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Compounds receptors ligands of gastrin and cholecystokinin (CCK), Pharmaceutical Composition and uses

机译:胃泌素和胆囊收缩素(CCK)的化合物受体配体,药物组合物和用途

摘要

1. Claim 1: use of a formula compound (1),Among them, R1 and R5 are independent h, C1-6 (C1-6 tar) oxy, uncle (C1-6 tar) uncle, anthrax, anthrax (C1-6 tar),1. Carbonate (C1-6 tar), carbon (C1-6 tar), oxygen carbonate (C1-6 tar), carbonate, nitric acid, trihalomethyl, hydroxy, hydroxy (C1-6 tar);1. Amino (C1-6 tar) amino, di (C1-6 tar) amine, amine, aminano, carbonilo, halo, halo (hydrocarbon 1-6),aminosulfonyl, (C1-6alkyl) sulfonylamino, (C1-6alkyl) aminocarbonyl, di (C1-6alkyl) aminocarbonyl, [NZ] - (C1-6alkyl) carbonylamino, formyloxy, formed, (C1-6alkyl) aminosulfonyl, di (C1-6 alkyl) aminosulfonyl, [NZ] - (C1-6 alkyl) sulfonylamino or cyano; or R1 and R5 together form a methylenedioxy group; R2 is an optionally substituted C1-18 hydrocarbyl group wherein up to three C atoms can optionally be replaced by N, O and / or S atoms; R3 is - (CR11R12) m-X- (CR13R14) p-R9; m is 0, 1 or 2; p is 0, 1 or 2; X is a bond, -CR15 = CR16-,-CSC...This is life. This is life.I am me, I am me.C (O) O, NHC (O) NH, NHC (O) O, OC (O) NH, NH, O, CO, SO2, SO2NH, C (O) NHNH, or is a residue selected from the group of formula ( two);R9 is No. h, C1-6 tar; or phenyl, nafilo, pyridilol, benzimidazolello, indazollo, quinol Nile, isoginolinello, tetrahydroisomer benzene, indolillo, isoindia Lillo or 2-pyridonia, all of which are independently selected from: - L-Q by groups 1, 2, or 3, of which l is the contact person, Or a set of formulas - (cr17r18) v-y-cr17r18) W, where V and W are independent of 0, 1, 2 or 3, e is a link, - Cr15 = cr16 -.thiazolyl, imidazolyl, oxazolyl, isoxazolyl, pyrazolyl, isoxazolonyl, piperazinyl, piperidinyl, morpholinyl, or pyrrolidinyl; and Q is H; (C1-6alkyl) oxy, [NZ] - (C1-6alkyl) oxy (C1-6alkyl) amino, thio, (C1-6alkyl) thio, carboxy (C1-6alkyl) thio, carboxy, carboxy ( C1-6alkyl),carboxi (alquenilo C1-6)Carcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcar8 [N-Z] (C1-6 tar) carbonate (tar 1-6 amine, halo, halo (C1-6 tar),sulfamoyl, [NZ] (C1-6 alkyl) sulfonylamino, (C1-6 alkyl) sulfonylaminocarbonyl, carboxy (C1-6 alkyl) sulfonyl, carboxy (C1-6 