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1. 发明授权

US06320049B1 Alpha 1a adrenergic receptor antagonists 失效
标题翻译： Alpha 1a肾上腺素能受体拮抗剂
公开(公告)号：US06320049B1
公开(公告)日：2001-11-20
申请号：US09563203
申请日：2000-05-02
申请人： Daniel R. Sidler , Robert D. Larsen , Wenjie Li
发明人： Daniel R. Sidler , Robert D. Larsen , Wenjie Li
IPC分类号： C07D23922
CPC分类号： C07D239/22 , C07D401/04 , C07D401/14
摘要： This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.
摘要翻译：本发明涉及可用于治疗良性前列腺增生的α1α肾上腺素能受体拮抗剂，化合物A的结晶药学上可接受的盐。还公开了使用结晶盐的药物组合物，以及制备和使用化合物A的结晶盐和药物组合物的方法。本发明还涉及用于获得可用于合成终产物α1α肾上腺素能受体拮抗剂的对映体纯中间体的方法。最终产品化合物可用于治疗良性前列腺增生和放松下尿路组织。本发明还涉及一种制备其中化合物A为成员的一类二氢嘧啶酮化合物的方法，其中该方法包括使二氢嘧啶酮化合物去质子化，然后将去质子化衍生物与伯胺偶联。

2. 发明授权

US06372911B1 Process for preparing &bgr;-hydroxycarbamates and their conversion to oxazolidinones 失效
标题翻译：制备β-羟基氨基甲酸酯及其转化为恶唑烷酮的方法
公开(公告)号：US06372911B1
公开(公告)日：2002-04-16
申请号：US09482799
申请日：2000-01-13
申请人： Nancy Barta , Robert D. Larsen , Daniel R. Sidler , Steven A. Weissman
发明人： Nancy Barta , Robert D. Larsen , Daniel R. Sidler , Steven A. Weissman
IPC分类号： C07D41312
CPC分类号： C07D413/12 , C07C271/16 , C07D211/18 , C07D263/38
摘要： A process for preparing a &bgr;-hydroxy carbamate product is disclosed. The process comprises reacting an olefin compound containing at least one carbon-carbon double bond with a carbamate in an aqueous solvent and in the presence of a base, an osmium catalyst, a co-oxidant selected from a halohydantoin, a haloisocyanuric acid, and an alkali metal salt of a haloisocyanuric acid, and optionally an asymmetric ligand, to form a reaction mixture containing the &bgr;-hydroxy carbamate product. The process optionally further comprises treating the &bgr;-hydroxy carbamate product with additional base to form an oxazolidinone. The oxazolidinones are useful as chiral auxiliary agents and as intermediates for the formation of pharmaceutically active substances such as alpha 1 a adrenergic receptor antagonists. A process for preparing nitrogen-functionalized derivatives of the oxazolidinones is also disclosed.
摘要翻译：公开了一种制备β-羟基氨基甲酸酯产物的方法。该方法包括使含有至少一个碳 - 碳双键的烯烃化合物与氨基甲酸酯在水溶剂中反应，并在碱，锇催化剂，选自卤代乙内酰脲，卤代异氰脲酸和卤代异氰尿酸的碱金属盐和任选的不对称配体，以形成含有β-羟基氨基甲酸酯产物的反应混合物。该方法任选地还包括用另外的碱处理β-羟基氨基甲酸酯产物以形成恶唑烷酮。恶唑烷酮可用作手性助剂，也可用作形成药物活性物质如α1肾上腺素能受体拮抗剂的中间体。还公开了制备恶唑烷酮的氮官能化衍生物的方法。

