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41. 发明申请

US20130109718A1 1-CYCLOALKYL- OR 1-HETEROCYCLYL-HYDROXYIMINO-3-PHENYL-PROPANES 审中-公开
公开(公告)号：US20130109718A1
公开(公告)日：2013-05-02
申请号：US13658878
申请日：2012-10-24
申请人： Hoffmann-La Roche Inc.
发明人： Henrietta Dehmlow , Rainer E. Martin , Patrizio Mattei , Ulrike Obst Sander , Hans Richter
IPC分类号： C07C251/42 , C07D211/28 , C07D309/04 , C07D335/02 , C07C317/32 , A61K31/45 , A61K31/4545 , A61K31/445 , A61K31/351 , A61K31/382 , A61K31/15 , A61P3/00 , A61P29/00 , A61P3/10 , C07D211/76
CPC分类号： C07D401/10 , C07C251/42 , C07C317/32 , C07C2601/04 , C07C2601/14 , C07D211/28 , C07D211/76 , C07D309/04 , C07D335/02
摘要： This invention relates to novel 1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.

42. 发明授权

US07148380B2 Bio-energy muscle relaxants 失效
公开(公告)号：US07148380B2
公开(公告)日：2006-12-12
申请号：US09764417
申请日：2001-01-19
申请人： Chong Gang Wang , Yisheng Zhang , Pei Wang
发明人： Chong Gang Wang , Yisheng Zhang , Pei Wang
IPC分类号： C07C251/38 , C07C251/42 , A61K31/15
CPC分类号： A61K31/15
摘要： Human muscle tissues involve striated and smooth muscles. Each muscle tissue possesses its own special function. Differences of physiology functions among the muscle tissues are mainly determined by their various initiation and signal transmission systems, defined as the pre-muscle molecular motor mechanism, or initiating and regulating mechanism. The current medications, drugs, and therapies for diseases and symptoms related abnormal increased muscle tone or excessive muscle contraction are aimed just at the pre-muscle molecular motor mechanisms, whereas without directly intending to effect on the muscle molecular motor mechanism i.e. the contractile apparatus mechanism at all, which, however, is in common for all kinds of muscle tissues. The muscle molecular motor mechanism mainly involves recycling of actin-myosin filament cross-bridge formation and sliding movement. In the process, bio-energy provided by ATP hydrolysis is necessarily required. Therefore, abnormal increased muscle tone or excessive contraction of muscle tissues under diseased conditions may be modified by inhibition of the muscle molecular motor with the actin-myosin ATPase inhibitor, which blocks hydrolysis of ATP, then reduces release of bio-energy for the muscle contraction.Our studies in vitro and in vivo have demonstrated that BDM, an ATPase inhibitor, thereby, its analogues, derivatives, and other chemicals possessing similar effect on ATPase may be used as bio-energy muscle relaxants (general muscle relaxants).

43. 发明申请

US20060229471A1 Oxidation catalyst 审中-公开
标题翻译：氧化催化剂
公开(公告)号：US20060229471A1
公开(公告)日：2006-10-12
申请号：US10565886
申请日：2004-07-22
申请人： Ken Suzuki
发明人： Ken Suzuki
IPC分类号： B01J31/00 , C07C251/42
CPC分类号： B01J31/0237 , B01J31/006 , B01J2231/70 , B01J2231/72 , B01J2231/763 , C07C249/04 , Y02P20/582 , C07C251/44
摘要： An oxidation catalyst for use in the oxidation of a substrate with a molecular oxygen, comprising at least one member selected from the group consisting of a specific hydrazyl radical (such as 2,2-diphenyl-1-picrylhydrazyl) and a specific hydrazine compound (such as 2,2-diphenyl-1-picrylhydrazine). A method for producing a chemical compound, comprising contacting a substrate with a molecular oxygen in the presence of the above-mentioned oxidation catalyst.
摘要翻译：一种氧化催化剂，用于氧化分子氧的底物，其包含选自特定的肼基（例如2,2-二苯基-1-苦基肼基）和特定的肼化合物中的至少一种如2,2-二苯基-1-辛基肼）。一种化合物的制造方法，其特征在于，在上述氧化催化剂的存在下，使基材与分子氧接触。

