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1. 发明申请

WO2003007954A3 SULFONYL ARYL HYDROXAMATES AND THEIR USE AS MATRIX METALLOPROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2003007954A3
公开(公告)日：2003-01-30
申请号：PCT/US2002/023219
申请日：2002-07-19
申请人： PHARMACIA CORPORATION , MCDONALD, Joseph, J. , BARTA, Thomas, E. , BECKER, Daniel, P. , BEDELL, Louis, J. , RAO, Shashidhar, N. , FRESKOS, John, N. , DE CRESCENZO, Gary, A. , MISCHKE, Brent, V. , GETMAN, Daniel, P. , VILLAMIL, Clara, I.
发明人： MCDONALD, Joseph, J. , BARTA, Thomas, E. , BECKER, Daniel, P. , BEDELL, Louis, J. , RAO, Shashidhar, N. , FRESKOS, John, N. , DE CRESCENZO, Gary, A. , MISCHKE, Brent, V. , GETMAN, Daniel, P. , VILLAMIL, Clara, I.
IPC分类号： A61K31/445
摘要： The invention is directed to sulfonyl aromatic hydroxamic acid compounds and salts thereof that, inter alia , inhibit matrix metalloprotease (MMP) activity and/or aggrecanase activity. In some particularly preferred embodiments, the compound corresponds in structure to one of the following formulas: (I) (II) wherein W 2 , the R groups, and -A-R-E-Y are described in more detail in Applicants'specification. This invention also is directed to a process that comprises administering such a compound or pharmaceutically acceptable salt thereof to a host animal having a condition associated with MMP activity.

2. 发明申请

WO2003007930A3 USE OF SULFONYL ARYL OR HETEROARYL HYDROXAMIC ACIDS AND DERIVATIVES THEREOF AS AGGRECANASE INHIBITORS 审中-公开
公开(公告)号：WO2003007930A3
公开(公告)日：2003-01-30
申请号：PCT/US2002/022867
申请日：2002-07-19
申请人： PHARMACIA CORPORATION , MCDONALD, Joseph, J. , BARTA, Thomas, A. , ARNER, Elizabeth , BOEHM, Terri, L. , BECKER, Daniel, P. , DECRESCENZO, Gary, A.
发明人： MCDONALD, Joseph, J. , BARTA, Thomas, A. , ARNER, Elizabeth , BOEHM, Terri, L. , BECKER, Daniel, P. , DECRESCENZO, Gary, A.
IPC分类号： A61K31/445
摘要： This invention is directed to a process for inhibiting aggrecanase activity. The process comprises administering a therapeutically effective amount of a sulfonyl aromatic or heteroaromatic hydroxamic acid, a derivative thereof, or a pharmaceutically acceptable salt of the hydroxamic acid or derivative to a host animal. The compound generally corresponds in structure to the following formula: , wherein W and the R groups are described in more detail in Applicants' specification.

3. 发明申请

WO1992015590A1 NEW MESO-AZACYCLIC AROMATIC ACID AMIDES AND ESTERS AS NOVEL SEROTONERGIC AGENTS 审中-公开
标题翻译：新型谷物酸性氨基酸和酯类作为新型血清代谢剂
公开(公告)号：WO1992015590A1
公开(公告)日：1992-09-17
申请号：PCT/US1992001525
申请日：1992-03-04
申请人： G.D. SEARLE & CO. , BECKER, Daniel, P. , FLYNN, Daniel, L. , MOORMANN, Alan, Edward , NOSAL, Roger , VILLAMIL, Clara, I.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D487/04
CPC分类号： C07D471/08 , C07D487/04 , C07D487/08
摘要： Meso-azacyclic aromatic acid amides and esters of formula Ar-(CO-X)p-Z wherein Ar represents a radical of formulae (A, B) and when p is 1, Ar represents a radical of formulae (C, D, E, F, G, H) and Z represents a radical of formulae (I, J) are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrome, and the like. Additionally, they find utility as antagonists of serotonin 5-HT3 receptors, and are useful for the treatment of humans and animals wherein antagonism of 5-HT3 receptors is beneficial. Therapy is indicated for the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, they may find utility as enhancers of nasal absorption of bioactive compounds.
摘要翻译：中间阿唑环芳酰胺和式Ar-（CO-X）pZ的酯，其中Ar表示式（A，B）的基团，当p为1时，Ar表示式（C，D，E，F ，G，H）和Z表示式（I，J）的基团可用于治疗中枢神经系统和胃肠动力障碍，例如胃食管反流，非溃疡性消化不良，胃排空迟缓，肠梗阻，肠易激综合征，等等。另外，它们可用作5-羟色胺5-HT 3受体的拮抗剂，并且可用于治疗其中5-HT 3受体拮抗作用有益的人和动物。治疗指示用于治疗焦虑，精神病，抑郁症（特别是伴有焦虑症的抑郁症），认知障碍，药物滥用依赖和/或戒断，肠易激综合征，由化学治疗剂引起的呕吐和内脏痛。此外，它们可能发现作为生物活性化合物的鼻吸收的增强剂。

