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71. 发明专利

JP2005047930A Substituted 6,5-hetero-bicyclic derivative 审中-公开
标题翻译：取代6,5-杂环双环衍生物
公开(公告)号：JP2005047930A
公开(公告)日：2005-02-24
申请号：JP2004273978
申请日：2004-09-21
申请人： Pfizer Inc , ファイザー・インク
发明人： CHEN YUHPYNG LIANG
IPC分类号： A61K31/00 , A61K31/435 , A61K31/4353 , A61K31/437 , A61K31/505 , A61K31/519 , A61K31/529 , A61P1/00 , A61P1/04 , A61P1/12 , A61P1/14 , A61P3/00 , A61P3/04 , A61P3/08 , A61P5/24 , A61P5/42 , A61P7/12 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/00 , A61P13/02 , A61P15/00 , A61P15/06 , A61P15/08 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/00 , A61P21/02 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P29/00 , A61P31/00 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/04 , A61P37/08 , A61P43/00 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide substituted 6,5-hetero-bicyclic derivatives effective as medicines. SOLUTION: The derivatives are compounds represented by formula (1), wherein dotted lines stand optionally for double bonds; A is N or CR 7 ; B is NR 1 R 2 , CR 1 R 2 R 10 , C(C=CR 2 R 11 )R 1 , NHCR 1 R 2 R 10 , OCR 1 R 2 R 10 , SCR 1 R 2 R 10 , CR 2 R 10 NHR 1 , CR 2 R 10 OR 1 , CR 2 R 10 SR 1 or COR 2 ; J and K are independently N or C; J and K are not simultaneously N; D and E are each independently selected from N, CR 4 , C=O, C=S, S, O, CR 4 R 6 and NR 8 ; and G is N or C. Applications thereof for preventing or inhibiting diseases treatable by antagonizing CRF (corticotropin releasing factor) are provided. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：提供作为药物有效的取代的6,5-杂双环衍生物。该衍生物是式（1）表示的化合物，其中虚线任选地用于双键; A是N或CR 7 ; B是NR 1 R 2 ，CR 1 R 2 R 10 （C = CR 2 R 11 ）R 1 ，NHCR 1 R 10 ，OCR 1 R 2 R 10 ，SCR 1 R 2 R 10 ，CR 2 R 10 NHR 1 ，CR / SP> R 10 或 1 ，CR 2 R 10 SR 1 COR 2 ; J和K独立地为N或C; J和K不同时为N; D和E各自独立地选自N，CR 4，或者C = O，C = S，S，O，CR 4 R 6 和NR 8 ; 并且G是N或C.用于预防或抑制通过拮抗CRF（促皮质激素释放因子）可治疗的疾病的应用。版权所有（C）2005，JPO＆NCIPI

72. 发明专利

JP2005015466A Method for administering azithromycin 审中-公开
标题翻译：用于治疗AZITHROMYCIN的方法
公开(公告)号：JP2005015466A
公开(公告)日：2005-01-20
申请号：JP2004128641
申请日：2004-04-23
申请人： Pfizer Inc , ファイザー・インク
发明人： CURATOLO WILLIAM J , FOULDS GEORGE H , FRIEDMAN HYLAR L
IPC分类号： C07H17/00 , A61K9/00 , A61K9/10 , A61K9/14 , A61K9/20 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61K47/02 , A61P31/00 , A61P31/04 , C07H17/08
CPC分类号： A61K31/70 , A61K9/0095 , Y10S514/96
摘要： PROBLEM TO BE SOLVED: To provide a preparation capable of administering azithromycin to a patient just beginning to take a food. SOLUTION: This oral administration preparation of the azithromycin capable of being administered to a mammal capable of taking the food is provided by containing the azithromycin, without showing an disadvantageous effect of the food substantially, and achieving approximately 90 % dissolution of the azithromycin within 30 min in a USP-2 dissolution testing device under a strict condition similar to the below: a preparation corresponding to 250 mg azithromycin is tested in a phosphate buffer of 900 ml of pH6.0 at 37°C with a paddle rotating by 100 rpm, as indicated in the USP test . Provided that, the preparation is not a capsule preparation, but the oral preparation characterized by containing an alkaline earth metal oxide or hydroxide in an amount less than a taste-blocking amount and not exhibiting the bad effect of the food. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：要解决的问题：提供一种能够将阿奇霉素施用于刚刚开始食用的患者的制剂。解决方案：能够给予能够摄取食物的哺乳动物的阿奇霉素的口服给药制剂通过含有阿奇霉素而提供，而不显示食物的不利影响，并且实现阿奇霉素约90％的溶解在USP-2溶出测试装置的30分钟内，在类似于以下条件的严格条件下，在37℃下，在900ml pH6.0的磷酸盐缓冲液中，用桨转动100 rpm，如USP测试<711>所示。前提是制剂不是胶囊制剂，而是口服制剂，其特征在于含有小于味道阻断量的碱土金属氧化物或氢氧化物，并且不显示食物的不良影响。版权所有（C）2005，JPO＆NCIPI

