US2010093785A1PendingUtilityA1

Diamine derivatives

Assignee: DAIICHI SEIYAKU COPriority: Jun 20, 2001Filed: Dec 30, 2008Published: Apr 15, 2010
Est. expiryJun 20, 2021(expired)· nominal 20-yr term from priority
A61P 7/00A61P 9/00A61P 7/02A61P 9/10A61P 43/00A61P 29/00C07D 401/14C07D 417/12C07D 487/04A61K 31/429C07D 209/42A61K 31/4439C07D 498/04A61K 31/444C07D 401/12A61K 31/4365A61K 31/428C07K 5/0827C07K 5/06191A61K 31/454A61K 31/437C07D 417/14C07D 495/04A61K 31/4545C07D 513/04C07D 513/14
66
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Claims

Abstract

A compound represented by the general formula (1): -Q 1 -Q 2 -T 0 -N(R 1 )-Q 3 -(R 2 )T 1 Q 4   (1) wherein R 1 and R 2 are hydrogen atoms or the like; Q 1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q 2 is a single bond or the like; Q 3 is a group in which Q 5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T 0 and T 1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

Claims

exact text as granted — not AI-modified
1 - 59 . (canceled) 
     
     
         60 . A method for treating thrombosis or embolism, the method comprising administering to a patient in need thereof an effective amount of N 1 -(5-chloropyridin-2-yl)-N 2 -(4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide, represented by Formula (I), or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         61 . A method for treating thrombosis or embolism, the method comprising administering to a patient in need thereof an effective amount of N 1 -(5-chloropyridin-2-yl)-N 2 -(4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate, represented by Formula (II): 
       
         
           
           
               
               
           
         
       
     
     
         62 . A method for treating thrombosis or embolism, the method comprising administering to a patient in need thereof an effective amount of N 1 -(5-chloropyridin-2-yl)-N 2 -(4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate monohydrate, represented by Formula (III): 
       
         
           
           
               
               
           
         
       
     
     
         63 . A method for treating thrombosis or embolism, the method comprising administering to a patient in need thereof an effective amount of N 1 -(5-chloropyridin-2-yl)-N 2 -((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide, represented by Formula (IV), or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         64 . A method for treating thrombosis or embolism, the method comprising administering to a patient in need thereof an effective amount of N 1 -(5-chloropyridin-2-yl)-N 2 -((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate, represented by Formula (V): 
       
         
           
           
               
               
           
         
       
     
     
         65 . A method for treating thrombosis or embolism, the method comprising administering to a patient in need thereof an effective amount of N 1 -(5-chloropyridin-2-yl)-N 2 -((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate monohydrate, represented by Formula (VI): 
       
         
           
           
               
               
           
         
       
     
     
         66 . A method for treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary embolism, deep venous thrombosis, thrombus formation after valve or joint replacement, or thrombus formation and reocclusion after angioplasty, the method comprising administering to a patient in need thereof an effect amount of N 1 -(5-chloropyridin-2-yl)-N 2 -(4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide, represented by Formula (I), or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         67 . A method for treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary embolism, deep venous thrombosis, thrombus formation after valve or joint replacement, or thrombus formation and reocclusion after angioplasty, the method comprising administering to a patient in need thereof an effect amount of N 1 -(5-chloropyridin-2-yl)-N 2 -(4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate, represented by Formula (II): 
       
         
           
           
               
               
           
         
       
     
     
         68 . A method for treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary embolism, deep venous thrombosis, thrombus formation after valve or joint replacement, or thrombus formation and reocclusion after angioplasty, the method comprising administering to a patient in need thereof an effect amount of N 1 -(5-chloropyridin-2-yl)-N 2 -(4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate monohydrate, represented by Formula (III): 
       
         
           
           
               
               
           
         
       
     
     
         69 . A method for treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary embolism, deep venous thrombosis, thrombus formation after valve or joint replacement, or thrombus formation and reocclusion after angioplasty, the method comprising administering to a patient in need thereof an effect amount of N 1 -(5-chloropyridin-2-yl)-N 2 -((1 S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide, represented by Formula (IV), or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         70 . A method for treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary embolism, deep venous thrombosis, thrombus formation after valve or joint replacement, or thrombus formation and reocclusion after angioplasty, the method comprising administering to a patient in need thereof an effect amount of N 1 -(5-chloropyridin-2-yl)-N 2 -((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate, represented by Formula (V): 
       
         
           
           
               
               
           
         
       
     
     
         71 . A method for treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary embolism, deep venous thrombosis, thrombus formation after valve or joint replacement, or thrombus formation and reocclusion after angioplasty, the method comprising administering to a patient in need thereof an effect amount of N 1 -(5-chloropyridin-2-yl)-N 2 -((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate monohydrate, represented by Formula (VI):

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