44. 发明申请

US20040073064A1 Process for producing 2-halogenocycloalkanone oxime 失效
标题翻译： 2-卤代环烷酮肟的制备方法
公开(公告)号：US20040073064A1
公开(公告)日：2004-04-15
申请号：US10468880
申请日：2003-08-20
申请人： Ube Industries,Ltd.
发明人： Katzumasa Harada , Yasuhisa Fukuda , Yoshinori Yamanaka
IPC分类号： C07C251/42
CPC分类号： C07C249/12 , C07C2601/20 , C07C251/44
摘要： The present invention relates to a process for preparing 2-halogenocycloalkanone oxime which comprises subjecting a 2-halogenocycloalkenone oxime compound to reduction with hydrogen in the presence of a platinum-carried catalyst.
摘要翻译：本发明涉及一种2-卤代环烷酮肟的制备方法，该方法包括在铂载体催化剂存在下，用氢气还原2-卤代环烯酮肟化合物。

45. 发明授权

US6147260A Preparation of 5-(3-butyryl-2,4,6-trimethyl)-2-(1-(ethoxyimino)propyl)-3-hydroxycyclohe x-2-en-1-one 失效
标题翻译：制备5-（3-丁酰基-2,4,6-三甲基）-2-（1-（乙氧基亚氨基）丙基）-3-羟基环己-2-烯-1-酮
公开(公告)号：US6147260A
公开(公告)日：2000-11-14
申请号：US230678
申请日：1999-06-21
申请人： Graham John Bird , Keith Geoffrey Watson
发明人： Graham John Bird , Keith Geoffrey Watson
IPC分类号： C07B61/00 , C07C45/46 , C07C49/83 , C07C49/835 , C07C249/04 , C07C249/08 , C07C251/42
CPC分类号： C07C249/08 , C07C45/46 , C07C49/83 , C07C49/835 , C07C2101/16
摘要： A process of preparing the compound of formula (I) which comprises: (a) reacting butyryl chloride with the compound of formula (IV) in the presence of a Friedel-Crafts catalyst in an inert diluent to produce a compound of formula (II) and (b) reacting the compound of formula (II) with ethoxyamine. Compound (II) is also claimed.
摘要翻译： PCT No.PCT / AU97 / 00471 Sec。 371 1999年6月21日第 102（e）1999年6月21日PCT PCT 1997年7月25日PCT公布。第WO98 / 04510号公报日本公开日1998年2月5日制备式（I）化合物的方法，其包括：（a）在Friedel-Crafts催化剂存在下，在惰性稀释剂中使丁酰氯与式（Ⅳ）化合物反应，生成化合物式（II）和（b）使式（II）化合物与乙氧基胺反应。化合物（II）也被要求保护。

