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1.发明授权公开(公告)号：US08022255B2
公开(公告)日：2011-09-20
申请号：US12388779
申请日：2009-02-19
Applicant: Alain Cotte , Matthias Gotta , Lukas Goossen , Felix Rudolphi , Christoph Oppel , Nuria Rodriguez Garrido
Inventor： Alain Cotte , Matthias Gotta , Lukas Goossen , Felix Rudolphi , Christoph Oppel , Nuria Rodriguez Garrido
CPC classification number: C07C45/68 , C07C221/00 , C07C253/30 , C07D213/50 , C07D307/46 , C07D333/22 , C07C49/782 , C07C49/788 , C07C49/76 , C07C49/813 , C07C49/84 , C07C225/22 , C07C255/56
Abstract: A process for preparing ketones of the general formula (III) where R is an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted alkyl radical or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms, and R1 is an optionally substituted carbocyclic aromatic radical having 6 to 24 carbon atoms or an optionally substituted heteroaromatic radical having 5 to 24 carbon atoms, by reacting alpha-oxo carboxylates of the general formula (I) wherein n and m is a number in the range from 1 to 6, M(m+) is a cation, and R has the meaning indicated for formula (III), with aryl bromides of the general formula (II) R1—Br (II) where R1 has the meaning indicated for formula (III), in the presence of two transition metals or compounds thereof as catalyst, is described.
Abstract translation: 一种制备通式（III）的酮的方法，其中R是具有6至24个碳原子的任选取代的碳环芳族基团或任选取代的烷基或任选取代的具有5至24个碳原子的杂芳族基团，R 1是 任选取代的碳原子数为6〜24的碳环芳基或具有5〜24个碳原子的任意取代的杂芳基，通式（I）的α-氧代羧酸盐反应，其中n和m为1〜 6，M（m +）为阳离子，R为式（III）所示的含义，通式（II）的芳基溴R1-Br（Ⅱ）其中R1具有式（Ⅲ）所示的含义， 在两种过渡金属或其化合物作为催化剂的存在下进行了描述。
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2.发明申请Process for Producing Phosphonium Borate Compound, Novel Phosphonium Borate Compound, and Method of Using the Same 有权制备硼酸鏻化合物，新型硼酸鏻化合物的方法及其使用方法公开(公告)号：US20110166389A1
公开(公告)日：2011-07-07
申请号：US12947311
申请日：2010-11-16
Applicant: Shin MASAOKA , Hideyuki IWAZAKI
Inventor： Shin MASAOKA , Hideyuki IWAZAKI
IPC: C07F5/02
CPC classification number: B01J31/32 , B01J31/0268 , B01J31/04 , B01J31/146 , B01J31/2234 , B01J31/24 , B01J31/2404 , B01J31/26 , B01J31/28 , B01J2231/4205 , B01J2231/4283 , B01J2531/72 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2531/828 , B01J2531/84 , C07C1/325 , C07C1/326 , C07C29/32 , C07C41/16 , C07C45/68 , C07C67/343 , C07C209/10 , C07C213/08 , C07C227/08 , C07C253/30 , C07F9/54 , C07C49/782 , C07C49/796 , C07C69/612 , C07C69/618 , C07C211/54 , C07C215/68 , C07C229/44 , C07C255/41 , C07C255/49 , C07C33/483 , C07C33/30 , C07C43/263 , C07C43/275
Abstract: The invention relates to novel phosphonium borate compounds represented by the Formula: (R1)(R2)(R3)PH.BAr4, wherein R1, R2, R3 and Ar4 are as defined herein, and compositions including such phosphonium borate compounds in combination with a transition metal, transition metal salt, transition metal oxide or transition metal complex for use in carbon-carbon bond forming reactions, carbon-nitrogen bond forming reactions and carbon-oxygen bond forming reactions.