4. 发明申请

WO2011085022A1 INHALATION DEVICE AND METHOD 审中-公开
标题翻译：吸入装置和方法
公开(公告)号：WO2011085022A1
公开(公告)日：2011-07-14
申请号：PCT/US2011/020252
申请日：2011-01-05
申请人： MICRODOSE THERAPEUTX, INC. , AKOUKA, Henri, M. , BECKER, Daniel, P.
发明人： AKOUKA, Henri, M. , BECKER, Daniel, P.
IPC分类号： A61M15/00 , A61M16/00
CPC分类号： A61M15/0051 , A61M15/001 , A61M15/0021 , A61M15/0043 , A61M15/0045 , A61M15/005 , A61M15/0055 , A61M15/0065 , A61M15/0085 , A61M2016/0021 , A61M2202/0266 , A61M2202/062 , A61M2202/064 , A61M2205/0294 , A61M2205/12 , A61M2205/8206 , A61M2250/00
摘要： The present disclosure provides a method and device for delivering a pharmaceutical to the airway of a human or animal patient. In one aspect, the device includes a dose drum formed into a cylinder and including a plurality of dose compartments for containing individual doses. In another aspect, the device may include a reservoir containing a pharmaceutical material in bulk form and a metering recess for metering the pharmaceutical material to form a pharmaceutical dose. Another aspect provides an inhaler with a combined reservoir and dosing chamber configured to contain multiple doses of a pharmaceutical material.
摘要翻译：本公开提供了用于将药物递送到人或动物患者的气道的方法和装置。在一个方面，该装置包括形成为圆柱体并包括用于容纳各个剂量的多个剂量隔室的剂量鼓。在另一方面，该装置可以包括容纳散装形式的药物材料的储存器和用于计量药物材料以形成药物剂量的计量凹槽。另一方面提供一种具有组合储存器和剂量室的吸入器，其配置成容纳多剂量的药物材料。

5. 发明申请

WO2002092588A2 AROMATIC SULFONE HYDROXAMATES AND THEIR USE AS PROTEASE INHIBITORS 审中-公开
标题翻译：芳香磺酸羟肟酸酯及其作为蛋白酶抑制剂的用途
公开(公告)号：WO2002092588A2
公开(公告)日：2002-11-21
申请号：PCT/US2002/015257
申请日：2002-05-10
申请人： PHARMACIA CORPORATION , BARTA, Thomas, E. , BECKER, Daniel, P. , BEDELL, Louis, J. , BOEHM, Terri, L. , FOBIAN, Yvette, M. , FRESKOS, John, N. , HOCKERMAN, Susan L. , KASSAB, Darren, J. , KOLODZIEJ, Steve, A. , MCDONALD, Joseph, J. , NORTON, Monica, B. , RICO, Joseph, G. , TALLEY, John, J. , VILLAMIL, Clara, I. , WANG, Tijuan, Jane
发明人： BARTA, Thomas, E. , BECKER, Daniel, P. , BEDELL, Louis, J. , BOEHM, Terri, L. , FOBIAN, Yvette, M. , FRESKOS, John, N. , HOCKERMAN, Susan L. , KASSAB, Darren, J. , KOLODZIEJ, Steve, A. , MCDONALD, Joseph, J. , NORTON, Monica, B. , RICO, Joseph, G. , TALLEY, John, J. , VILLAMIL, Clara, I. , WANG, Tijuan, Jane
IPC分类号： C07D309/08
CPC分类号： C07D401/12 , A61K31/351 , A61K31/41 , A61K31/453 , A61K31/454 , C04B35/632 , C07D211/66 , C07D309/08 , C07D309/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , Y02A50/411
摘要： This invention is directed to aromatic sulfone hydroxamates (also known as "aromatic sulfone hydroxamic acids") and salts thereof that, inter alia , inhibit matrix metalloproteinase (also known as "matrix metalloprotease" or "MMP") activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
摘要翻译：本发明涉及芳族砜异羟肟酸盐（也称为“芳族砜异羟肟酸”）及其盐，其特别是抑制基质金属蛋白酶（也称为“基质金属蛋白酶”或“MMP”）活性和/或蛋白聚糖蛋白聚糖酶活性。本发明还涉及一种预防或治疗方法，其包括将有效量的MMP抑制和/或聚集蛋白聚糖蛋白酶抑制剂的这种化合物或盐施用于动物，特别是哺乳动物，所述动物特别是哺乳动物具有（或设置为）具有相关的病理状态具有MMP和/或蛋白聚糖蛋白聚糖酶活性。