46. 发明授权

US6002014A Oxazole derivatives and use thereof 失效
标题翻译：恶唑衍生物及其用途
公开(公告)号：US6002014A
公开(公告)日：1999-12-14
申请号：US302498
申请日：1999-04-30
申请人： Junichi Haruta , Hiromasa Hashimoto , Mutsuyoshi Matsushita
发明人： Junichi Haruta , Hiromasa Hashimoto , Mutsuyoshi Matsushita
IPC分类号： C12N9/99 , A61K31/42 , A61K31/421 , A61K31/422 , A61P25/04 , A61P29/00 , A61P43/00 , C07C45/00 , C07C49/567 , C07C49/813 , C07C69/007 , C07C233/31 , C07C233/47 , C07C251/42 , C07C311/16 , C07C311/29 , C07C311/32 , C07C311/37 , C07C317/24 , C07C317/32 , C07D263/32 , C07D413/04
CPC分类号： C07D413/04 , C07C233/31 , C07C233/47 , C07C251/42 , C07C311/16 , C07C311/29 , C07C311/32 , C07C311/37 , C07C317/24 , C07C317/32 , C07C45/004 , C07C49/567 , C07C49/813 , C07C69/007 , C07D263/32 , C07C2101/14
摘要： Oxazole derivatives of the formula (I) ##STR1## wherein one of R and R.sub.1 is a methylsulfonylphenyl, an aminosulfonylphenyl or an alkylaminosulfonylphenyl, and the other is a cycloalkyl having 5 to 7 carbon atoms which is optionally substituted by lower alkyl, a thienyl optionally substituted by lower alkyl or halogen atom or a furanyl optionally substituted by lower alkyl or halogen atom, and R.sub.2 is a lower alkyl, and pharmaceutically acceptable salts thereof. The oxazole derivatives and pharmaceutically acceptable salts thereof have superior antipyretic action, analgesic action, anti-inflammatory action, and particularly, selective inhibitory action on cyclooxygenase-2 (COX-2), and are expected to be useful as an antipyretic agent, an analgesic agent and an anti-inflammatory agent with less side-effects such as disorders in the digestive tract.
摘要翻译：式（I）的恶唑衍生物，其中R和R 1中的一个是甲基磺酰基苯基，氨基磺酰基苯基或烷基氨基磺酰基苯基，另一个是任选被低级烷基取代的碳原子数5〜7的环烷基，烷基或卤素原子或任选被低级烷基或卤原子取代的呋喃基，R2是低级烷基，及其药学上可接受的盐。恶唑衍生物及其药学上可接受的盐具有优异的解热作用，止痛作用，抗炎作用，特别是对环氧合酶-2（COX-2）的选择性抑制作用，并且预期可用作解热剂，止痛剂药剂和消炎剂等副作用减轻的消炎剂。

47. 发明授权

US5770622A Method of preserving materials using 4-methylene-2-amino-cyclopentane-1-carboxylic acids 失效
标题翻译：使用4-亚甲基-2-氨基 - 环戊烷-1-羧酸保存材料的方法
公开(公告)号：US5770622A
公开(公告)日：1998-06-23
申请号：US709073
申请日：1996-09-06
申请人： Joachim Mittendorf , Franz Kunisch , Michael Matzke , Hans-Christian Militzer , Rainer Endermann , Karl Georg Metzger , Klaus-Dieter Bremm , Manfred Plempel
发明人： Joachim Mittendorf , Franz Kunisch , Michael Matzke , Hans-Christian Militzer , Rainer Endermann , Karl Georg Metzger , Klaus-Dieter Bremm , Manfred Plempel
IPC分类号： C07C61/15 , C07C61/20 , C07C61/35 , C07C61/39 , C07C61/40 , C07C69/74 , C07C69/753 , C07C69/757 , C07C229/48 , C07C237/04 , C07C251/42 , C07C271/22 , C07C271/24 , C07C271/34 , C07C271/36 , C07D265/12 , C07D307/93 , A01N37/00
CPC分类号： C07C251/42 , C07C229/48 , C07C237/04 , C07C271/22 , C07C271/24 , C07C271/34 , C07C271/36 , C07C61/15 , C07C61/20 , C07C61/35 , C07C61/39 , C07C61/40 , C07C69/74 , C07C69/753 , C07C69/757 , C07D265/12 , C07D307/93 , C07C2101/08 , C07C2101/10 , C07C2103/18
摘要： The invention relates to cyclopentane- and -pentene-.beta.-amino acids, processes for their preparation and their use as medicaments, and to prevent contamination of materials such as wood and leather.
摘要翻译：本发明涉及环戊烷和戊烯-β-氨基酸，其制备方法及其作为药物的用途，并且防止木材和皮革等材料的污染。