73. 发明专利

JP2005013237A Assaying method for identifying agent for treating female sexual dysfunction (fsd), method and kit for detecting female sexual dysfunction, and non-human animal model of female sexual dysfunction 审中-公开
标题翻译：用于鉴别用于检测女性性功能障碍的女性性功能障碍（FSD），方法和套件的识别方法和女性性功能的非人类动物模型的测定方法
公开(公告)号：JP2005013237A
公开(公告)日：2005-01-20
申请号：JP2004268608
申请日：2004-09-15
申请人： Pfizer Inc , ファイザー・インク
发明人： MAW GRAHAM NIGEL , WAYMAN CHRISTOPHER PETER
IPC分类号： C12N9/99 , A01K67/027 , A61K20060101 , A61K31/00 , A61K31/122 , A61K31/137 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/19 , A61K31/191 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/197 , A61K31/198 , A61K31/215 , A61K31/216 , A61K31/223 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/352 , A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/41 , A61K31/4164 , A61K31/4166 , A61K31/4184 , A61K31/421 , A61K31/433 , A61K31/437 , A61K31/438 , A61K31/44 , A61K31/4402 , A61K31/4412 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4706 , A61K31/495 , A61K31/496 , A61K31/4985 , A61K31/499 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/53 , A61K31/548 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , A61K31/65 , A61K31/661 , A61K31/675 , A61K38/00 , A61K38/12 , A61K38/46 , A61K38/55 , A61K45/00 , A61P5/30 , A61P9/14 , A61P15/00 , A61P15/02 , A61P15/08 , A61P15/12 , A61P25/02 , A61P43/00 , C07C233/58 , C07C233/60 , C07C311/51 , C07D207/26 , C07D207/27 , C07D209/12 , C07D213/64 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/85 , C07D215/40 , C07D223/10 , C07D223/16 , C07D233/72 , C07D233/78 , C07D239/95 , C07D251/48 , C07D257/06 , C07D263/34 , C07D267/14 , C07D285/135 , C07D295/02 , C07D295/08 , C07D307/14 , C07D307/24 , C07D307/54 , C07D401/04 , C07D401/12 , C07D403/06 , C07D471/14 , C07D473/30 , C07D473/34 , C07D487/04 , C07D513/04 , C07K14/47 , C07K14/705 , C12N9/64 , C12N9/88 , C12N15/09 , C12Q1/37 , C12Q1/42 , C12Q1/44 , C12Q1/68 , G01N33/15 , G01N33/50 , G01N33/53 , G01N33/573 , G01N33/68
CPC分类号： G01N33/6893 , A01K67/027 , A01K2227/107 , A61K31/00 , A61K31/192 , A61K31/195 , A61K31/352 , A61K31/4015 , A61K31/44 , A61K31/4412 , A61K31/4985 , A61K31/519 , A61K31/52 , A61K31/55 , C12Q1/44 , G01N33/5088 , G01N33/5308 , G01N33/689 , G01N2500/00
摘要： PROBLEM TO BE SOLVED: To provide an effective method for treating a female suffering from female sexual dysfunction (FSD), in particular, female sexual arousal dysfunction (FSAD). SOLUTION: The method comprises assaying an agent capable of potentiating cAMP in the genital argans of the female suffering from the female sexual dysfunction, in particular, female sexual arousal dysfunction. The agent is an inhibitor of a neutral endopeptidase (I:NEP). The method includes an anesthetized female animal including a means for measuring change in blood flow in the genital organs of the animal accompanied with pelvic nerve stimulation. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：要解决的问题：提供一种治疗女性性功能障碍（FSD），特别是女性性唤醒功能障碍（FSAD）的女性的有效方法。解决方案：该方法包括测定能够增强女性性功能障碍的女性生殖器官中的cAMP，特别是女性性唤起功能障碍的药剂。该试剂是中性肽链内切酶（I：NEP）的抑制剂。该方法包括麻醉的雌性动物，包括用于测量伴随着盆腔神经刺激的动物的生殖器官中的血流变化的装置。版权所有（C）2005，JPO＆NCIPI

