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1. 发明申请

WO1994011361A1 PYRAN-2-ONES AND 5,6-DIHYDROPYRAN-2-ONES USEFUL FOR TREATING HIV AND OTHER RETROVIRUSES 审中-公开
标题翻译： PYRAN-2-ONES和5,6-DIHYDROPYRAN-2-ONES用于治疗艾滋病毒和其他肝炎病毒
公开(公告)号：WO1994011361A1
公开(公告)日：1994-05-26
申请号：PCT/US1993010645
申请日：1993-11-09
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit , YANG, Chih-Ping , STROHBACH, Joseph, Walter , TURNER, Steven, Ronald , ROMERO, Donna, Lee , SKALETZKI, Louis, L, , ARISTOFF, Paul, Adrian , GAMMILL, Ronald, B, , JOHNSON, Paul, D. , SKULNICK, Harvey, Irving , PIPER, Richard, C, , TOMMASI, Ruben, A. , ZHANG, Qingwei
发明人： THE UPJOHN COMPANY
IPC分类号： C07D309/38
CPC分类号： C07D405/06 , C07D309/32 , C07D309/38 , C07D311/96 , C07D405/12 , C07D407/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12
摘要： The present invention relates to compounds of formula (I) which are pyran-2-ones and 5,6-dihydropyran-2-ones useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus.
摘要翻译：本发明涉及可用于在感染该逆转录病毒的哺乳动物细胞中抑制逆转录病毒的吡喃-2-酮和5,6-二氢吡喃-2-酮的式（I）化合物。

2. 发明申请

WO1993023384A1 OXAZOLIDINONES CONTAINING A SUBSTITUTED DIAZINE MOIETY AND THEIR USE AS ANTIMICROBIALS 审中-公开
标题翻译：含有取代的DIAZINE MOIETY的OXAZOLIDONON及其作为抗微生物剂的用途
公开(公告)号：WO1993023384A1
公开(公告)日：1993-11-25
申请号：PCT/US1993003570
申请日：1993-04-21
申请人： THE UPJOHN COMPANY , HUTCHINSON, Douglas, K. , BRICKNER, Steven, Joseph , BARBACHYN, Michael, Robert , GAMMILL, Ronald, B. , PATEL, Mahest, V.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D263/20
CPC分类号： C07D263/20 , C07D413/10 , C07D413/12
摘要： A compound of structural formula (I) or pharmaceutically acceptable salts thereof wherein: Y is chosen from a-n as defined herein; wherein each occurrence of said C1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR , CO2R , CN, SR , or R (where R is a hydrogen or C1-4 alkyl); X and Z are independently C1-6 alkyl, C3-12 cycloalkyl or hydrogen, or X and Z form a C0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C1-6 alkyl, F, Cl, Br, hydrogen or a C1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C1-12 alkyl, C3-12 cycloalkyl, C1-6 alkoxy, C1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.
摘要翻译：结构式（I）的化合物或其药学上可接受的盐，其中：Y选自如本文所定义的a-n; 其中所述C 1-6烷基的每次出现可以被一个或多个F，Cl，Br，I，OR 1，CO 2 R 1，CN，SR 1或R 1取代（其中R 1， 1是氢或C 1-4烷基）; X和Z独立地是C 1-6烷基，C 3-12环烷基或氢，或X和Z形成C0-3桥连基，优选X和Z是氢; U，V和W独立地是C 1-6烷基，F，Cl，Br，氢或被F，Cl，Br或I中的一个或多个取代的C 1-6烷基，优选U和V是F，W是氢; R是氢，C 1-12烷基，C 3-12环烷基，C 1-6烷氧基，被一个或多个F，Cl，Br，I或OH取代的C 1-6烷基; q为0〜4。具有与N-芳基环结合的取代的二嗪部分的恶唑烷酮衍生物是有效的抗微生物剂，其对许多人类和兽医病原体有效，包括多重耐药性葡萄球菌和链球菌，以及厌氧生物体如杀菌剂和梭菌属物种，以及耐酸生物如结核分枝杆菌和鸟分枝杆菌。

