Heterocyclic thrombin inhibitors
Patent 5583146 Issued on December 10, 1996. Estimated Expiration Date: 
January 17, 2015. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
January 17, 2015. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.Patent References hydroxy tripeptide substrates N2 -Arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof Novel peptidyl-arginine aldehyde derivatives and process for the preparation thereof Novel anticoagulant agmatine derivatives and process for the preparation thereof Phenol derivatives S-nitrosocaptopril compounds and the use thereof Tripeptide derivatives and protease inhibitor composition comprising the same Peptide aldehydes as antithrombotic agents Patent #: 5380713 InventorsAssigneeApplicationNo. 373334 filed on 01/17/1995US Classes:514/326, The additional ring is a hetero ring514/19, 2 peptide repeating units in known peptide chain514/183, Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI514/200, 1-thia-5-aza-bicyclo (4.2.0) octane ring containing (including dehydrogenated) (e.g., cephalosporins, etc.)514/210.18, Additional hetero ring attached directly or indirectly to the four-membered hetero ring by nonionic bonding514/217.04, The additional hetero ring is six-membered and contains nitrogen514/217.06, The additional hetero ring is a 1,3 diazine (including hydrogenated)514/217.07, Polycyclo ring system having the additional six-membered hetero ring as one of the cyclos514/217.08, The additional hetero ring is five-membered and contains nitrogen514/231.5, Additional hetero ring attached directly or indirectly to the morpholine ring by nonionic bonding514/233.8, Plural ring hetero atoms in the bicyclo ring system514/234.5, Plural ring nitrogens in the bicyclo ring system514/235.2, Ring nitrogen in the bicyclo ring system514/235.5, Ring nitrogen in the additional hetero ring514/235.8, Plural ring nitrogens in the additional hetero ring (e.g., imidazole, pyrazine, etc.)514/236.8, Ring chalcogen in the additional hetero ring (e.g., oxazole, etc.)514/237.2, The additional hetero ring is attached indirectly to the morpholine ring by an acyclic chain having a hetero atom as a chain member514/252.03, The additional hetero ring is six-membered consisting of one nitrogen and five carbon atoms514/252.05, The additional hetero ring is a five-membered nitrogen hetero ring514/255.05, Additional hetero ring attached directly or indirectly to the 1,4-diazine ring by nonionic bonding514/256, 1,3-diazines (e.g., pyrimidines, etc.)514/263.22, The additional hetero ring is six-membered consisting of one nitrogen and five carbons514/303, Exactly three ring nitrogens in the bicyclo ring system514/314, Additional hetero ring attached directly or indirectly to the quinoline ring system by nonionic bonding514/316, Plural piperidine rings514/318, The additional ring is a six-membered hetero ring consisting of one nitrogen and five carbon atoms514/319, The additional ring is one of the cyclos in a polycyclo ring system514/321, Plural hetero atoms in the polycyclo ring system540/200, Hetero ring is four-membered containing nitrogen and having chalcogen double bonded directly to a ring carbon which is adjacent to the ring nitrogen540/354, Additional chalcogen bonded directly to the hetero ring540/480, Additional hetero ring attached directly or indirectly to the hetero ring by nonionic bonding540/483, Plural nitrogens attached indirectly to the hetero ring by acyclic nonionic bonding540/544, The hetero ring contains chalcogen540/553, The hetero ring contains plural nitrogens (e.g., 1,3-diazepines, etc.)540/597, The additional hetero ring is six-membered and contains nitrogen540/600, The additional hetero ring is 1,3-diazine (including hydrogenated)540/603, Plural hetero atoms in the additional hetero ring544/124, Six-membered ring consisting of one nitrogen and five carbons (e.g., pyridine, etc.)544/127, The additional six-membered hetero ring is one of the cyclos in a bicyclo ring system544/128, Quinoline or isoquinoline (including hydrogenated)544/129, Piperidine ring544/130, Double bonded divalent chalcogen containing544/133, The five-membered hetero ring has at least sulfur and nitrogen as ring hetero atoms544/135, Benzothiazoles (including hydrogenated)544/137, The five-membered hetero ring has at least oxygen and nitrogen as ring hetero atoms544/139, 1,3-Diazole ring (including hydrogenated)544/141, Five-membered hetero ring consisting of one nitrogen and four carbons544/238, 1,2-diazines which contain an additional hetero ring544/242, 1,3-diazines544/277, Nitrogen attached directly or indirectly to the purine ring system by nonionic bonding544/283, The other cyclo in the bicyclo ring system is a benzene ring (e.g., quinazoline, etc.)544/336, 1,4-diazines546/118, Three ring nitrogens in the bicyclo ring system546/152, Quinolines (including hydrogenated)546/190, Having -C(=X)-, wherein X is chalcogen, attached indirectly to a piperdine ring by nonionic bonding546/193, Pyridine ring or partially hydrogenated pyridine ring546/198, Ring nitrogen in the polycyclo ring system546/208, Ring nitrogen in the additional hetero ring546/209, Ring sulfur or ring oxygen in the additional hetero ring546/210, Plural ring nitrogens in the additional hetero ring546/211, 1,2-diazole (including hydrogenated)546/212, The additional hetero ring consists of one sulfur and four carbons546/214The additional hetero ring consists of one oxygen and four carbonsExaminersPrimary: Chang, CeilaAttorney, Agent or FirmForeign Patent References
International ClassesA61K 031/445A61K 031/40 C07D 401/12 C07D 207/09 C07D 211/ 28.09 AbstractHeterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R1, R2, R3, G, Gx, R6', Ra, Xa, R6, Rb, R3, p, Q, A and R4 are as defined herein.Other References
Field of SearchHetero ring is four-membered containing nitrogen and having chalcogen double bonded directly to a ring carbon which is adjacent to the ring nitrogenAdditional chalcogen bonded directly to the hetero ring Additional hetero ring attached directly or indirectly to the hetero ring by nonionic bonding Plural nitrogens attached indirectly to the hetero ring by acyclic nonionic bonding The hetero ring contains chalcogen The hetero ring contains plural nitrogens (e.g., 1,3-diazepines, etc.) The additional hetero ring is six-membered and contains nitrogen The additional hetero ring is 1,3-diazine (including hydrogenated) Plural hetero atoms in the additional hetero ring Six-membered ring consisting of one nitrogen and five carbons (e.g., pyridine, etc.) The additional six-membered hetero ring is one of the cyclos in a bicyclo ring system Quinoline or isoquinoline (including hydrogenated) Piperidine ring Double bonded divalent chalcogen containing The five-membered hetero ring has at least sulfur and nitrogen as ring hetero atoms Benzothiazoles (including hydrogenated) The five-membered hetero ring has at least oxygen and nitrogen as ring hetero atoms 1,3-Diazole ring (including hydrogenated) Five-membered hetero ring consisting of one nitrogen and four carbons 1,2-diazines which contain an additional hetero ring 1,3-diazines Nitrogen attached directly or indirectly to the purine ring system by nonionic bonding The other cyclo in the bicyclo ring system is a benzene ring (e.g., quinazoline, etc.) 1,4-diazines Three ring nitrogens in the bicyclo ring system Quinolines (including hydrogenated) Having -C(=X)-, wherein X is chalcogen, attached indirectly to a piperdine ring by nonionic bonding Pyridine ring or partially hydrogenated pyridine ring Ring nitrogen in the polycyclo ring system Ring nitrogen in the additional hetero ring Ring sulfur or ring oxygen in the additional hetero ring Plural ring nitrogens in the additional hetero ring 1,2-diazole (including hydrogenated) The additional hetero ring consists of one sulfur and four carbons The additional hetero ring consists of one oxygen and four carbons Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI 1-thia-5-aza-bicyclo (4.2.0) octane ring containing (including dehydrogenated) (e.g., cephalosporins, etc.) Additional hetero ring attached directly or indirectly to the morpholine ring by nonionic bonding Plural ring hetero atoms in the bicyclo ring system Plural ring nitrogens in the bicyclo ring system Ring nitrogen in the bicyclo ring system Ring nitrogen in the additional hetero ring Plural ring nitrogens in the additional hetero ring (e.g., imidazole, pyrazine, etc.) Ring chalcogen in the additional hetero ring (e.g., oxazole, etc.) The additional hetero ring is attached indirectly to the morpholine ring by an acyclic chain having a hetero atom as a chain member 1,3-diazines (e.g., pyrimidines, etc.) |
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