Abstract translation: 本发明涉及由式（R1）（R2）（R3）PH.BAr4表示的新的硼酸鏻化合物，其中R1，R2，R3和Ar4如本文所定义，组合物包括这种硼酸鏻化合物与 过渡金属，过渡金属盐，用于碳 - 碳键形成反应的过渡金属氧化物或过渡金属络合物，碳 - 氮键形成反应和碳 - 氧键形成反应。
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3.发明授权Chalcone and its analogs as agents for the inhibition of angiogenesis and related disease states 失效查耳酮及其类似物作为抑制血管生成和相关疾病状态的药剂公开(公告)号：US07872029B2
公开(公告)日：2011-01-18
申请号：US12229340
申请日：2008-08-22
Applicant: J. Phillip Bowen , Thomas Philip Robinson , Tedman Ehlers , David Goldsmith , Jack Arbiser
Inventor： J. Phillip Bowen , Thomas Philip Robinson , Tedman Ehlers , David Goldsmith , Jack Arbiser
IPC: C07D213/02 , A61K31/44
CPC classification number: C07D207/333 , C07C49/217 , C07C49/223 , C07C49/233 , C07C49/235 , C07C49/683 , C07C49/697 , C07C49/782 , C07C49/796 , C07C49/813 , C07C49/84 , C07D213/50 , C07D307/46
Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, including angiogenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.
Abstract translation: 本发明涉及可用作血管发生抑制剂的查耳酮和查耳酮衍生物和类似物。 合成成本低的本发明化合物作为血管生成抑制剂表现出意想不到的良好活性。 本发明还涉及查耳酮及其类似物作为抗肿瘤/抗癌剂并用于治疗血管生成是其中一个因素的一些病症或疾病状态，包括血管生成皮肤疾病如牛皮癣，痤疮，酒渣鼻，疣，湿疹 ，血管瘤，淋巴管生成等等，以及慢性炎性疾病如关节炎。
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4.发明授权Process for producing phosphonium borate compound, novel phosphonium borate compound, and method of using the same 有权硼酸鏻化合物的制造方法，新型硼酸鏻化合物及其使用方法公开(公告)号：US07728176B2
公开(公告)日：2010-06-01
申请号：US10580699
申请日：2004-11-26
Applicant: Shin Masaoka , Hideyuki Iwazaki
Inventor： Shin Masaoka , Hideyuki Iwazaki
IPC: C07F9/02
CPC classification number: B01J31/32 , B01J31/0268 , B01J31/04 , B01J31/146 , B01J31/2234 , B01J31/24 , B01J31/2404 , B01J31/26 , B01J31/28 , B01J2231/4205 , B01J2231/4283 , B01J2531/72 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2531/828 , B01J2531/84 , C07C1/325 , C07C1/326 , C07C29/32 , C07C41/16 , C07C45/68 , C07C67/343 , C07C209/10 , C07C213/08 , C07C227/08 , C07C253/30 , C07F9/54 , C07C49/782 , C07C49/796 , C07C69/612 , C07C69/618 , C07C211/54 , C07C215/68 , C07C229/44 , C07C255/41 , C07C255/49 , C07C33/483 , C07C33/30 , C07C43/263 , C07C43/275
Abstract: The invention relates to a phosphonium borate compound represented by Formula (I) (hereinafter, the compound (I)). The invention has objects of providing (A) a novel process whereby the compound is produced safely on an industrial scale, by simple reaction operations and in a high yield; (B) a novel compound that is easily handled; and (C) novel use as catalyst. Formula (I): (R1)(R2)(R3)PH.BAr4 (I) wherein R1, R2, R3 and Ar are as defined in the specification. The process (A) includes reacting a phosphine with a) HCl or b) H2SO4 to produce a) a hydrochloride or b) a sulfate; and reacting the salt with a tetraarylborate compound. The compound (B) has for example a secondary or tertiary alkyl group as R1 and is easily handled in air without special attention. The use (C) is characterized in that the compound (I) is used instead of an unstable phosphine compound of a transition metal complex catalyst for catalyzing C—C bond, C—N bond and C—O bond forming reactions and the compound produces an effect that is equal to that achieved by the transition metal complex catalyst.