3. 发明授权

US06204387B1 Process for making diaryl pyridines useful as COX-2 inhibitors 失效
标题翻译：制备二芳基吡啶的方法可用作COX-2抑制剂
公开(公告)号：US06204387B1
公开(公告)日：2001-03-20
申请号：US09509230
申请日：2000-03-23
申请人： Ian W. Davies , Linda Gerena , Michel Journet , Robert D. Larsen , Philip J. Pye , Kai Rossen
发明人： Ian W. Davies , Linda Gerena , Michel Journet , Robert D. Larsen , Philip J. Pye , Kai Rossen
IPC分类号： C07D21361
CPC分类号： C07D213/50 , C07D213/61
摘要： The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
摘要翻译：本发明包括制备式I化合物可用于治疗环氧合酶-2介导的疾病的方法。

4. 发明授权

US6140515A Process of making 3-aryloxy, 4-aryl furan-2-ones useful as inhibitors of COX-2 失效
标题翻译：制备3-芳氧基，4-芳基呋喃-2-酮可用作COX-2抑制剂的方法
公开(公告)号：US6140515A
公开(公告)日：2000-10-31
申请号：US153403
申请日：1998-09-15
申请人： Cheng Y. Chen , Lushi Tan , Robert D. Larsen
发明人： Cheng Y. Chen , Lushi Tan , Robert D. Larsen
IPC分类号： C07D307/60 , C07D307/12 , C07C315/00 , C07D307/26 , C07D401/12 , C07D405/12
CPC分类号： C07D307/60
摘要： Described is a process of preparing 3-aryl, 4-aryloxy furan-5-ones which are useful as inhibitors of cyclooxygenase-2 (COX-2). Such compounds are useful as anti-inflammatory agents. The process is directed to an asymmetric synthesis which involves: a trisubstituted styrene derivative preparation via Horner-Wadsworth-Emmons reaction and subsequent one pot trifluoromethylation of the allylic alcohol; preparation of the .alpha.-hydroxyl ketone using Sharpless asymmetric dihydroxylation and Swern oxidation; the esterification of the .alpha.-hydroxyl ketone with the phenoxy acetic acid; and the Dieckman condensation of the resulting ester.
摘要翻译：描述了可用作环加氧酶-2（COX-2）抑制剂的3-芳基，4-芳氧基呋喃-5-酮的方法。这些化合物可用作抗炎剂。该方法涉及不对称合成，其包括：通过Horner-Wadsworth-Emmons反应的三取代的苯乙烯衍生物制备和随后的烯丙醇的一锅三氟甲基化; 使用Sharpless不对称二羟基化和Swern氧化制备α-羟基酮; α-羟基酮与苯氧基乙酸的酯化反应; 和所得酯的Dieckman缩合。

5. 发明授权

US5545758A Process for the preparation of diisopinocampheylchloroborane 失效
标题翻译：制备二异蒎烯氯代硼烷的方法
公开(公告)号：US5545758A
公开(公告)日：1996-08-13
申请号：US289077
申请日：1994-08-11
申请人： Anthony O. King , Robert D. Larsen , Thomas R. Verhoeven , Mangzhu Zhao
发明人： Anthony O. King , Robert D. Larsen , Thomas R. Verhoeven , Mangzhu Zhao
IPC分类号： C07B41/02 , C07B41/06 , C07B53/00 , C07D215/14 , C07D215/18 , C07D417/06 , C07D495/04 , C07F5/02
CPC分类号： C07D495/04 , C07D215/14 , C07D215/18 , C07F5/027 , Y02P20/55
摘要： The present invention relates to an improved process for the in situ preparation of diisopinocampheylchloroborane which comprises reacting sodium borohydride and boron trichloride with .alpha.-pinene. The diisopinocampheylchloroborane thus obtained may be used, without isolation, to reduce prochiral ketones to their corresponding alcohols in high optical purity.
摘要翻译：本发明涉及一种二异蒎烷基氯代硼烷的原位制备改进方法，其包括使硼氢化钠和三氯化硼与α-蒎烯反应。这样得到的二蒎烯yl yl chlor chlor ob or or may。。。。。。。，，，。。。。。。。。。。。。。