3. 发明申请

WO1993012113A1 3-SUBSTITUTED IMIDAZO (1,5-a) AND IMIDAZO (1,5-a)-TRIAZOLO (1,5-c) QUINOXALINES AND QUINAZOLINES WITH CNS ACTIVITY 审中-公开
标题翻译： 3-取代的咪唑（1,5-a）和咪唑（1,5-a） - 三唑（1,5-c）喹喔啉和喹唑啉与CNS活性
公开(公告)号：WO1993012113A1
公开(公告)日：1993-06-24
申请号：PCT/US1992010388
申请日：1992-12-07
申请人： THE UPJOHN COMPANY , GAMMILL, Ronald, B. , SKALETZKY, Louis, L.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/495 , A61K31/505 , C07D487/14
摘要： An oxoimidazo(1,5-a)quinoxaline and a oxoimidazo(1,5-a)quinazoline of formula (I), an imidazo(1,5-a)-1,2,4-triazolo-(4,3-c)quinazoline and an imidazo(1,5-a)-1,2,4-triazolo-(4,3-c)quinozoline of formula (II), and an imidazo(1,5-a)quinoxaline of formula (III). The R-groups and other variables are as defined herein. The compounds are useful in the treatment of central nervous system disorders associated with the benzodiazepine receptors in a subject in need of such treatment comprising administering to the subject a therapeutically-effective amount of a formula I, II, or III compound for alleviation of such disorder. Typically, the compound of formula I, II, or III is administered in the form of a pharmaceutical composition comprising a pharmaceutically-acceptable carrier or diluent.
摘要翻译：式（I）的氧代咪唑并（1,5-a）喹喔啉和氧代咪唑并（1,5-a）喹唑啉，咪唑并（1,5-a）-1,2,4-三唑并（4,3- c）喹唑啉和式（II）的咪唑并（1,5-a）-1,2,4-三唑并（4,3-c）喹唑啉和式（I）的咪唑并（1,5-a）喹喔啉 III）。 R基团和其它变量如本文所定义。该化合物可用于治疗需要这种治疗的受试者中与苯并二氮杂受体相关的中枢神经系统疾病，其包括向受试者施用治疗有效量的式I，II或III化合物以减轻这种病症。通常，式I，II或III的化合物以包含药学上可接受的载体或稀释剂的药物组合物的形式施用。

4. 发明申请

WO1991019707A2 ANTIATHEROSCLEROTIC AND ANTITHROMBOTIC 1-BENZOPYRAN-4-ONES AND 2-AMINO-1,3-BENZOXAZINE-4-ONES 审中-公开
标题翻译：抗真菌剂和抗坏血酸的1-苯并噻吩-4-酮和2-氨基-1,3-苯并恶唑-4-酮
公开(公告)号：WO1991019707A2
公开(公告)日：1991-12-26
申请号：PCT/US1991004140
申请日：1991-06-18
申请人： THE UPJOHN COMPANY , GAMMILL, Ronald, B. , JUDGE, Thomas, M. , MORRIS, Joel
发明人： THE UPJOHN COMPANY
IPC分类号： C07D311/22
CPC分类号： C07D265/22 , C07D311/22 , C07D405/12 , C07D405/14 , C07D413/10 , C07D417/12
摘要： This invention relates to compounds of formula (I) which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of formula (I) are useful inhibitors of cell proliferation.
摘要翻译：本发明涉及与作为抗动脉粥样硬化剂的药物载体结合使用的式（I）化合物。此外，各种式（I）化合物是细胞增殖的有用抑制剂。

5. 发明申请

WO1990012799A1 ANTIBACTERIAL PYRIDO(1,2,3-DE)-1,4-BENZOXAZINONE AGENTS 审中-公开
标题翻译：抗菌素（1,2,3-DE）-1,4-苯并恶唑酮代谢物
公开(公告)号：WO1990012799A1
公开(公告)日：1990-11-01
申请号：PCT/US1990000286
申请日：1990-01-22
申请人： THE UPJOHN COMPANY , BISAHA, Sharon, N. , GAMMILL, Ronald, B. , JUDGE, Thomas, M.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D498/06
CPC分类号： C07D498/06
摘要： This invention concerns novel benzoxazinone carboxylic acids having a novel dimethyl 1,2-dicarboxyethylene substituent and their use in treating bacterial infections in warm blooded animals and man. The compounds of this invention (Formula I) are readily prepared by conventional chemical reactions.
摘要翻译：本发明涉及具有新的二甲基1,2-二羧基乙烯取代基的新的苯并恶嗪酮羧酸及其在治疗温血动物和人类中的细菌感染的用途。本发明的化合物（式I）通过常规化学反应容易地制备。

