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61. 发明公开

EP0597540A1 Aryl-fused and hetaryl-fused-2,4-diazocine antiarrhythmic agents 失效
标题翻译： Aryl und Hetaryl annelierte 2,4-Diazocine als anti-arryhthmische Wirkstoffe。
公开(公告)号：EP0597540A1
公开(公告)日：1994-05-18
申请号：EP93203115.6
申请日：1993-11-06
申请人： STERLING WINTHROP INC.
发明人： Johnson, Robert Ed., c/o Sterling Winthrop Inc. , Schlegel, Donald Charles., c/o Sterling Win. Inc. , Ezrin, Alan Mark., c/o Sterling Winthrop Inc.
IPC分类号： C07D243/04 , A61K31/55 , C07D409/04 , C07D405/12 , C07D413/06 , C07D401/04 , C07D405/06 , C07D495/04
CPC分类号： C07D401/04 , C07D243/04 , C07D245/06 , C07D401/06 , C07D405/04 , C07D487/04 , C07D495/04
摘要： Aryl-fused- and hetaryl-fused-2,4-diazepines of formula XXXVI,

wherein
A is an aryl, cycloalkyl or hetaryl or substituted aryl ring
R¹ is hydrogen, alkyl, aralkyl, aryl, hetaryl or substituted aryl;
R² is hydrogen, alkyl, aralkyl, aryl or substituted alkyl or aryl;
R³ is alkyl, aryl, aralkyl, hetaryl or heteroatom substituted alkyl, aryl, aralkyl or hetaryl;
R⁴ is hydrogen, alkyl or substituted alkyl;
R⁵ is hydrogen, alkyl, aryl, aralkyl, hetaryl or substituted aryl,
pharmaceutical compositions containing these and methods of treating cardiac arrhythmia with the compounds of formula XXXVI are disclosed.
摘要翻译：其中A是芳基，环烷基或杂芳基或取代的芳基环R 1的芳基 - 稠合 - 和杂芳基 - 稠合-2,4-二氮杂，其中A是芳基，环烷基或杂芳基或取代的芳基环R 1是氢，烷基，芳烷基，芳基，杂芳基或取代的芳基; R 2是氢，烷基，芳烷基，芳基或取代的烷基或芳基; R 3是烷基，芳基，芳烷基，杂芳基或杂原子取代的烷基，芳基，芳烷基或杂芳基; R 4是氢，烷基或取代的烷基; R 5是氢，烷基，芳基，芳烷基，杂芳基或取代的芳基，含有这些的药物组合物和用式XXXVI化合物治疗心律不齐的方法。

62. 发明公开

EP0588430A1 (S)-(+)-Hydroxychloroquine 失效
标题翻译：（S） - （+） - 羟氯喹
公开(公告)号：EP0588430A1
公开(公告)日：1994-03-23
申请号：EP93202641.2
申请日：1993-09-11
申请人： STERLING WINTHROP INC.
发明人： Stecher, Vera Johanna, c/o STERLING WINTHROP INC. , Michne, William Francis, c/o STERLING WINTHROP INC
IPC分类号： C07D215/46 , A61K31/47
CPC分类号： C07D215/46 , Y10S514/825 , Y10S514/895
摘要： The present invention provides (S)-(+)-Hydroxychloroquine substantially free of (R)-(―)-hydroxychloroquine, or a pharmaceutically acceptable acid-addition salt thereof, the use in the manufacture of a medicament for treatment of malaria, lupus erythematosus or rheumatoid arthritis and a composition containing it for the treatment of such diseases. The weight ratio of (S)-(+)-Hydroxychloroquine to (R)-(―)-hydroxychloroquine is preferably at least 90:10, most preferably at least 98:2.
摘要翻译：本发明提供基本上不含（R） - （ - ） - 羟氯喹或其药学上可接受的酸加成盐的（S） - （+） - 羟氯喹，在制备用于治疗疟疾，狼疮红斑狼疮或类风湿性关节炎以及含有它的组合物用于治疗这些疾病。（S） - （+） - 羟基氯喹与（R） - （ - ） - 羟基氯喹的重量比优选为至少90:10，最优选至少98:2。