74. 发明专利

JP2004217668A Indazole derivatives and their use as inhibitor of phosphodiesterase (pde) type iv and production of tumor necrosis factor (tnf) 审中-公开
公开(公告)号：JP2004217668A
公开(公告)日：2004-08-05
申请号：JP2004083812
申请日：2004-03-23
申请人： Pfizer Inc , ファイザー・インク
发明人： MARFAT ANTHONY
IPC分类号： A61K31/00 , A61K31/415 , A61K31/416 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61K31/4709 , A61K31/505 , A61K31/506 , A61P1/00 , A61P1/04 , A61P3/00 , A61P3/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P25/00 , A61P27/16 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/08 , A61P43/00 , C07D231/56 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/04
CPC分类号： C07D403/12 , C07D231/56 , C07D401/12 , C07D409/04
摘要： PROBLEM TO BE SOLVED: To provide a pharmaceutical composition containing a compound or pharmaceutically acceptable salt thereof, and a method of using the compound or pharmaceutically acceptable salt thereof for inhibition of phosphodiesterase (PDE) type IV or production of tumor necrosis factor (TNF) in a mammal, and to provide an intermediate useful for preparation of the compound. SOLUTION: The pharmaceutical composition contains the compound expressed by the formula I or the pharmaceutically acceptable salts thereof. (In the formula I, R is a phenyl group, R 1 is a 1-9C alkyl group, R 2 is a phenyl, naphthyl, pyrrolyl, furanyl, thienyl, oxazolyl, pyridinyl, pyrimidinyl, pyridazinyl. quinolinyl, isoquinolinyl, 5, 6, 7, 8-tetrahydroquinolinyl or 5, 6, 7, 8-tetrahydroisoquinolinyl). COPYRIGHT: (C)2004,JPO&NCIPI

75. 发明专利

JP2004107324A Therapeutic agent containing 4-arylpiperidine and method for producing the same 审中-公开
标题翻译：包含4-亚氨基哌啶的治疗剂及其制备方法
公开(公告)号：JP2004107324A
公开(公告)日：2004-04-08
申请号：JP2003206497
申请日：2003-08-07
申请人： Pfizer Inc , ファイザー・インク
发明人： RICHARD EDWARD ARMOUR , DAVID MORRIS GEESHIN , STEPHEN PAUL GIBSON , IVAN TOMASINI
IPC分类号： A61K31/445 , A61K31/451 , A61P1/00 , A61P1/08 , A61P1/10 , A61P15/00 , A61P17/00 , A61P17/04 , A61P19/00 , A61P25/00 , A61P25/24 , A61P25/30 , A61P25/32 , A61P25/34 , A61P37/00 , A61P37/02 , C07D211/14 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/34
CPC分类号： C07D211/34 , C07D211/14 , C07D211/22 , C07D211/32
摘要： PROBLEM TO BE SOLVED: To obtain a therapeutic agent containing a 4-arylpiperidine, and to provide a method for producing the same compound. SOLUTION: The therapeutic agent contains a compound expressed by formula (1) [e.g. 1-hexyl-3, 4-dimethyl-4-(3-cyanophenyl)piperidine]. The therapeutic agent is useful for the prevention and treatment of diseases mediated by an opiate receptor (e.g. itching symptom). COPYRIGHT: (C)2004,JPO
摘要翻译：待解决的问题：获得含有4-芳基哌啶的治疗剂，并提供其制备方法。治疗剂含有式（1）表示的化合物[例如， 1-己基-3,4-二甲基-4-（3-氰基苯基）哌啶]。治疗剂可用于预防和治疗由阿片受体介导的疾病（例如瘙痒症状）。版权所有（C）2004，JPO

