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21. 发明授权

US5767088A Tachykinin antagonists 失效
标题翻译：速激肽拮抗剂
公开(公告)号：US5767088A
公开(公告)日：1998-06-16
申请号：US697992
申请日：1996-09-04
申请人： David Christopher Horwell , William Howson , Martyn Clive Pritchard , Jennifer Raphy
发明人： David Christopher Horwell , William Howson , Martyn Clive Pritchard , Jennifer Raphy
IPC分类号： A61K38/00 , A61P1/00 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/24 , A61P25/26 , A61P29/00 , C07C271/10 , C07C271/20 , C07C317/28 , C07K5/02 , C07K5/06 , C07K5/065 , C07K7/06 , A61K38/05
CPC分类号： C07K7/06 , C07C271/20 , C07K5/021 , C07K5/06078 , C07K5/06191 , A61K38/00
摘要： The small compounds of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK.sub.3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.
摘要翻译：本发明的小化合物是速激肽拮抗剂。这些化合物是高选择性和功能性的NK3拮抗剂，预期可用于治疗疼痛，抑郁症，焦虑症，恐慌症，精神分裂症，神经痛，成瘾症，炎性疾病，胃肠道疾病，血管疾病和神经病理学障碍。

22. 发明授权

US5728728A Methods of providing neuroprotection 失效
标题翻译：提供神经保护的方法
公开(公告)号：US5728728A
公开(公告)日：1998-03-17
申请号：US632338
申请日：1996-04-10
申请人： Walter E. Kozachuk
发明人： Walter E. Kozachuk
IPC分类号： A61K31/24 , A61K31/00 , A61K31/27 , A61K31/451 , A61K31/4706 , A61K31/498 , A61P25/00 , A61P31/00 , C07C271/10
CPC分类号： A61K31/501 , A61K31/27 , A61K31/451 , A61K31/4706 , A61K31/498 , Y10S514/909
摘要： Novel methods are disclosed for treating acute and chronic neurological disease and attenuating further neuronal cell death in neurological diseases, employing a glycine site antagonist at the NMDA (N-methyl-D-aspartate) complex, e.g., 2-phenyl-1,3-propanediol dicarbamate (felbamate).
摘要翻译：公开了用于治疗急性和慢性神经疾病并减轻神经疾病中进一步的神经元细胞死亡的新方法，在NMDA（N-甲基-D-天冬氨酸）复合物中使用甘氨酸位点拮抗剂，例如2-苯基-1,3- 丙二醇二氨基甲酸酯（纤维素）。

23. 发明授权

US5712418A Synthesis and use of amino acid fluorides as peptide coupling reagents 失效
公开(公告)号：US5712418A
公开(公告)日：1998-01-27
申请号：US284964
申请日：1994-08-02
申请人： Louis A. Carpino , Ayman Ahmed El-Faham
发明人： Louis A. Carpino , Ayman Ahmed El-Faham
IPC分类号： C07C237/22 , C07C255/14 , C07C271/10 , C07C271/34 , C07C275/40 , C07C275/70 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/18 , C07C321/14 , C07C321/20 , C07C323/14 , C07D207/16 , C07D209/20 , C07D233/64 , C07D233/68 , C07D295/215 , C07D317/18 , C07K1/06 , C07K1/08 , C07K1/10 , C07K1/113 , C07D233/02 , C07C257/14 , C07C257/18 , C07D207/02
CPC分类号： C07D295/215 , C07C271/10 , C07C271/34 , C07C275/40 , C07C275/70 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/18 , C07C321/14 , C07C321/20 , C07C323/14 , C07D207/16 , C07D209/20 , C07D233/68 , C07K1/088 , C07K1/10 , C07C2103/18 , Y02P20/55
摘要： The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting group AA is an amino acid residue and X is H or a protecting group useful, and the first amino and peptide have a free amino group and a blocked carboxy end.

