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81. 发明申请

WO1994009017A1 PYRIMIDINE BISPHOSPHONATE ESTERS AND (ALKOXYMETHYLPHOSPHINYL)ALKYL PHOSPHONIC ACIDS AS ANTI-INFLAMMATORIES 审中-公开
标题翻译：吡嗪二磷酸酯酯和（烷氧基甲基苯基）亚磷酸酯作为抗炎药
公开(公告)号：WO1994009017A1
公开(公告)日：1994-04-28
申请号：PCT/US1993008626
申请日：1993-09-20
申请人： THE UPJOHN COMPANY , DUNN, Colin, John , CHIN, Jia-En , NUGENT, Richard, Allen , WHITE, David, R. , FRITZEN, Edward, L., Jr.
发明人： THE UPJOHN COMPANY
IPC分类号： C07F09/6561
CPC分类号： C07F9/657181 , C07F9/6512 , C07F9/65583 , C07F9/6561
摘要： Compounds useful in the treatment of inflammation structurally represented as Formulae (1), (2), (3) wherein X is O or S, X is OR24, SR24, morpholinyl, piperazinyl, piperidinyl, imidazolidinyl, pyrazolidinyl, isoxazolyl, pyrrolyl, imidazolyl, pyrazolyl, pyridyl, pyrazinyl, pyrimidinyl or pyridazinyl; and the R groups are as herein defined. The compounds are useful as anti-inflammatory and anti-arthritic agents and in the safe and effective treatment of diseases characterized by abnormal phosphate and calcium metabolism, and as a treatment of inflammation. These diseases include osteoporosis, Paget's disease, periodontal disease, rheumatoid arthritis, osteoarthritis, neuritis, bursitis, soft tissue mineralization disorders, ankylosing spondylitis, atherosclerosis, multiple myeloma of bone, metastatic bone disease, and mitral valve calcification.
摘要翻译：式（1），（2），（3）其中X是O或S，X 1的结构上用于治疗炎症的化合物是OR24，SR24，吗啉基，哌嗪基，哌啶基，咪唑烷基，吡唑烷基，异恶唑基，吡咯基，咪唑基，吡唑基，吡啶基，吡嗪基，嘧啶基或哒嗪基; 并且R基团如本文所定义。该化合物可用作抗炎和抗关节炎药物，并且以安全和有效的方式治疗以磷酸盐和钙代谢异常为特征的疾病，以及作为炎症的治疗。这些疾病包括骨质疏松症，佩吉特氏病，牙周病，类风湿性关节炎，骨关节炎，神经炎，滑囊炎，软组织矿化病，强直性脊柱炎，动脉粥样硬化，骨多发性骨髓瘤，转移性骨病和二尖瓣钙化。

82. 发明申请

WO1994003463A1 PHOSPHONOACETIC ESTERS AND ACIDS AS ANTI-INFLAMMATORIES 审中-公开
标题翻译：磷酸酯和酸作为抗炎药
公开(公告)号：WO1994003463A1
公开(公告)日：1994-02-17
申请号：PCT/US1993005365
申请日：1993-06-09
申请人： THE UPJOHN COMPANY , NUGENT, Richard, Allen , ANDERSON, David, John , SCHLACHTER, Stephen, Thomas
发明人： THE UPJOHN COMPANY
IPC分类号： C07F09/40
CPC分类号： C07F9/4059 , C07F9/4018 , C07F9/58 , C07F9/65031 , C07F9/6512 , C07F9/65583 , C07F9/6561 , C07F17/02 , Y10S514/825
摘要： Compounds useful in the treatment of inflammation structurally represented as formula (I), one of X or Y is H and the other is selected from the group consisting of a), b), c), d), e): ferrocenyl COCH2CH2-, f), g) or X and Y are taken together to form a ring selected from the group consisting of i), ii), iii), iv) as herein defined. The compounds are useful as anti-inflammatory and anti-arthritic agents.
摘要翻译：用于治疗结构上用式（I）表示的炎症的化合物，X或Y之一是H，另一个选自a），b），c），d），e）：二茂铁基COCH2CH2- ，f），g）或X和Y一起形成选自如本文所定义的i），ii），iii），iv）所示的环。该化合物可用作抗炎和抗关节炎药物。