6. 发明申请

WO1990006921A1 ANTIATHEROSCLEROTIC AND ANTITHROMBOTIC 1-BENZOPYRAN-4-ONES AND 2-AMINO-1,3-BENZOXAZINE-4-ONES 审中-公开
标题翻译：抗真菌剂和抗坏血酸的1-苯并噻吩-4-酮和2-氨基-1,3-苯并恶唑-4-酮
公开(公告)号：WO1990006921A1
公开(公告)日：1990-06-28
申请号：PCT/US1989005526
申请日：1989-12-15
申请人： THE UPJOHN COMPANY , GAMMILL, Ronald, B. , JUDGE, Thomas, M. , MORRIS, Joel
发明人： THE UPJOHN COMPANY
IPC分类号： C07D311/22
CPC分类号： C07D265/22 , C07D311/22 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of formula (I) which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of formula (I) are useful inhibitors of cell proliferation.
摘要翻译：本发明涉及与作为抗动脉粥样硬化剂的药物载体结合使用的式（I）化合物。此外，各种式（I）化合物是细胞增殖的有用抑制剂。

7. 发明申请

WO1990002129A1 BIVALENT LIGANDS EFFECTIVE FOR BLOCKING ACAT ENZYME 审中-公开
标题翻译：有效阻止ACAT酶的双重配体
公开(公告)号：WO1990002129A1
公开(公告)日：1990-03-08
申请号：PCT/US1989002572
申请日：1989-06-16
申请人： THE UPJOHN COMPANY , GAMMILL, Ronald, B. , BELL, Frank, P.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D493/04
CPC分类号： C07D519/00 , C07F7/0814
摘要： Bivalent ligand compounds synthesized from a tether composition joining two heterocyclic groups comprising furochromones, furobenzoxazinones, and benzobisdifurans. These compounds show pharmacological activity in blocking ACAT enzymes which are major regulators of cholesterol metabolism. They are useful in the prevention or treatment of the constriction or obstruction of arterial vessels and atherosclerosis.
摘要翻译：从连接两个含有呋喃酮酮，呋喃并恶嗪酮和苯并双歧杆菌的杂环基的连接臂组合物合成的二价配体化合物。这些化合物显示了阻断作为胆固醇代谢的主要调节剂的ACAT酶的药理活性。它们可用于预防或治疗动脉血管和动脉粥样硬化的收缩或阻塞。

8. 发明申请

WO2004096768A1 ANTI-DIABETIC AGENTS 审中-公开
标题翻译：抗糖尿病药
公开(公告)号：WO2004096768A1
公开(公告)日：2004-11-11
申请号：PCT/IB2004/001400
申请日：2004-04-23
申请人： PFIZER PRODUCTS INC. , BUSSOLOTTI, Donald, L. , GAMMILL, Ronald, B.
发明人： BUSSOLOTTI, Donald, L. , GAMMILL, Ronald, B.
IPC分类号： C07D209/42
CPC分类号： C07D401/12 , C07D209/42 , C07D405/12 , C07D409/12 , C07D417/12 , C07D495/04
摘要： The invention provides compounds of formula (I) the prodrugs thereof, and the pharmaceutically acceptable salts of the compounds and prodrugs; wherein R', R", R"', X, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof in treating diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, and tissue ischemia.
摘要翻译：本发明提供式（I）化合物及其药物前体药物及其药学上可接受的盐; 其中R'，R“，R”'，X和Z如本文所定义; 其药物组合物; 及其用于治疗糖尿病，胰岛素抵抗，糖尿病性神经病，糖尿病性肾病，糖尿病性视网膜病变，白内障，高血糖症，高胆固醇血症，高血压，高胰岛素血症，高脂血症，动脉粥样硬化和组织缺血的用途。

