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1. 发明申请

WO2005123702A1 NEUTRAL ENDOPEPTIDASE INHIBITOR POLYMORPH 审中-公开
标题翻译：中性内切酶抑制剂多聚体
公开(公告)号：WO2005123702A1
公开(公告)日：2005-12-29
申请号：PCT/IB2005/001911
申请日：2005-06-03
申请人： PFIZER LIMITED , PFIZER INC. , DACK, Kevin, Neil , GYMER, Geoffrey, Edward
发明人： DACK, Kevin, Neil , GYMER, Geoffrey, Edward
IPC分类号： C07D263/32
CPC分类号： C07D263/32
摘要： Disclosed are (2S)-2-{1-[(1S)-1-Isobutoxycarbonyl-2-(5-phenyl-oxazol-2-yl)-ethylcarbamoyl]-cyclopentylmethyl}-4-methoxy-butyric, Potassium-(2S)-2-{1-[(1S)-1-Isobutoxycarbonyl-2-(5-phenyl-oxazol-2-yl)-ethylcarbamoyl]-cyclopentylmethyl}-4-methoxy-butyrate, monohydrate and its Form I polymorph. Also disclosed are compositions of the described forms, kits including the described forms, and methods of using the described forms for the treatment diseases or disorders where the use of a neutral endopeptidase inhibitor is indicated, including cardiovascular diseases and conditions.
摘要翻译：公开了（2S）-2- {1 - [（1S）-1-异丁氧基羰基-2-（5-苯基 - 恶唑-2-基） - 乙基氨基甲酰基] - 环戊基甲基} -4-甲氧基 - 丁酸钾 - （2S ）-2- {1 - [（1S）-1-异丁氧基羰基-2-（5-苯基 - 恶唑-2-基） - 乙基氨基甲酰基] - 环戊基甲基} -4-甲氧基 - 丁酸乙酯，一水合物及其I型多晶型物。还公开了所述形式的组合物，包括所述形式的试剂盒，以及使用所述形式用于治疗使用中性内肽酶抑制剂的疾病或病症（包括心血管疾病和病症）的方法。

2. 发明申请

WO2003057688A2 OXO OR OXY-PYRIDINE COMPOUNDS AS 5-HT4 RECEPTOR MODULATORS 审中-公开
标题翻译： OXO或OXY-吡啶化合物作为5-HT4受体调节剂
公开(公告)号：WO2003057688A2
公开(公告)日：2003-07-17
申请号：PCT/IB2002/005600
申请日：2002-12-20
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , UCHIDA, Chikara , MIHARA, Sachiko , MORITA, Mikio , KAWAMURA, Kiyoshi , NUKUI, Seiji , STOBIE, Alan , GYMER, Geoffrey, Edward
发明人： UCHIDA, Chikara , MIHARA, Sachiko , MORITA, Mikio , KAWAMURA, Kiyoshi , NUKUI, Seiji , STOBIE, Alan , GYMER, Geoffrey, Edward
IPC分类号： C07D401/12
CPC分类号： C07D401/06 , C07D401/12 , C07D401/14
摘要： This invention provides compounds of the formula (I) and (II) or the phannaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein R 1 is hydrogen or halo; R 2 and R 3 are independently hydrogen or C 1-6 alkyl; R 4 and R 5 are independently hydrogen or C 1-6 alkyl; R 6 is hydrogen, C l-12 alkyl, C 1-6 alkoxy (C 1-6 )alkyl or C 1-12 alkyl substituted by up to 3 substituents selected from the groups consisting of C 3-8 cycloalkyl, aryl, heteroaryl and heterocyclic; R 7 and R 8 are hydrogen or taken together may form alkylene chain having one or two carbon atoms; R 9 is C 1-6 alkyl or C 3-8 cycloalkyl; R 10 is C 1-6 alkyl or NR 11 R 12 ; L is (CR 11 R 12 )n or NR 11 ; M is NR 11 or (CR 11 R 12 )n ; R 11 and R 12 are independently hydrogen or C 1-6 alkyl; n is an integer from 0 to 5; and. m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and C 1-6 alkyl; with the proviso that when R 9 is C 1-6 alkyl, L is not NR 11 . These compounds have 5-HT 4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）和（II）化合物或其药学上可接受的酯及其药学上可接受的盐：其中R 1是氢或卤素; R 2和R 3独立地是氢或C 1-6烷基; R 4和R 5独立地是氢或C 1-6烷基; R 6是氢，C 1-12烷基，C 1-6烷氧基（C 1-6）烷基或被至多3个选自C 3-8环烷基，芳基，杂芳基和杂环基; R 7和R 8是氢或一起可以形成具有一个或两个碳原子的亚烷基链; R 9是C 1-6烷基或C 3-8环烷基; R 10是C 1-6烷基或NR 11 R 12; L是（CR 11 R 12）n或NR 11; M是NR 11或（CR 11 R 12）n; R 11和R 12独立地是氢或C 1-6烷基; n为0〜5的整数，和。 m为0〜2的整数; 所述杂环，芳基和杂芳基是未取代的或被至少一个选自卤素和C 1-6烷基的取代基取代; 条件是当R 9为C 1-6烷基时，L不为NR 11。这些化合物具有5-HT 4受体的结合活性，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，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。