Abstract translation: 本发明涉及由式（I）表示的硼酸鏻化合物（以下称为化合物（I））。 本发明的目的是提供（A）通过简单的反应操作和高产率使化合物在工业规模上安全生产的新方法; （二）易于处理的新型化合物; 和（C）新型用作催化剂。 式（I）：（R1）（R2）（R3）PH.BAr4（I）其中R1，R2，R3和Ar如说明书中所定义。 方法（A）包括使膦与a）HCl或b）H 2 SO 4反应以产生a）盐酸盐或b）硫酸盐; 并使该盐与四芳基硼酸盐化合物反应。 化合物（B）具有例如作为R 1的仲或叔烷基，并且容易在空气中处理而没有特别注意。 使用（C）的特征在于，使用化合物（I）来代替用于催化C-C键，C-N键和C-O键形成反应的过渡金属络合物催化剂的不稳定膦化合物，并且化合物产生 其效果等于过渡金属络合物催化剂所达到的效果。
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5.发明申请Process for producing phosphonium borate compound, novel phosphonium borate compound, and method of using the same 审中-公开硼酸鏻化合物的制造方法，新型硼酸鏻化合物及其使用方法公开(公告)号：US20090305877A1
公开(公告)日：2009-12-10
申请号：US12420300
申请日：2009-04-08
Applicant: Shin Masaoka , Hideyuki Iwazaki
Inventor： Shin Masaoka , Hideyuki Iwazaki
CPC classification number: B01J31/32 , B01J31/0268 , B01J31/04 , B01J31/146 , B01J31/2234 , B01J31/24 , B01J31/2404 , B01J31/26 , B01J31/28 , B01J2231/4205 , B01J2231/4283 , B01J2531/72 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2531/828 , B01J2531/84 , C07C1/325 , C07C1/326 , C07C29/32 , C07C41/16 , C07C45/68 , C07C67/343 , C07C209/10 , C07C213/08 , C07C227/08 , C07C253/30 , C07F9/54 , C07C49/782 , C07C49/796 , C07C69/612 , C07C69/618 , C07C211/54 , C07C215/68 , C07C229/44 , C07C255/41 , C07C255/49 , C07C33/483 , C07C33/30 , C07C43/263 , C07C43/275
Abstract: The invention relates to a phosphonium borate compound represented by Formula (I) (hereinafter, the compound (I)). The invention has objects of providing (A) a novel process whereby the compound is produced safely on an industrial scale, by simple reaction operations and in a high yield; (B) a novel compound that is easily handled; and (C) novel use as catalyst. Formula (I): (R1)(R2)(R3)PH.BAr4 (I) wherein R1, R2, R3 and Ar are as defined in the specification. The process (A) includes reacting a phosphine with a) HCl or b) H2SO4 to produce a) a hydrochloride or b) a sulfate; and reacting the salt with a tetraarylborate compound.The compound (B) has for example a secondary or tertiary alkyl group as R1 and is easily handled in air without special attention.The use (C) is characterized in that the compound (I) is used instead of an unstable phosphine compound of a transition metal complex catalyst for catalyzing C—C bond, C—N bond and C—O bond forming reactions and the compound produces an effect that is equal to that achieved by the transition metal complex catalyst.
Abstract translation: 本发明涉及由式（I）表示的硼酸鏻化合物（以下称为化合物（I））。 本发明的目的是提供（A）通过简单的反应操作和高产率使化合物在工业规模上安全生产的新方法; （二）易于处理的新型化合物; 和（C）新型用作催化剂。 式（I）：（R1）（R2）（R3）PH.BAr4（I）其中R1，R2，R3和Ar如说明书中所定义。 方法（A）包括使膦与a）HCl或b）H 2 SO 4反应以产生a）盐酸盐或b）硫酸盐; 并使该盐与四芳基硼酸盐化合物反应。 化合物（B）具有例如作为R 1的仲或叔烷基，并且容易在空气中处理而没有特别注意。 使用（C）的特征在于，使用化合物（I）代替用于催化CC键，CN键和CO键形成反应的过渡金属络合物催化剂的不稳定膦化合物，并且该化合物产生等于 这通过过渡金属络合物催化剂实现。
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Patent Agency Ranking
6.发明申请公开(公告)号：US20090203652A1
公开(公告)日：2009-08-13
申请号：US12327767
申请日：2008-12-03
Applicant: Marcello ALLEGRETTI , Riccardo Bertini , Cinzia Bizzarri , Maria Candida Cesta , Francesco Colotta
Inventor： Marcello ALLEGRETTI , Riccardo Bertini , Cinzia Bizzarri , Maria Candida Cesta , Francesco Colotta
IPC: A61K31/12 , A61K31/192 , A61K31/662 , A61K31/10 , A61K31/44 , A61P29/00
CPC classification number: C07C69/738 , C07B2200/07 , C07C45/562 , C07C45/673 , C07C45/676 , C07C49/213 , C07C49/215 , C07C49/782 , C07C271/18 , C07C309/65 , C07C311/21 , C07C317/24 , C07D209/46 , C07D213/50 , C07D319/06 , C07F9/4059
Abstract: The compounds of formula (I): where Ar is an aromatic ring and Ra, Rb, are as defined in the description, are useful in therapy as drugs for the treatment of diseases mediated by infiltrations of neutrophils induced by IL-8, such as psoriasis, rheumatoid arthritis, ulcerative cholitis and for the treatment of damages caused by ischemia and reperfusion.
