公开(公告)号：US4118591A

公开(公告)日：1978-10-03

申请号：US809254

申请日：1977-06-23

申请人： David C. Peterson

发明人： David C. Peterson

IPC分类号： C07C53/21 ,  C07C405/00 ,  C07D263/04 ,  C07D307/24 ,  C07D307/935 ,  C07D309/12 ,  C07D313/06 ,  C07D319/06 ,  C07D339/06 ,  C07F9/40 ,  C07C69/76 ,  C07C177/00

CPC分类号： C07D263/04 ,  C07C405/00 ,  C07C405/0025 ,  C07C53/21 ,  C07D307/24 ,  C07D307/935 ,  C07D309/12 ,  C07D313/06 ,  C07D319/06 ,  C07D339/06 ,  C07F9/4006

摘要： Prostaglandin analogs with the following cyclopentane ring structure: ##STR1## are disclosed along with intermediates useful in their preparation and processes for their preparation. These analogs are useful for some of the same pharmacological purposes as the prostaglandins, particularly and especially as blood platelet aggregation inhibitors.

公开(公告)号：US20020082448A1

公开(公告)日：2002-06-27

申请号：US09903713

申请日：2001-07-13

申请人： The Upjohn Company

发明人： Scott D. Larsen ,  Valerie A. Vaillancourt ,  Paul D. May ,  Steven P. Tanis ,  John A. Tucker ,  Martin D. Meglasson ,  Heinrich J. Schostarez

IPC分类号： A61K031/195 ,  C07C251/02

CPC分类号： C07C281/16 ,  A61K31/195

摘要： The present invention provide for a method of reducing blood glucose levels in a patient by administering an effective amount of a compound of the formula III or a pharmaceutically acceptable salt thereof; 1 wherein R3 is hydrogen, methyl, ethyl, CH2phenyl, or n-hexyl.

摘要翻译： 本发明提供通过施用有效量的式III化合物或其药学上可接受的盐来降低患者血糖水平的方法; 其中R 3是氢，甲基，乙基，CH 2苯基或正己基。

公开(公告)号：US5650427A

公开(公告)日：1997-07-22

申请号：US460449

申请日：1995-06-02

申请人： Hakan Vilhelm Wikstrom ,  Per Arvid Emil Carlsson ,  Bengt Ronny Andersson ,  Kjell Anders Ivan Svensson ,  Stig Thomas Elebring ,  Nils Peter Stjernlof ,  Arthur Glenn Romero ,  Susanne R. Haadsma-Svensson ,  Chiu-Hong Lin ,  Michael Dalton Ennis

发明人： Hakan Vilhelm Wikstrom ,  Per Arvid Emil Carlsson ,  Bengt Ronny Andersson ,  Kjell Anders Ivan Svensson ,  Stig Thomas Elebring ,  Nils Peter Stjernlof ,  Arthur Glenn Romero ,  Susanne R. Haadsma-Svensson ,  Chiu-Hong Lin ,  Michael Dalton Ennis

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/407 ,  A61K31/435 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/454 ,  A61K31/475 ,  A61P11/14 ,  A61P25/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D209/56 ,  C07D209/60 ,  C07D209/66 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D409/12 ,  C07D413/04 ,  C07D471/04 ,  C07D491/04 ,  C07D491/052 ,  C07D495/04