48. 发明授权

US5631286A Compounds useful for treating allergic or inflammatory diseases 失效
标题翻译：可用于治疗过敏性或炎性疾病的化合物
公开(公告)号：US5631286A
公开(公告)日：1997-05-20
申请号：US449633
申请日：1995-05-24
申请人： Siegfried B. Christensen, IV , Paul E. Bender , Cornelia J. Forster
发明人： Siegfried B. Christensen, IV , Paul E. Bender , Cornelia J. Forster
IPC分类号： C07D295/00 , A61K31/12 , A61K31/24 , A61K31/275 , A61K31/33 , A61P11/06 , A61P29/00 , A61P37/08 , C07C45/44 , C07C45/51 , C07C45/71 , C07C47/47 , C07C47/575 , C07C49/603 , C07C49/613 , C07C49/753 , C07C49/757 , C07C233/56 , C07C235/82 , C07C251/42 , C07C255/46 , C07C255/54 , C07C255/64 , C07D213/00 , C07D215/00 , C07D233/00 , C07D239/00 , C07D257/00 , C07D261/00 , C07D263/00 , C07D277/00 , C07D307/00 , C07D309/00 , C07F7/08
CPC分类号： C07C255/46 , C07C233/56 , C07C235/82 , C07C45/44 , C07C45/515 , C07C45/71 , C07C47/47 , C07C47/575 , C07C49/753 , C07C49/757 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要： Novel cyclohexanes of formulas (I) and (II) are described herein. They inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production: these compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV. ##STR1##
摘要翻译：本文描述了式（I）和（II）的新型环己烷。它们抑制肿瘤坏死因子的产生，可用于治疗由TNF产生介导或加重的疾病状态：这些化合物也可用于调节或抑制磷酸二酯酶IV的酶促或催化活性。（一）

49. 发明授权

US5554582A Cyclohexenone compounds, their preparation and their use for controlling undesirable plant growth 失效
标题翻译：环己烯酮化合物，它们的制备及其用于控制不期望的植物生长的用途
公开(公告)号：US5554582A
公开(公告)日：1996-09-10
申请号：US983604
申请日：1992-11-30
申请人： Michael Keil , Ulrich Schirmer , Dieter Kolassa , Juergen Kast , Bruno Wuerzer , Norbert Meyer
发明人： Michael Keil , Ulrich Schirmer , Dieter Kolassa , Juergen Kast , Bruno Wuerzer , Norbert Meyer
IPC分类号： A01N35/10 , A01N43/28 , A01N43/32 , C07C251/06 , C07C251/42 , C07C251/52 , C07C323/46 , C07C323/47 , C07C323/52 , C07D317/26 , C07D319/06 , C07D327/02 , C07D333/28 , C07D339/06 , C07D339/08 , A01N33/24 , A01N43/18 , C07C251/44
CPC分类号： C07C251/52 , A01N35/10 , A01N43/28 , A01N43/32 , C07C251/06 , C07C323/46 , C07C323/47 , C07C323/52 , C07D317/26 , C07D319/06 , C07D327/02 , C07D339/06 , C07D339/08 , C07C2101/16
摘要： Cyclohexenone compounds of the formula ##STR1## where R.sup.1 is alkyl of 1 to 4 carbon atoms, alkenyl or alkynyl of 3 or 4 carbon atoms, haloalkenyl of 3 or 4 carbon atoms and 1 to 3 halogen substituents, or is thenyl which is unsubstituted or substituted by halo and/or alkyl, R.sup.2 is alkyl of 1 to 4 carbon atoms, and R.sup.3 is formyl, a radical of the general formula R.sup.4 XCHXR.sup.5, where X is oxygen or sulfur, and R.sup.4 and R.sup.5 are identical or different alkyl, or together denote alkylene of 1 to 4 carbon atoms and which is unsubstituted or substituted by alkyl, alkoxy, alkylthio, hydroxy, halogen, cyano or N,N-dialkylamino, have a good herbicidal action preferably on species from the grass family.
摘要翻译：其中R 1为1至4个碳原子的烷基，3或4个碳原子的链烯基或炔基，3或4个碳原子的卤代烯基和1至3个卤素取代基，或其中R 1为未被取代或被卤素和/或烷基取代，R 2是1至4个碳原子的烷基，R 3是甲酰基，通式为R 4 XCHXR 5的基团，其中X是氧或硫，R 4和R 5是相同或不同的烷基或一起表示1至4个碳原子的亚烷基，其未被取代或被烷基，烷氧基，烷硫基，羟基，卤素，氰基或N，N-二烷基氨基取代，优选地对来自草类的物种具有良好的除草作用。