83. 发明申请

WO1993022445A1 A PROCESS FOR PRODUCING PIOGLITAZONE METABOLITE 审中-公开
标题翻译：生产PIOGLITAZONE代谢物的方法
公开(公告)号：WO1993022445A1
公开(公告)日：1993-11-11
申请号：PCT/US1993003569
申请日：1993-04-21
申请人： THE UPJOHN COMPANY , JOHNSON, Roy, A. , MARSHALL, Vincent, P. , LI, Grace, P.
发明人： THE UPJOHN COMPANY
IPC分类号： C12P17/16
CPC分类号： C12R1/55 , C12P17/167
摘要： The present invention provides a method for making pharmaceutical compounds. More particularly the present invention provides a new method for making oxygenated pioglitazone derivatives of formulas (I) and (II), which are metabolites of pioglitazone and useful for the treatment of diabetes and as insulin sensitizing agents.
摘要翻译：本发明提供制备药物化合物的方法。更具体地，本发明提供了制备式（I）和（II）的氧合吡格列酮衍生物的新方法，其是吡格列酮的代谢物并且可用于治疗糖尿病和作为胰岛素敏化剂。

84. 发明申请

WO1993009826A1 AN INJECTION DEVICE 审中-公开
标题翻译：注射装置
公开(公告)号：WO1993009826A1
公开(公告)日：1993-05-27
申请号：PCT/US1992009260
申请日：1992-11-04
申请人： THE UPJOHN COMPANY , DELTA WEST PTY. LIMITED , UNSWORTH, Rodney, William , CARTER, Stephen, John
发明人： THE UPJOHN COMPANY , DELTA WEST PTY. LIMITED
IPC分类号： A61M05/28
CPC分类号： A61M5/348 , A61M5/282 , A61M5/3202 , A61M5/46 , A61M2005/3128
摘要： The present invention provides an injection device (1) adapted to engage a deformable plastic ampoule (2) having a reservoir (3) and a neck portion (4), said device comprising: a body (5) having a continuous fluid conduit (6) therethrough, the fluid conduit comprising at one end a male frusto-conical extending member (8) forming a sealing surface with a corresponding parallel walled or frusto-conical female recess (10) on the neck portion (4) of said ampoule (2) when the ampoule and the device are cooperatively engaged. This device is simple to use and is suitable for self-injection by patients.
摘要翻译：本发明提供了一种适于接合具有储存器（3）和颈部（4）的可变形塑料安瓿（2）的注射装置（1），所述装置包括：主体（5），具有连续的流体导管），所述流体导管在一端包括形成密封表面的雄性截头圆锥形延伸构件（8），所述密封表面在所述安瓿（2）的颈部（4）上具有对应的平行的壁或截头圆锥形的凹形凹部（10））当安瓿和装置合作接合时。该装置使用简单，适合患者自我注射。

85. 发明申请

WO1993003724A1 PHARMACEUTICAL COMPOSITION CONTAINING 3-GUANIDINOPROPIONIC ACID AND PIOGLITAZONE GLIBENCLAMIDE OR GLIMEPIRIDE 审中-公开
标题翻译：含有3-胍基酸和PIOGLITAZONE GLIBENCLAMIDE或GLIMEPIRIDE的药物组合物
公开(公告)号：WO1993003724A1
公开(公告)日：1993-03-04
申请号：PCT/US1992006776
申请日：1992-08-19
申请人： THE UPJOHN COMPANY , MEGLASSON, Martin, Durham
发明人： THE UPJOHN COMPANY
IPC分类号： A61K31/44
CPC分类号： A61K31/44 , A23L2/52 , A23L33/10 , A23V2002/00 , A61K31/197 , A61K31/64 , Y10S514/866 , Y10S514/909 , A61K31/195 , A61K2300/00 , A23V2250/30
摘要： The present invention provides a new composition, food product and uses for a known compound. More particularly, the present invention provides a new pharmaceutical composition containing 3-guanidinopropionic acid and a method of using 3-guanidinopropionic acid to prevent or treat obesity in non-insulin dependent diabetic (NIDDM) patients that is caused by treatment with anti-diabetic drugs, such as an insulin sensitizing drug or an insulin secretion stimulating drug. Examples of insulin sensitizing drugs are pioglitazone and pioglitazone hydrochloride. Examples of insulin secretion stimulating drugs are glyburide and glimepiride. The present invention also provides a new food product containing 3-guanidinopropionic acid and a method of using 3-guanidinopropionic acid to increase endurance, stamina and exercise capacity.
摘要翻译：本发明提供新的组合物，食品和已知化合物的用途。更具体地，本发明提供了含有3-胍基丙酸的新型药物组合物和使用3-胍基丙酸预防或治疗由抗糖尿病药物治疗引起的非胰岛素依赖性糖尿病（NIDDM）患者的肥胖症的方法，例如胰岛素敏化药物或胰岛素分泌刺激药物。胰岛素敏化药物的实例是吡格列酮和盐酸吡格列酮。胰岛素分泌刺激药物的实例是格列本脲和格列美脲。本发明还提供了含有3-胍基丙酸的新食品和使用3-胍基丙酸提高耐力，耐力和运动能力的方法。

