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1. 发明授权

US5541204A Aryloxypropanolamine .beta. 3 adrenergic agonists 失效
标题翻译： Aryloxypropanolamine beta 3肾上腺素能激动剂
公开(公告)号：US5541204A
公开(公告)日：1996-07-30
申请号：US352824
申请日：1994-12-02
申请人： Philip M. Sher , William N. Washburn , Kathleen M. Poss
发明人： Philip M. Sher , William N. Washburn , Kathleen M. Poss
IPC分类号： A61K31/135 , A61K31/165 , A61K31/18 , A61K31/215 , A61K31/275 , A61K31/357 , A61K31/36 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/47 , A61P1/00 , A61P3/04 , A61P3/08 , A61P3/10 , A61P25/02 , A61P43/00 , C07C217/30 , C07C217/58 , C07C217/84 , C07C237/30 , C07C311/08 , C07C317/32 , C07C317/36 , C07D209/42 , C07D215/22 , C07D215/227 , C07D215/26 , C07D235/26 , C07D249/18 , C07D263/58 , C07D317/58 , C07D405/12
CPC分类号： C07D215/227 , C07C217/30 , C07C217/58 , C07C217/84 , C07C237/30 , C07C317/32 , C07D209/42 , C07D215/26 , C07D235/26 , C07D249/18 , C07D263/58 , C07D317/58 , C07D405/12
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1. These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.
摘要翻译：式I化合物及其药学上可接受的盐，其中：R 1至R 9如本文所定义，m为0或1的整数。这些化合物为β3肾上腺素能受体激动剂，因此可用于例如治疗的糖尿病，肥胖，胃肠道疾病和贲门失弛缓症。

2. 发明授权

US5208212A Herbicidal compositions containing triazolinones 失效
标题翻译：含有三唑啉酮的除草组合物
公开(公告)号：US5208212A
公开(公告)日：1993-05-04
申请号：US969648
申请日：1992-10-30
申请人： Kathleen M. Poss , Frederick W. Hotzman , Jacques Meyer
发明人： Kathleen M. Poss , Frederick W. Hotzman , Jacques Meyer
IPC分类号： A01N39/02 , A01N39/04 , A01N43/653 , A01N47/36 , A01P13/00 , C07D249/00 , C07D249/12
CPC分类号： A01N43/653 , C07D249/12
摘要： This invention relates to compositions comprising 1-aryl-4,5-dihydro-1,2,4-triazol-5(1H)-ones (triazolinones) in combination with the herbicide (2,4-dichlorophenoxy)acetic acid (2,4-D), or like substituted phenoxyalkanoic acids, or esters, or alkali metal or ammonium salts thereof; or with certain herbicidal sulfonylureas, or mixtures of these classes of compounds, to provide herbicidal compositions which are highly effective against a broad array of crop weeds, particularly broadleaf weeds, in crops such as wheat.
摘要翻译：本发明涉及包含1-芳基-4,5-二氢-1,2,4-三唑-5（1H） - 酮（三唑啉酮）与除草剂（2,4-二氯苯氧基）乙酸（2， 4-D）或类似的取代的苯氧烷酸，或其酯或其碱金属或铵盐; 或具有某些除草磺酰脲类或这些类化合物的混合物，以提供对作物如小麦中广泛的作物杂草，特别是阔叶杂草高度有效的除草组合物。