6. 发明授权

US4111245A Tree delimber 失效
标题翻译： TREE DELIMBER
公开(公告)号：US4111245A
公开(公告)日：1978-09-05
申请号：US754058
申请日：1976-12-23
申请人： Carl M. McCrary , Robert D. Larsen
发明人： Carl M. McCrary , Robert D. Larsen
IPC分类号： A01G23/097 , B27L1/00
CPC分类号： A01G23/097
摘要： An apparatus for delimbing felled trees is described, wherein the trees are pulled individually or, in some cases, in bundles through the delimber. The delimber is provided with a base; a lower impact shear blade which is a notched steel plate supported upon the base, the notch bounding the under half circumference of a tree in the delimber; upper impact shear blades which are a pair of arcuate arms pivoted on the base, designed and arranged such that a tree resting in the notched plate is bound substantially about its upper half circumference by the arcuate arms pivoted into contact with the tree; and an activating plate, pivoted upon the base, interconnected with the arcuate arms such that the weight and force of a tree pulled through the delimber in contact with the notched plate, acts upon the activating plate causing it to pivot thereby pulling the arms into contact with the tree. Additionally, a biasing system is described which maintains the arcuate arms in an open position for receiving a tree to be delimbed, which system causes the arcuate arms to remain pivoted outboard the delimber center line whenever there is no tree acting upon the activating plate.

7. 发明授权

US6040319A Process for synthesizing COX-2 inhibitors 有权
标题翻译：合成COX-2抑制剂的方法
公开(公告)号：US6040319A
公开(公告)日：2000-03-21
申请号：US298127
申请日：1999-04-23
申请人： Edward G. Corley , Ian W. Davies , Robert D. Larsen , Philip J. Pye , Kai Rossen
发明人： Edward G. Corley , Ian W. Davies , Robert D. Larsen , Philip J. Pye , Kai Rossen
IPC分类号： C07D213/34 , A61K31/44 , A61K31/4418 , A61K31/444 , A61P29/00 , A61P31/12 , A61P31/16 , A61P35/00 , A61P35/04 , A61P43/00 , C07C251/12 , C07C251/30 , C07D213/61 , C12N1/00 , A01N43/40 , C07D211/30 , C07D211/72 , C07D211/78 , C07D213/62
CPC分类号： C07D213/61 , C07C251/30
摘要： The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1##
摘要翻译：本发明包括制备式I化合物可用于治疗环氧合酶-2介导的疾病的方法。

8. 发明授权

US5808064A Palladium catalyzed indolization 失效
标题翻译：钯催化吲哚化
公开(公告)号：US5808064A
公开(公告)日：1998-09-15
申请号：US908683
申请日：1997-08-07
申请人： Cheng-Yi Chen , Robert D. Larsen
发明人： Cheng-Yi Chen , Robert D. Larsen
IPC分类号： C07D209/12 , C07D209/14 , C07D521/00 , C07F7/08 , C07D413/12 , C07D209/04
CPC分类号： C07D231/12 , C07D209/12 , C07D209/14 , C07D233/56 , C07D249/08 , C07F7/0818 , C07F7/083 , Y02P20/55
摘要： We have found that 2-unsubstituted indoles of structural formula (IV) can be cost-effectively synthesized in high yield by the palladium-catalyzed coupling/ring closure of a 2-halo or 2-trifluoromethylsulfonyloxy aniline (I) and an acyl silane derivative (II), followed by deprotection of the silyl protecting groups. ##STR1## The process of the present invention is particularly useful to form indoles containing acid-labile substituents such as triazole, acetyl, ketal, cyano, and carbamate, or indoles having a good leaving group in the benzyl position. The advantages of the present process are that it does not require the use of triphenyl phosphine or tetrabutyl ammonium chloride or lithium chloride. When applied to 5-triazolyl substituted indoles, the present process also eliminates the tendency of triazolyl polymerization in the Fischer indole synthesis.
摘要翻译：我们已经发现，2-卤代或2-三氟甲基磺酰氧基苯胺（I）和酰基硅烷衍生物的钯催化偶联/闭环可以以高收率成本有效地合成结构式（Ⅳ）的2-未取代的吲哚（II），然后甲硅烷基保护基的脱保护。本发明的方法特别可用于形成含有酸不稳定取代基的吲哚，例如三唑，乙酰基，缩酮，氰基和氨基甲酸酯，或具有良好离去基团的吲哚苄基位置。本方法的优点是不需要使用三苯基膦或四丁基氯化铵或氯化锂。当应用于5-三唑基取代的吲哚时，本发明方法也消除了在费歇尔吲哚合成中三唑基聚合的倾向。