Abstract translation: 式（I）化合物：其中Ar是芳环，Ra，Rb如说明书中所定义，可用于治疗由IL-8诱导的嗜中性粒细胞浸润介导的疾病的药物，例如 牛皮癣，类风湿性关节炎，溃疡性胆囊炎和治疗由缺血和再灌注引起的损伤。
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7.发明申请Iron or Cobalt-Catalyzed Carbon-Carbon Coupling Reaction of Aryls, Alkenes and Alkines With Copper Reagents 审中-公开用铜试剂对芳基，烯烃和炔烃进行铁或钴催化的碳 - 碳偶联反应公开(公告)号：US20080269514A1
公开(公告)日：2008-10-30
申请号：US11576930
申请日：2005-10-11
Applicant: Paul Knochel , Ioannis Sapountzis , Tobias Korn , Wenwei Lin , Christiane Charlotte Kofink
Inventor： Paul Knochel , Ioannis Sapountzis , Tobias Korn , Wenwei Lin , Christiane Charlotte Kofink
CPC classification number: C07C253/30 , C07B37/04 , C07C45/68 , C07C67/343 , C07C303/30 , C07D209/04 , C07D213/50 , C07D213/57 , C07D213/61 , C07D295/192 , C07D317/54 , C07D317/58 , C07D333/22 , C07D333/56 , C07C49/782 , C07C49/784 , C07C49/84 , C07C69/76 , C07C255/56 , C07C255/57 , C07C309/65
Abstract: The present invention relates to a process for the formation of carbon-carbon bonds starting from a copper compound of an aryl, heteroaryl, alkene or alkine and an aryl, heteroaryl, alkene or alkine compound having a suitable leaving group. The copper compounds can be prepared inter alia by means of transmetalliziation from a Grignard or lithium compound. Cross-coupling of these compounds with e.g. a halogen-substituted aryl compound is carried out by means of an iron or cobalt catalyst using suitable solvents and suitable additives.
Abstract translation: 本发明涉及一种从具有合适的离去基团的芳基，杂芳基，烯烃或烯烃的铜化合物和芳基，杂芳基，烯烃或烯化合物开始形成碳 - 碳键的方法。 铜化合物可以特别通过格氏或锂化合物的金属化来制备。 这些化合物与例如四氢呋喃的交联。 卤素取代的芳基化合物通过使用合适的溶剂和合适的添加剂的铁或钴催化剂进行。
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8.发明授权公开(公告)号：US07223879B2
公开(公告)日：2007-05-29
申请号：US10731702
申请日：2003-12-09
Applicant: Stephen L. Buchwald , Xiaohua Huang , Danilo Zim
Inventor： Stephen L. Buchwald , Xiaohua Huang , Danilo Zim
IPC: C07F15/04 , C07F17/02 , C07F9/02 , C07C291/02 , C07C207/02
CPC classification number: C07D213/74 , C07B37/04 , C07C1/26 , C07C17/263 , C07C29/32 , C07C37/11 , C07C41/30 , C07C45/68 , C07C45/71 , C07C67/31 , C07C67/343 , C07C201/12 , C07C209/10 , C07C209/18 , C07C211/59 , C07C213/02 , C07C213/08 , C07C221/00 , C07C225/12 , C07C227/08 , C07C227/18 , C07C231/12 , C07C249/02 , C07C249/16 , C07C251/24 , C07C253/30 , C07C2601/02 , C07C2601/08 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/50 , C07D213/72 , C07D295/023 , C07D295/033 , C07D295/096 , C07D295/112 , C07D295/13 , C07D295/135 , C07D295/155 , C07D307/33 , C07D317/22 , C07D317/26 , C07D317/66 , C07D333/08 , C07D333/66 , C07D401/04 , C07F7/1892 , C07F9/4875 , C07F9/5018 , C07F9/5022 , C07F9/5027 , C07F9/5728 , C07F9/653 , C07F9/6547 , C07F9/65719 , C07F15/0066 , C07C25/18 , C07C49/245 , C07C49/782 , C07C49/67 , C07C49/755 , C07C49/683 , C07C49/213 , C07C49/255 , C07C47/575 , C07C49/84 , C07C49/657 , C07C49/215 , C07C69/92 , C07C69/76 , C07C69/616 , C07C69/612 , C07C211/45 , C07C211/48 , C07C211/52 , C07C211/55 , C07C217/40 , C07C217/84 , C07C217/92 , C07C225/22 , C07C229/36 , C07C229/60 , C07C233/07 , C07C233/43 , C07C235/46 , C07C237/30 , C07C251/86 , C07C255/33 , C07C255/50 , C07C255/54 , C07C255/56 , C07C255/58 , C07C205/04 , C07C205/06 , C07C43/205 , C07C43/225 , C07C39/15 , C07C33/24
