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    • 4. 发明申请
    • N-SUBSTITUTED PIPERIDINYL-IMIDAZOPYRIDINE COMPOUNDS AS 5-HT4 RECEPTOR MODULATORS
    • N-取代的哌嗪基咪唑啉化合物作为5-HT4受体调节剂
    • WO2004026868A1
    • 2004-04-01
    • PCT/IB2003/003945
    • 2003-09-08
    • PFIZER PHARMACEUTICALS INC.PFIZER INC.KATSU, YasuhiroKON-I, KanaMORITA, MikioNOGUCHI, HirohideUCHIDA, Chikara
    • KATSU, YasuhiroKON-I, KanaMORITA, MikioNOGUCHI, HirohideUCHIDA, Chikara
    • C07D471/04
    • C07D471/04
    • This invention provides a compound of the formula (I): wherein R l represents a hydrogen atom or a halogen atom; R 2 represents a hydrogen atom, etc.; R 3 represents an alkyl group having from 1 to 10 carbon atoms; said alkyl group in R 3 is substituted by at least one substituent selected from the group consisting of substituents α ; said substituents α are selected from the group consisting of aryl groups, hydroxy groups, oxo groups, etc.; said aryl groups have 6 to 10 carbon atoms; said aryl groups are unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic groups and heterocyclic moiety in heterocycliccarbonyl groups are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, etc.; or a pharmaceutically acceptable amide of such compound, or a pharmaceutically acceptable ester of such compound, and pharmaceutically acceptable salts thereof. These compounds have 5-HT 4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
    • 本发明提供式(I)的化合物:其中R 1表示氢原子或卤素原子; R 2表示氢原子等; R 3表示具有1至10个碳原子的烷基; R 3中的所述烷基被至少一个选自取代基α的取代基取代; 所述取代基α选自芳基,羟基,氧代基等; 所述芳基具有6至10个碳原子; 所述芳基是未取代的或被至少一个具有1至6个碳原子的烷基取代; 所述杂环基中的杂环基和杂环部分是含有1至4个选自氮原子等的杂原子的5-至10-元环状基团; 或这种化合物的药学上可接受的酰胺,或这种化合物的药学上可接受的酯及其药学上可接受的盐。 这些化合物具有5-HT4受体结合活性,因此可用于治疗哺乳动物,特别是人类的胃食管反流病,非溃疡性消化不良,功能性消化不良,肠易激综合征等。 本发明还提供了包含上述化合物的药物组合物。
    • 5. 发明申请
    • IMIDAZOPYRIDINE COMPOUNDS AS 5-HT4 RECEPTOR MODULATORS
    • 咪达唑啶化合物作为5-HT4受体调节剂
    • WO2003035649A1
    • 2003-05-01
    • PCT/IB2002/004098
    • 2002-10-03
    • PFIZER PHARMACEUTICALS INC.PFIZER INC.FENWICK, David, RoyGYMER, Geoffrey, EdwardNOGUCHI, HirohideSTOBIE, AlanUCHIDA, Chikara
    • FENWICK, David, RoyGYMER, Geoffrey, EdwardNOGUCHI, HirohideSTOBIE, AlanUCHIDA, Chikara
    • C07D471/04
    • C07D471/04
    • This invention provides a compound of the formula (I), or the pharmaceutically acceptable salts thereof wherein R 1 is hydrogen, halo or alkyl; R 2 and R 3 are independently hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl or hydroxyalkyl; or R 2 and R 3 taken together with the nitrogen atom to which they are attached may form hetrocyclic; R 4 is hydrogen, halo, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R 5 is hydrogen, halo, alkyl, alkenyl, alkynyl, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R 6 is hydrogen, alkyl or alkoxyalkyl; X is NR 9 wherein R 9 is hydrogen or alkyl; and Y is (CR 7 R 8 ) wherein n is an integer from 0 to 5. These compounds have 5-HT 4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, Functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
    • 本发明提供式(I)化合物或其药学上可接受的盐,其中R 1是氢,卤素或烷基; R 2和R 3独立地是氢,烷基,烯基,炔基,氨基烷基或羟烷基; 或R 2和R 3与它们所连接的氮原子一起可以形成环状的; R 4是氢,卤素,酰基,氨基,酰氨基,芳基,芳基烷基或杂芳基; R 5是氢,卤素,烷基,烯基,炔基,酰基,氨基,酰氨基,芳基,芳基烷基或杂芳基; R 6是氢,烷基或烷氧基烷基; X是NR 9,其中R 9是氢或烷基; 并且Y是(CR 7 R 8),其中n是0至5的整数。这些化合物具有5-HT 4受体结合活性,因此可用于治疗胃食管反流病,非溃疡性消化不良, 功能性消化不良,肠易激综合征等在哺乳动物,特别是人类。 本发明还提供了包含上述化合物的药物组合物。
    • 9. 发明申请
    • OXYINDOLE DERIVATIVES AS 5HT4 RECEPTOR AGONISTS
    • 氧化衍生物作为5HT4受体激动剂
    • WO2006090279A1
    • 2006-08-31
    • PCT/IB2006/000519
    • 2006-02-10
    • PFIZER JAPAN INC.PFIZER INC.KAWAMURA, KiyoshiSONE, HirokiUCHIDA, Chikara
    • KAWAMURA, KiyoshiSONE, HirokiUCHIDA, Chikara
    • C07D405/14C07D401/14C07D401/12A61K31/454A61P1/04
    • C07D401/12C07D401/14C07D405/14
    • This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, R 1 , R 2 , R 3 , R4 and R 5 are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT 4 agonisitic activity such as, but not limited to, as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes or apnea syndrome.
    • 本发明涉及式(I)化合物或其药学上可接受的盐,其中:A,R 1,R 2,R 3, 其中R 4和R 5各自如本文所述或其药学上可接受的盐,以及含有这些化合物的组合物以及这些化合物在治疗病症介导中的用途 通过5-HT 4激动剂活性,例如但不限于胃食管反流病,胃肠道疾病,胃动力障碍,非溃疡性消化不良,功能性消化不良,肠易激综合征(IBS),便秘 ,消化不良,食管炎,胃食管疾病,恶心,中枢神经系统疾病,阿尔茨海默病,认知障碍,呕吐,偏头痛,神经系统疾病,疼痛,心血管疾病,心力衰竭,心律失常,糖尿病或呼吸暂停综合征。