86. 发明申请

WO1993000915A1 COLESTIPOL HYDROCHLORIDE HIGH-CONTENT TABLETS 审中-公开
标题翻译： COLESTIPOL HYDROCHLORIDE高容量片剂
公开(公告)号：WO1993000915A1
公开(公告)日：1993-01-21
申请号：PCT/US1992005066
申请日：1992-06-23
申请人： THE UPJOHN COMPANY , SHEN, Robert, Wu-wei , PRICE, Jeffrey, Ellis
发明人： THE UPJOHN COMPANY
IPC分类号： A61K31/785
CPC分类号： A61K9/1688 , A61K9/2886 , A61K31/785 , Y10S514/824 , Y10S514/96 , Y10S514/961
摘要： The present invention provides a novel formulation of matter and a novel process for making it. In particular, the present invention provides unique and novel 1000 mg tablets of Colestipol hydrochloride having the advantageous properties of hardness and low friability and a novel process for making such tablets.
摘要翻译：本发明提供了一种新颖的物质配方及其制备方法。特别地，本发明提供具有硬度和低脆性的有利性质的独特和新颖的1000mg盐酸依立替斯片剂和制备这种片剂的新方法。

87. 发明申请

WO1993000891A1 ENZYME-SENSITIVE ENTERIC PREPARATION FOR ORAL ADMINISTRATION 审中-公开
标题翻译：用于口腔管理的酶敏感性制剂
公开(公告)号：WO1993000891A1
公开(公告)日：1993-01-21
申请号：PCT/US1992005245
申请日：1992-06-26
申请人： THE UPJOHN COMPANY , NISHIHATA, Toshiaki , NARITA, Mayumi , YAMAMOTO, Ken
发明人： THE UPJOHN COMPANY
IPC分类号： A61K09/48
CPC分类号： A61K9/4858 , A61K9/1617 , A61K31/405 , A61K31/425 , A61K31/495
摘要： The object of the invention is to provide an enteric preparation which has higher specificity and is enzyme-sensitive. The preparation wherein a medicine is dissolved in a vehicle containing one or more fatty acids selected from a group consisting of glycerol fatty acid ester, polyoxyethylene sorbitan fatty acid ester, propylene glycol fatty acid ester, polyethylene glycol fatty acid ester, ethylene glycol fatty acid ester and decaglycerol fatty acid ester.
摘要翻译：本发明的目的是提供一种具有较高特异度和酶敏感性的肠溶制剂。其中将药物溶解于含有一种或多种选自甘油脂肪酸酯，聚氧乙烯脱水山梨糖醇脂肪酸酯，丙二醇脂肪酸酯，聚乙二醇脂肪酸酯，乙二醇脂肪酸酯的脂肪酸的载体的制剂和十甘油脂肪酸酯。

88. 发明申请

WO1992022559A1 DIALKYL (DIALKOXYPHOSPHINYL)METHYL PHOSPHATES AS ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译： DIALKYL（DIALKOXYPHOSPHYYL）甲基磷酸酯作为抗炎剂
公开(公告)号：WO1992022559A1
公开(公告)日：1992-12-23
申请号：PCT/US1992004013
申请日：1992-05-21
申请人： THE UPJOHN COMPANY , JOHNSON, Roy, Allen
发明人： THE UPJOHN COMPANY
IPC分类号： C07F09/40
CPC分类号： C07F9/657181 , C07F9/4006 , C07F9/5728 , C07F9/58 , C07F9/6506
摘要： Provided are novel dialkyl (dialkoxyphosphinyl)methyl phosphates of formula (IV) which are useful as anti-inflammatory and anti-arthritic agents. The compounds are synthesized from the reaction of tetraethyl oxiranylidenebisphosphonate and unsubstituted or alkyl-amines. Representative compounds include 2-(benzylamino)-1-(diethoxyphosphinyl)ethyl phosphonic acid diethyl ester, 1-(diethoxyphosphinyl)-2-[2'-(1',2',3',4'-tetrahydro)napthylamino]ethyl phosphonic acid diethyl ester, 2-(3-fluorobenzylamino)-1-(diethoxyphosphinyl)ethyl phosphonic acid diethyl ester, and 5,5-dimethyl-2-[2-(3-fluorobenzyl)amino-1-[(5,5-dimethyl-1,3,2-dioxaph osphorinan-2-yl)oxy]ethyl]-1,3,2-dioxaphosphorinane P,2-dioxide.
摘要翻译：提供了可用作抗炎和抗关节炎剂的式（IV）的新型二烷基（二烷氧基氧膦基）甲基磷酸酯。该化合物是由四乙基亚硫酰亚基双膦酸酯与未取代的或烷基胺的反应合成的。代表性的化合物包括2-（苄基氨基）-1-（二乙氧基氧膦基）乙基膦酸二乙酯，1-（二乙氧基氧膦基）-2- [2' - （1'，2'，3'，4'-四氢）萘基氨基]乙基膦酸二乙酯，2-（3-氟苄基氨基）-1-（二乙氧基氧膦基）乙基膦酸二乙酯和5,5-二甲基-2- [2-（3-氟苄基）氨基-1 - [（5,5 - 二甲基-1,3,2-二氧杂环己酮-2-基）氧基]乙基] -1,3,2-二氧杂磷杂环戊烷P 2，二氧化物。