76. 发明专利

JP2004099618A Piperidine as ccr5 modulator 审中-公开
公开(公告)号：JP2004099618A
公开(公告)日：2004-04-02
申请号：JP2003358714
申请日：2003-10-20
申请人： Pfizer Inc , ファイザー・インク
发明人： ARMOUR DUNCAN ROBERT , PRICE DAVID ANTHONY , STAMMEN BLANDA LUZIA CHRISTA , WOOD ANTHONY , PERROS MANOUSSOS , EDWARDS MARTIN PAUL
IPC分类号： G01N33/50 , A61K20060101 , A61K31/4245 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/46 , A61K31/496 , A61K31/5377 , A61K45/00 , A61P11/00 , A61P11/06 , A61P27/00 , A61P29/00 , A61P31/00 , A61P31/14 , A61P31/18 , A61P43/00 , C07D20060101 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D451/02 , C07D451/04 , C07D498/08 , G01N33/15
CPC分类号： C07D451/02 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D451/04
摘要： PROBLEM TO BE SOLVED: To provide a therapeutic and preventive agent for antiinflammatory diseases, HIV-1 and genetic retrovirus infections. SOLUTION: The medicinal formulation comprising a piperidine derivative represented by chemical formula 1, chemical formula 2 or the like is useful as a modulator having chemokine activity. COPYRIGHT: (C)2004,JPO

77. 发明专利

JP2004099598A New isoxazole-sulfonamide endothelin antagonist 审中-公开
公开(公告)号：JP2004099598A
公开(公告)日：2004-04-02
申请号：JP2003198903
申请日：2003-07-18
申请人： Pfizer Inc , ファイザー・インク
发明人： BANKS BERNARD JOSEPH , CHUBB NATHAN ANTHONY LOGAN , ESHELBY JAMES JOHN , PACEY MICHAEL STEPHEN , SCHULZ DARREN JOHN
IPC分类号： C07D413/14 , A61K31/506 , A61P7/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/08 , A61P13/08 , A61P13/12 , A61P15/10 , A61P25/00 , A61P27/06 , A61P35/00 , A61P37/08 , A61P43/00 , C07D231/52 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
CPC分类号： C07D401/12 , C07D231/52 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： PROBLEM TO BE SOLVED: To obtain a new compound expressing preferable selectivity to ET
A than to ET
B to endothelin receptor.
SOLUTION: The new isoxazole sulfonamide compound is expressed by general formula 1, wherein R
1 expresses a phenyl, a 5- or 6-membered heterocycle or the like; R
2 expresses an aryl, a het
1 or the like; R
3 expresses H, an alkyl, an aryl, a het
1 or the like; het
1 expresses a 5- to 7-membered heterocyclic group which may be benzofused. For example, a compound expressed by the formula is cited.
COPYRIGHT: (C)2004,JPO

78. 发明专利

JP2004043477A Dipeptide derivative as growth hormone secretion-accelerating agent 有权
公开(公告)号：JP2004043477A
公开(公告)日：2004-02-12
申请号：JP2003271598
申请日：2003-07-07
申请人： Pfizer Inc , ファイザー・インク
发明人： CARPINO PHILIP ALBERT , GRIFFITH DAVID ANDREW , LEFKER BRUCE ALLEN
IPC分类号： A61K31/138 , A61K31/40 , A61K31/4168 , A61K31/4174 , A61K31/437 , A61K31/4439 , A61K31/4453 , A61K31/4535 , A61K31/4725 , A61K31/4985 , A61K31/565 , A61K31/663 , A61K38/00 , A61K38/04 , A61K38/22 , A61K38/23 , A61K38/27 , A61K45/00 , A61P3/00 , A61P3/02 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/06 , A61P5/10 , A61P7/00 , A61P9/04 , A61P13/12 , A61P15/00 , A61P15/14 , A61P17/00 , A61P17/02 , A61P19/00 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/02 , A61P25/20 , A61P43/00 , C07D471/04 , C07D487/04 , C07D491/04 , C07D498/04 , C07D513/04 , C07K1/02 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/062
CPC分类号： C07D487/04 , A61K38/00 , C07D471/04 , C07D491/04 , C07D513/04 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06026
摘要： PROBLEM TO BE SOLVED: To provide a compound having a growth hormone secretion-accelerating activity and increasing the level of endogeneous growth hormone and its pharmaceutically permissible salts, and a medicinal composition containing the same. SOLUTION: This dipeptide derivative expressed by formula 1 increases the endogeneous production or release of the growth hormone of human or other animals, and useful for the treatment and prevention of osteoporosis and/or weakness. Also, the medicinal composition obtained by combining a bisphosphonic acid salt compound such as alendronate, etc., estrogen, premarin, calcitonin, etc., with the dipeptide is useful for the treatment. COPYRIGHT: (C)2004,JPO