24. 发明授权

US5705676A Chromogenic leuco redox-dye-releasing compounds for photothermographic elements 失效
公开(公告)号：US5705676A
公开(公告)日：1998-01-06
申请号：US558525
申请日：1995-11-16
申请人： Raffaella Biavasco , Lori S. Harring , Larry R. Krepski , Daniel E. Mickus , Mark B. Mizen , Sharon M. Simpson , Cristina Soncini , Kim M. Vogel
发明人： Raffaella Biavasco , Lori S. Harring , Larry R. Krepski , Daniel E. Mickus , Mark B. Mizen , Sharon M. Simpson , Cristina Soncini , Kim M. Vogel
IPC分类号： G03C8/40 , C07C275/40 , C07C275/42 , C07C311/46 , G03C1/498 , C07C271/10 , C07C245/08 , C09B62/507
CPC分类号： C07C275/40 , C07C275/42 , C07C311/46 , G03C1/49854 , Y10S430/156
摘要： A photothermographic element comprising a support bearing at least one heat-developable, photosensitive, image-forming photothermographic emulsion layer comprising: (a) a photosensitive silver halide; (b) a non-photosensitive, reducible source of silver; (c) a chromogenic leuco dye reducing agent; and (d) a binder; wherein the chromogenic leuco dye reducing agent is a chromogenic leuco redox-dye-releasing compound of the general formula: ##STR1## wherein: (i) Cp is a coupler group; (ii) N--D is a photographic developer group; and (iii) R.sup.1 is a --C(O)--NH--A--Dye group wherein Dye represents the chromophore of a thermally mobile dye; and A represents a single bond or a divalent linking group of the formula --X--R.sup.5 --L--, wherein R.sup.5 is a divalent hydrocarbon chain containing up to 12 carbon atoms, L is a single bond or a divalent group that binds the chromophore of the thermally mobile dye to R.sup.5, and X represents a single bond or an --SO.sub.2 -- group.