9. 发明申请

WO9530670A3 PYRANONE COMPOUNDS USEFUL TO TREAT RETROVIRAL INFECTIONS 审中-公开
标题翻译：吡咯烷酮化合物可用于治疗复发性感染
公开(公告)号：WO9530670A3
公开(公告)日：1996-04-25
申请号：PCT/US9505219
申请日：1995-05-04
申请人： UPJOHN CO , ROMINES KAREN RENE , BUNDY GORDON L , SCHWARTZ THERESA M , TOMMASI RUBEN A , STROHBACH JOSEPH WALTER , TURNER STEVEN RONALD , THAISRIVONGS SUVIT , ARISTOFF PAUL ADRIAN , JOHNSON PAUL D , SKULNICK HARVEY IRVING , SKALETZKI LOUIS L , ANDERSON DAVID JOHN , MORRIS JOEL , GAMMILL RONALD B , LUKE GEORGE P
发明人： ROMINES KAREN RENE , BUNDY GORDON L , SCHWARTZ THERESA M , TOMMASI RUBEN A , STROHBACH JOSEPH WALTER , TURNER STEVEN RONALD , THAISRIVONGS SUVIT , ARISTOFF PAUL ADRIAN , JOHNSON PAUL D , SKULNICK HARVEY IRVING , SKALETZKI LOUIS L , ANDERSON DAVID JOHN , MORRIS JOEL , GAMMILL RONALD B , LUKE GEORGE P
IPC分类号： A61K31/365 , A61K31/366 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/47 , A61K31/4709 , A61K31/505 , A61K31/506 , A61K31/54 , A61P31/12 , C07D20060101 , C07D309/32 , C07D309/38 , C07D309/40 , C07D311/02 , C07D311/08 , C07D311/74 , C07D311/94 , C07D401/12 , C07D403/12 , C07D405/00 , C07D405/12 , C07D405/14 , C07D407/00 , C07D409/00 , C07D417/00 , C07D417/12
CPC分类号： C07D405/12 , C07D309/32 , C07D309/38 , C07D311/02 , C07D311/74 , C07D405/14
摘要： The present invention relates to compounds of formulae (I) and (II) which are pyran-2-ones, 5,6-dihydro-pyran-2-ones, 4-hydroxy-benzopyran-2-ones, 4-hydroxy-cycloalkyl[b]pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R10 and R20 taken together are formulae (III) and (IV).

10. 发明申请

WO1995030670A2 PYRANONE COMPOUNDS USEFUL TO TREAT RETROVIRAL INFECTIONS 审中-公开
标题翻译：吡咯烷酮化合物可用于治疗复发性感染
公开(公告)号：WO1995030670A2
公开(公告)日：1995-11-16
申请号：PCT/US1995005219
申请日：1995-05-04
申请人： THE UPJOHN COMPANY , ROMINES, Karen, Rene , BUNDY, Gordon, L. , SCHWARTZ, Theresa, M. , TOMMASI, Ruben, A. , STROHBACH, Joseph, Walter , TURNER, Steven, Ronald , THAISRIVONGS, Suvit , ARISTOFF, Paul, Adrian , JOHNSON, Paul, D. , SKULNICK, Harvey, Irving , SKALETZKI, Louis, L. , ANDERSON, David, John , MORRIS, Joel , GAMMILL, Ronald, B. , LUKE, George, P.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D309/32
CPC分类号： C07D405/12 , C07D309/32 , C07D309/38 , C07D311/02 , C07D311/74 , C07D405/14
摘要： The present invention relates to compounds of formulae (I) and (II) which are pyran-2-ones, 5,6-dihydro-pyran-2-ones, 4-hydroxy-benzopyran-2-ones, 4-hydroxy-cycloalkyl[b]pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R10 and R20 taken together are formulae (III) and (IV).
摘要翻译：本发明涉及式（I）和（II）的化合物，其为吡喃-2-酮，5,6-二氢 - 吡喃-2-酮，4-羟基 - 苯并吡喃-2-酮，4-羟基 - 环烷基 [b]吡喃-2-酮及其衍生物，其用于抑制感染所述逆转录病毒的哺乳动物细胞中的逆转录病毒，其中R10和R20一起是式（III）和（IV）。

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