3. 发明申请

WO2002083643A1 PHENYL HETEROCYCLYL ETHER DERIVATIVES AS SEROTONIN RE-UPTAKE INHIBITORS 审中-公开
标题翻译：苯基异喹啉酮衍生物作为丝氨酸还原抑制剂
公开(公告)号：WO2002083643A1
公开(公告)日：2002-10-24
申请号：PCT/IB2002/001032
申请日：2002-03-27
申请人： PFIZER LIMITED , PFIZER INC. , ADAM, Mavis, Diane , ANDREWS, Mark, David , GYMER, Geoffrey, Edward , HEPWORTH, David , HOWARD, Harry, Ralph, Jr. , MIDDLETON, Donald, Stuart , STOBIE, Alan
发明人： ADAM, Mavis, Diane , ANDREWS, Mark, David , GYMER, Geoffrey, Edward , HEPWORTH, David , HOWARD, Harry, Ralph, Jr. , MIDDLETON, Donald, Stuart , STOBIE, Alan
IPC分类号： C07D213/65
CPC分类号： C07D213/65 , C07D213/80 , C07D213/82 , C07D241/18 , C07D401/06
摘要： The invention relates to compounds of the formula (I) which exhibit activity as selective serotonin re-uptake inhibitors.
摘要翻译：本发明涉及作为选择性5-羟色胺再摄取抑制剂的活性的式（I）化合物。

4. 发明申请

WO2003057688A3 OXO OR OXY-PYRIDINE COMPOUNDS AS 5-HT4 RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2003057688A3
公开(公告)日：2003-07-17
申请号：PCT/IB2002/005600
申请日：2002-12-20
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , UCHIDA, Chikara , MIHARA, Sachiko , MORITA, Mikio , KAWAMURA, Kiyoshi , NUKUI, Seiji , STOBIE, Alan , GYMER, Geoffrey, Edward
发明人： UCHIDA, Chikara , MIHARA, Sachiko , MORITA, Mikio , KAWAMURA, Kiyoshi , NUKUI, Seiji , STOBIE, Alan , GYMER, Geoffrey, Edward
IPC分类号： C07D401/12
摘要： This invention provides compounds of the formula (I) and (II) or the phannaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein R 1 is hydrogen or halo; R 2 and R 3 are independently hydrogen or C 1-6 alkyl; R 4 and R 5 are independently hydrogen or C 1-6 alkyl; R 6 is hydrogen, C l-12 alkyl, C 1-6 alkoxy (C 1-6 )alkyl or C 1-12 alkyl substituted by up to 3 substituents selected from the groups consisting of C 3-8 cycloalkyl, aryl, heteroaryl and heterocyclic; R 7 and R 8 are hydrogen or taken together may form alkylene chain having one or two carbon atoms; R 9 is C 1-6 alkyl or C 3-8 cycloalkyl; R 10 is C 1-6 alkyl or NR 11 R 12 ; L is (CR 11 R 12 )n or NR 11 ; M is NR 11 or (CR 11 R 12 )n ; R 11 and R 12 are independently hydrogen or C 1-6 alkyl; n is an integer from 0 to 5; and. m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and C 1-6 alkyl; with the proviso that when R 9 is C 1-6 alkyl, L is not NR 11 . These compounds have 5-HT 4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

5. 发明申请

WO2003035649A1 IMIDAZOPYRIDINE COMPOUNDS AS 5-HT4 RECEPTOR MODULATORS 审中-公开
标题翻译：咪达唑啶化合物作为5-HT4受体调节剂
公开(公告)号：WO2003035649A1
公开(公告)日：2003-05-01
申请号：PCT/IB2002/004098
申请日：2002-10-03
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , FENWICK, David, Roy , GYMER, Geoffrey, Edward , NOGUCHI, Hirohide , STOBIE, Alan , UCHIDA, Chikara
发明人： FENWICK, David, Roy , GYMER, Geoffrey, Edward , NOGUCHI, Hirohide , STOBIE, Alan , UCHIDA, Chikara
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： 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.
摘要翻译：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。

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