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31. 发明授权

US4520025A Bicyclic nitrogen heterocyclic ethers and thioethers, and their pharmaceutical uses 失效
标题翻译：双环氮杂环醚和硫醚及其制药用途
公开(公告)号：US4520025A
公开(公告)日：1985-05-28
申请号：US400350
申请日：1982-07-21
申请人： Henry F. Campbell , Donald E. Kuhla , William L. Studt , Stuart A. Dodson
发明人： Henry F. Campbell , Donald E. Kuhla , William L. Studt , Stuart A. Dodson
IPC分类号： C07D217/02 , C07D217/04 , C07D217/10 , C07D217/14 , C07D217/22 , C07D217/24 , C07D217/26 , C07D401/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D417/00 , C07D417/12 , C07D491/00 , C07D491/04 , C07D495/00 , C07D495/04 , A61K31/47
CPC分类号： C07D401/12 , C07D217/02 , C07D217/04 , C07D217/10 , C07D217/14 , C07D217/22 , C07D217/24 , C07D217/26 , C07D401/14 , C07D405/14 , C07D417/12 , C07D491/04 , C07D495/04
摘要： A class of bicyclic nitrogen heterocyclic ether and thioether compounds exhibiting pharmacological activity including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.
摘要翻译：公开了一类具有包括抗分泌和抗溃疡活性的药理学活性的双环氮杂环醚和硫醚化合物，包含这些化合物的药物组合物，以及使用所述组合物治疗哺乳动物中的胃肠胃酸性和溃疡性疾病的方法。

32. 发明授权

US4387235A Intermediates for the preparation of gamma-pyrones 失效
标题翻译：用于制备γ-吡喃酮的中间体
公开(公告)号：US4387235A
公开(公告)日：1983-06-07
申请号：US311252
申请日：1981-10-14
申请人： Thomas M. Brennan , Daniel P. Brannegan , Paul D. Weeks , Donald E. Kuhla
发明人： Thomas M. Brennan , Daniel P. Brannegan , Paul D. Weeks , Donald E. Kuhla
IPC分类号： C07D309/32 , C07D309/40 , C07D309/22
CPC分类号： C07D309/40 , C07D309/32
摘要： 2-methyl-3-hydroxy-4H-pyran-4-one is prepared by contacting 1(2-furyl)-1-ethanol in aqueous solution with two equivalents of a halogen oxidant at room temperature and then heating until the hydrolysis of the formed 4-halo-dihydropyran intermediate is substantially complete. Other valuable related gammapyrones are prepared in analogous manner from appropriate alcohols.
摘要翻译：通过在室温下使1（2-呋喃基）-1-乙醇在水溶液中与2当量的卤素氧化剂接触，然后加热至水解，得到2-甲基-3-羟基-4H-吡喃-4-酮形成的4-卤代 - 二氢吡喃中间体基本上完成。其他有价值的相关的吉司他林以适当的醇类似的方式制备。

33. 发明授权

US4368331A 3,4-Dihalo-tetrahydrophyran-5-one useful as intermediates for the preparation of gamma-pyrones 失效
标题翻译：可用作制备γ-吡喃酮的中间体的3,4-二卤代 - 四氢化间-5-酮
公开(公告)号：US4368331A
公开(公告)日：1983-01-11
申请号：US93629
申请日：1979-11-13
申请人： Thomas M. Brennan , Daniel P. Brannegan , Donald E. Kuhla , Paul D. Weeks
发明人： Thomas M. Brennan , Daniel P. Brannegan , Donald E. Kuhla , Paul D. Weeks
IPC分类号： C07D309/32 , C07D309/40 , C07D309/22
CPC分类号： C07D309/32 , C07D309/40
摘要： (2-methyl-3-hydroxy-4h-pyran-4-one is prepared by contacting 1(2-furyl)-1-ethanol in aqueous solution with two equivalents of a halogen oxidant at room temperature and then heating until the hydrolysis of the formed 4-halo-dihydro-pyran intermediate is substantially complete. Other valuable related gamma-pyrones are prepared in analogous manner from appropriate alcohols.
摘要翻译：（2-甲基-3-羟基-4H-吡喃-4-酮通过在室温下将1（2-呋喃基）-1-乙醇与2当量卤素氧化剂接触，然后加热至水解形成的4-卤代 - 二氢 - 吡喃中间体基本上是完全的。其它有价值的相关的γ-吡喃酮类似地由合适的醇制备。

