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1. 发明申请

WO2005123670A3 CRYSTALLINE FORM OF A SUBSTITUTED PYRROLIDINE COMPOUND 审中-公开
标题翻译：取代的吡咯烷酮化合物的结晶形式
公开(公告)号：WO2005123670A3
公开(公告)日：2006-02-09
申请号：PCT/US2005020282
申请日：2005-06-09
申请人： THERAVANCE INC , LI LI , CHAO ROBERT S , HUGHES ADAM , JI YU-HUA , KHOSSRAVI DAVAR , ZHANG WEIJIANG
发明人： LI LI , CHAO ROBERT S , HUGHES ADAM , JI YU-HUA , KHOSSRAVI DAVAR , ZHANG WEIJIANG
IPC分类号： C07D207/09 , A61K31/40 , A61P11/06 , A61P11/08 , C07D207/30
CPC分类号： C07D207/09
摘要： The invention provides a crystalline naphthalene-1,5-disulfonic acid salt of 2-[(S)-1-(8-methylaminooctyl)pyrrolidin-3-yl]-2,2-diphenylacetamide or a solvate thereof. This invention also provides pharmaceutical compositions comprising the salt or prepared using the salt; processes and intermediates for preparing the salt; and methods of using the salt to treat a pulmonary disorder.
摘要翻译：本发明提供2 - [（S）-1-（8-甲基氨基辛基）吡咯烷-3-基] -2,2-二苯基乙酰胺或其溶剂合物的结晶萘-1,5-二磺酸盐。本发明还提供了包含该盐或使用该盐制备的药物组合物; 制备盐的方法和中间体; 以及使用盐治疗肺部疾病的方法。

2. 发明申请

WO1994020505A1 CRYSTALLINE CEFTIOFUR FREE ACID 审中-公开
标题翻译：结晶CEFTIOFUR自由酸
公开(公告)号：WO1994020505A1
公开(公告)日：1994-09-15
申请号：PCT/US1994001862
申请日：1994-03-07
申请人： THE UPJOHN COMPANY , DUNN, Michael, J. , BERGREN, Michael, S. , HARDEE, Gregory, E. , SHEPHARD, Kenneth, Paul , CHAO, Robert, S. , HAVENS, Jeffrey, L.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D501/36
CPC分类号： C07D501/00 , A61K31/545
摘要： Anhydrous and crystalline free acid form of the cephalosporin antiobiotic ceftiofur, processes for its manufacture, and pharmaceutical compositions containing it are provided.
摘要翻译：提供了头孢菌素抗生素头孢噻呋的无水和结晶游离酸形式，其制备方法和含有其的药物组合物。

3. 发明申请

WO2004032854A2 PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF PARKINSON'S DISEASE 审中-公开
标题翻译：用于治疗帕金森病的药物组合物
公开(公告)号：WO2004032854A2
公开(公告)日：2004-04-22
申请号：PCT/US2003/031657
申请日：2003-10-02
申请人： PHARMACIA CORPORATION , HAWLEY, Michael , BERGREN, Michael, S. , NIXON, Phillip, R. , HALSTEAD, Gordon, W. , CHAO, Robert, S. , JU, Tzu-chi, R.
发明人： HAWLEY, Michael , BERGREN, Michael, S. , NIXON, Phillip, R. , HALSTEAD, Gordon, W. , CHAO, Robert, S. , JU, Tzu-chi, R.
IPC分类号： A61K
CPC分类号： C07D471/06 , A61K31/538 , A61K31/542 , A61K31/551 , A61K31/553 , A61K31/554
摘要： A pharmaceutical composition comprising a salt, preferably a crystalline salt, of an organic acid of low water solubility and a compound of formula (I) is provided. The salts are useful in treating Parkinson's disease. Also provided are methods of treatment using the salts and methods of making crystalline forms of the salts.
摘要翻译：提供了包含低水溶性有机酸和式（I）化合物的盐，优选结晶盐的药物组合物。这些盐可用于治疗帕金森病。还提供了使用盐的方法和制备盐的结晶形式的方法。

