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51. 发明申请

WO00023187A1 HYDROFORMYLATION PROCESS USING CHLOROPHOSPHITE-METAL CATALYST SYSTEM 审中-公开
标题翻译：使用氯代磷酸盐金属催化剂体系的氢化方法
公开(公告)号：WO00023187A1
公开(公告)日：2000-04-27
申请号：PCT/US1999/024412
申请日：1999-10-15
IPC分类号： B01J31/22 , B01J31/18 , C07B61/00 , C07C45/50 , C07C47/02 , C07C47/12 , C07F9/146 , C07F9/6574 , C07F15/00 , C07F13/00
CPC分类号： C07F15/008 , B01J31/185 , B01J2231/321 , B01J2531/822 , C07C45/50 , C07C47/02
摘要： Disclosed are catalyst systems comprising one or more transition metals selected from the Group VIII metals and rhenium and one or more chlorophosphite compounds having general Formula (I), wherein R and R are aromatic hydrocarbyl radicals. Also disclosed are catalyst solutions comprising one or more the above chlorophosphite compounds, rhodium and a hydroformylation solvent, and hydroformylation processes wherein olefins are contacted with carbon monoxide, hydrogen and the catalyst solution to produce aldehydes.
摘要翻译：公开了包含一种或多种选自VIII族金属和铼的过渡金属和一种或多种具有通式（I）的氯代亚磷酸酯化合物的催化剂体系，其中R 1和R 2是芳族烃基。还公开了包含一种或多种上述氯代亚磷酸酯化合物，铑和加氢甲酰化溶剂的催化剂溶液，以及其中烯烃与一氧化碳，氢气和催化剂溶液接触以产生醛的加氢甲酰化方法。