89. 发明申请

WO1992020655A1 CARBOXAMIDO-(1,2N)-CARBOCYCLIC-2-AMINOTETRALIN DERIVATIVES 审中-公开
标题翻译：羧酰胺 - （1,2N） - 链烷基-2-氨基嘌呤衍生物
公开(公告)号：WO1992020655A1
公开(公告)日：1992-11-26
申请号：PCT/US1992003871
申请日：1992-05-13
申请人： THE UPJOHN COMPANY , LIN, Chiu-Hong , HAADSMA-SVENSSON, Susanne, R. , MCCALL, Robert, B. , ROMERO, Arthur, G. , DARLINGTON, William, Harold , ENNIS, Michael, D.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D209/60
CPC分类号： C07D209/60 , C07D221/10
摘要： This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of formula (I), wherein X is -(CH2)n- or -C(R1)(H)-; R is C1-C8 alkyl; and R1 and R2 are the same or different and are selected from the group consisting of hydrogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, aryl and benzyl. These compounds are useful to treat central nervous system disorders and are unexpectedly resistant to metabolism by the liver and have superior oral plasma bioavailability.
摘要翻译：本发明是治疗上有用的式（I）的四氢化萘及其药学上可接受的酸加成盐，其中X是 - （CH 2）n - 或-C（R 1）（H） - ; R是C 1 -C 8烷基; 并且R 1和R 2相同或不同，并且选自氢，C 1 -C 8烷基，C 2 -C 8烯基，C 2 -C 8炔基，芳基和苄基。这些化合物可用于治疗中枢神经系统疾病，并且意外地耐受肝脏代谢并具有优异的口服血浆生物利用度。

90. 发明申请

WO1992019211A2 IMIDAZOBENZOQUINONES AND COMPOSITION FOR PREVENTING OR TREATING HYPERTENSION OR CONGESTIVE HEART FAILURE CONTAINING THE SAME 审中-公开
标题翻译：咪达唑仑和组合物，用于预防或治疗包含其中的高血压或心律失常
公开(公告)号：WO1992019211A2
公开(公告)日：1992-11-12
申请号：PCT/US1992003440
申请日：1992-04-30
申请人： THE UPJOHN COMPANY , KOH, Keiko , ITOH, Noriie , OZAWA, Kazunori , KUSHIDA, Hiroshi , MCWHORTER, William, W., Jr.
发明人： THE UPJOHN COMPANY
IPC分类号： A61K0
CPC分类号： C07D235/02 , C07D235/08 , C07D403/10
摘要： There are provided pharmacologically active compounds which are highly effective to treat hypertension or congestive heart failure, and are well absorbed into the body and have long-lasting action. Thus, the present invention provides a compound represented by general formula (I) or a pharmacologically acceptable ester or salt thereof, and a pharmaceutical composition for preventing or treating hypertension or congestive heart failure which comprises the compound as an active ingredient.
摘要翻译：提供了治疗高血压或充血性心力衰竭非常有效的药理活性化合物，并且被良好地吸收到身体中并且具有持久的作用。因此，本发明提供由通式（I）表示的化合物或其药理学上可接受的酯或其盐，以及用于预防或治疗高血压或充血性心力衰竭的药物组合物，其包含该化合物作为活性成分。

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