6. 发明申请

WO1996037485A1 2-AMINO-BENZOXAZINONES FOR THE TREATMENT OF VIRAL INFECTIONS 审中-公开
标题翻译：用于治疗病毒感染的2-氨基苯甲酰胺
公开(公告)号：WO1996037485A1
公开(公告)日：1996-11-28
申请号：PCT/US1996007526
申请日：1996-05-23
申请人： G.D. SEARLE & CO. , ABOOD, Norman , FLYNN, Daniel, L. , BECKER, Daniel, P. , BAX, Brian, M. , LI, Hui , NOSAL, Roger, A. , SCHRETZMAN, Lori, A. , VILLAMIL, Clara, I. , BENNETT, Michael, J. , BEDELL, John, L. , WILLIAMS, Kenneth
发明人： G.D. SEARLE & CO.
IPC分类号： C07D265/24
CPC分类号： C07D265/24 , C07D413/04 , C07D413/12 , C07D417/12
摘要： A class of compounds for the treatment of viral infections. Compounds of particular interest are defined by formula (I) wherein R - R are as defined herein, or a pharmaceutically-acceptable salt thereof.
摘要翻译：一类用于治疗病毒感染的化合物。特别感兴趣的化合物由式（I）定义，其中R-R 4如本文所定义，或其药学上可接受的盐。