Abstract: One aspect of the present invention relates to ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
Abstract translation: 本发明的一个方面涉及过渡金属配体。 本发明的第二方面涉及包含这些配体的催化剂在过渡金属催化的碳 - 杂原子和碳 - 碳键形成反应中的用途。 本发明方法提供了过渡金属催化反应的许多特征的改进，包括合适底物的范围，反应条件和效率。
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公开(公告)号：US07154007B2
公开(公告)日：2006-12-26
申请号：US10491788
申请日：2002-10-10
Applicant: Michihiro Saito , Ernoe Pretsch
Inventor： Michihiro Saito , Ernoe Pretsch
IPC: C07C319/00 , C07C49/00 , C07C231/00 , C07C233/00 , G01N33/566
CPC classification number: C07D333/24 , C07C45/455 , C07C45/46 , C07C45/68 , C07C45/71 , C07C49/80 , C07C49/813 , C07C49/84 , C07C225/22 , C07C323/22 , C07C2601/14 , G01N2458/40 , C07C49/782 , C07C49/784
Abstract: This invention provides: a compound represented by formula (I): R—Y—(—X-Phe-COCH2COCnF2n+1)m (I) wherein R denotes hydrogen, alkyl, phenyl, or a group capable of binding to a protein, peptide, amino acid, nucleic acid, or nucleotide; Y denotes CH2, a carbocyclic ring, or a heterocyclic ring; X denotes O, S, NH, CH2, OCH2, CONH, or NHCO; Phe denotes phenylene; n is an integer between 1 and 5; and m is 1, 2, or 3. This inventions also provides a luminous complex of such compound and a rare earth ion, a labeling reagent comprising such compound or luminous complex, and a process for labeling a protein, peptide, amino acid, nucleic acid, or nucleotide using such labeling reagent.
Abstract translation: 本发明提供：式（I）表示的化合物：<？in-line-formula description =“In-line formula”end =“lead”→RY-（-X-Phe-COCH 2） （I）<？in-line-formula description =“在线公式”结束 =“尾”→其中R表示氢，烷基，苯基或能够结合蛋白质，肽，氨基酸，核酸或核苷酸的基团; Y表示CH 2 2，碳环或杂环; X表示O，S，NH，CH 2，OCH 2，CONH或NHCO; Phe表示亚苯基; n是1和5之间的整数; 本发明还提供了这种化合物和稀土离子的发光配合物，包含这种化合物或发光络合物的标记试剂，以及标记蛋白质，肽，氨基酸，核酸的方法 酸或核苷酸。
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10.发明申请Nucleophilic heterocyclic carbene derivatives of Pd(acac)2 for cross-coupling reactions 有权Pd（acac）2的亲核杂环卡宾衍生物用于交叉偶联反应公开(公告)号：US20060287544A1
公开(公告)日：2006-12-21
申请号：US11441825
申请日：2006-05-26
Applicant: Dino Amoroso , Andrew Bell , Oscar Fernandez , Steven Nolan , Nicolas Marion
Inventor： Dino Amoroso , Andrew Bell , Oscar Fernandez , Steven Nolan , Nicolas Marion
IPC: C07F15/00
CPC classification number: C07B43/04 , C07B37/04 , C07C45/68 , C07D233/10 , C07F15/006 , C07C49/813 , C07C49/782 , C07C49/67 , C07C49/84 , C07C49/657
Abstract: Embodiments in accordance with the present invention provide for a palladium complex characterized by the general formula: where A is a bidentate monoanionic ligand, NHC is a nucleophilic heterocyclic carbene, and Z is an anionic ligand. Such palladium complexes are useful in initiating cross-coupling reactions.
Abstract translation: 根据本发明的实施方案提供了一种钯络合物，其特征在于以下通式：其中A是双齿单阴离子配体，NHC是亲核性杂环卡宾，Z是阴离子配体。 这种钯络合物可用于引发交叉偶联反应。
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