25. 发明授权

US5610183A Phenylglycine derivatives pharmaceutical compositions containing them and their use in therapy 失效
标题翻译：含有它们的苯基甘氨酸衍生物药物组合物及其在治疗中的应用
公开(公告)号：US5610183A
公开(公告)日：1997-03-11
申请号：US167870
申请日：1993-12-17
申请人： Andrew P. Owens , Brian J. Williams
发明人： Andrew P. Owens , Brian J. Williams
IPC分类号： A61K31/165 , A61K31/19 , A61K31/215 , A61K31/275 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/695 , A61K38/00 , A61P3/08 , A61P11/00 , A61P17/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/28 , A61P29/00 , A61P37/00 , A61P37/08 , C07C211/29 , C07C217/48 , C07C217/64 , C07C229/10 , C07C229/14 , C07C229/36 , C07C233/18 , C07C233/22 , C07C233/73 , C07C237/06 , C07C237/08 , C07C237/20 , C07C237/22 , C07C255/13 , C07C255/24 , C07C255/54 , C07C261/04 , C07C271/16 , C07C271/20 , C07C271/22 , C07C271/28 , C07C275/10 , C07C275/24 , C07C275/28 , C07C311/04 , C07C317/18 , C07C323/23 , C07D207/28 , C07D209/04 , C07D233/64 , C07D235/04 , C07D241/08 , C07D257/04 , C07D295/084 , C07D295/185 , C07K5/06 , A61K31/195 , C07C233/00 , C07C255/03 , C07C271/10
CPC分类号： C07D295/185 , C07C211/29 , C07C217/48 , C07C217/64 , C07C229/10 , C07C229/14 , C07C229/36 , C07C233/18 , C07C233/22 , C07C233/73 , C07C237/06 , C07C237/08 , C07C237/20 , C07C255/13 , C07C255/24 , C07C255/54 , C07C271/16 , C07C271/20 , C07C271/22 , C07C275/10 , C07C275/24 , C07C275/28 , C07C311/04 , C07D207/28 , C07D241/08 , C07D295/092 , C07K5/06026 , A61K38/00 , C07C2101/02
摘要： Compounds of Formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein Q is optionally substituted phenyl or naphthyl;X and Y are each H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or X and Y are together .dbd.O;Z is O or S;R.sup.1 is H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl (C.sub.1-4 alkyl), C.sub.2-6 alkenyl, COC.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;R.sup.2 is substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.p optionally substituted by oxo;R.sup.3 is H [or C.sub.1-6 alkyl];R.sup.4 is H, C.sub.1-6 alkyl or phenyl; andR.sup.5 is optionally substituted (CH.sub.2).sub.q phenyl; are tachykinin antagonists useful for treating pain.
摘要翻译： PCT No.PCT / GB92 / 01241 Sec。 371日期：1993年12月17日 102（e）日期1993年12月17日PCT提交1992年7月8日PCT公布。出版物WO93 / 01165 日期1993年1月21日式（I）化合物及其药学上可接受的盐：其中Q是任选取代的苯基或萘基; X和Y各自为H，C 1-6烷基，C 2-6烯基或X和Y一起= O; Z是O或S; R 1是H，任选取代的C 1-6烷基，任选取代的苯基（C 1-4烷基），C 2-6烯基，COC 1-6烷基卤素，CORA，COORa，CONHRa，COC 1-6烷基NR a R b或CONR a C 1-6烷基CONR a R b; R 2是取代的C 1-6烷基，任选取代的苯基（C 1-4烷基），C 2-6烯基，C 1-6烷基卤代，CORA，COORa，CONHRa，COC 1-6烷基NR a R b或CONR a C 1-6烷基CONR a R b; 或R 1和R 2一起形成任选被氧代取代的链（CH 2）p; R3是H [或C1-6烷基]; R4是H，C1-6烷基或苯基; 并且R 5是任选取代的（CH 2）q苯基; 是用于治疗疼痛的速激肽拮抗剂。

26. 发明授权

US5552471A Solid support reagents for the synthesis of 3'-Nitrogen containing polynucleotides 失效
标题翻译：用于合成含3'-氮的多核苷酸的固体支持试剂
公开(公告)号：US5552471A
公开(公告)日：1996-09-03
申请号：US293637
申请日：1994-08-17
申请人： Sam L. Woo , Steven Fung
发明人： Sam L. Woo , Steven Fung
IPC分类号： C12N15/09 , C07C217/20 , C07C271/10 , C07C271/16 , C07C271/66 , C07C317/18 , C07C333/04 , C07H21/00 , C07H21/04 , C03C12/00 , C08L25/06
CPC分类号： C07H21/00 , Y02P20/55
摘要： The compounds are exemplified by the class of sulfoethyl oxygen-substituted carbamates, such compounds being useful as support reagents for automated polynucleotide synthesis of 3'-nitrogen functionalized polynucleotides. The invention includes, in one aspect, a polynucleotide synthesis reagent having the structure: ##STR1## where T is an acid-cleavable hydroxyl protecting group, e.g., 4,4'-dimethoxytritil; Q is a linker connecting the nitrogen and oxygen, e.g., n-hexyl; R.sub.1 is a nitrogen substituent, e.g., hydrogen; R.sub.2 through R.sub.4 are separately hydrogen or lower alkyl; Y is an atom which is electronegative with respect to carbon, e.g., oxygen or sulfur; X.sub.1 is an atom which is electronegative with respect to carbon, e.g., sulfone; Z is a bond or spacer arm, e.g., ethylsuccinate; and W is a derivatized solid synthesis support capable of linking to Z, e.g., an amino-dirivitized controlled pore glass. In a second aspect, the present invention includes a polynucleotide synthesis reagent having the structure: ##STR2## where T, Q, R.sub.1, R.sub.2 -R.sub.3, X.sub.2, Z, and W are as defined above.
摘要翻译：所述化合物的例子是磺乙氧基取代的氨基甲酸酯类，这些化合物可用作3'-氮官能化多核苷酸的自动多核苷酸合成的载体试剂。在一个方面，本发明包括具有以下结构的多核苷酸合成试剂：其中T是酸可裂解的羟基保护基，例如4,4'-二甲氧基苦味; Q是连接氮和氧的接头，例如正己基; R1是氮取代基，例如氢; R2至R4分别为氢或低级烷基; Y是相对于碳例如氧或硫具有电负性的原子; X1是相对于碳电负性的原子，例如砜; Z是键或间隔臂，例如乙基琥珀酸盐; 并且W是能够与Z连接的衍生的固体合成载体，例如氨基 - 二硝基化的受控孔玻璃。在第二方面，本发明包括具有以下结构的多核苷酸合成试剂：其中T，Q，R 1，R 2，R 3，X 2，Z和W如上所定义。