3. 发明授权

US5035740A Herbicidal compounds 失效
标题翻译：除草剂
公开(公告)号：US5035740A
公开(公告)日：1991-07-30
申请号：US352794
申请日：1989-05-16
申请人： Kathleen M. Poss
发明人： Kathleen M. Poss
IPC分类号： A01N43/653 , A01N43/713 , C07D249/12 , C07D253/075 , C07D257/04
CPC分类号： C07D253/075 , A01N43/653 , A01N43/713 , C07D249/12 , C07D257/04
摘要： A herbicidal compound of the formula ##STR1## in which Q is --CR.sup.1 (R.sup.2)C(R.sup.3)(R.sub.4)Q' or --CR.sup.1 .dbd.C(R.sup.4)Q';R.sup.1, R.sup.2 and R.sup.3 are each, independently, hydrogen, halogen, or lower alkyl;R.sup.4 is hydrogen or lower alkyl;Q' is COOH, COOZ, COOR.sup.5, CON (R.sup.6)(R.sup.7), CN, CHO or C(O)R.sup.5 ;Z is a salt-forming cation;R.sup.5 is alkyl, cycloalkyl or aralkyl;each of R.sup.6 and R.sup.7 is, independently, hydrogen alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, phenyl, benzyl, or SO.sub.2 R.sup.8 or is one of said radicals substituted by halogen, alkyl, or cyano, R.sup.8 being the same as R.sup.6 other than hydrogen or SO.sub.2 R.sup.8 ;NHet is a monovalent nitrogen-containing organic group; andNHet, X and Y are such that the Methoxy Analog or Propargyloxy Analog of said compound is a herbicide.
摘要翻译：其中Q为-CR1（R2）C（R3）（R4）Q'或-CR1 = C（R4）Q'的式IMAGE的除草化合物; R 1，R 2和R 3各自独立地为氢，卤素或低级烷基; R4是氢或低级烷基; Q'是COOH，COOZ，COOR5，CON（R6）（R7），CN，CHO或C（O）R5; Z是成盐阳离子; R5是烷基，环烷基或芳烷基; R6和R7各自独立地是氢烷基，环烷基，烯基，炔基，烷氧基，苯基，苄基或SO2R8，或者是被卤素，烷基或氰基取代的所述基团之一，R8与除氢以外的R6相同或SO2R8; NHet是一价含氮有机基团; 并且NHet，X和Y使得所述化合物的甲氧基类似物或炔丙氧基类似物是除草剂。

4. 发明授权

US4913724A Herbicidal tetrazolinones 失效
标题翻译：除草四唑啉酮
公开(公告)号：US4913724A
公开(公告)日：1990-04-03
申请号：US338029
申请日：1989-04-14
申请人： Kathleen M. Poss
发明人： Kathleen M. Poss
IPC分类号： A01N43/713 , C07D257/04
CPC分类号： C07D257/04 , A01N43/713
摘要： A herbicidal compound which is a Q-substituted 1-phenyl-4-substituted-1,4-dihydro-5H-tetrazol-5-one in which the Q-substituent is bonded to the ring-carbon atom at the 5-position of the phenyl group and in which:Q is --CH(R.sup.2)C(R.sup.3) (R.sup.4)Q' or --C(R.sup.2).dbd.C(R.sup.4)Q';R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, or halogen;R.sup.4 is hydrogen or lower alkyl;Q' is COOH, COOZ, COOR.sup.5, CON(R.sup.6) (R.sup.7), CN, CHO or C(O)R.sup.5 ;Z is a salt-forming cation;R.sup.5 is alkyl, cycloalkyl or aralkyl;each of R.sup.6 and R.sup.7 is, independently, hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, phenyl, benzyl or SO.sub.2 R.sup.8, or is one of said radicals substituted by halogen, alkyl or cyano, R.sup.8 being the same as R.sup.6 other than hydrogen or SO.sub.2 R.sup.8 ; said compound being one whose 5-Methoxy Analog and 5-Propargyloxy Analog are herbicides.
摘要翻译：作为Q取代的1-苯基-4-取代-1,4-二氢-5H-四唑-5-酮的除草化合物，其中Q-取代基与5-位的环碳原子键合苯基，其中：Q为-CH（R2）C（R3）（R4）Q'或-C（R2）= C（R4）Q'; R2和R3各自独立地为氢，烷基或卤素; R4是氢或低级烷基; Q'是COOH，COOZ，COOR5，CON（R6）（R7），CN，CHO或C（O）R5; Z是成盐阳离子; R5是烷基，环烷基或芳烷基; R 6和R 7各自独立地为氢，烷基，环烷基，烯基，炔基，烷氧基，苯基，苄基或SO 2 R 8，或者是被卤素，烷基或氰基取代的所述基团之一，R 8与除氢或SO2R8; 所述化合物是其5-甲氧基类似物和5-炔丙氧基类似物是除草剂的化合物。