CPC分类号： C07D401/12 ,  C07D209/66 ,  C07D409/12 ,  C07D491/04

摘要： A compound of Formula I ##STR1## or pharmaceutically acceptable salts of Formula I, where R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, --(CH.sub.2).sub.n CONH.sub.2 where n is 2 to 6, (CH2).sub.n -1-(4,4-dimethylpiperidine-2,6-dione-yl), or cyclopropylmethyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl or combined with R.sup.1 to form a C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 akynyl, (CH.sub.2).sub.n --X--Ar where X is O, S, or NH, 3,3,3-trifluoropropyl, --(CH.sub.2).sub.m --R.sup.9 where m is 2 or 3 and R.sup.9 is phenyl, 2-thiophenyl or 3-thiophenyl; R.sup.3 is hydrogen, C.sub.1 -C.sub.3 alkyl, 2,2,2-trifluoroethyl, 3,3,3-trifluoropropyl, formyl, CN, halogen, CH.sub.2 OR.sup.2, C(O)C(O)OR.sup.1, C(O)CO NR.sup.1 R.sup.2, --(CH.sub.2).sub.q --NR.sup.1 R.sup.2 where q is 0 to 5, C.dbd.NOR.sup.2, 2(4,5-dihydro)oxazolyl, or COR.sup.10 where R.sup.10 is H, R.sup.1, NR.sup.1 R.sup.2 or CF.sub.3 ; R.sup.4 is hydrogen, C.sub.1 -C.sub.3 alkyl, cyclopropylmethyl, CF.sub.3, 2,2,2-trifluoroethyl, CN, CONR.sup.1 R.sup.2, .dbd.O, 2(4,5-dihydro)imidazolyl, 2(4,5-dihydro)oxazolyl, 2-oxazolyl, 3-oxadiazolyl, or 3,3,3-trifluoropropyl; R.sup.5 is hydrogen, R.sup.1, OCH.sub.3, C(O)CH.sub.3 or C(O)OR.sup.1 ; X is (a) a valence bond, (b) CH.sub.2, or (c) O, S or NR.sup.5 where R.sup.5 is H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, benzyl, COR.sup.6 where R.sup.6 is a C.sub.1 -C.sub.3 alkyl, phenyl, or CONR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are independently H or C.sub.1 -C.sub.3 alkyl; andZ is a hydrogen or halogen; provided that when X is CH.sub.2, at least one of R.sub.3 and R.sub.4 is other than hydrogen or C.sub.1 -C.sub.3 alkyl. The compounds of Formula I are suitable for treating disorders of the central nervous system, particularly as 5-HT.sub.1A receptor agonists.

摘要翻译： 其中R1为H，C1-C3烷基， - （CH2）nCONH2，其中n为2-6，（CH2）n-1-（4,4-二甲氧基苯基） 二甲基哌啶-2,6-二酮基）或环丙基甲基; R2是氢，C1-C8烷基，C3-C8环烷基或与R1结合以形成C 3 -C 8环烷基，C 2 -C 8烯基，C 2 -C 8炔基，（CH 2）n X-Ar，其中X是O，S或NH ，3,3,3-三氟丙基， - （CH 2）m -R 9，其中m为2或3，R 9为苯基，2-噻吩基或3-噻吩基; R3是氢，C1-C3烷基，2,2,2-三氟乙基，3,3,3-三氟丙基，甲酰基，CN，卤素，CH2OR2，C（O）C（O）OR1，C（O） - （CH2）q-NR1R2其中q为0至5，C = NOR2,2（4,5-二氢）恶唑基或COR 10，其中R 10为H，R 1，NR 1 R 2或CF 3; R4是氢，C1-C3烷基，环丙基甲基，CF3,2,2,2-三氟乙基，CN，CONR1R2，= 2,2（4,5-二氢）咪唑基，2（4,5-二氢）恶唑基， 恶唑基，3-恶二唑基或3,3,3-三氟丙基; R5是氢，R1，OCH3，C（O）CH3或C（O）OR1; X是（a）价键，（b）CH 2或（c）O，S或NR 5，其中R 5是H，C 1 -C 8烷基，C 3 -C 8环烷基，苄基，COR 6，其中R 6是C 1 -C 3烷基， 苯基或CONR 7 R 8，其中R 7和R 8独立地为H或C 1 -C 3烷基; Z为氢或卤素; 条件是当X是CH 2时，R 3和R 4中的至少一个不是氢或C 1 -C 3烷基。 式I化合物适用于治疗中枢神经系统疾病，特别是5-HT 1A受体激动剂。

公开(公告)号：US5621123A

公开(公告)日：1997-04-15

申请号：US247169

申请日：1994-05-20

申请人： Roy A. Johnson ,  Gordon L. Bundy ,  Gilbert A. Youngdale ,  Douglas R. Morton ,  Donald P. Wallach, deceased ,  Vera M. Wallach, legal representative

发明人： Roy A. Johnson ,  Gordon L. Bundy ,  Gilbert A. Youngdale ,  Douglas R. Morton ,  Donald P. Wallach, deceased ,  Vera M. Wallach, legal representative

IPC分类号： C07D213/38 ,  C07F9/22 ,  C07F9/24 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00

CPC分类号： C07J51/00 ,  C07D213/38 ,  C07F9/224 ,  C07F9/2458 ,  C07J41/0005 ,  C07J41/005 ,  C07J41/0072 ,  C07J43/003 ,  Y10S514/866

摘要： Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.