27. 发明授权

US5538986A Tricyclic derivatives, compositions and methods of use 失效
标题翻译：三环衍生物，组合物和使用方法
公开(公告)号：US5538986A
公开(公告)日：1996-07-23
申请号：US162744
申请日：1993-12-06
申请人： Pauline C. Ting , Daniel M. Solomon , Richard J. Friary , Frank J. Villani , John J. Piwinski , Joe F. Lee , Dhiru B. Vashi
发明人： Pauline C. Ting , Daniel M. Solomon , Richard J. Friary , Frank J. Villani , John J. Piwinski , Joe F. Lee , Dhiru B. Vashi
IPC分类号： C07D295/02 , A61K31/125 , A61K31/135 , A61K31/18 , A61K31/195 , A61K31/335 , A61K31/40 , A61K31/4025 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/44 , A61K31/443 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/08 , A61P43/00 , C07C33/38 , C07C45/44 , C07C47/235 , C07C47/453 , C07C69/608 , C07C69/618 , C07C211/26 , C07C211/32 , C07C215/42 , C07C217/52 , C07C229/14 , C07C233/05 , C07C233/18 , C07C233/73 , C07C251/40 , C07C271/10 , C07C271/12 , C07C271/16 , C07C311/03 , C07C311/04 , C07C311/17 , C07D207/16 , C07D209/08 , C07D209/44 , C07D209/48 , C07D213/89 , C07D221/16 , C07D261/02 , C07D295/03 , C07D295/084 , C07D313/12 , C07D405/06 , C07D313/00 , A61K31/35 , A61K31/41 , C07C211/00 , C07C233/00 , A61K31/138
CPC分类号： C07D295/03 , A61K31/00 , A61K31/135 , C07C211/32 , C07C217/52 , C07C229/14 , C07C233/18 , C07C233/73 , C07C251/40 , C07C271/12 , C07C271/16 , C07C311/04 , C07C311/17 , C07D221/16 , C07D295/092 , C07D313/12 , C07C2101/02 , C07C2103/32
摘要： Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.
摘要翻译：公开了式I的化合物：其中：R 3是烷基，烯基，炔基，芳基，烷芳基，芳烷基，环烷基，酰氧基甲基，烷氧基，烷氧基甲基或被环烷基 R4是H，烷基，烯基，烷氧基或-OH。还公开了含有式I化合物，抑制肿瘤坏死因子-α的药物组合物和通过给予式I化合物治疗败血性休克，炎症或过敏性疾病的方法的药物组合物。