5. 发明授权

US5770615A Catecholamine surrogates useful as .beta..sub.3 agonists 失效
标题翻译：儿茶酚胺替代物可用作β3激动剂
公开(公告)号：US5770615A
公开(公告)日：1998-06-23
申请号：US825309
申请日：1997-03-28
申请人： Peter T. W. Cheng , Gregory S. Bisacchi , Ashvinikumar V. Gavai , Kathleen M. Poss , Denis E. Ryono , Philip M. Sher , Chong-qing Sun , William N. Washburn
发明人： Peter T. W. Cheng , Gregory S. Bisacchi , Ashvinikumar V. Gavai , Kathleen M. Poss , Denis E. Ryono , Philip M. Sher , Chong-qing Sun , William N. Washburn
IPC分类号： C07C311/08 , C07C311/39 , C07C311/46 , C07D263/32 , C07D277/28 , C07F9/40 , A61K31/425 , A61K31/165 , C07C321/00
CPC分类号： C07C311/46 , C07C311/08 , C07C311/39 , C07D263/32 , C07D277/28 , C07F9/4056
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof. These compounds are beta three adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
摘要翻译：式Ⅰ化合物及其药学上可接受的盐。这些化合物是β三肾上腺素能受体激动剂，因此可用于例如治疗糖尿病，肥胖症和胃肠道疾病。

6. 发明授权

US5776983A Catecholamine surrogates useful as .beta..sub.3 agonists 失效
标题翻译：儿茶酚胺替代物作为β3激动剂有用
公开(公告)号：US5776983A
公开(公告)日：1998-07-07
申请号：US346543
申请日：1994-12-02
申请人： William N. Washburn , Ravindar N. Girotra , Philip M. Sher , Amarendra B. Mikkilineni , Kathleen M. Poss , Arvind Mathur , Gregory S. Bisacchi , Ashvinikumar V. Gavai
发明人： William N. Washburn , Ravindar N. Girotra , Philip M. Sher , Amarendra B. Mikkilineni , Kathleen M. Poss , Arvind Mathur , Gregory S. Bisacchi , Ashvinikumar V. Gavai
IPC分类号： C07D295/12 , A61K31/18 , A61K31/215 , A61K31/275 , A61K31/336 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61P1/00 , A61P3/04 , A61P3/08 , A61P3/10 , C07C311/08 , C07C311/13 , C07C311/21 , C07D213/38 , C07D213/64 , C07D213/69 , C07D213/71 , C07D257/00 , C07D303/36 , C07D317/58 , C07D317/66 , C07D333/20 , C07D333/58 , A61K31/22
CPC分类号： C07D213/64 , C07C311/08 , C07C311/13 , C07C311/21 , C07D213/38 , C07D213/69 , C07D317/58 , C07D317/66 , C07D333/20 , C07D333/58 , Y10S514/866 , Y10S514/909 , Y10S514/91
摘要： Compounds of the formula ##STR1## or pharmaceutically acceptable salts thereof wherein: A is a bond, --(CH.sub.2).sub.n -- or --CH(B)--, where n is an integer of 1 to 3 and B is --CN, --CON(R.sup.9)R.sup.9' or --CO.sub.2 R.sup.7 ; R.sup.1 is lower alkyl, aryl or arylalkyl; R.sup.2 is hydrogen, hydroxy, alkoxy, --CH.sub.2 OH, cyano, --C(O)OR.sup.7, --CO.sub.2 H, --CONH.sub.2, tetrazole, --CH.sub.2 NH.sub.2 or halogen; ##STR2## R.sup.3 is hydrogen, alkyl, heterocycle or R.sup.4 is hydrogen, alkyl or B; R.sup.5, R.sup.5', R.sup.8, R.sup.8' or R.sup.8" are independently hydrogen, alkoxy, lower alkyl, halogen, --OH, --CN, --(CH.sub.2).sub.n NR.sup.6 COR.sup.7, --CON(R.sup.6)R.sup.6', --CON(R.sup.6)OR.sup.6', --CO.sub.2 R.sup.6, --SR.sup.7, --SOR.sup.7, --SO.sub.2 R.sup.7, --N(R.sup.6)SO.sub.2 R.sup.1, --N(R.sup.6)R.sup.6', --NR.sup.6 COR.sup.7, --OCH.sub.2 CON(R.sup.6)R.sup.6', --OCH.sub.2 CO.sub.2 R.sup.7 or aryl; orR.sup.5 and R.sup.5' or R.sup.8 and R.sup.8' may together with the carbon atoms to which they are attached form an aryl or heterocycle; R.sup.6 and R.sup.6' are independently hydrogen or lower alkyl; and R.sup.7 is lower alkyl; R.sup.9 is hydrogen, lower alkyl, alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl; or R.sup.9 and R.sup.9' may together with the nitrogen atom to which they are attached form a heterocycle; with the proviso that when A is a bond or --(CH.sub.2).sub.n and R.sup.3 is hydrogen or unsubstituted alkyl, then R.sup.4 is B or substituted alkyl. These compounds are beta.sub.3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
摘要翻译：式I的化合物或其药学上可接受的盐，其中：A为键， - （CH 2）n - 或-CH（B） - ，其中n为1至3的整数，B为-CN， - CON（R9）R9'或-CO2R7; R1是低级烷基，芳基或芳基烷基; R 2是氢，羟基，烷氧基，-CH 2 OH，氰基，-C（O）OR 7，-CO 2 H，-CONH 2，四唑，-CH 2 NH 2或卤素; R 3是氢，烷基，杂环或R 4是氢，烷基或B; R5，R5'，R8，R8'或R8“独立地是氢，烷氧基，低级烷基，卤素，-OH，-CN， - （CH2）nNR6COR7，-CON（R6）R6'，-CON （R 6）SO 2 R 1，-N（R 6）R 6'，-NR 6 COR 7，-OCH 2 CON（R 6）R 6'，-OCH 2 CO 2 R 7或芳基; 或R5和R5'或R8和R8'可以与它们所连接的碳原子一起形成芳基或杂环; R6和R6'独立地是氢或低级烷基; 并且R 7为低级烷基; R9是氢，低级烷基，烷基，环烷基，芳烷基，芳基，杂芳基; 或R 9和R 9'可以与它们所连接的氮原子一起形成杂环; 条件是当A为键或 - （CH 2）n且R 3为氢或未取代的烷基时，则R 4为B或取代的烷基。这些化合物是β3肾上腺素能受体激动剂，因此可用于例如治疗糖尿病，肥胖症和胃肠道疾病。