7. 发明申请

WO1995029897A1 METHOD OF USING (H+/K+) ATPase INHIBITORS AS ANTIVIRAL AGENTS 审中-公开
标题翻译：使用（H + / K +）ATP酶抑制剂作为抗病毒剂的方法
公开(公告)号：WO1995029897A1
公开(公告)日：1995-11-09
申请号：PCT/US1995005021
申请日：1995-05-01
申请人： G.D. SEARLE & CO. , MOORMANN, Alan, E. , BECKER, Daniel, P. , FLYNN, Daniel, L. , LI, Hui , VILLAMIL, Clara, I.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D235/28
CPC分类号： C07D401/12 , A61K31/00 , A61K31/4164 , A61K31/4184 , A61K31/437 , A61K31/4402 , A61K31/4439 , C07D235/28 , C07D403/12
摘要： A class of compounds which are (H /K ) ATPase inhibitors can be used for the treatment of viral infections. Compounds of particular interest are defined by formula (III), wherein D is N or CH; wherein R is one or more radicals selected from hydrido, alkoxy, amino, cyano, nitro, hydroxyl, alkyl, halo, haloalkyl, carboxyl, alkanoyl, nitro, amino, alkylamino, aminocarbonyl, aminosulfonyl, alkylaminocarbonyl, alkylcarbonylamino, alkoxycarbonyl, alkylaminosulfonyl, alkylsulfonylamino, alkylthio, alkylsulfinyl and alkylsulfonyl; wherein R is selected from hydrido, alkyl and cycloalkyl; wherein R is one or more radicals selected from hydrido, alkoxy, amino, alkyl, halo, cyano, nitro, hydroxyl, haloalkyl, nitro, carboxyl, alkanoyl, amino, alkylamino, dialkylamino, aminocarbonyl, alkylaminocarbonyl, alkylcarbonylamino, aminosulfonyl, alkylaminosulfonyl, alkylsulfonylamino, alkoxycarbonyl, alkylthio, alkylsulfinyl and alkylsulfonyl; and wherein R and R are independently selected from hydrido, alkyl, aryl, alkylcarbonyl and arylcarbonyl wherein the aryl ring may be further substituted with one or more radicals selected from alkyl, halo, hydrazidylcarbonyl, aminocarbonyl and alkoxy; or wherein R and R together with the nitrogen atom form a heterocyclic ring; or a pharmaceutically acceptable salt thereof.
摘要翻译：一类作为（H + / K +）ATP酶抑制剂的化合物可用于治疗病毒感染。特别感兴趣的化合物由式（III）定义，其中D是N或CH; 其中R 7是一个或多个选自氢，烷氧基，氨基，氰基，硝基，羟基，烷基，卤素，卤代烷基，羧基，烷酰基，硝基，氨基，烷基氨基，氨基羰基，氨基磺酰基，烷基氨基羰基，烷基羰基氨基，烷氧基羰基，烷基氨基磺酰基，烷基磺酰基氨基，烷硫基，烷基亚磺酰基和烷基磺酰基; 其中R 8选自氢，烷基和环烷基; 其中R 9是一个或多个选自氢，烷氧基，氨基，烷基，卤素，氰基，硝基，羟基，卤代烷基，硝基，羧基，烷酰基，氨基，烷基氨基，二烷基氨基，氨基羰基，烷基氨基羰基，烷基羰基氨基，氨基磺酰基，烷基氨基磺酰基，烷基磺酰基氨基，烷氧基羰基，烷硫基，烷基亚磺酰基和烷基磺酰基; 并且其中R 10和R 11独立地选自氢，烷基，芳基，烷基羰基和芳基羰基，其中所述芳基环可以进一步被一个或多个选自烷基，卤素，肼基羰基，氨基羰基和烷氧基的基团取代; 或其中R 10和R 11与氮原子一起形成杂环; 或其药学上可接受的盐。

8. 发明申请

WO1992015593A1 NEW IMIDAZOPYRIDINES AS SEROTONERGIC 5-HT3 ANTAGONISTS 审中-公开
标题翻译：新的咪达唑啶作为SERONONGIC 5-HT3拮抗剂
公开(公告)号：WO1992015593A1
公开(公告)日：1992-09-17
申请号：PCT/US1992001524
申请日：1992-03-04
申请人： G.D. SEARLE & CO. , BECKER, Daniel, P. , FLYNN, Daniel, L. , MOORMANN, Alan, Edward , NOSAL, Roger , VILLAMIL, Clara, I.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D519/00
CPC分类号： C07D471/04
摘要： The imidazopyridines compounds of the present invention are serotonergic 5-HT3 antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.