摘要翻译： 提供式I的环状烃与氨基烷基侧链可用于治疗磷脂酶A2介导的病症，糖尿病和肥胖症。

公开(公告)号：US5599841A

公开(公告)日：1997-02-04

申请号：US101350

申请日：1993-08-02

申请人： Martin D. Meglasson

发明人： Martin D. Meglasson

IPC分类号： A61K31/195 ,  A61K31/19 ,  A61K31/155

CPC分类号： A61K31/195

摘要： The present invention provides a method for treating or preventing certain metabolic disorders comprising the systemic administration of 3-guanidinopropionic acid.

摘要翻译： 本发明提供了治疗或预防包括全身给予3-胍基丙酸的某些代谢紊乱的方法。

公开(公告)号：US5594024A

公开(公告)日：1997-01-14

申请号：US455474

申请日：1995-05-31

申请人： Kjell A. I. Svensson ,  Hakan V. Wikstrom ,  Per A. E. Carlsson ,  Anna M. P. Boije ,  R. Nicholas Waters ,  Clas A. Sonesson ,  Nils P. Stjernlof ,  Bengt R. Andersson ,  Lars O. Hansson

发明人： Kjell A. I. Svensson ,  Hakan V. Wikstrom ,  Per A. E. Carlsson ,  Anna M. P. Boije ,  R. Nicholas Waters ,  Clas A. Sonesson ,  Nils P. Stjernlof ,  Bengt R. Andersson ,  Lars O. Hansson

IPC分类号： A61K31/44 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/451 ,  A61K31/535 ,  A61K31/55 ,  A61P25/00 ,  A61P25/02 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P43/00 ,  C07D207/08 ,  C07D207/09 ,  C07D211/08 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/24 ,  C07D211/26 ,  C07D211/28 ,  C07D211/30 ,  C07D211/34 ,  C07D211/76 ,  C07D223/04 ,  C07D227/04 ,  C07D401/00 ,  C07D401/10 ,  C07D403/00 ,  C07D405/00 ,  C07D405/10 ,  C07D409/06 ,  C07D409/10 ,  C07D411/10 ,  C07D413/00 ,  C07D413/10 ,  C07D417/00 ,  C07D455/02 ,  C07D471/04 ,  C07D487/04 ,  C07D207/04

CPC分类号： C07D207/08 ,  C07D207/09 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/24 ,  C07D211/28 ,  C07D211/34 ,  C07D211/76 ,  C07D223/04 ,  C07D409/06 ,  C07D409/10 ,  C07D455/02 ,  C07D487/04

摘要： A compound or Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 1 or 2; R.sup.1 and R.sup.2 are independently H (provided only one is H at the same time), --OH, CN, CH.sub.2 CN, 2- or 4-CF.sub.3, CH.sub.2 CF.sub.3, CH.sub.2 CHF.sub.2, CH.dbd.CF.sub.2, (CH.sub.2).sub.2 CF.sub.3, ethenyl, 2-propenyl, OSO.sub.2 CH.sub.3, OSO.sub.2 CF.sub.3, SSO.sub.2 CF.sub.3, COR, COOR, CON(R).sub.2, SO.sub.x CH.sub.3 (where, x is 0-2), SO.sub.x CF.sub.3, O(CH.sub.2).sub.x CF.sub.3, SO.sub.2 N(R).sub.2, CH.dbd.NOR, COCOOR, COCOON(R).sub.2, C.sub.1-8 alkyls, C.sub.3-8 cycloalkyls, CH.sub.2 OR, CH.sub.2 (R).sub.2, NRSO.sub.2 CF.sub.3, NO.sub.2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R.sup.3 is hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, --(CH.sub.2).sub.m --R.sup.5 (where m is 1-8), CH.sub.2 SCH.sub.3 or a C.sub.4 -C.sub.8 alkylene bonded to said nitrogen and one of its adjacent carbon atoms inclusive whereby a heterocyclic structure is formed; R.sup.4 and R are independently selected from hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, --(CH.sub.2).sub.m --R.sup.5 where m is 1-8; R.sup.5 is phenyl, phenyl (substituted with a CN, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 alkynyl), 2-thiophenyl, 3-thiophenyl, --NR.sup.6 CONR.sup.6 R.sup.7, or --CONR.sup.6 R.sup.7 ; R.sup.6 and R.sup.7 are independently hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkylmethyl, C.sub.2 -C.sub.8 alkenyl or C.sub.2 -C.sub.8 alkynyl; and with the proviso that when R.sup.1 is CN, R.sup.2 and R.sup.4 are H, R.sup.3 is n-Pr and n is 1, then such compound is a pure enantiomer, and when R.sup.1 or R.sup.2 is OH, halogen, CONH.sub.2 or alkyl, then R.sup.4 is not hydrogen. The Formula I compounds possess selective pharmacological properties and are useful in treating central nervous system disorders related to dopamine receptor activity including depression symptoms, geriatric disorders in the improvement of mental and motor functions, schizophrenia, narcolepsy, MBD, obesitas, and disturbances of sexual functions and impotence.