52. 发明申请

WO9945016A9 NOVEL PRODRUGS FOR PHOSPHORUS-CONTAINING COMPOUNDS 审中-公开
标题翻译：含磷化合物的新产品
公开(公告)号：WO9945016A9
公开(公告)日：2000-03-02
申请号：PCT/US9904908
申请日：1999-03-05
申请人： METABASIS THERAPEUTICS INC
发明人： ERION MARK D , REDDY K RAJA , ROBINSON EDWARD D
IPC分类号： C07H19/213 , A61K31/665 , A61K31/675 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K49/00 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P31/12 , A61P33/00 , A61P35/00 , A61P43/00 , C07F9/6571 , C07F9/6574 , C07H19/10 , C07H19/11 , C07H19/20 , C07H19/207 , C07H19/00
CPC分类号： C07H19/10 , C07F9/657154 , C07F9/657181 , C07F9/65742 , C07F9/65744 , C07H19/20 , C07H19/207
摘要： Prodrugs of formula (I), their uses, their intermediates, and their method of manufacture are described, wherein V is selected from the group consisting of -H, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, 1-alkynyl, and -R ; or together V and Z are connected via 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, substituted with hydroxy, acyloxy, alkoxycarbonyloxy, or aryloxycarbonyloxy attached to a carbon atom that is three atoms from an oxygen attached to the phosphorus; or together V and Z are connected via 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, that is fused to an aryl group at the beta and gamma position to the oxygen attached to the phosphorus; or together V and W are connected via 3 carbon atoms to form an optionally substituted cyclic group containing 6 carbon atoms and substituted with one substituent selected from the group consisting of hydroxy, acyloxy, alkoxycarbonyloxy, alkylthiocarbonyloxy, and aryloxycarbonyloxy, attached to a carbon atom that is three atoms from an oxygen attached to the phosphorus; W and W' are independently selected from the group consisting of -H, alkyl, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, 1-alkynyl, and -R ; Z is selected from the group consisting of -CHR OH, -CHR OC(O)R , -CHR OC(S)R , -CHR OC(S)OR , -CHR OC(O)SR , -CHR OCO2R , -OR , -SR , -CHR N3, -CH2aryl, -CH(aryl)OH, -CH(CH=CR 2)OH, -CH(CCR )OH, -R , -NR 2, -OCOR , -OCO2R , -SCOR , -SCO2R , -NHCOR , -NHCO2R , -CH2NHaryl, -(CH2)p-OR , and -(CH2)p-SR ; R is an R or -H; R is selected from the group consisting of alkyl, aryl, aralkyl, and alicyclic; and R is selected from the group consisting of alkyl, aralkyl, and alicyclic; p is an integer from 2 to 3; with the provisos that a) V, Z, W, and W' are not all -H; and b) when z is -R , then at least one of V and W is not -H, or -R ; and M is selected from the group that attached to PO3 , P2O6 , or P3O9 is biologically active in vivo, and that is attached to the phosphorus in formula (I) via a carbon, oxygen, or nitrogen atom; and pharmaceutically acceptable prodrugs and salts thereof.
摘要翻译：描述了式（I）的前药，其用途，其中间体及其制备方法，其中V选自-H，芳烷基，脂环族，芳基，取代的芳基，杂芳基，取代的杂芳基，1-烯基，1-炔基和-R 9; 或一起V和Z通过3-5个原子连接形成环状基团，任选地含有1个被连接到磷上的氧原子连接到三个原子上的羟基，酰氧基，烷氧基羰基氧基或芳氧基羰基氧基的杂原子; 或一起V和Z通过3-5个原子连接以形成任选地含有1个杂原子的环状基团，其在β和γ位置处的芳基与连接到磷的氧融合; 或者一起V和W通过3个碳原子连接形成任选取代的含有6个碳原子的环状基团，并被一个选自羟基，酰氧基，烷氧基羰基氧基，烷硫基羰基氧基和芳氧基羰基氧基的一个取代基取代，是从附着于磷的氧的三个原子; W和W'独立地选自-H，烷基，芳烷基，脂环族，芳基，取代的芳基，杂芳基，取代的杂芳基，1-烯基，1-炔基和-R 9。 Z选自-CHR 2 OH，-CHR 2 OC（O）R 3，-CHR 2 OC（S）R 3，-CHR 2 OC（ S）OR 3，-CHR 2 OC（O）SR 3，-CHR 2 OCO 2 R 3，-OR 2，-SR 2，-CHR 2 N 3， -CH 2芳基，-CH（芳基）OH，-CH（CH = CR 2）OH，-CH（CCR 2）OH，-R 2，-NR 2，-OCOR 3 ，-OCO 2 R 3，-SCOR 3，-SCO 2 R 3，-NHCOR 2，-NHCO 2 R 3，-CH 2 NH芳基， - （CH 2）p -OR 2和 - （CH 2 ）对 - SR <2>; R 2是R 3或-H; R 3选自烷基，芳基，芳烷基和脂环族; 并且R 9选自烷基，芳烷基和脂环族; p是2至3的整数; 条件是a）V，Z，W和W'不全为-H; 和b）当z是-R 2时，V和W中的至少一个不是-H或-R 9; 并且M选自附着于PO 3 2-，P 2 O 6 3-或P3O 9 4-的基团在体内具有生物活性，并且通过碳与式（I）中的磷连接，氧或氮原子; 及其药学上可接受的前药及其盐。