50. 发明授权

US5411936A Cyclohexenone oxime ethers, and their use as herbicides 失效
标题翻译：环己烯酮肟醚及其作为除草剂的用途
公开(公告)号：US5411936A
公开(公告)日：1995-05-02
申请号：US5428
申请日：1993-01-19
申请人： Juergen Kast , Dieter Kolassa , Norbert Meyer , Ulrich Schirmer , Albrecht Harreus , Jochen Wild , Karl-Otto Westphalen , Bruno Wuerzer
发明人： Juergen Kast , Dieter Kolassa , Norbert Meyer , Ulrich Schirmer , Albrecht Harreus , Jochen Wild , Karl-Otto Westphalen , Bruno Wuerzer
IPC分类号： C07D317/26 , A01N35/06 , A01N35/10 , A01N37/22 , A01N43/14 , A01N43/16 , A01N43/18 , A01N43/40 , A01N43/80 , A01P13/00 , C07C251/42 , C07C251/50 , C07C251/52 , C07C255/62 , C07C323/19 , C07C323/47 , C07D213/53 , C07D261/08 , C07D307/16 , C07D309/06 , C07D309/08 , C07D333/22 , C07D335/02 , C07D339/06 , C07C255/34 , C07C251/38 , C07D213/84
CPC分类号： C07D213/53 , A01N35/10 , A01N37/22 , A01N43/14 , A01N43/40 , A01N43/80 , C07C251/42 , C07C251/52 , C07C323/47 , C07D261/08 , C07D309/06 , C07D309/08 , C07D335/02 , C07C2101/16
摘要： Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, A is substituted or unsubstituted C.sub.4 -alkylene or C.sub.4 -alkenylene,x is nitro, cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and/or phenyl,n is from 0 to 3 or from 1 to 5 when X is halogen,R.sup.2 is C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.7 -cycloalkenyl,a substituted or unsubstituted 5-membered saturated heterocyclic radical which contains one or two oxygen and/or sulfur atoms as heteroatoms,a substituted or unsubstituted 6- or 7-membered heterocyclic radical which contains one or two oxygen and/or sulfur atoms and one or two double bonds,a substituted or unsubstituted 5-membered heteroaromatic radical containing one or two nitrogen atoms and an oxygen or a sulfur atom,substituted or unsubstituted phenyl or pyridyl,and their agriculturally useful salts and esters of C.sub.1 -C.sub.10 -carboxylic acids and inorganic acids, methods of manufacturing them, and their use as herbicides.
摘要翻译：其中R1是C1-C6-烷基，A是取代或未取代的C4-亚烷基或C4-亚烯基，x是硝基，氰基，卤素，C1-C4-烷基， C 1 -C 4 - 烷氧基，C 1 -C 4 - 烷硫基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，羧基，C 1 -C 4烷氧基羰基，取代或未取代的苄氧基羰基和/或苯基，n为0至3或1 当X是卤素时，R 2是C 1 -C 6烷氧基-C 1 -C 6烷基或C 1 -C 4烷硫基-C 1 -C 6烷基，取代或未取代的C 3 -C 7 - 环烷基或C 5 -C 7 - 环烯基，取代或含有一个或两个氧原子和/或硫原子作为杂原子的未取代的5元饱和杂环基，取代或未取代的含有一个或两个氧和/或硫原子的六元或七元杂环基和一个或两个双键，取代或未取代的含有一个或两个氮原子和氧或硫原子的5元杂芳族基团，取代或未取代的苯基或吡啶基，以及它们在农业上可用的C1-C10-羧酸和无机酸的盐和酯，它们的制备方法及其作为除草剂的用途。

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