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1. 发明专利

JP2003014728A Prediction method and system of medicine dynamic study physical property 审中-公开
标题翻译：医学动态研究物理性质的预测方法与系统
公开(公告)号：JP2003014728A
公开(公告)日：2003-01-15
申请号：JP2001179774
申请日：2001-06-14
申请人： Pfizer Pharmaceuticals Inc , ファイザー製薬株式会社
发明人： HATTORI KAZUNARI , SHIMADA KAORU , UCHIYAMA MAMORU
IPC分类号： G01N33/48 , G01N33/15 , G01N33/68 , G06F19/00 , G06F19/16 , G06Q10/00
CPC分类号： G01N33/6803 , G06F19/704
摘要： PROBLEM TO BE SOLVED: To provide the prediction method and system of medicine dynamic study physical properties that can predict the medicine dynamic study physical properties of a molecule before synthesis without any labor-intensive and time- consuming experiments. SOLUTION: The prediction method includes a process (a) for preparing the two-dimensional structure of a molecule used as a training set, a process (b) for building a two-dimensional finger print by using internal development macro automatically, or by manually counting the number of descriptors that comprise atoms/fragments being prescribed in advance or 20-80 substructures and may relate to medicine dynamic study physical properties, a process (c) for analyzing the obtained two-dimensional finger print by a statistical analysis method for correlating with the medicine dynamic study properties of the molecule to obtain a quantitative structure property relationship(QSPR) model, and a process (d) for using the QSPR model for calculating the medicine dynamic study physical properties of a test molecule. The system includes a means for executing the processes.
摘要翻译：要解决的问题：提供药物动态研究的物理性质的预测方法和系统，可以预测药物在合成前动态研究分子的物理性质，而无需任何劳动密集型和耗时的实验。解决方案：预测方法包括用于制备用作训练集的分子的二维结构的方法（a），用于通过自动使用内部显影宏来构建二维指纹的方法（b），或通过手动计算包含预先规定的原子/片段的描述符的数量或20-80个亚结构，并且可以涉及药物动态研究物理性质，用于通过统计分析方法分析获得的二维指纹的方法（c）与药物动力学研究性质的分子获得定量结构性质关系（QSPR）模型，以及使用QSPR模型计算药物动力学研究物理性质的方法（d）。该系统包括用于执行过程的手段。

2. 发明专利

JP2003055376A Pyrazoloquinoline derivative as protein kinase c inhibitor 有权
标题翻译：吡唑啉衍生物作为蛋白激酶C抑制剂
公开(公告)号：JP2003055376A
公开(公告)日：2003-02-26
申请号：JP2002182550
申请日：2002-06-24
申请人： Pfizer Pharmaceuticals Inc , ファイザー製薬株式会社
发明人： KAWAMURA KIYOSHI , MIHARA SACHIKO , NUKUI SEIJI , UCHIDA TSUTOMU
IPC分类号： A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/551 , A61P1/00 , A61P1/04 , A61P3/10 , A61P9/02 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P25/00 , A61P25/04 , A61P25/28 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/18 , A61P37/02 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide a protein kinase inhibitor useful for treatment of diseases such as neuropathic ache, diabetic neuropathy and septicemia. SOLUTION: This protein kinaze inhibitor is a compound represented by the general formula (I) or its pharmaceutically permissible salt. (The broken line is an optional double bond; C , C , C and C are each C; R is an alkyl; R is H, amino or the like; R is H, a halo-CH2 , an alkyl or Q -alkyl; Q is a (hetero atom-having) 4- to 12-membered monocyclic or bicyclic ring; Y , Y , Y and Y are each H; and Y , Y , Y and Y are each H, a halo, an alkyl, a heterocycle-substituted alkyl or the like).
摘要翻译：要解决的问题：提供可用于治疗诸如神经性疼痛，糖尿病性神经病和败血病等疾病的蛋白激酶抑制剂。解决方案：该蛋白激酶抑制剂是由通式（I）表示的化合物或其药学上可允许的盐。（虚线是任选的双键; C 1，C 2，C 3和C 4各自为C; R 1为烷基; R 2为H，氨基或 R 3为H，卤代-CH 2，烷基或Q 1 - 烷基; Q为（具有杂原子的）4至12元单环或双环; Y 5， Y 6，Y 7和Y 8各自为H; Y 1，Y 2，Y 3和Y 4各自为H，卤素，烷基，杂环取代的烷基等）。

