CN107875387A - 一种含有吡咯磺酰类衍生物的复方药物及其用途 - Google Patents
一种含有吡咯磺酰类衍生物的复方药物及其用途 Download PDFInfo
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- CN107875387A CN107875387A CN201610863035.7A CN201610863035A CN107875387A CN 107875387 A CN107875387 A CN 107875387A CN 201610863035 A CN201610863035 A CN 201610863035A CN 107875387 A CN107875387 A CN 107875387A
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- alkyl
- aryl
- compound medicine
- heterocyclylalkyl
- heteroaryl
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- 239000003814 drug Substances 0.000 title claims abstract description 31
- 150000001875 compounds Chemical class 0.000 title claims abstract description 29
- KAESVJOAVNADME-UHFFFAOYSA-N 1H-pyrrole Natural products C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title abstract description 5
- 239000003120 macrolide antibiotic agent Substances 0.000 claims abstract description 7
- 239000003782 beta lactam antibiotic agent Substances 0.000 claims abstract description 6
- 239000002132 β-lactam antibiotic Substances 0.000 claims abstract description 6
- 229940124586 β-lactam antibiotics Drugs 0.000 claims abstract description 6
- 125000000217 alkyl group Chemical group 0.000 claims description 22
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical class O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 claims description 20
- 125000003118 aryl group Chemical group 0.000 claims description 19
- 150000003233 pyrroles Chemical class 0.000 claims description 19
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- 241000590002 Helicobacter pylori Species 0.000 claims description 16
- LSQZJLSUYDQPKJ-NJBDSQKTSA-N amoxicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=C(O)C=C1 LSQZJLSUYDQPKJ-NJBDSQKTSA-N 0.000 claims description 14
- 229960003022 amoxicillin Drugs 0.000 claims description 14
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 14
- LSQZJLSUYDQPKJ-UHFFFAOYSA-N p-Hydroxyampicillin Natural products O=C1N2C(C(O)=O)C(C)(C)SC2C1NC(=O)C(N)C1=CC=C(O)C=C1 LSQZJLSUYDQPKJ-UHFFFAOYSA-N 0.000 claims description 14
- 125000001072 heteroaryl group Chemical group 0.000 claims description 13
- -1 nitro, hydroxyl Chemical group 0.000 claims description 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 12
- 229910052736 halogen Inorganic materials 0.000 claims description 12
