CAS: 102146-07-6; 8-Cyclopentyl-1,3-Dipropyl-1H-Purine-2,6(3H,7H)-Dione

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📜环戊甲酰胺,N-(6-氨基-1,2,3,4-四氢-2,4-二羰基-1,3-二丙基-5-嘧啶基)-置于sodium Hydroxide体系中,用 水 用作溶剂,化学反应 1.0H,反应生成8-环戊烷基-1,3-二丙基黄嘌呤
参考文献:1,3,8-三取代的黄嘌呤.取代模式对腺苷受体a1 / A2亲和力的影响.
标题:1,3,8-三取代的黄嘌呤.取代模式对腺苷受体a1 / A2亲和力的影响.
摘要:一系列11个8-取代的黄嘌呤,在1和3位上具有三个不同的取代模式(模式a(r1 = R3 = Ch2Ch2Ch3),B(r1 = Ch2Ch2Ch3,R3 = Ch3)和c(r1 = Ch3,制备r 3 = Ch 2 Ch 2 Ch 3)].评估这些化合物与腺苷a1和a2受体结合的亲和力和选择性.在a1受体上具有最大亲和力的化合物具有1,3取代模式a.除了一个例外,具有模式a的化合物在a2受体上的结合力也最强.但是,几种具有模式c的化合物在a2受体上与那些具有模式a的化合物等价.此外,这些8取代的黄嘌呤的1和3位上的取代基对于确定与a1受体的最大亲和力同样重要,而3位的取代基比1位的取代基对a2受体的效力更重要.结果,可以通过选择1-位和3-位取代基来最大化对a1受体的选择性.然而,以最大的a1选择性所需要的r1 / R3取代模式也以不完全理解的方式取决于8位的取代基.
Doi:10.1021/jm00108A029

专利信息

专利号:WO-9614060-A1
优先权日:1994-11-04
标题 :Use of receptor agonists to stimulate superoxide dismutase activity
发明人：MARKLUND STEFAN L; STRAALIN PONTUS
权利人:MARKLUND STEFAN L; STRAALIN PONTUS
摘要:The present invention relates to the use of a substance for the manufacture of a composition for stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells. In particular, the invention relates to the use of a substance for the manufacture of a composition for prophylaxis or treatment of a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical. Further, the invention relates to a method for determining the effect of a substance with respect to stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells and to substances which have been selected by said method. Within the scope of the invention is a method of preventing, diminishing, controlling or inhibiting a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical in a patient who has been established to have a high risk of developing a such disease or disorder, or who has developed a such disease or disorder, the method comprising administering an effective amount of a substance which is capable of stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells.

专利号:US-8501941-B2
优先权日:2005-02-25
标题 :Methods for the synthesis of unsymmetrical cycloakyl substituted xanthines
发明人：WANG GUOQUAN; RIEGER JAYSON M; THOMPSON ROBERT D
权利人:WANG GUOQUAN; RIEGER JAYSON M; THOMPSON ROBERT D; DOGWOOD PHARMACEUTICALS INC
摘要:The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A 2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents. Also provided are processes for the preparation of the compounds and their intermediates.

专利号:US-2007105821-A1
优先权日:2005-02-25
标 题 :Methods for the synthesis of unsymmetrical cycloalkyl substituted xanthines

专利号:US-2023271983-A1
优先权日:2020-07-29
标题 :Functionalized isonitriles and products, preparation and uses thereof
发明人：SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA
权利人:UNIV SANTIAGO COMPOSTELA
摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.

专利号:US-7645754-B2
优先权日:2001-12-20
标题 :Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use
发明人：CASTELHANO ARLINDO; MCKIBBEN BRYAN; STEINIG ARNO
权利人:OSI PHARM INC
摘要:The subject invention provides compounds having the structure: n n n n n n n n n n n n wherein,n R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O) R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH 2 ) 2 OH or —CH 2 C(â•?O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxy, or —NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is —(CH 2 ) m OR 6 , —CHNOR 7 , —C(â•?O)NR 8 R 9 , —(CH 2 ) m C(â•?O)OR 10 , —(CH 2 ) k C(â•?O)NR 11 R 12 ;n wherein R 6 is a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R 7 is hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl; R 8 and R 9 are each independently hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl, (C 1 -C 30 )alkylamino, (C 1 -C 30 )alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R 8 , N, and R 9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R 10 is hydrogen or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R 11 , N and R 12 together form a 4-8 membered heterocyclic ring; R a and R b are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3,n nor a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A 2b adenosine receptor in a sbject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.

专利号:US-2012226040-A1
优先权日:2005-02-25
标题 :Methods for the synthesis of unsymmetrical cycloakyl substituted xanthines