53. 发明申请

WO9948897B1 SYNTHESIS OF COMPOUNDS AND LIBRARIES OF COMPOUNDS 审中-公开
标题翻译：化合物和化合物的合成
公开(公告)号：WO9948897B1
公开(公告)日：2000-01-20
申请号：PCT/US9906233
申请日：1999-03-22
申请人： HARVARD COLLEGE
发明人： VERDINE GREGORY L , CHYTIL MILAN , DIDIUK MARY T , MALINKY TIFFANY
IPC分类号： C12N15/09 , C07B61/00 , C07C271/16 , C07C327/22 , C07D207/16 , C07D223/10 , C07D263/22 , C07F7/18 , C07F9/6574 , C07K1/00 , C07K1/04 , C40B40/02 , C40B40/04 , C40B40/16 , C40B50/00 , C40B50/06
CPC分类号： C07K1/047 , C07B2200/11 , C07C271/16 , C07D207/16 , C07D223/10 , C07D263/22 , C07F9/65742 , C40B40/00
摘要： The present invention provides a system for the production of chemical compounds and libraries of compounds that are complex, stereochemically and regioselectively pure, and may mimic the structural or functional properties of a peptide. The invention provides methods for producing collections of peptidomimetic compounds which, in one preferred embodiment, comprises (1) providing two diversifiable monomers containing terminal reactive moieties; (2) reacting the monomers under conditions that allow for the control of stereochemistry as well as chemoselectivity; and (3) generating diversifiable isolable compounds or libraries of compounds. In another preferred embodiment, a collection of peptidomimetic compounds is provided by (1) providing at least one diversifiable monomer containing terminal reactive moieties; (2) reacting the monomer with a reagent under conditions that allow for the control of stereochemistry as well as chemoselectivity; and (3) generating diversifiable isolable compounds or libraries of compounds. In another broader aspect, the present invention provides for the synthesis of a collection of compounds comprising peptidomimetics and non-peptidomimetics alike having stereodiversity. This method involves the steps of (1) selecting desired synthetic precursors having a predefined stereochemical relationship; (2) reacting the synthetic precursors so that a compound having a specific stereochemistry is obtained; and (3) repeating these steps of selecting and reacting until a desired library of compounds having stereochemical diversity is obtained. In certain preferred embodiments, a library of compounds having only diversity of stererochemistry is provided. In certain other preferred embodiments, a library of compounds having structural diversity and stereochemical diversity is provided. The present invention also provides various chemical compounds useful in the inventive methods for production of complex peptidomimetic libraries. The peptidomimetic and stereodiverse compounds of the inventive method are useful for interactions with receptors in cells and may emulate the structure and functionality of peptides.
摘要翻译：本发明提供了一种用于制备复合物，立体化学和区域选择性纯化合物的化合物和文库的系统，并且可以模拟肽的结构或功能性质。本发明提供了生产肽模拟化合物的方法，在一个优选的实施方案中，其包含（1）提供含有末端反应性部分的两种可分散的单体; （2）在允许控制立体化学和化学选择性的条件下使单体反应; 和（3）产生可分离的可分离化合物或化合物文库。在另一个优选的实施方案中，肽模拟化合物的集合通过以下方式提供：（1）提供至少一种含有末端反应性部分的可分散单体; （2）在允许控制立体化学和化学选择性的条件下使单体与试剂反应; 和（3）产生可分离的可分离化合物或化合物文库。在另一个更广泛的方面，本发明提供了合成包含拟肽的化合物和非肽模拟物的集合，其具有立体异构。该方法包括以下步骤：（1）选择具有预定立体化学关系的所需合成前体; （2）使合成前体反应，得到具有特定立体化学的化合物; 和（3）重复这些选择和反应的步骤，直到获得具有立体化学多样性的所需化合物文库。在某些优选实施方案中，提供了仅具有立体化学多样性的化合物文库。在某些其它优选实施方案中，提供了具有结构多样性和立体化学多样性的化合物文库。本发明还提供了用于生产复合肽模拟文库的本发明方法中的各种化合物。本发明方法的拟肽和立体异构化合物可用于与细胞中的受体的相互作用，并且可以模拟肽的结构和功能。

