylene Substances 0.000 abstract 1
- 229910006069 SO3H Inorganic materials 0.000 abstract 1
- 108090000190 Thrombin Proteins 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 239000003146 anticoagulant agent Substances 0.000 abstract 1
- 229940127219 anticoagulant drug Drugs 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 150000001732 carboxylic acid derivatives Chemical group 0.000 abstract 1
- 230000002860 competitive effect Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 abstract 1
- 230000003278 mimic effect Effects 0.000 abstract 1
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 abstract 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 229960004072 thrombin Drugs 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Landscapes
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Abstract of corresponding document: EP 0530167 (A1) The invention relates to new competitive inhibitors of thrombin, their synthesis, pharmaceutical compositions containing the compounds as active ingredients, and the use of the compounds as anticoagulants for prophylaxis and treatment of thromboembolic diseases, according to the formula <CHEM> wherein: A represents -CH2-, -CH=CH-, -CH2-CH2- or -CH2-CH2-CH2- ; R<1> and R<2> are the same or different and each represents H or X-B-, where B is a straight or branched alkylene group having 1-3 carbon atoms and X is H, methyl, ethyl, a cycloalkyl group having 3-6 carbon atoms or R min CO-, where R min is OH, a straight or branched alkoxy group having 1-4 carbon atoms, NH2 or NHR sec , where R sec is a straight or branched alkyl group having 1-4 carbon atoms, or X is a carboxylic acid mimic, known per se, selected from -PO(OR sec min )2, -SO3H and 5-(1H)-tetrazolyl, and R sec min is H, methyl or ethyl, or B is -SO2- and X is methyl or ethyl; m is 0, 1 or 2, R<3> represents a cyclohexyl group and R<3A> represents H: or m is 1 and R<3> represents a cyclohexyl or phenyl group and R<3A> forms an ethylene bridge together with R<1> ; Y represents O or S(O)p, where p is 0, 1 or 2; R<4> represents H; a straight or branched alkyl or a cycloalkyl having 1 to 6 carbon atoms unsubstituted or substituted with one or more fluoro atoms and/or substituted with a phenyl group: a substituted or unsubstituted aromatic ring selected from phenyl, 4-methoxy-phenyl, 4-tertiary-butyl-phenyl, 4-methyl-phenyl, 2-, 3- or 4-trifluoro-methyl-phenyl, phenyl substituted with 1-5 fluoro atoms: or -CH(CF3)-phenyl, either as such or in the form of a physiologically acceptable salt and including stereoisomers.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JO19931734A JO1734B1 (en) | 1993-02-18 | 1993-02-18 | New isosteric peptides |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JO19931734A JO1734B1 (en) | 1993-02-18 | 1993-02-18 | New isosteric peptides |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JO1734B1 true JO1734B1 (en) | 1993-06-15 |
Family
ID=48092582
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JO19931734A JO1734B1 (en) | 1993-02-18 | 1993-02-18 | New isosteric peptides |
Country Status (1)
| Country | Link |
|---|---|
| JO (1) | JO1734B1 (en) |
-
1993
- 1993-02-18 JO JO19931734A patent/JO1734B1/en active
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