9. 发明申请

WO2004048368A3 HETEROARYLSULFONYLMETHYL HYDROXAMIC ACIDS AND AMIDES AND THEIR USE AS PROTEASE INHIBITORS 审中-公开
标题翻译：羟丙基甲基羟乙酸和氨基酸及其作为蛋白酶抑制剂的用途
公开(公告)号：WO2004048368A3
公开(公告)日：2004-08-12
申请号：PCT/US0337942
申请日：2003-11-24
申请人： PHARMACIA CORP , BECKER DANIEL P , CARROLL JEFFERY N , FOBIAN YVETTE M , GRAPPERHAUS MARGARET L , HANSEN DONALD W JR , HEINTZ ROBERT M , KASSAB DARREN J , MASSA MARK A , MCDONALD JOSEPH J , NAGY MARK A , PITZELE BARNETT S , RICO JOSEPH G , SCHMIDT MICHELLE A , SPANGLER DALE P
发明人： BECKER DANIEL P , CARROLL JEFFERY N , FOBIAN YVETTE M , GRAPPERHAUS MARGARET L , HANSEN DONALD W JR , HEINTZ ROBERT M , KASSAB DARREN J , MASSA MARK A , MCDONALD JOSEPH J , NAGY MARK A , PITZELE BARNETT S , RICO JOSEPH G , SCHMIDT MICHELLE A , SPANGLER DALE P
IPC分类号： A61P9/10 , A61P19/00 , A61P35/00 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07D513/04 , A61K31/41 , A61K31/425 , A61K31/435
CPC分类号： C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： This invention is directed generally to heteroarylsulfonylmethyl hydroxamic acids and amides that, inter alia, tend to inhibit protease activity, particularly matrix metalloproteinase (also known as "matrix metalloprotease" or "MMP") activity and/or aggrecanase activity. This invention also is directed to compositions of such compounds; intermediates for the syntheses of such compounds; methods for making such compounds; and methods for treating conditions associated with MMP, tumor necrosis factors (or "TNFs"), and/or aggrecanase activity, particularly pathological conditions.
摘要翻译：本发明通常涉及杂芳基磺酰基甲基异羟肟酸和酰胺，其特别是倾向于抑制蛋白酶活性，特别是基质金属蛋白酶（也称为“基质金属蛋白酶”或“MMP”）活性和/或软骨聚集蛋白聚糖酶活性。本发明还涉及这些化合物的组合物; 用于合成这些化合物的中间体; 制备这些化合物的方法; 以及用于治疗与MMP相关的病症，肿瘤坏死因子（或“TNFs”）和/或软骨聚集蛋白聚糖酶活性，特别是病理状况的方法。

10. 发明申请

WO2004048368A2 HETEROARYLSULFONYLMETHYL HYDROXAMIC ACIDS AND AMIDES AND THEIR USE AS PROTEASE INHIBITORS 审中-公开
标题翻译：杂芳基磺酰基甲基羟肟酸和酰胺及其作为蛋白酶抑制剂的用途
公开(公告)号：WO2004048368A2
公开(公告)日：2004-06-10
申请号：PCT/US2003/037942
申请日：2003-11-24
申请人： PHARMACIA CORPORATION , BECKER, Daniel, P. , CARROLL, Jeffery, N. , FOBIAN, Yvette, M. , GRAPPERHAUS, Margaret, L. , HANSEN, Donald, W., Jr. , HEINTZ, Robert, M. , KASSAB, Darren, J. , MASSA, Mark, A. , MCDONALD, Joseph, J. , NAGY, Mark, A. , PITZELE, Barnett, S. , RICO, Joseph, G. , SCHMIDT, Michelle, A. , SPANGLER, Dale, P.
发明人： BECKER, Daniel, P. , CARROLL, Jeffery, N. , FOBIAN, Yvette, M. , GRAPPERHAUS, Margaret, L. , HANSEN, Donald, W., Jr. , HEINTZ, Robert, M. , KASSAB, Darren, J. , MASSA, Mark, A. , MCDONALD, Joseph, J. , NAGY, Mark, A. , PITZELE, Barnett, S. , RICO, Joseph, G. , SCHMIDT, Michelle, A. , SPANGLER, Dale, P.
IPC分类号： C07D409/00
CPC分类号： C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： This invention is directed generally to heteroarylsulfonylmethyl hydroxamic acids and amides that, inter alia, tend to inhibit protease activity, particularly matrix metalloproteinase (also known as "matrix metalloprotease" or "MMP") activity and/or aggrecanase activity. This invention also is directed to compositions of such compounds; intermediates for the syntheses of such compounds; methods for making such compounds; and methods for treating conditions associated with MMP, tumor necrosis factors (or "TNFs"), and/or aggrecanase activity, particularly pathological conditions.
摘要翻译：本发明通常涉及杂芳基磺酰基甲基异羟肟酸和酰胺，其特别倾向于抑制蛋白酶活性，特别是基质金属蛋白酶（也称为“基质金属蛋白酶”或 “MMP”）活性和/或聚集蛋白聚糖酶活性。本发明还涉及这些化合物的组合物; 用于合成这些化合物的中间体; 制造这种化合物的方法; 和治疗与MMP，肿瘤坏死因子（或“TNF”）和/或聚集蛋白聚糖酶活性，特别是病理学病症有关的病症的方法。

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