34. 发明授权

US4173572A Preparation of gamma-pyrones from 3-substituted furans 失效
标题翻译：从3-取代呋喃制备γ-吡喃酮
公开(公告)号：US4173572A
公开(公告)日：1979-11-06
申请号：US937407
申请日：1978-08-28
申请人： Thomas M. Brennan , Daniel P. Brannegan , Paul D. Weeks , Donald E. Kuhla
发明人： Thomas M. Brennan , Daniel P. Brannegan , Paul D. Weeks , Donald E. Kuhla
IPC分类号： C07D309/40 , C07D309/22
CPC分类号： C07D309/40
摘要： Gamma-pyrones are prepared by contacting a 3-halo-furfuryl alcohol or a 3-alkoxy-furfuryl alcohol with one equivalent of a halogen, peracid or peroxide oxidant and then heating until hydrolysis of the formed 4-substituted-dihydropyran intermediate is substantially complete. Maltol (2-methyl-3-hydroxy-4H-pyran-4-one) is prepared by this process from 2(1-hydroxyethyl)-3-alkoxy furans or 2(1-hydroxyethyl)-3-halo-furans. Gamma-pyrones are also prepared by contacting the corresponding 3-substituted-2,5-dialkoxy-furfuryl alcohols with acid until conversion to the gamma-pyrones is substantially complete.
摘要翻译：通过使3-卤代 - 糠醇或3-烷氧基 - 糠醇与一当量的卤素，过酸或过氧化物氧化剂接触，然后加热直到所形成的4-取代二氢吡喃中间体的水解基本上完成。通过该方法由2（1-羟乙基）-3-烷氧基呋喃或2（1-羟基乙基）-3-卤代呋喃制备麦芽酚（2-甲基-3-羟基-4H-吡喃-4-酮）。还可以通过使相应的3-取代-2,5-二烷氧基 - 糠醇与酸接触来制备γ-吡喃糖酮，直到转化成γ-吡喃酮的方法基本上完成。

35. 发明授权

US4132847A 4-Pyrone prostaglandin antagonists 失效
标题翻译： 4-吡喃酮前列腺素拮抗剂
公开(公告)号：US4132847A
公开(公告)日：1979-01-02
申请号：US818043
申请日：1977-07-22
申请人： Donald E. Kuhla , Jacob J. Plattner
发明人： Donald E. Kuhla , Jacob J. Plattner
IPC分类号： A61K31/35 , A61K31/351 , A61P43/00 , C07D309/40 , C07D309/22
CPC分类号： C07D309/40
摘要： Novel 2,3,6-substituted-4-pyrones having activity as prostaglandin antagonists are disclosed, together with intermediates useful for the preparation thereof. Methods of using the compounds of this invention as prostaglandin antagonists are described.
摘要翻译：公开了具有作为前列腺素拮抗剂活性的新型2,3,6-取代-4-吡咯烷酮以及可用于其制备的中间体。描述了将本发明化合物用作前列腺素拮抗剂的方法。

36. 发明授权

US4129567A Quaternary salts as hypoglycemic agents 失效
公开(公告)号：US4129567A
公开(公告)日：1978-12-12
申请号：US822738
申请日：1977-08-08
申请人： Donald E. Kuhla
发明人： Donald E. Kuhla
IPC分类号： C07D213/48 , C07D213/73 , C07D487/00
CPC分类号： C07D213/73 , C07D213/48 , Y10S514/866
摘要： The synthesis of imidazo[1,2-a]pyridinium, imidazo[1,5-a]pyridinium, pyrrolo[1,2-a]pyrazinium, pyrazolo[1,5-a]pyridinium, imidazo[2,1-a]isoquinolinium and imidazo[5,1-a]isoquinolinium quaternary salts and their use as hypoglycemic agents.

37. 发明授权

US4126624A Preparation of gamma-pyrones from 3-substituted furans 失效
标题翻译：从3替代的粉末中制备游离丙烯
公开(公告)号：US4126624A
公开(公告)日：1978-11-21
申请号：US741348
申请日：1976-11-12
申请人： Thomas M. Brennan , Daniel P. Brannegan , Paul D. Weeks , Donald E. Kuhla
发明人： Thomas M. Brennan , Daniel P. Brannegan , Paul D. Weeks , Donald E. Kuhla
IPC分类号： C07D309/32 , C07D309/40 , C07D309/22
CPC分类号： C07D309/40
摘要： Gamma-pyrones are prepared by contacting a 3-halo-furfuryl alcohol or a 3-alkoxy-furfuryl alcohol with one equivalent of a halogen, peracid or peroxide oxidant and then heating until hydrolysis of the formed 4-substituted-dihydropyran intermediate is substantially complete. Maltol (2-methyl-3-hydroxy-4H-pyran-4-one) is prepared by this process from 2(1-hydroxyethyl)-3-alkoxy furans or 2(1-hydroxyethyl)-3-halo-furans. Gamma-pyrones are also prepared by contacting the corresponding 3-substituted-2,5-dialkoxy-furfuryl alcohols with acid until conversion to the gamma-pyrones is substantially complete.