63. 发明公开

EP0577218A1 Heterocyclyl-phenoxyalkyl-piperidinylpyridazines as antiviral agents 失效
标题翻译：杂环 - 苯氧基烷基 - 哌啶基哒嗪酮抗病毒剂Wirkung。
公开(公告)号：EP0577218A1
公开(公告)日：1994-01-05
申请号：EP93201899.7
申请日：1993-06-30
申请人： STERLING WINTHROP INC.
发明人： Diana, Guy Dominic, c/o Sterling Winthrop Inc.
IPC分类号： C07D413/14 , A61K31/50
CPC分类号： C07D413/14
摘要： Compounds of formula

wherein Het is

R₁ is a C₁-C₃ lower-alkyl;
R₂ and R₃ can each independently be hydrogen or fluorine;
R₄ is methyl or trifluoromethyl;
with the proviso that when Het is

R₁ is methyl and R₂ is fluorine; and when Het is

R₁ is methyl, R₂ is 2-fluoro, R₃ is hydrogen and
R₄ is methyl;
or pharmaceutically acceptable acid addition salts thereof, are useful as antiviral agents, particularly against picornaviruses.
摘要翻译：其中Het为CHEM的式CHEM的化合物为C1-C3低级烷基; R2和R3各自独立地为氢或氟; R4是甲基或三氟甲基; 条件是当Het为 R 1为甲基且R 2为氟时; 当Het为CHEM时，R 1为甲基，R 2为2-氟，R 3为氢，R 4为甲基; 或其药学上可接受的酸加成盐可用作抗病毒剂，特别是对小核糖核酸病毒。

64. 发明授权

EP0354368B1 Connector for hypodermic syringe pistons 失效转让
标题翻译：耦合注射器用于皮下注射的活塞件。
公开(公告)号：EP0354368B1
公开(公告)日：1993-12-01
申请号：EP89112689.8
申请日：1989-07-11
申请人： STERLING WINTHROP INC.
发明人： Ray, Jefferson Leroy , Cooper, Michael Edwin
IPC分类号： A61M5/315
CPC分类号： A61M5/31511 , A61M5/31515

65. 发明公开

EP0558141A1 Lactose-hydrolyzed milk with suppressed sweetness 失效
标题翻译：抑制甜味的乳糖水解牛奶
公开(公告)号：EP0558141A1
公开(公告)日：1993-09-01
申请号：EP93200507.7
申请日：1993-02-23
申请人： STERLING WINTHROP INC.
发明人： Flynn, Robert George , Bakal, Abraham Itshak , Snyder, Margaret Ann
IPC分类号： A23C9/12 , A23C9/13 , A23L1/236
CPC分类号： A23C9/1206 , A23C9/152 , A23L27/204 , A23L27/33
摘要： A lactose-hydrolyzed fluid milk comprising fluid milk, the normal lactose content of which has been reduced by at least about 70% by lactase hydrolysis, having incorporated therein from about 1 to about 10 ppm of 2-(4-methoxyphenoxy)propanoic acid or a salt thereof, a method of preparation thereof and a method of suppressing perceived sweetness of lactose-hydrolyzed milk by incorporating 2-(4-methoxyphenoxy)propanoic acid or a salt thereof in the milk.
摘要翻译：包含流体乳的乳糖水解流体牛奶，其乳糖含量已被乳糖酶水解降低至少约70％，其中掺入约1至约10ppm的2-（4-甲氧基苯氧基）丙酸或其盐，其制备方法和通过将2-（4-甲氧基苯氧基）丙酸或其盐掺入乳中来抑制乳糖水解乳的感觉甜味的方法。

66. 发明公开

EP0550112A1 2-Saccharinylmethyl aryl and aryloxy acetates useful as proteolytic enzyme inhibitors and pharmaceutical compositions contaning them 失效
标题翻译： 2- Saccharinylmethyl芳基和Aryloxycarboxylate作为蛋白水解酶抑制剂，以及含有它们的药物组合物。
公开(公告)号：EP0550112A1
公开(公告)日：1993-07-07
申请号：EP92204072.0
申请日：1992-12-23
申请人： STERLING WINTHROP INC.
发明人： Latimer, Lee Hamilton, c/o Eastman Kodak Company , Dunlap, Richard Paul, c/o Eastman Kodak Company
IPC分类号： C07D275/06 , A61K31/425 , C07D513/04
CPC分类号： C07D275/06 , A61K31/425 , C07D513/04
摘要： 4-R⁴-R⁵-2-Saccharinylmethyl aryl and aryloxy acetates, having the formula:

wherein:

m is zero or one, n is zero or one, and the sum of m + n is zero or one;
R 1 is hydrogen or lower-alkyl;
R 2 is hydrogen or lower-alkyl;
R 3 is phenyl or phenyl substituted by from one to three, the same or different, members of the group consisting of lower-alkyl perfluorolower-alkyl, lower-alkoxy and halogen;
R 4 is hydrogen, halogen, lower-alkyl, perfluorolower-alkyl, perchlorolower-alkyl, lower-alkenyl, lower-alkynyl, cyano, carboxamido, amino, lower-alkylamino, dilower-alkylamino, lower-alkoxy, benzyloxy, lower-alkoxycarbonyl, hydroxy or phenyl; and
R 5 is hydrogen or from one to two substituents in any of the 5-, 6- or 7-positions.

The compounds of the present invention inhibit the activity of serine proteases, specifically human leukocyte elastase and the chymotrypsin-like enzymes, and are thus useful in the treatment of degenerative disease conditions such as emphysema, rheumatoid arthritis, pancreatitis, cysticfibrosis, chronic bronchitis, adult respiratory distress syndrome, inflammatory bowel disease, psoriasis, bullous pemphigoid and alpha-1-antitrypsin deficiency.
摘要翻译： 4-R <4> -R <5> -2- Saccharinylmethyl芳基和芳氧基乙酸盐，具有下式： worin：m是0或1，n是0或1，并且m + n之和是零或1; [R <1>是氢或低级烷基; [R <2>是氢或低级烷基; [R <3>是从一至三个苯基或苯基substituiertem，基团选自低级烷基的相同或不同的，成员perfluorolower - 烷基，低级 - 烷氧基和卤素; [R <4>是氢，卤素，低级烷基，perfluorolower烷基，perchlorolower - 烷基，低级 - 烯基，低级炔基，氰基，甲酰氨基，氨基，低级烷基氨基，二低级烷基氨基，低级烷氧基，苄氧基，低级烷氧基羰基，羟基或苯基; 且R <5>是氢或1-2个取代基在任何5-，6-或7-位的。本发明的化合物抑制丝氨酸蛋白酶，特别是人白细胞弹性蛋白酶和胰凝乳蛋白酶样酶的活性，并且在退化性疾病的病症的治疗因此可用于：如肺气肿，类风湿性关节炎，胰腺炎，囊肿性纤维化，慢性支气管炎，成人呼吸窘迫综合征，炎性肠疾病，牛皮癣，大疱性类天疱疮和α-1-抗胰蛋白酶缺乏症。

67. 发明公开

EP0550111A1 2-Saccharinylmethyl heterocyclic carboxylates useful as proteolytic enzyme inhibitors and pharmaceutical compositions containing them 失效
标题翻译： 2- Saccharinylmethyl杂环羧酸盐作为蛋白质分解酶抑制剂，以及含有它们的药物组合物。
公开(公告)号：EP0550111A1
公开(公告)日：1993-07-07
申请号：EP92204071.2
申请日：1992-12-23
申请人： STERLING WINTHROP INC.
发明人： Hlasta, Dennis John, c/o Sterling Winthrop Inc. , Desai, Ranjit Chimanlal, c/o Sterling Winthrop Inc , Subramanyam, Chakrapani, c/o Sterling Winthrop Inc , Court, John Joseph, c/o Sterling Winthrop Inc. , Bell, Malcolm Rice, c/o Sterling Winthrop Inc. , Kumar, Virendra, c/o Sterling Winthrop Inc. , Dunlap, Richard Paul, c/o Eastman Kodak Company , Latimer, Lee Hamilton, c/o Eastman Kodak Company
IPC分类号： C07D417/12 , A61K31/425 , A61K31/44
CPC分类号： C07D417/12
摘要： 4-R⁴-R⁵-2-Saccharinylmethyl heterocyclic carboxylates, having the formula:

wherein:
Het is a 5- or 6-membered monocyclic heterocycle or a 9- or 10-membered bicyclic heterocycle containing from 1 to 2 heteroatoms selected from oxygen, nitrogen and sulfur or said heterocycles substituted by from one to three, the same or different, members of the group consisting of lower-alkyl, perfluorolower-alkyl, lower-alkoxy, oxo, phenyl, halogen, and -O-(C₂-C₁₀ alkylene)-N=B where N=B is dilower-alkylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, or 4-lower-alkyl-1-piperazinyl;
R⁴ is hydrogen, halogen , lower-alkyl, perfluorolower-alkyl, perchlorolower-alkyl, lower-alkenyl, lower-alkynyl, cyano, carboxamido, amino, lower-alkylamino, dilower-alkylamino, lower-alkoxy, benzyloxy, lower-alkoxycarbonyl, hydroxy or phenyl; and
R⁵ is hydrogen or from one to two substituents in any of the 5-, 6- or 7-positions.
The compounds of the present invention inhibit the activity of serine proteases, specifically human leukocyte elastase and the chymotrypsin-like enzymes, and are thus useful in the treatment of degenerative disease conditions such as emohysema, rheumatoid arthritis, pancreatitis, cystic fibrosis, chronic bronchitis, adult respiratory distress syndrome, inflammatory bowel disease, psoriasis, bullous pemphigoid and alpha-1-antitrypsin deficiency.
摘要翻译： 4-R <4> -R <5> -2- Saccharinylmethyl杂环羧酸盐，具有下式： worin：Het为5-或6-元单环杂环或9-或10-元双环杂环由含 1至2个杂选自氧，氮和硫原子中的或所述杂环从一个substituiertem由三个，所述组选自：低级 - 烷基中的相同或不同的，构件，perfluorolower - 烷基，低级 - 烷氧基，氧代，苯基，卤素，和-O-（C 2 -C 10亚烷基）-N = B，其中N = B是二低级烷基氨基，1-吡咯烷基，1-哌啶基，4-吗啉基，1-哌嗪基或4-低级烷基-1-哌嗪基; [R <4>是氢，卤素，低级烷基，perfluorolower烷基，perchlorolower - 烷基，低级 - 烯基，低级炔基，氰基，甲酰氨基，氨基，低级烷基氨基，二低级烷基氨基，低级烷氧基，苄氧基，低级烷氧基羰基，羟基或苯基; 且R <5>是氢或1-2个取代基在任何5-，6-或7-位的。本发明的化合物抑制丝氨酸蛋白酶，特别是人白细胞弹性蛋白酶和胰凝乳蛋白酶样酶的活性，并因此在变性疾病的病症的治疗有用：如emohysema，类风湿关节炎，胰腺炎，囊性纤维化，慢性支气管炎，成人呼吸窘迫综合征，炎性肠病，牛皮癣，大疱性类天疱疮和α-1-抗胰蛋白酶缺乏症。

68. 发明公开

EP0547654A1 Contrast agents for ultrasound imaging 失效
标题翻译： KontrastmittelfürEchographie，enthaltend Human Serum Albumin-umhüllteFettsäuren。
公开(公告)号：EP0547654A1
公开(公告)日：1993-06-23
申请号：EP92203684.3
申请日：1992-11-28
申请人： STERLING WINTHROP INC.
发明人： Yudelson, Joseph, c/o Eastman Kodak Company , Power, Susan E., c/o Eastman Kodak Company
IPC分类号： A61K49/00
CPC分类号： A61K49/225
摘要： Particles having an average diameter of less than about 12 microns comprising fatty acid cores encapsulated with human serum albumin and methods for their preparation are disclosed. These materials are useful as contrast agents in ultrasonic imaging, having scattering intensities that are equivalent to or greater than those obtained from dispersed microbubbles but being much more stable, both in storage and when used in vivo , than are contrast agents based on dispersed microbubbles.
摘要翻译：公开了平均直径小于约12微米的包含用人血清白蛋白包裹的脂肪酸核心的颗粒及其制备方法。这些材料可用作超声成像中的造影剂，其散射强度等于或大于从分散的微泡获得的散射强度，但在储存和使用时比在基于分散的微泡的造影剂中更稳定。