7. 发明授权

US5286746A Sulfur-substituted mevinic acid derivatives 失效
标题翻译：硫取代的维甲酸衍生物
公开(公告)号：US5286746A
公开(公告)日：1994-02-15
申请号：US811124
申请日：1991-12-20
申请人： Kathleen M. Poss
发明人： Kathleen M. Poss
IPC分类号： C07C309/27 , C07D309/30 , A61K31/35
CPC分类号： C07C309/27 , C07D309/30 , C07C2102/28
摘要： Antihypercholesterolemic activity is exhibited by compounds of the formula ##STR1## wherein: X is hydrogen, alkali metal or ammonium;Y is hydrogen, alkyl, cycloalkyl, aryl, or aralkyl; ##STR2## R is hydrogen, alkyl, ammonium, alkylammonium, or alkali metal (such as Na, Li, or K); andn is 1 or 2.
摘要翻译：抗高血胆固醇活性由下式化合物表现：其中：X为氢，碱金属或铵; Y是氢，烷基，环烷基，芳基或芳烷基; R是氢，烷基，铵，烷基铵或碱金属（如Na，Li或K）; n为1或2。

8. 发明授权

US5217520A Herbicidal triazolinones 失效
标题翻译：除草剂三唑啉酮
公开(公告)号：US5217520A
公开(公告)日：1993-06-08
申请号：US852424
申请日：1992-03-16
申请人： Kathleen M. Poss
发明人： Kathleen M. Poss
IPC分类号： A01N43/653 , C07D249/12
CPC分类号： C07D249/12 , A01N43/653
摘要： A herbicidal compound which is a Q-substituted 1-phenyl-4,5-dihydro-1,2,4-triazol-5(1H)-one in which the Q-substituent is bonded to the ring-carbon atom at the 5-position of the phenyl group and in which:Q is --CH(R.sup.2)C(R.sup.3) (R.sup.4)Q' or --CH.dbd.C(R.sup.4)Q';R.sup.2 and R.sup.3 are each, independently, H or halogen;R.sup.4 is H or lower alkyl;Q' is COOH, COOZ, COOR.sup.5, CON(R.sup.6) (R.sup.7), CN, CHO or C(O)R.sup.5 ;Z is a salt-forming group;R.sup.5 is alkyl, alkoxycarbonylalkyl, cycloalkyl or aralkyl;each of R.sup.6 and R.sup.7 is, independently, a radical which is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, phenyl, benzyl or SO.sub.2 R.sup.6 or is one of said radicals substituted by halogen, alkyl or cyano; said compound being one whose 5-Methoxy Analogs and 5-Propargyloxy Analog are herbicides.
摘要翻译：作为Q取代的1-苯基-4,5-二氢-1,2,4-三唑-5（1H） - 酮的除草化合物，其中Q取代基在5位上与环碳原子连接 - 其中：Q是-CH（R2）C（R3）（R4）Q'或-CH = C（R4）Q'; R2和R3各自独立地为H或卤素; R4是H或低级烷基; Q'是COOH，COOZ，COOR5，CON（R6）（R7），CN，CHO或C（O）R5; Z是成盐基团; R5是烷基，烷氧基羰基烷基，环烷基或芳烷基; R 6和R 7各自独立地为烷基，环烷基，烯基，炔基，烷氧基，苯基，苄基或SO 2 R 6基团，或者是被卤素，烷基或氰基取代的所述基团之一; 所述化合物是其5-甲氧基类似物和5-炔丙基氧基类似物是除草剂的化合物。

9. 发明授权

US5723489A Aryloxypropanolamine beta 3 adrenergic agonists 失效