79. 发明专利

JP2004002309A NON-PEPTIDIC GnRH AGENT, PHARMACEUTICAL COMPOSITION, AND METHOD OF USING THEM 审中-公开
公开(公告)号：JP2004002309A
公开(公告)日：2004-01-08
申请号：JP2003034331
申请日：2003-02-12
申请人： Pfizer Inc , ファイザー・インク
发明人： CHRISTIE LANCE CHRISTOPHER , ANDERSON MARK BRIAN , FENG JUN , HONG YUFENG , PATHAK VED PRAKASH , RAJAPAKSE RANJAN JAGATH , TOMPKINS EILEEN VALENZUELA , VAZIR HARESH NARENDRA , LI HAITAO
IPC分类号： A61K31/506 , A61K31/519 , A61K31/5355 , A61P5/02 , A61P5/04 , A61P13/08 , A61P15/00 , A61P15/08 , A61P15/16 , A61P19/04 , A61P25/20 , A61P35/00 , C07D405/12 , C07D405/14 , C07D407/14 , C07D471/04
CPC分类号： C07D405/14 , C07D405/12 , C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide a non-peptidic GnRH agent inhibiting the activity of gonadotropin-releasing hormone, and to provide a pharmaceutical composition containing the agent. SOLUTION: The non-peptidic GnRH agent is a compound of formula(I)[ e.g. 5-(1,1,3,3,6-pentamethyl-1,3-dihydro-isobenzofuran-5-ylmethyl)-furan-2-carboxylic acid (2,4,6-trimethoxy-pyrimidin-5-yl)-amide ] or a compound of formula(II)[ e.g. N-(2-ä[3-(dimethylamino)propyl]amino}-4,6-dimethoxypyrimidin-5-yl)-5-[(3,3,4,6,-tetramethyl-2,3-dihydro-1-benzofuran-7-yl)methyl]-2-furamide ]. The pharmaceutical composition, when expressing gonadotropin release inhibition, is useful for treating the reproduction disorders and steroid hormone dependent tumors and modulating the fertility of mammals. COPYRIGHT: (C)2004,JPO

80. 发明专利

JP2003286195A Controlling agent for activity of pde11a 审中-公开
标题翻译： PDE11A活性控制剂
公开(公告)号：JP2003286195A
公开(公告)日：2003-10-07
申请号：JP2003043929
申请日：2003-02-21
申请人： Pfizer Inc , ファイザー・インク
发明人： BURSLEM MARTYN FRANK , HARROW IAN DENNIS , LANFEAR JEREMY , PHILLIPS STEPHEN CHARLES , WAYMAN CHRISTOPHER PETER
IPC分类号： C12N15/09 , A61K31/00 , A61K31/498 , A61K31/4985 , A61K31/517 , A61K45/00 , A61P15/00 , A61P15/08 , A61P15/16 , A61P15/18 , C07D403/04 , C07D405/14 , C07D487/14
CPC分类号： A61K31/498 , A61K31/00 , A61K31/4985
摘要： PROBLEM TO BE SOLVED: To obtain a medicinal composition containing a controlling agent for activity of PDE11A, for controlling capacitation of sperm in vitro or ex vivo. SOLUTION: This invention relates to controlling efficacy of the PDE11A to male capacitation, male contraception, and female sexual function disorder (FSD), especially female sexual arousal disorder (FSAD), female orgasmic disorder (FOD), hypoactivity of sexual drive disturbance (HSDD) or disorders due to vaginal spasm. COPYRIGHT: (C)2004,JPO

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