54. 发明申请

WO99052916A1 PREPARATION OF SPIRO BIS-PHOSPHITES USING FINELY GROUND PENTAERYTHRITOL 审中-公开
标题翻译：使用精细地面香料制备螺旋双磷酸盐
公开(公告)号：WO99052916A1
公开(公告)日：1999-10-21
申请号：PCT/US1999/007054
申请日：1999-03-30
IPC分类号： C07F9/6574
CPC分类号： C07F9/65746
摘要： A process for producing organo-phosphites of formula (I), wherein R and R are each 2,4-di-tert-butyl and R is hydrogen is provided. The process involves heating a reaction mixture containing pentaerythritol wherein the pentaerythritol has an average particle size of about 250 microns or less, preferably the pentaerythritol has an average particle size of about 150 microns or less, phosphorous trihalide, a phenolic compound of formula (II), wherein each R and R is t-butyl and R is hydrogen, a solvent selected from the group consisting of heptane, hexane, octane, xylene, toluene, and mixtures of the solvents containing at least one of the aforementioned and a catalyst. The process utilizing the aforementioned pentaerythritol particle size has the unexpected advantages of short reaction times as compared to the same process using a larger pentaerythritol particle size.
摘要翻译：提供式（I）的有机亚磷酸酯的方法，其中R 1和R 2各自为2,4-二叔丁基，R 3为氢。该方法包括加热含有季戊四醇的反应混合物，其中季戊四醇的平均粒度为约250微米或更小，优选季戊四醇的平均粒度为约150微米或更小，三卤化磷，式（II）的酚类化合物，，其中每个R 1和R 2是叔丁基，R 3是氢，选自庚烷，己烷，辛烷，二甲苯，甲苯的溶剂和至少含有的溶剂的混合物上述之一和催化剂。与使用较大的季戊四醇颗粒尺寸的相同方法相比，利用上述季戊四醇颗粒尺寸的方法具有短的反应时间的意想不到的优点。

55. 发明申请

WO99048900A1 PROCESS FOR THE PREPARATION OF SPIRO BISPHOSPHITES 审中-公开
标题翻译：制备SPIRO双相磷灰石的方法
公开(公告)号：WO99048900A1
公开(公告)日：1999-09-30
申请号：PCT/US1999/005206
申请日：1999-03-10
IPC分类号： C07F9/6574
CPC分类号： C07F9/65746
摘要： A process for producing organo-phosphites of formula (I) wherein R and R are each 2,4-di-tert-butyl and R is hydrogen is provided. The process involves heating a mixture of a pentaerythritol bis-phosphorohalidite and a phenolic compound and applying a vacuum of at least about 10 inches of mercury wherein the temperature of the reaction mixture is maintained between about 30 DEG C and about 140 DEG C. Conversions to the organic spiro bisphosphite is at least twice that of the same process without a vacuum.
摘要翻译：提供式（I）的有机亚磷酸酯的方法，其中R 1和R 2各自为2,4-二叔丁基，R 3为氢。该方法包括加热季戊四醇双 - 卤代磷酸酯和酚类化合物的混合物并施加至少约10英寸汞柱的真空，其中反应混合物的温度保持在约30℃至约140℃之间。转化为有机螺二磷酸亚铁是没有真空的相同工艺的有机螺旋二亚磷酸酯的至少两倍。