公开(公告)号：US5723489A
公开(公告)日：1998-03-03
申请号：US646164
申请日：1996-05-07
申请人： Philip M. Sher , William N. Washburn , Kathleen M. Poss
发明人： Philip M. Sher , William N. Washburn , Kathleen M. Poss
IPC分类号： A61K31/135 , A61K31/165 , A61K31/18 , A61K31/215 , A61K31/275 , A61K31/357 , A61K31/36 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/47 , A61P1/00 , A61P3/04 , A61P3/08 , A61P3/10 , A61P25/02 , A61P43/00 , C07C217/30 , C07C217/58 , C07C217/84 , C07C237/30 , C07C311/08 , C07C317/32 , C07C317/36 , C07D209/42 , C07D215/22 , C07D215/227 , C07D215/26 , C07D235/26 , C07D249/18 , C07D263/58 , C07D317/58 , C07D405/12 , A61K31/335 , C07C217/32 , C07C217/34
CPC分类号： C07D215/227 , C07C217/30 , C07C217/58 , C07C217/84 , C07C237/30 , C07C317/32 , C07D209/42 , C07D215/26 , C07D235/26 , C07D249/18 , C07D263/58 , C07D317/58 , C07D405/12
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1. These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.

10. 发明授权

US5369123A Nitrogen-substituted mevinic acid derivatives useful as HMG-CoA reductase inhibitors 失效
标题翻译：可用作HMG-CoA还原酶抑制剂的氮取代的维甲酸衍生物
公开(公告)号：US5369123A
公开(公告)日：1994-11-29
申请号：US958849
申请日：1992-10-09
申请人： Dinos P. Santafianos , Kathleen M. Poss , Eric M. Gordon , Peggy J. McCann
发明人： Dinos P. Santafianos , Kathleen M. Poss , Eric M. Gordon , Peggy J. McCann
IPC分类号： C07C229/46 , C07C233/81 , C07C235/14 , C07C237/12 , C07C237/38 , C07C271/24 , C07C275/26 , C07C307/08 , C07D295/155 , C07D309/30 , A61K31/40 , A61K31/365 , C07C69/74
CPC分类号： C07D295/155 , C07C229/46 , C07C233/81 , C07C235/14 , C07C237/12 , C07C237/38 , C07C271/24 , C07C275/26 , C07C307/08 , C07D309/30 , C07C2102/28
摘要： Novel nitrogen-substituted mevinic acid derivatives which inhibit the activity of HMG-CoA reductase. Pharmaceutical compositions, and methods of use for the treatment or prevention of hypercholesterolemia, atherosclerosis, hyperlipoproteinaemia and hyperlipidemia are provided, as are novel methods for preparation and intermediate compounds.
摘要翻译：抑制HMG-CoA还原酶活性的新型含氮取代的维甲酸衍生物。还提供了用于治疗或预防高胆固醇血症，动脉粥样硬化，高脂蛋白血症和高脂血症的药物组合物和方法，以及新制备方法和中间体化合物。

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