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 239000001257 hydrogen Substances 0.000 claims description 12
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 11
- 239000000612 proton pump inhibitor Substances 0.000 claims description 9
- 208000007107 Stomach Ulcer Diseases 0.000 claims description 6
- 201000005917 gastric ulcer Diseases 0.000 claims description 6
- 125000001188 haloalkyl group Chemical group 0.000 claims description 6
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- 102100021904 Potassium-transporting ATPase alpha chain 1 Human genes 0.000 claims description 5
- 108010083204 Proton Pumps Proteins 0.000 claims description 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 5
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- 125000004185 ester group Chemical group 0.000 claims description 4
- 230000002147 killing effect Effects 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 3
- 125000003368 amide group Chemical group 0.000 claims description 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 3
- 125000003262 carboxylic acid ester group Chemical group [H]C([H])([*:2])OC(=O)C([H])([H])[*:1] 0.000 claims description 3
- 239000003795 chemical substances by application Substances 0.000 claims description 3
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 3
- WDLWHQDACQUCJR-ZAMMOSSLSA-N (6r,7r)-7-[[(2r)-2-azaniumyl-2-(4-hydroxyphenyl)acetyl]amino]-8-oxo-3-[(e)-prop-1-enyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)/C=C/C)C(O)=O)=CC=C(O)C=C1 WDLWHQDACQUCJR-ZAMMOSSLSA-N 0.000 claims description 2
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- KEJCWVGMRLCZQQ-YJBYXUATSA-N Cefuroxime axetil Chemical compound N([C@@H]1C(N2C(=C(COC(N)=O)CS[C@@H]21)C(=O)OC(C)OC(C)=O)=O)C(=O)\C(=N/OC)C1=CC=CO1 KEJCWVGMRLCZQQ-YJBYXUATSA-N 0.000 claims description 2
- UIOFUWFRIANQPC-JKIFEVAISA-N Floxacillin Chemical compound N([C@@H]1C(N2[C@H](C(C)(C)S[C@@H]21)C(O)=O)=O)C(=O)C1=C(C)ON=C1C1=C(F)C=CC=C1Cl UIOFUWFRIANQPC-JKIFEVAISA-N 0.000 claims description 2
- VYWWNRMSAPEJLS-MDWYKHENSA-N Rokitamycin Chemical compound C1[C@](OC(=O)CC)(C)[C@@H](OC(=O)CCC)[C@H](C)O[C@H]1O[C@H]1[C@H](N(C)C)[C@@H](O)[C@H](O[C@@H]2[C@H]([C@H](O)CC(=O)O[C@H](C)C/C=C/C=C/[C@H](O)[C@H](C)C[C@@H]2CC=O)OC)O[C@@H]1C VYWWNRMSAPEJLS-MDWYKHENSA-N 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