56. 发明申请

WO9933850A8 NOVEL beta -LACTAMASE AND DD-PEPTIDASE INHIBITORS 审中-公开
标题翻译：新型β-LACTAMASE和DD-肽酶抑制剂
公开(公告)号：WO9933850A8
公开(公告)日：1999-09-10
申请号：PCT/US9827518
申请日：1998-12-23
申请人： METHYLGENE INC , WESLEYAN UNIVERSITY , BESTERMAN JEFFREY M , RAHIL JUBRAIL , PRATT REX
发明人： BESTERMAN JEFFREY M , RAHIL JUBRAIL , PRATT REX
IPC分类号： A61K31/662 , A61P31/04 , A61P43/00 , C07F9/09 , C07F9/40 , C07F9/6571 , C07F9/6574 , A61K31/66
CPC分类号： C07F9/4093 , C07F9/096 , C07F9/098 , C07F9/657181 , C07F9/65742 , C07F9/65744
摘要： The invention provides novel beta -lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic beta -lactamase inhibitors presently available, and which do not possess beta -lactam pharmacophore. These new inhibitors are fully synthetic, allowing ready access to a wide variety of structurally related analogs. Certain embodiments of these new inhibitors also bind bacterial DD-peptidases, thus potentially acting both as beta -lactamase inhibitors and as antibiotics.
摘要翻译：本发明提供新颖的β-内酰胺酶抑制剂，其在结构上与目前可获得的天然产物和半合成β-内酰胺酶抑制剂无关，并且不具有β-内酰胺药效团。这些新的抑制剂是完全合成的，可以方便地访问各种结构相关的类似物。这些新抑制剂的某些实施方案也结合细菌DD-肽酶，因此潜在地作为β-内酰胺酶抑制剂和作为抗生素。

57. 发明申请

WO99038832A1 IMPROVED SEPARATION PROCESSES 审中-公开
标题翻译：改进的分离方法
公开(公告)号：WO99038832A1
公开(公告)日：1999-08-05
申请号：PCT/US1999/002090
申请日：1999-02-01
IPC分类号： B01J31/18 , B01J31/40 , C07B63/00 , C07C45/50 , C07C45/80 , C07C47/02 , C07C51/373 , C07C51/48 , C07C59/147 , C07F9/02 , C07F9/144 , C07F9/145 , C07F9/50 , C07F9/6574
CPC分类号： B01J31/0259 , B01J31/0267 , B01J31/1845 , B01J31/185 , B01J31/24 , B01J31/2404 , B01J31/4015 , B01J31/4046 , B01J31/4053 , B01J2231/32 , B01J2231/321 , B01J2231/52 , B01J2231/641 , B01J2531/822 , B01J2531/90 , C07C45/50 , Y02P20/582 , Y02P20/584 , C07C47/02
摘要： This invention relates to a process for separating one or more products from a reaction product fluid comprising a metal-organophosphorus ligand complex catalyst, optionally free organophosphorus ligand, a nonpolar solvent and said one or more products, wherein said process comprises (1) mixing said reaction product fluid with a polar solvent to obtain by phase separation a nonpolar phase comprising said metal-organophosphorus ligand complex catalyst, optionally free organophosphorus ligand and said nonpolar solvent and a polar phase comprising said one or more products and polar solvent, and (2) recovering said polar phase from said nonpolar phase; wherein said organophosphorus ligand has a partition coefficient between the nonpolar solvent and the polar solvent of greater than about 5, and said one or more products have a partition coefficient between the polar solvent and the nonpolar solvent of greater than about 0.5.
摘要翻译：本发明涉及从反应产物流体中分离一种或多种产物的方法，该反应产物流体包括金属 - 有机磷配体配合物催化剂，任选的游离有机磷配体，非极性溶剂和所述一种或多种产物，其中所述方法包括（1）将反应产物流体与极性溶剂通过相分离获得包含所述金属 - 有机磷配体配合物催化剂，任选的游离有机磷配体和所述非极性溶剂的非极性相和包含所述一种或多种产物和极性溶剂的极性相，和（2）从所述非极性相中回收所述极性相; 其中所述有机磷配体在非极性溶剂和极性溶剂之间的分配系数大于约5，并且所述一种或多种产物在极性溶剂和非极性溶剂之间具有大于约0.5的分配系数。

58. 发明申请

WO99006418A1 SELECTIVE SYNTHESIS OF ORGANODIPHOSPHITE COMPOUNDS 审中-公开
标题翻译：选择性合成有机磷化合物
公开(公告)号：WO99006418A1
公开(公告)日：1999-02-11
申请号：PCT/US1998/015429
申请日：1998-07-24
IPC分类号： C07F9/145 , C07F9/6574
CPC分类号： C07F9/65746 , C07F9/145
摘要： A process for the preparation of organodiphosphites of the formula (ORO)P(OZO)P(ORO) wherein R and Z are different substituted or unsubstituted aryl groups.
摘要翻译：制备式（ORO）P（OZO）P（ORO）的有机亚磷酸酯的方法，其中R和Z是不同的取代或未取代的芳基。