alkyl) sulfinyl, tetrazolyl, [NZ] tetrazolylamino, cyano, amidino, amidinothio , SO3H, formyloxy, formamido, C3-8 cycloalkyl, (C1-6 alkyl) -sulfamoyl, di (C1-6 alkyl) sulfamoyl, (C1-6 alkyl) -carbonylaminosulfonyl or 5-oxo-2,5-dihydro- [ 1,2,4] oxadiazolyl; Z is H, C1-6 alkyl, t-butoxycarbonyl, acetyl, benzoyl, or benzyl; R4 is an optionally substituted C1-18 hydrocarbyl group wherein up to three C atoms can optionally be replaced by N, O and / or S atoms; and R11, R12, R13, R14, R15, R16,R17 and R18 are independent h or c1-3 bitumens or their pharmaceutically acceptable salts that can be used in the treatment of gastrointestinal diseases. Claim 18: an ingredient in accordance with claim 16 or 17, with a proton pump inhibitor and a formula compound (1) each accounting for one quantity, has a beneficial therapeutic effect on patients with gastrointestinal diseases.
机译:1.权利要求1:式化合物(1)的用途,其中,R 1和R 5独立为h,C 1-6(C 1-6焦油)氧基,叔叔(C 1-6焦油)叔叔,炭疽,炭疽(C 1- 6焦油),1。碳酸盐(C1-6焦油),碳(C1-6焦油),碳酸氧(C1-6焦油),碳酸盐,硝酸,三卤甲基,羟基,羟基(C1-6焦油); 1。氨基(C1-6焦油)氨基,二(C1-6焦油)胺,胺,氨基,羰基,卤素,卤代(烃1-6),氨基磺酰基,(C1-6烷基)磺酰基氨基,(C1-6烷基)氨基羰基,二(C1-6烷基)氨基羰基,[NZ]-(C1-6烷基)羰基氨基,甲氧基,已形成的(C1-6烷基)氨基磺酰基,二(C1-6烷基)氨基磺酰基,[NZ]-(C1-6烷基)磺酰基氨基或氰基; R1和R5一起形成亚甲二氧基;或R 2是任选取代的C 1-18烃基,其中最多三个C原子可任选被N,O和/或S原子取代; R3是-(CR11R12)m-X-(CR13R14)p-R9; m为0、1或2; p是0、1或2; X是一个键,-CR15 = CR16-,-CSC ...这就是生命。这就是生活。我是我,我是我C(O)O,NHC(O)NH,NHC(O)O,OC(O)NH,NH,O,CO,SO2,SO2NH,C(O)或为选自式(2)的基团的残基; R 9为h,C 1-6焦油;或苯基,萘菲洛,吡咯洛尔,苯并咪唑,吲唑洛,喹诺尔尼罗,异喹啉基,四氢异构体苯,吲哚洛,异印度利略或2-吡啶酮,它们全部独立地选自:-LQ有1、2或3组,其中l是联系人,或者是一组公式-(cr17r18)vy-cr17r18)W,其中V和W独立于0、1、2或3,e是一个链接,-Cr15 = cr16 -.thiazolyl,咪唑基,恶唑基,异恶唑基,吡唑基,异恶唑酮基,哌嗪基,哌啶基,吗啉基或吡咯烷基; Q是H; (C 1-6烷基)氧基,[NZ]-(C 1-6烷基)氧基,(C 1-6烷基)氨基,硫基,(C 1-6烷基)硫基,羧基(C 1-6烷基)硫基,羧基,羧基(C 1-6烷基), carboxi(alquenilo C1-6)Carcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcarcar8 [NZ](C1-6 tar)carbonate(tar 1-6 amine,halo,halo(C1-6 alkon,Culfyl(C1-6 tar)s, -6烷基)磺酰基氨基羰基,羧基(C1-6烷基)磺酰基,羧基(C1-6烷基)亚磺酰基,四唑基,[NZ]四唑基氨基,氰基,a基,a基硫代,SO3H,甲酰氧基,甲酰胺基,C3-8环烷基,(C1 -6烷基)-氨磺酰基,二(C1-6烷基)氨磺酰基,(C1-6烷基)-羰基氨基磺酰基或5-氧代-2,5-二氢-[1,2,4]恶二唑基; Z为H,C1- 6个烷基,叔丁氧羰基,乙酰基,苯甲酰基或苄基; R4为任选取代的C1-18烃基,其中至多三个C原子可任选被N,O和/或S原子取代;和R11,R12,R13 , R14,R15,R16,R17和R18是独立的h或c1-3沥青或其药学上可接受的盐,可用于治疗胃肠道疾病。权利要求18:根据权利要求16或17的成分,其中质子泵抑制剂和式化合物(1)各自占一个量,对胃肠道疾病患者具有有益的治疗作用。

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