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- NBFNMSULHIODTC-CYJZLJNKSA-N cefadroxil monohydrate Chemical compound O.C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C)C(O)=O)=CC=C(O)C=C1 NBFNMSULHIODTC-CYJZLJNKSA-N 0.000 claims description 2
- AFZFFLVORLEPPO-UVYJNCLZSA-N cefditoren pivoxil Chemical compound S([C@@H]1[C@@H](C(N1C=1C(=O)OCOC(=O)C(C)(C)C)=O)NC(=O)\C(=N/OC)C=2N=C(N)SC=2)CC=1\C=C/C=1SC=NC=1C AFZFFLVORLEPPO-UVYJNCLZSA-N 0.000 claims description 2
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- OKBVVJOGVLARMR-QSWIMTSFSA-N cefixime Chemical compound S1C(N)=NC(C(=N\OCC(O)=O)\C(=O)N[C@@H]2C(N3C(=C(C=C)CS[C@@H]32)C(O)=O)=O)=C1 OKBVVJOGVLARMR-QSWIMTSFSA-N 0.000 claims description 2
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- RDLPVSKMFDYCOR-UEKVPHQBSA-N cephradine Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C)C(O)=O)=CCC=CC1 RDLPVSKMFDYCOR-UEKVPHQBSA-N 0.000 claims description 2
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- LQOLIRLGBULYKD-JKIFEVAISA-N cloxacillin Chemical compound N([C@@H]1C(N2[C@H](C(C)(C)S[C@@H]21)C(O)=O)=O)C(=O)C1=C(C)ON=C1C1=CC=CC=C1Cl LQOLIRLGBULYKD-JKIFEVAISA-N 0.000 claims description 2
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- 229960004273 floxacillin Drugs 0.000 claims description 2
- QRSPJBLLJXVPDD-XFAPPKAWSA-M hetacillin potassium Chemical compound [K+].C1([C@@H]2C(=O)N(C(N2)(C)C)[C@H]2[C@H]3SC([C@@H](N3C2=O)C([O-])=O)(C)C)=CC=CC=C1 QRSPJBLLJXVPDD-XFAPPKAWSA-M 0.000 claims description 2
- 229960002041 hetacillin potassium Drugs 0.000 claims description 2
- 229950007634 kitasamycin Drugs 0.000 claims description 2
- XYJOGTQLTFNMQG-KJHBSLKPSA-N leucomycin V Chemical compound CO[C@H]1[C@H](O)CC(=O)O[C@H](C)C\C=C\C=C\[C@H](O)[C@H](C)C[C@H](CC=O)[C@@H]1O[C@H]1[C@H](O)[C@@H](N(C)C)[C@H](O[C@@H]2O[C@@H](C)[C@H](O)[C@](C)(O)C2)[C@@H](C)O1 XYJOGTQLTFNMQG-KJHBSLKPSA-N 0.000 claims description 2
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- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 2
- HCTVWSOKIJULET-LQDWTQKMSA-M phenoxymethylpenicillin potassium Chemical compound [K+].N([C@H]1[C@H]2SC([C@@H](N2C1=O)C([O-])=O)(C)C)C(=O)COC1=CC=CC=C1 HCTVWSOKIJULET-LQDWTQKMSA-M 0.000 claims description 2
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- SUBDBMMJDZJVOS-UHFFFAOYSA-N 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole Chemical compound N=1C2=CC(OC)=CC=C2NC=1S(=O)CC1=NC=C(C)C(OC)=C1C SUBDBMMJDZJVOS-UHFFFAOYSA-N 0.000 description 5