4. 发明申请

WO2003099797A1 SALTS OF BIS-ARYLSULFONES FOR THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗中枢神经系统疾病的双侧。。。。。。。。。。
公开(公告)号：WO2003099797A1
公开(公告)日：2003-12-04
申请号：PCT/US2003/014535
申请日：2003-05-20
申请人： PHARMACIA & UPJOHN COMPANY , ACKER, Brad, A. , CHAO, Robert, S. , HAWLEY, Michael
发明人： ACKER, Brad, A. , CHAO, Robert, S. , HAWLEY, Michael
IPC分类号： C07D243/08
CPC分类号： C07D243/08
摘要： The present invention provides compounds of the Formula (I): wherein X is selected from HCI, HOC(O)CF 3 , cis-HO(CO)-CH=CH-(CO)OH, and Formula (II). In another aspect, the invention further provides a pharmaceutical composition including a compound of the Formula (I) and a pharmaceutically acceptable carrier. In certain embodiments of this aspect of the invention, the composition includes a therapeutically effective amount of a compound of the Formula (I). In another aspect, the present invention further provides a method for treating or preventing diseases or disorders of the central nervous system comprising administering a therapeutically effective amount of a compound of the Formula (I) to a mammal. In certain embodiment, the compound of the Formula (I) may be used to prepare a medicament for treating or preventing diseases or disorders of the central nervous system. In yet another aspect, the invention provides a method for treating a disease or condition in a mammal wherein a 5-HT receptor is implicated and modulation of a 5-HT function is desired comprising administering to the mammal a therapeutically effective amount of a compound of the Formula (I).
摘要翻译：本发明提供式（I）的化合物：其中X选自HCl，HOC（O）CF 3，顺式-OC（CO）-CH = CH-（CO）OH和式（II））。另一方面，本发明还提供包含式（I）的化合物和药学上可接受的载体的药物组合物。在本发明该方面的某些实施方案中，组合物包括治疗有效量的式（I）化合物。另一方面，本发明还提供了治疗或预防中枢神经系统疾病或病症的方法，包括向哺乳动物施用治疗有效量的式（I）化合物。在某些实施方案中，式（I）化合物可用于制备用于治疗或预防中枢神经系统疾病或病症的药物。另一方面，本发明提供了一种治疗哺乳动物疾病或病症的方法，其中涉及5-HT受体并需要调节5-HT功能，包括向哺乳动物施用治疗有效量的化合物式（I）。

5. 发明申请

WO2004032854A3 PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF PARKINSON'S DISEASE 审中-公开
标题翻译：用于治疗帕金森病的药物组合物
公开(公告)号：WO2004032854A3
公开(公告)日：2004-09-30
申请号：PCT/US0331657
申请日：2003-10-02
申请人： PHARMACIA CORP , HAWLEY MICHAEL , BERGREN MICHAEL S , NIXON PHILLIP R , HALSTEAD GORDON W , CHAO ROBERT S , JU TZU-CHI R
发明人： HAWLEY MICHAEL , BERGREN MICHAEL S , NIXON PHILLIP R , HALSTEAD GORDON W , CHAO ROBERT S , JU TZU-CHI R
IPC分类号： A61K31/538 , A61K31/542 , A61K31/551 , A61K31/553 , A61K31/554 , C07D471/06 , C07D241/36 , A61K31/415 , A61K31/498 , C07D235/02
CPC分类号： C07D471/06 , A61K31/538 , A61K31/542 , A61K31/551 , A61K31/553 , A61K31/554
摘要： A pharmaceutical composition comprising a salt, preferably a crystalline salt, of an organic acid of low water solubility and a compound of formula (I) is provided. The salts are useful in treating Parkinson's disease. Also provided are methods of treatment using the salts and methods of making crystalline forms of the salts.
摘要翻译：提供了包含盐，优选结晶盐，低水溶性有机酸和式（I）化合物的药物组合物。这些盐可用于治疗帕金森病。还提供了使用盐的处理方法和制备盐的结晶形式的方法。

6. 发明申请

WO2006023454A1 CRYSTALLINE FORM OF A BIPHENYL COMPOUND 审中-公开
标题翻译：苯乙烯化合物的结晶形式
公开(公告)号：WO2006023454A1
公开(公告)日：2006-03-02
申请号：PCT/US2005/029013
申请日：2005-08-15
申请人： THERAVANCE, INC. , CHAO, Robert S. , RAPTA, Miroslav , COLSON, Pierre-Jean
发明人： CHAO, Robert S. , RAPTA, Miroslav , COLSON, Pierre-Jean
IPC分类号： C07D401/12 , A61K31/4709 , A61P11/00
CPC分类号： C07D401/12
摘要： The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[( R )-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
摘要翻译：本发明提供联苯-2-基氨基甲酸1- [2-（2-氯-4 - {[（R）-2-羟基-2-（8-羟基-2- -2-氧代-1,2-二氢喹啉-5-基）乙基氨基]甲基} -5-甲氧基苯基氨基甲酰基）乙基]哌啶-4-基酯或其溶剂合物。本发明还提供了包含这种盐或使用这种盐制备的药物组合物; 制备这种盐的方法和中间体; 以及使用这种盐治疗肺部疾病的方法。