3. 发明专利

JP2003040777A Pharmaceutical composition piperidylaminomethyltrifluoromethyl cyclic ether compound as substance p antagonist 审中-公开
标题翻译：药物组合物作为物质P ANTAGONIST的PIPERIDYLAMINOMETHYLTRIFLUOROMETHYL循环醚化合物
公开(公告)号：JP2003040777A
公开(公告)日：2003-02-13
申请号：JP2002177452
申请日：2002-06-18
申请人： Pfizer Pharmaceuticals Inc , ファイザー製薬株式会社
发明人： SATAKE KUNIO
IPC分类号： A61K20060101 , A61K31/443 , A61K31/445 , A61K31/4453 , A61K31/452 , A61K31/4523 , A61K31/4525 , A61K31/453 , A61P1/00 , A61P1/04 , A61P1/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/02 , A61P15/00 , A61P15/10 , A61P17/00 , A61P17/02 , A61P19/02 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/04 , A61P37/00 , A61P37/08 , A61P43/00 , C07D20060101 , C07D211/06 , C07D211/56 , C07D295/00 , C07D307/78 , C07D307/87 , C07D311/76 , C07D405/12
CPC分类号： C07D307/87 , C07D311/76 , C07D405/12
摘要： PROBLEM TO BE SOLVED: To provide a substance P antagonist improved in activity and further reduced in adverse effect. SOLUTION: The invention relates to a pharmaceutical composition comprising a compound represented by the formula (1) [R is a 1-6C alkyl; R is hydrogen, a 1-6C alkyl, a halo-1-6C alkyl or phenyl; R is hydrogen or a halogen; R and R are independently hydrogen, a 1-6C alkyl or a halo-1-6C alkyl; n is 1, 2 or 3] and a pharmaceutically acceptable salt thereof and useful as a analgesic or antiinflammatory agent or useful in treatment of diseases, disorder or harmful state caused by cardiovascular diseases, allergic diseases, angiogenesis, CNS disorder, vomiting, gastrointestinal injury, solar dermatitis, urinary incontinence or Helicobacter pylori in mammal, particularly human.
摘要翻译：要解决的问题：提供一种改善活性的物质P拮抗剂，进一步减少不利影响。解决方案：本发明涉及包含由式（1）表示的化合物的药物组合物[R 1是1-6C烷基; R 2是氢，1-6C烷基，卤代C 1-6烷基或苯基; R 3是氢或卤素; R 4和R 5独立地是氢，1-6C烷基或卤代-C 1-6烷基; n为1,2或3]及其药学上可接受的盐，可用作镇痛或抗炎剂或可用于治疗由心血管疾病，过敏性疾病，血管发生，CNS紊乱，呕吐，胃肠道损伤引起的疾病，病症或有害状态，太阳皮炎，尿失禁或幽门螺杆菌在哺乳动物，特别是人类。

4. 发明申请

WO2004026869A1 IMIDAZOPYRIDINE COMPUNDS AS 5-HT4 RECEPTOR AGONISTS 审中-公开
标题翻译：咪达唑啶计算机作为5-HT4受体激动剂
公开(公告)号：WO2004026869A1
公开(公告)日：2004-04-01
申请号：PCT/IB2003/003971
申请日：2003-09-08
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , IGUCHI, Satoru , KATSU, Yasuhiro , KON-I, Kana , NOGUCHI, Hirohide , UCHIDA, Chikara
发明人： IGUCHI, Satoru , KATSU, Yasuhiro , KON-I, Kana , NOGUCHI, Hirohide , 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): (I) 5 wherein Rl represents a hydrogen atom or a halogen atom; R2 represents a methyl group or an ethyl group; R3 represents a branched alkyl group having from 3 to 6 carbon atoms or an alkyl group having from 3 to 6 carbon atoms substituted by an alkoxy group having from 1 to 6 carbon atoms; with the proviso that when the terminal carbon atom of said alkyl group is substituted by said alkoxy goroup, said alkyl group is a branched alkyl group; and pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor binding activity, and thus are usefulfor 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：（I）5其中R1代表氢原子或卤素原子; R2表示甲基或乙基; R3表示碳原子数为3〜6的支链烷基或碳原子数1〜6的烷氧基取代的碳原子数3〜6的烷基。条件是当所述烷基的末端碳原子被所述烷氧基取代时，所述烷基是支链烷基; 及其药学上可接受的盐。这些化合物具有5-HT 4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

WO2004026868A1 N-SUBSTITUTED PIPERIDINYL-IMIDAZOPYRIDINE COMPOUNDS AS 5-HT4 RECEPTOR MODULATORS 审中-公开
标题翻译： N-取代的哌嗪基咪唑啉化合物作为5-HT4受体调节剂
公开(公告)号：WO2004026868A1
公开(公告)日：2004-04-01
申请号：PCT/IB2003/003945
申请日：2003-09-08
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , KATSU, Yasuhiro , KON-I, Kana , MORITA, Mikio , NOGUCHI, Hirohide , UCHIDA, Chikara
发明人： KATSU, Yasuhiro , KON-I, Kana , MORITA, Mikio , NOGUCHI, Hirohide , 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): 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.
摘要翻译：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。