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- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- FCPVYOBCFFNJFS-LQDWTQKMSA-M benzylpenicillin sodium Chemical compound [Na+].N([C@H]1[C@H]2SC([C@@H](N2C1=O)C([O-])=O)(C)C)C(=O)CC1=CC=CC=C1 FCPVYOBCFFNJFS-LQDWTQKMSA-M 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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Abstract
本发明提供一种含有吡咯磺酰类衍生物的复方药物及其在医药中的用途，复方药物包含吡咯磺酰类衍生物，β‑内酰胺类抗生素和大环内酯类抗生素。该复方药物能更有效地抑制或杀灭幽门螺旋杆菌，可用于治疗十二指肠溃疡、胃溃疡和/或慢性胃炎。
Description
技术领域
本发明涉及一种用于抑制或杀灭幽门螺旋杆菌的复方药物，具体涉及一种包含吡咯磺酰类衍生物的复方药物及其用途。
背景技术
胃幽门螺旋杆菌，又名幽门螺杆菌 (Helicobacter pylori,H.pylori)，是一种革兰阴性，S性或弧形弯曲的专性微需氧菌。H.pylori 是世界上感染率最高的病原菌，其感染呈全世界范围分布，发展中国家比发达国家发病率高，感染率随年龄而升高，男女差异不大。我国属H.pylori高感染率国家，人群H.pylori感染率在40%~70%左右。
H.pylori 感染可破坏消化道粘膜表面的粘液屏障，紧接着 H+ 不断地向粘膜内扩散，引发一系列病理进程，最终导致胃肠道粘膜充血、水肿、出血、糜烂乃至溃疡的发生。H.pylori 是上消化道疾病的重要致病菌，慢性胃炎、消化性溃疡、早期胃癌术后、胃粘膜相关淋巴组织淋巴瘤等消化系统疾病均应根除 H.pylori 治疗。
目前治疗H.pylori的主要方法为传统的三联或四联疗法，《2010WGO全球指南：发展中国家幽门螺旋杆菌感染》指南中一线疗法为质子泵抑制剂（PPI）+阿莫西林+克拉霉素7天；当克拉霉素耐药性大于20%地区：PPI+铋+四环素+甲硝唑7-10天；克拉霉素耐药性不明确地区：PPI+阿莫西林+克拉霉素7天；PPI+铋+四环素+甲硝唑7-10天；PPI+甲硝唑+克拉霉素+阿莫西林14天；PPI+呋喃唑酮+克拉霉素；序贯疗法：PPI+阿莫西林（5天）PPI+克拉霉素+甲硝唑（5天），主要为PPI抑制剂加两种抗生素或额外添加一种铋剂。目前常用的PPI抑制剂主要为奥美拉唑、兰索拉唑、雷贝拉唑、泮托拉唑、伊索美拉唑、来明拉唑、泰妥拉唑等，而本发明所述的吡咯磺酰类衍生物质子泵抑制剂为新一代质子泵抑制剂，属于钾离子（K+）竞争性酸阻滞剂（P-CAB），是一种可逆性质子泵抑制剂，在胃壁细胞泌酸的最后步骤，通过抑制K+与H+-K+-ATP酶的结合，终止胃酸的分泌，达到抑酸效果。包含吡咯磺酰类衍生物质子泵抑制剂的复方药物治疗幽门螺旋杆菌的应用尚未见报告。
发明内容
本发明提供了一种用于抑制或杀灭幽门螺旋杆菌的复方药物，可用于治疗幽门螺旋杆菌、十二指肠溃疡、胃溃疡和/或慢性胃炎。
本发明采用以下技术方案来实现：
一种用于抑制或杀灭幽门螺杆菌的复方药物，该复方药物包含吡咯磺酰类衍生物质子泵抑制剂，用药剂量范围为10~30mg，β-内酰胺类抗生素和大环内酯类抗生素，用药剂量范围均为100~200mg。
在上述复方药物中，吡咯磺酰类衍生物质子泵抑制剂如化学结构式（I）所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式、或药学上可接受的盐：
式中：
X选自CR4或N；
Y选自O或NR5；
R1选自烷基、环烷基、杂环烷基、芳基或杂芳基，其中所述烷基、环烷基、杂环烷基、芳基或杂芳基任意被一个或多个选自氢、卤素、氰基、硝基、羟基、烷基、卤代烷基、羟烷基、环烷基、杂环烷基、芳基、杂芳基、-OR6、-NR6R7、-C(O)NR6R7、-S(O)mR6、-C(O)R6、-O C(O)R6或- C(O) O R6的取代基所取代；
R2为氢、卤素、烷基、氰基、硝基、羟基、芳基、或者酯基；
R3为氢、卤素、烷基、氰基、硝基、羟基、芳基、或者酯基；
R4为氢、卤素、烷基、氰基、硝基、或者羟基；
R5为氢、烷基、或者芳基；
R6或R7各自独立地选自氢原子、烷基、环烷基、杂环烷基、芳基或杂芳基，其中所述烷基、环烷基、杂环烷基、芳基或杂芳基任意被一个或多个选自卤素、氰基、羟基、氨基、烷基、卤代烷基、羟烷基、烷氧基、环烷基、杂环烷基、芳基、杂芳基、羧基、酰胺基或羧酸酯基的取代基所取代；
m选自0、1或2。
在上述复方药物中，β-内酰胺类抗生素可选阿莫西林、氨苄西林、青霉素V钾、苯唑青霉素钠、氟氯西林、萘夫西林、海他西林钾、氯唑西林、头孢拉丁、头孢羟氨苄、头孢氯氨苄、头孢呋辛酯、头孢丙烯、头孢克肟、头孢妥仑、头孢布坦中的一种或多种，优选为阿莫西林。
在上述复方药物中，大环内酯类抗生素可选克拉霉素、红霉素、罗红霉素、麦迪霉素、乙酰螺旋霉素、麦白霉素、吉他霉素、琥乙红霉素、罗他霉素、阿奇霉素中的一种或多种，优选为克拉霉素。