59. 发明申请

WO99006358A1 HYDROCYANATION PROCESSES AND MULTIDENTATE PHOSPHITE LIGAND AND NICKEL CATALYST COMPOSITIONS THEREFOR 审中-公开
标题翻译：氢化方法和多种磷酸盐配体和镍催化剂组合物
公开(公告)号：WO99006358A1
公开(公告)日：1999-02-11
申请号：PCT/US1998/015305
申请日：1998-07-23
IPC分类号： B01J31/18 , B01J31/28 , C07C253/10 , C07C255/04 , C07F9/145 , C07F9/6574 , C07C255/03
CPC分类号： C07F9/65746 , B01J31/185 , B01J31/28 , B01J2231/323 , B01J2531/0266 , B01J2531/847 , C07C253/10 , C07F9/145 , C07C255/04
摘要： A process for hydrocyanation of an aliphatic monoethylenically unsaturated compound, in which the ethylenic double bond is not conjugated to any other unsaturated group in the molecule, or a monoethylenically unsaturated compound in which the ethylenic double bond is conjugated to an ester group, which process uses a catalyst composition comprising a zero-valent nickel and a multidentate phosphite ligand in the presence of a Lewis acid promoter.
摘要翻译：其中乙烯性双键不与分子中的任何其它不饱和基团共轭的脂肪族单烯键式不饱和化合物的氢化，或其中烯键式双键与酯基结合的单烯属不饱和化合物，该方法使用在路易斯酸启动子存在下，包含零价镍和多齿亚磷酸酯配体的催化剂组合物。

60. 发明申请

WO9210504A3 PHOSPHONIC ACID DERIVATIVES USEFUL AS ANTIINFLAMMATORY AGENTS 审中-公开
标题翻译：用作抗炎药物的磷酸衍生物
公开(公告)号：WO9210504A3
公开(公告)日：1992-09-17
申请号：PCT/US9108817
申请日：1991-12-03
申请人： UPJOHN CO
发明人： JOHNSON ROY ALLEN , SMITH HERMAN WALDEN
IPC分类号： A61K31/66 , A61K31/665 , A61K31/675 , A61P29/00 , A61P43/00 , C07F9/38 , C07F9/40 , C07F9/6509 , C07F9/6561 , C07F9/6571 , C07F9/6574
CPC分类号： C07F9/650994 , C07F9/3839 , C07F9/4025 , C07F9/657181
摘要： Novel acids, esters, and salts of phenyl, naphtyl, quinoxalinyl, and biphenyl bisphosphonic acids and 1,2-oxaphosphepins are described. These compounds are useful as antiinflammatory and anti-arthritic agents. Also described are known compounds of the phenyl, naphthyl, quinoxalinyl, and biphenyl bisphosphonate classes which are also useful as antiinflammatory and anti-arthritic agents. Representative compounds include [1,2-phenyldiyl]-bis(methylene)bisphosphonic acid tetramethyl ester, [2,3-quinoxalindiyl]bis(methylene)bisphosphonic acid tetramethyl ester, [[3-(propyl)-4-(methoxy)-1,8-naphthalenediyl]bis-(methylene)]bisphosphonic acid tetramethyl ester, [2,6-naphthalenediylbis(methylene)bisphosphonic acid tetraethyl ester, and [2,2'-biphenylenebis(methyl)]bisphosphonic acid tetramethyl ester. Representative oxaphosphepins include the preferred 3,4-dihydro-3-methoxy-7-(phenylmethoxy)-1H-naphth[1,8de][1,2]oxaphosphepin-3-oxide.

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