69. 发明公开

EP0543454A2 Encapsulated particles useful as contrast agents in ultrasound and X-ray imaging compositions and methods 失效
标题翻译：包封的颗粒用作超声造影剂和X射线成像的组合物和方法。
公开(公告)号：EP0543454A2
公开(公告)日：1993-05-26
申请号：EP92203491.3
申请日：1992-11-13
申请人： STERLING WINTHROP INC.
发明人： Bailey, Denis M., c/o Sterling Winthrop Inc. , Yudelson, Joseph S., c/o Eastman Kodak Company , James, Robert O., c/o Eastman Kodak Company
IPC分类号： A61K49/04 , A61K49/00
CPC分类号： A61K49/0433 , A61K49/225
摘要： Stable particles comprising a core consisting of a water-insoluble ester or amide of 3,5-diacetamido-2,4,6-triiodobenzoic acid encapsulated with methyl cellulose, such particles having an average particle size of less than about 10 µm, dispersions containing such particles, and methods for the preparation thereof are disclosed. The particles are particularly useful as contrast agents for use in x-ray and ultrasound diagnostic imaging compositions and methods.
摘要翻译：稳定的颗粒包括芯由...组成3,5-二乙酰-2,4,6-三碘苯甲酸封装有甲基纤维素的水不溶性酯或酰胺，检查上具有小于约10微米平均颗粒尺寸的颗粒，分散体含有寻求颗粒，和方法，用于其制备的游离缺失光盘。颗粒是作为用于在X射线和超声诊断成像的组合物和方法中使用的造影剂是特别有用的。

70. 发明公开

EP0518414A1 Thioxanthenone antitumor agents 失效转让
标题翻译： Thioxanthenon-Antitumormittel。
公开(公告)号：EP0518414A1
公开(公告)日：1992-12-16
申请号：EP92201587.0
申请日：1992-06-03
申请人： STERLING WINTHROP INC.
发明人： Miller, Theodore Charles , Collins, Joseph Charles , Wentland, Mark Philip , Perni, Robert Bruno , Corbett, Thomas Hughes , Mattes, Kenneth Charles, c/o Eastman Kodak Company
IPC分类号： C07D335/16 , C07F9/24 , A61K31/38
CPC分类号： C07F9/655372 , C07D335/16
摘要： 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones having the formula

wherein n is 2 or 3;
R¹ and R² are independently lower-alkyl;
Q is a residue chosen from the group consisting of CH₂NHR³, CH₂N(R⁴)SO₂R⁷, CH₂NHCHO, CH=N-Ar, C(O)NR⁵R⁶, CH₂N(R⁴)C(O)R⁷, CH₂N(C₂H₅)CHO, and CH₂N(R⁴)P(O)(O-lower-alkyl)₂;
R³ is hydrogen or lower-alkyl;
R⁴ is hydrogen or lower-alkyl;
R⁵ is hydrogen, lower-alkyl or Ar;
R⁶ is hydrogen or lower-alkyl;
R⁷ is lower-alkyl, or Ar;
R⁸ is hydrogen, lower-alkyl, lower-alkoxy, or halogen; and
Ar is phenyl or phenyl substituted with methyl, methoxyl, halogen or nitro;
or a pharmaceutically acceptable acid-addition salt or solvate thereof, are disclosed as antitumor agents. Compositions containing the thioxanthenones and the method of use of thioxanthenones for treating tumors and cancer in mammals are also disclosed.
摘要翻译： 1 - [[（二烷基氨基）烷基]氨基] -4-取代的噻吨-9-酮，其具有式CHEM，其中n为2或3; R 1和R 2独立地为低级烷基; Q是选自由CH 2 NHR 3，CH 2 N（R 4）SO 2 R 7，CH 2 NHCHO，CH = N-Ar，C（O）NR 5 R 6，CH 2 N（ R 4）C（O）R 7，CH 2 N（C 2 H 5）CHO和CH 2 N（R 4）P（O）（O-低级 - 烷基）2; R 3是氢或低级烷基; R 4是氢或低级烷基; R 5是氢，低级烷基或Ar; R 6是氢或低级烷基; R 7是低级烷基或Ar; R 8是氢，低级烷基，低级烷氧基或卤素; 并且Ar是苯基或被甲基，甲氧基，卤素或硝基取代的苯基; 或其药学上可接受的酸加成盐或其溶剂合物作为抗肿瘤剂公开。还公开了含有噻吨酮的组合物和用于治疗哺乳动物肿瘤和癌症的噻吨酮的方法。

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