7. 发明申请

WO2005123670A2 CRYSTALLINE FORM OF A SUBSTITUTED PYRROLIDINE COMPOUND 审中-公开
标题翻译：取代的吡咯烷酮化合物的结晶形式
公开(公告)号：WO2005123670A2
公开(公告)日：2005-12-29
申请号：PCT/US2005/020282
申请日：2005-06-09
申请人： THERAVANCE, INC. , LI, Li , CHAO, Robert S. , HUGHES, Adam , JI, Yu-Hua , KHOSSRAVI, Davar , ZHANG, Weijiang
发明人： LI, Li , CHAO, Robert S. , HUGHES, Adam , JI, Yu-Hua , KHOSSRAVI, Davar , ZHANG, Weijiang
IPC分类号： C07D207/09
CPC分类号： C07D207/09
摘要： The invention provides a crystalline naphthalene-1,5-disulfonic acid salt of 2-[(S)-1-(8-methylaminooctyl)pyrrolidin-3-yl]-2,2-diphenylacetamide or a solvate thereof. This invention also provides pharmaceutical compositions comprising the salt or prepared using the salt; processes and intermediates for preparing the salt; and methods of using the salt to treat a pulmonary disorder.
摘要翻译：本发明提供2 - [（S）-1-（8-甲基氨基辛基）吡咯烷-3-基] -2,2-二苯基乙酰胺或其溶剂合物的结晶萘-1,5-二磺酸盐。本发明还提供了包含该盐或使用该盐制备的药物组合物; 制备盐的方法和中间体; 以及使用盐治疗肺部疾病的方法。

8. 发明申请

WO2004014338A1 COMPOSITION AND METHOD FOR RECTAL DELIVERY OF A LINCOSAMIDE ANTIBACTERIAL DRUG 审中-公开
标题翻译：用于线性递送林酰胺抗生素药物的组合物和方法
公开(公告)号：WO2004014338A1
公开(公告)日：2004-02-19
申请号：PCT/US2002/003628
申请日：2002-02-05
申请人： PHARMACIA & UPJOHN COMPANY , PENA, Lorraine, E. , BOWMAN, Phil, B. , CHAO, Robert, S. , PESHECK, Carolyn, V. , JACOBSEN, Clayton, W.
发明人： PENA, Lorraine, E. , BOWMAN, Phil, B. , CHAO, Robert, S. , PESHECK, Carolyn, V. , JACOBSEN, Clayton, W.
IPC分类号： A61K9/02
CPC分类号： A61K9/02
摘要： A suppository composition and method for rectal administration of a lincosamide antibacterial drug, such as clindamycin, lincomycin, or pirlimycin, is disclosed. The composition is a rectal suppository containing an antimicrobially effective amount of the linconsamide in particulate form dispersed in a Hard Fat suppository base, preferably a Hard Fat NF suppository base. The most preferred suppository compositions of the present invention have long term storage stability, while maintaining effectiveness against bacterial infections.
摘要翻译：公开了用于直肠给药林可酰胺抗菌药物的栓剂组合物和方法，例如克林霉素，林可霉素或普瑞霉素。该组合物是含有抗微生物有效量的分散在硬脂肪栓剂基质，优选硬脂肪NF栓剂基质中的颗粒形式的林可酰胺的直肠栓剂。本发明最优选的栓剂组合物具有长期的保存稳定性，同时保持对细菌感染的有效性。

9. 发明申请

WO2003020736A1 CRYSTALINE CLINDAMYCIN FREE BASE 审中-公开
标题翻译：水晶蛋白酶自由基
公开(公告)号：WO2003020736A1
公开(公告)日：2003-03-13
申请号：PCT/US2002/027159
申请日：2002-08-26
申请人： PHARMACIA CORPORATION , CHAO, Robert, S. , HAWLEY, Michael , REEDER, Lisa, M. , JONES, Donald, P.
发明人： CHAO, Robert, S. , HAWLEY, Michael , REEDER, Lisa, M. , JONES, Donald, P.
IPC分类号： C07H15/00
CPC分类号： C07H13/10 , C07H15/16 , C07H15/26
摘要： The antibiotic drug clindamycin is provided as a crystalline free base. Three polymorphic/pseudopolymorphic forms of crystalline clindamycin free base are disclosed. Also provided are pharmaceutical compositions comprising crystalline clindamycin free base. Processes for preparing crystalline clindamycin free base and compositions thereof are also provided along with methods for treating medical conditions with the pharmaceutical compositions.
摘要翻译：提供抗生素药物克林霉素作为结晶游离碱。公开了结晶克林霉素游离碱的三种多晶型/假多晶型形式。还提供了包含结晶克林霉素游离碱的药物组合物。还提供了制备结晶克林霉素游离碱及其组合物的方法以及用药物组合物治疗医学病症的方法。

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