6. 发明申请

WO2004020998A1 EVALUATION METHOD FOR PREDICTING PHARMACOKINETICS OF PM USING PM LIVER CELLS OF DRUG METABOLIZING ENZYME CYTOCHROME P450 HAVING A GENETIC POLYMORPHISM 审中-公开
标题翻译：使用具有遗传多态性的酶代谢酶细胞色素P450的PM的肝细胞预测PM的药代动力学的评估方法
公开(公告)号：WO2004020998A1
公开(公告)日：2004-03-11
申请号：PCT/IB2003/003802
申请日：2003-08-25
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , SHIMADA, Kaoru , TAKASHIMA, Tadayuki
发明人： SHIMADA, Kaoru , TAKASHIMA, Tadayuki
IPC分类号： G01N33/50
CPC分类号： C12Q1/26 , G01N2333/90209 , G01N2500/10
摘要： There is provided a novel evaluation method for predicting the pharmacokinetics of PM using PM liver cells of drug metabolizing enzyme cytochrome P450 having a genetic polymorphism. According to the present invention, the pharmacokinetics (metabolism) of PM can be predicted by using PM liver cells of CYP2D6 among drug metabolizing enzyme cytochrome P450 known to have a genetic polymorphism.
摘要翻译：提供了一种新的评估方法，用于预测具有遗传多态性的药物代谢酶细胞色素P450的PM肝细胞的PM的药代动力学。根据本发明，可以通过使用已知具有遗传多态性的药物代谢酶细胞色素P450中的CYP2D6的PM肝细胞来预测PM的药代动力学（代谢）。

7. 发明申请

WO2003086390A1 IMIDAZOLE COMPOUNDS AS ANTI-INFLAMMATORY AND ANALGESIC AGENTS 审中-公开
标题翻译：咪唑化合物作为抗炎和灭菌剂
公开(公告)号：WO2003086390A1
公开(公告)日：2003-10-23
申请号：PCT/IB2003/001275
申请日：2003-04-02
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , HIRANO, Misato , IGUCHI, Satoru , NAKAO, Kazunari , YAMAGISHI, Tatsuya
发明人： HIRANO, Misato , IGUCHI, Satoru , NAKAO, Kazunari , YAMAGISHI, Tatsuya
IPC分类号： A61K31/4164
CPC分类号： C07D233/64 , C07D233/88 , C07D235/08 , C07D401/12 , C07D521/00
摘要： This invention provides a compound of the formula (1) wherein: R 1 represents a hydrogen atom, an alkyl group, etc.; R 2 represents a hydrogen atom, a halogen atom, etc.; R 3 represents a hydrogen atom, an alkyl group, etc.; R 4 represents an aryl group, etc.; A represents an aryl 1 , etc; B represents an alkylene etc.; X represents NH, etc.; or a phannaceutically acceptable ester of such compound, and pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of medical conditions mediated by prostaglandins such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（1）的化合物，其中：R 1表示氢原子，烷基等; R 2表示氢原子，卤素原子等; R 3表示氢原子，烷基等; R 4表示芳基等; A表示芳基等; B表示亚烷基等。 X表示NH等。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。这些化合物可用于治疗前列腺素介导的医疗状况，例如疼痛，发热或炎症等。本发明还提供包含上述化合物的药物组合物。

8. 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.

9. 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。

10. 发明申请

WO1998030209A1 RAPIDLY RELEASING AND TASTE-MASKING PHARMACEUTICAL DOSAGE FORM 审中-公开
标题翻译：快速释放和吸收药物药物剂型
公开(公告)号：WO1998030209A1
公开(公告)日：1998-07-16
申请号：PCT/IB1997001471
申请日：1997-11-20
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , ITOH, Akinori , NIWA, Toshiyuki
发明人： PFIZER PHARMACEUTICALS INC. , PFIZER INC.
IPC分类号： A61K09/54
CPC分类号： A61K9/5078 , A61K9/1623 , A61K9/1652 , A61K9/5015 , A61K9/5026 , A61K9/5073
摘要： The present invention provides a rapidly releasing and taste-masking pharmaceutical dosage form comprising a core containing a pharmaceutically active ingredient, low-substituted hydroxypropyl cellulose and microcrystalline cellulose, the amount of the microcrystalline cellulose being at least 26.0 weight percent based on the total weight of the core; an inner coating layer formed on the core and containing a water-soluble polymer; and an outer coating layer formed on the inner coating layer and containing a saliva-insoluble polymer. A process for preparing such oral dosage form is also disclosed.
摘要翻译：本发明提供了一种快速释放和掩味的药物剂型，其包含含有药物活性成分，低取代羟丙基纤维素和微晶纤维素的核心，微晶纤维素的量基于总重量的至少26.0重量％核心; 形成在芯上并含有水溶性聚合物的内涂层; 以及形成在内涂层上并含有唾液不溶性聚合物的外涂层。还公开了制备这种口服剂型的方法。

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