本发明提供了上述复方药物在治疗幽门螺旋杆菌、十二指肠溃疡、胃溃疡和/或慢性胃炎的药物中的用途。
本发明的药物组合物的剂型为口服固体制剂，如片剂、胶囊、颗粒等。
具体实施方式
以下参照具体的实施例来说明本发明。这些实施例仅用于说明本发明，其不以任何方式限制本发明的范围。
实施例1：包含吡咯磺酰类衍生物质子泵抑制剂的复方药物抗幽门螺杆菌活性的研究
本实施例考察包含吡咯磺酰类衍生物质子泵抑制的复方药物对幽门螺杆菌临床分离菌株的抑制作用。本实施例中吡咯磺酰类衍生物质子泵抑制的结构式如（II）所示，β-内酰胺类抗生素为阿莫西林，大环内酯类抗生素为克拉霉素，采用琼脂稀释法测定三联用药，即该复方药物对临床分离的幽门螺杆菌菌株的最低抑菌浓度 (MICs)。
三联用药分为如下 2 组 ：吡咯磺酰类衍生物+阿莫西林+克拉霉素 ；奥美拉唑+阿莫西林+克拉霉素。
用无菌水将吡咯磺酰类衍生物和抗生素（阿莫西林、克拉霉素）连续稀释 2 倍，具体浓度如下 ：阿莫西林为 0.6-0.015μg/ml，克拉霉素为 1.2-0.05μg/ml，吡咯磺酰类衍生物和奥美拉唑均为 14.5-1.8μg/ml。 三联用药抗幽门螺杆菌的最低抑菌浓度的结果见表1。
由表1可知，吡咯磺酰类衍生物+阿莫西林+克拉霉素在最小浓度时可抑制62.5%的临床分离菌株。尽管在最小浓度时未抑制所有临床分离菌株，吡咯磺酰类衍生物+阿莫西林+克拉霉素组对 #3、 #5、#11、#14、#15 菌株显示出比奥美拉唑+阿莫西林+克拉霉素组更强的活性。
实施例2：含有吡咯磺酰类衍生物、克拉霉素、阿莫西林复方药物对幽门螺杆菌的根除和消化性溃疡的作用。吡咯磺酰类衍生物、克拉霉素、阿莫西林的用药剂量分为高中低剂量组，分别为低剂量组10mg、100mg、100mg；中剂量组20mg、150mg、150mg；高剂量组30mg、200mg、200mg
药效学验证：以大鼠为实验动物，醋酸法造胃溃疡模型，灌胃给予对克拉霉素有抗药性的幽门螺杆菌。设立阴性空白对照组、阳性对照组给予奥美拉唑+克拉霉素+阿莫西林，每组20 只动物。连续灌胃给药 7天，通过与阳性对照组比较计算幽门螺杆菌根除率和胃溃疡愈合率，实验结果见表2。
结果表明，实验组和阳性对照组与空白组呈显著性差异，同时实验组高中低剂量组在幽门螺杆菌根除率和溃疡愈合率方面均优于阳性对照组，说明该复方药物能更有效地抑制或杀灭幽门螺旋杆菌，可用于治疗胃溃疡。
Claims (7)
1.一种用于抑制或杀灭幽门螺旋杆菌的复方药物，其特征在于所述复方药物包含吡咯磺酰类衍生物质子泵抑制剂，β-内酰胺类抗生素和大环内酯类抗生素，所述吡咯磺酰类衍生物用药剂量范围为10~30mg，β-内酰胺类抗生素和大环内酯类抗生素的用药剂量范围均为100~200mg。
2.根据权利要求1所述的复方药物，其特征在于吡咯磺酰类衍生物为一种质子泵抑制剂，如化学结构式（I）所示的化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式、或药学上可接受的盐：
式中：
X选自CR4或N：
Y选自O或NR5：
R1选自烷基、环烷基、杂环烷基、芳基或杂芳基，其中所述烷基、环烷基、杂环烷基、芳基或杂芳基任意被一个或多个选自氢、卤素、氰基、硝基、羟基、烷基、卤代烷基、羟烷基、环烷基、杂环烷基、芳基、杂芳基、-OR6、-NR6R7、-C(O)NR6R7、-S(O)mR6、-C(O)R6、-O C(O)R6或- C(O) O R6的取代基所取代；
R2为氢、卤素、烷基、氰基、硝基、羟基、芳基、或者酯基；
R3为氢、卤素、烷基、氰基、硝基、羟基、芳基、或者酯基；
R4为氢、卤素、烷基、氰基、硝基、或者羟基；
R5为氢、烷基、或者芳基；
R6或R7各自独立地选自氢原子、烷基、环烷基、杂环烷基、芳基或杂芳基，其中所述烷基、环烷基、杂环烷基、芳基或杂芳基任意被一个或多个选自卤素、氰基、羟基、氨基、烷基、卤代烷基、羟烷基、烷氧基、环烷基、杂环烷基、芳基、杂芳基、羧基、酰胺基或羧酸酯基的取代基所取代；
m选自0、1或2。
3.根据权利要求2所述的复方药物，其特征在于所述吡咯磺酰类衍生物质子泵抑制剂的R1选自被一个或多个取代基取代的：
所述取代基为卤素、氰基、硝基、羟基、烷基、卤代烷基、羟烷基、环烷基、杂环烷基、-OR6、-NR6R7、-C(O)NR6R7、-S(O)mR6、-C(O)R6、-O C(O)R6或- C(O) OR6的取代基所取代；
R6或R7各自独立地选自氢原子、烷基；其中所述烷基芳基任意被一个或多个选自卤素、氰基、羟基、氨基、烷基、卤代烷基、羟烷基、烷氧基、环烷基、杂环烷基、芳基、杂芳基、羧基、酰胺基或羧酸酯基的取代基所取代；
m选自0、1或2。
4.根据权利要求2或3所述的复方药物，其特征为所述的吡咯磺酰类衍生物质子泵抑制剂选自以下任意一个化合物：
。
5.根据权利要求1所述的复方药物，其特征在于所述β-内酰胺类抗生素为阿莫西林、氨苄西林、青霉素V钾、苯唑青霉素钠、氟氯西林、萘夫西林、海他西林钾、氯唑西林、头孢拉丁、头孢羟氨苄、头孢氯氨苄、头孢呋辛酯、头孢丙烯、头孢克肟、头孢妥仑、头孢布坦。
6.根据权利要求1所述的复方药物，其特征在于所述大环内酯类抗生素为卡拉霉素、红霉素、罗红霉素、麦迪霉素、乙酰螺旋霉素、麦白霉素、吉他霉素、琥乙红霉素、罗他霉素、阿奇霉素。
7.根据权利要求1至6任一项所述复方药物，其特征在于可用于制备治疗幽门螺旋杆菌、十二指肠溃疡、胃溃疡和/或慢性胃炎的药物。
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