38. 发明授权

US4082717A Preparation of gamma-pyrones 失效
标题翻译：制备GAMMA-PYRONES
公开(公告)号：US4082717A
公开(公告)日：1978-04-04
申请号：US721885
申请日：1976-09-09
申请人： Thomas M. Brennan , Daniel P. Brannegan , Paul D. Weeks , Donald E. Kuhla
发明人： Thomas M. Brennan , Daniel P. Brannegan , Paul D. Weeks , Donald E. Kuhla
IPC分类号： C07D309/32 , C07D309/40 , C11B9/00 , C07D309/22
CPC分类号： C07D309/40 , C07D309/32
摘要： 2-METHYL-3-HYDROXY-4H-pyran-4-one is prepared by contacting 1(2-furyl)-1-ethanol in aqueous solution with two equivalents of a halogen oxidant at room temperature and then heating until the hydrolysis of the formed 4-halo-dihydropyran intermediate is substantially complete. Other valuable related gamma-pyrones are prepared in analogous manner from appropriate alcohols.

39. 发明授权

US3933830A Process for the synthesis of 4-(2-pyridylamido ethyl) piperidines 失效
标题翻译：合成4-（2-吡啶基酰氨基乙基）哌啶的方法
公开(公告)号：US3933830A
公开(公告)日：1976-01-20
申请号：US504826
申请日：1974-09-10
申请人： Wayne E. Barth , Donald E. Kuhla
发明人： Wayne E. Barth , Donald E. Kuhla
IPC分类号： A61K31/445 , C07D213/82 , C07D401/12 , C07D211/02
CPC分类号： C07D213/82 , A61K31/445 , C07D401/12 , Y10S514/866
摘要： Disclosed herein is an improved process for the preparation of known hypoglycemic piperidinesulfamylureas of the structure ##EQU1## wherein R is selected from the group consisting of 3-(2-methoxy)pyridyl, 3-(2-ethoxy)pyridyl and 2-(4-chloro)pyridyl and R' is selected from the group consisting of bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl, bicyclo[2.2.1]hept-2-yl-endo-methyl, 7-oxabicyclo[2.2.1]hept-2-yl-methyl, 1-adamantyl and cycloalkyl having from five to eight carbon atoms.Said process comprises contacting 4-(2-pyridyl-amidoethyl) piperidine of the structure ##EQU2## with substantially one equivalent of sulfamide thereby exclusively sulfonating the piperidine nitrogen atom. Said 4-(2-pyridylamidoethyl)piperidines from the corresponding 4-(2-pyridylamidoethyl) pyridines by selectively activating the more basic nitrogen atom of said pyridine compound either by N-alkylation or by contact with acid and then exclusively reducing the activated pyridine ring with either hydrogen alone or in combination with a metal hydride. Said 4-(2-pyridylamidoethyl)pyridines are produced by contacting 4-(2-aminoethyl)pyridine with a pyridyl acid chloride of the formula R(C=O)Cl. The piperidine sulfonamides produced by the process of the instant invention are converted to the desired hypoglycemic agent by methods well-known to those skilled in the art.The 4-(2-pyridylamidoethyl)pyridines and piperidines of the instant invention are themselves novel compounds useful as intermediates in the synthesis of piperidine sulfamylurea hypoglycemic agents.
摘要翻译：本文公开了一种改进的制备以下结构的已知降血糖哌啶磺酰胺的制备方法：OO PARALLEL PARALLEL R-CNH（CH 2）2 -SO 2 NHC-NHR'，其中R选自3-（2-甲氧基）吡啶基，3 - （2-乙氧基）吡啶基和2-（4-氯）吡啶基，R'选自双环[2.2.1]庚-5-烯-2-基 - 内 - 甲基，双环[2.2。 1]庚-2-基 - 内 - 甲基，7-氧杂双环[2.2.1]庚-2-基 - 甲基，1-金刚烷基和具有5-8个碳原子的环烷基。

40. 发明授权

US4959485A Hexahydrodibenzofuran carboxylic acid derivatives 失效
标题翻译：六氢二苯并呋喃羧酸衍生物
公开(公告)号：US4959485A
公开(公告)日：1990-09-25
申请号：US351625
申请日：1989-05-15
申请人： Raymond D. Youssefyeh , Henry F. Campbell , Donald E. Kuhla
发明人： Raymond D. Youssefyeh , Henry F. Campbell , Donald E. Kuhla
IPC分类号： C07D405/12 , C07D451/14 , C07D453/02 , C07D471/08 , C07D498/08
CPC分类号： C07D405/12 , C07D451/14 , C07D453/02 , C07D471/08
摘要： This invention is directed to certain dibenzofurancarboxamides and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. This invention also describes novel processes necessary for their preparation.
摘要翻译：本发明涉及某些二苯并呋喃甲酰胺及其作为5HT3拮抗剂的用途，其具有独特的CNS，抗呕吐和胃动力学活性，没有任何显着的D2受体结合性质。本发明还描述了其制备所需的新方法。

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