9. 发明授权

US5567824A Palladium catalyzed ring closure of triazolyltryptamine 失效
标题翻译：钯催化三唑基色胺的闭环
公开(公告)号：US5567824A
公开(公告)日：1996-10-22
申请号：US248288
申请日：1994-05-24
申请人： Cheng Y. Chen , Robert D. Larsen , Thomas R. Verhoeven
发明人： Cheng Y. Chen , Robert D. Larsen , Thomas R. Verhoeven
IPC分类号： C07D403/06 , A61K31/41 , A61K31/415 , A61P9/00 , A61P25/04 , A61P43/00 , C07D521/00 , C07D401/12
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： A new process is described for the synthesis of the triazolyl tryptamine: ##STR1## and related compounds. The process involves a palladium-catalyzed ring closure between a substituted ortho-iodoaniline and a protected 1-alkynol. The process is carded out at high temperature, e.g. 100.degree. C., in a dry inert solvent, e.g., DMF and in the presence of a proton acceptor, e.g., Na.sub.2 CO.sub.3 or a trialkylamine. The triazolyl tryptamine, as well as acid addition salts thereof, is a 5 HT.sub.1 D receptor agonist having anti-migraine properties.
摘要翻译：描述了三唑基色胺的合成的新方法：＆lt; IMAGE＆gt;和相关化合物。该方法涉及取代的邻碘苯胺和被保护的1-炔醇之间的钯催化的闭环。该过程在高温下梳理，例如在干惰性溶剂如DMF中并在质子受体例如Na 2 CO 3或三烷基胺存在下进行。三唑基色胺及其酸加成盐是具有抗偏头痛性质的5 HT1D受体激动剂。

10. 发明授权

US5310928A Process for preparing biphenyltetrazole compounds 失效
标题翻译：联苯四唑化合物的制备方法
公开(公告)号：US5310928A
公开(公告)日：1994-05-10
申请号：US911812
申请日：1992-07-10
申请人： Young S. Lo , Lucius T. Rossano , Robert D. Larsen , Anthony O. King
发明人： Young S. Lo , Lucius T. Rossano , Robert D. Larsen , Anthony O. King
IPC分类号： C07F5/02 , C07F5/05 , C07D257/04 , C07D257/06 , C07D403/06
CPC分类号： C07F5/025 , C07F5/05
摘要： Method for the preparing biphenyltetrazole compounds which are angiotensin II receptor antagonists or which are useful intermediates to prepare angiotensin II receptor antagonists. An illustrative biphenyl tetrazole compound is 2-n-butyl-4-chloro-1-[(2'-(tetrazol-5-yl)-1,1'-biphenyl-4-yl)methyl]-1H-imidazole-5-methanol, potassium salt.
摘要翻译：制备作为血管紧张素II受体拮抗剂的联苯四唑化合物或制备血管紧张素II受体拮抗剂的有用中间体的方法。示例性的联苯四唑化合物是2-正丁基-4-氯-1 - [（2' - （四唑-5-基）-1,1'-联苯-4-基）甲基] -1H-咪唑-5 - 甲醇，钾盐。

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