公开(公告)号：US5565468A

公开(公告)日：1996-10-15

申请号：US313684

申请日：1994-09-27

申请人： Scott D. Larsen ,  Charles H. Spilman

发明人： Scott D. Larsen ,  Charles H. Spilman

IPC分类号： A61K31/415 ,  A61K31/435 ,  A61P9/10 ,  C07D471/04 ,  C07D487/04 ,  C07F7/08 ,  C07F7/10 ,  A61K31/44

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07F7/0814

摘要： Imidazopyridino- and pyrazolopyridino- substituted oximes are disclosed having the formulas ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and a are as described in the claims. for the treatment of atherosclerosis and hypercholesterolemia.

摘要翻译： 公开了具有下式的咪唑并吡啶并 - 吡唑并吡啶并 - 取代的肟。其中R 1，R 2，R 3，R 4，R 5和a如权利要求书中所述，其中R 1，R 2，R 3，R 4，R 5和 。 用于治疗动脉粥样硬化和高胆固醇血症。

公开(公告)号：US5552152A

公开(公告)日：1996-09-03

申请号：US469715

申请日：1995-06-06

申请人： Robert W. Shen

发明人： Robert W. Shen

IPC分类号： A61K9/52 ,  A61K9/00 ,  A61K9/20 ,  A61K9/22 ,  A61K9/32 ,  A61K9/50 ,  A61K31/19 ,  A61P25/04 ,  A61P29/00 ,  A61K9/58

CPC分类号： A61K9/2081 ,  A61K31/19 ,  A61K9/0056 ,  A61K9/5026

摘要： A chewable taste-masked ibuprofen tablet having controlled release characteristics.

摘要翻译： 具有控制释放特征的可咀嚼口味的布洛芬片剂。

公开(公告)号：US5525742A

公开(公告)日：1996-06-11

申请号：US257856

申请日：1994-06-10

申请人： Robert C. Gadwood ,  Vincent E. Groppi, Jr.

发明人： Robert C. Gadwood ,  Vincent E. Groppi, Jr.

IPC分类号： C07C279/28

CPC分类号： C07C279/28

摘要： This invention comprises novel compounds that are useful and effective as photoaffinity probes useful for the identification of the biochemical components that form K.sub.ATP channels in smooth muscle cells. The probes are described by the formula below, ##STR1## where R.sub.1 is H, C.sub.1-3 alkyl; R.sub.2 is H, C.sub.1-3 alkyl; orR.sub.1 and R.sub.2 may be joined together to form C.sub.3-6 cycloalkyl, or C.sub.3-6 cycloalkyl optionally substituted with C.sub.1-4 alkyl;R.sub.3 is C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with 1-3 Halogens; or suitable salts thereof.

摘要翻译： 本发明包括作为光亲和探针有用和有效的新型化合物，其可用于鉴定在平滑肌细胞中形成KATP通道的生化成分。 探针由下式描述，烷基： 或者R 1和R 2可以连接在一起形成C 3-6环烷基或任选被C 1-4烷基取代的C 3-6环烷基; R3是C1-6烷基或任选被1-3个卤素取代的C 6-12芳基; 或其合适的盐。

公开(公告)号：US5510537A

公开(公告)日：1996-04-23

申请号：US427935

申请日：1995-04-26

申请人： Paul M. Herrinton

发明人： Paul M. Herrinton

IPC分类号： C07C45/27 ,  C07C49/203 ,  C07C49/213 ,  C07C49/603 ,  C07C49/794 ,  C07D493/04 ,  C07C45/00

CPC分类号： C07D493/04 ,  C07C45/27

摘要： A process for oxidizing silyl enone ethers to alpha, beta-unsaturated enodes having the formulas ##STR1## which comprises reacting the appropriate silyl enone ether with a radical generated by the metal catalyst decomposition of a peroxide composition.

摘要翻译： 将甲硅烷基醚醚氧化为具有式II'的α，β-不饱和烯酸的方法，其包括使合适的甲硅烷基醚与由过氧化物组合物的金属催化剂分解产生的自由基反应。