28. 发明授权

US5198322A Positively operating radiation-sensitive mixture containing a polyfunctional .alpha.-diazo-.beta.-keto ester and radiation-sensitive recording material containing this mixture 失效
标题翻译：含有多官能（ALPHA）-DIAZO-（BETA）-KETO ESTER和含有该混合物的辐射敏感记录材料的正确操作的辐射敏感性混合物
公开(公告)号：US5198322A
公开(公告)日：1993-03-30
申请号：US466007
申请日：1990-01-12
申请人： Peter Wilharm , Hans-Joachim Merrem , Georg Pawlowski , Ralph Dammel
发明人： Peter Wilharm , Hans-Joachim Merrem , Georg Pawlowski , Ralph Dammel
IPC分类号： G03F7/039 , A61K8/00 , A61Q17/04 , C07C245/18 , C07C271/10 , C07C271/20 , C07C271/24 , C07C275/10 , C07C275/26 , C07C275/32 , C07C275/40 , C07C323/12 , C07D209/48 , C07D251/34 , C07D295/14 , C08F2/50 , C09K3/00 , G03C1/52 , G03F7/004 , G03F7/016 , H01L21/027 , H01L21/30
CPC分类号： C07C245/18 , G03F7/0163 , C07C2101/14
摘要： A positively operating radiation-sensitive mixture comprising a binder which is insoluble in water but soluble or at least swellable in aqueous alkaline solution, and as a photoactive component a polyfunctional .alpha.-diazo-.beta.-keto ester of the general formula I ##STR1## in which R.sup.1 denotes an aliphatic, cycloaliphatic or araliphatic or aromatic radical having 4 to 20 carbon atoms, in which individual CH.sub.2 groups can be replaced by oxygen or sulfur atoms or by ##STR2## or NH groups and/or contain keto groups, X denotes an aliphatic, cycloaliphatic, carbocyclic, heterocyclic or araliphatic radical having 2 to 22 carbon atoms, in which individual CH.sub.2 groups can be replaced by oxygen or sulfur atoms or by the groups --NR.sup.2 --, --C(O)--O--, --C(O)--NR.sup.2 --, --C(O)-- ##STR3## --NR.sup.2 --C(O)--NR.sup.3 --, --O--C(O)--NR.sup.2 --, --C(O)-- ##STR4## or --O--C(O)--O--, or CH groups can be replaced by ##STR5## in which R.sup.2 and R.sup.3 independently of one another represent hydrogen or an aliphatic, carbocyclic or araliphatic radical,m denotes an integer from 2 to 10 andn denotes an integer from 0 to 2, whereinm-n is .gtoreq.2,is described.The radiation-sensitive mixture is particularly suitable for exposure using radiation of wavelength 190 to 300 nm.
摘要翻译：一种正面工作的辐射敏感性混合物，其包含不溶于水但在碱性水溶液中可溶或至少可溶胀的粘合剂，以及作为光活性组分的通式I的多官能α-重氮基β-酮酯（IMAGE）（ I），其中R1表示具有4至20个碳原子的脂族，脂环族或芳脂族或芳族基团，其中各个CH 2基团可以被氧或硫原子替代，或者通过<或>或/或含有酮基， X表示具有2至22个碳原子的脂族，脂环族，碳环，杂环或芳脂族基团，其中各个CH 2基团可被氧或硫原子替代，或由-NR 2 - ， - C（O）-O-， -C（O）-NR 2 - ， - C（O）-NR 2 -C（O）-NR 3 - ， - OC（O）-NR 2 - ， - C（O）（O）-O-或CH基团可以被其中R 2和R 3彼此独立地表示氢或脂族，碳环或芳脂族基团的“IMAGE”代替，m表示 s为2至10的整数，n表示0至2的整数，其中m-n为> / = 2。辐射敏感的混合物特别适用于使用波长为190至300nm的辐射的曝光。

29. 发明授权

US4881945A Fuel compositions containing very long chain alkylphenyl poly(oxyalkylene) aminocarbonates 失效
标题翻译：含有非常长链烷基苯基聚（氧化烯）氨基碳酸酯的燃料组合物
公开(公告)号：US4881945A
公开(公告)日：1989-11-21
申请号：US112901
申请日：1987-10-23
申请人： Thomas F. Buckley, III
发明人： Thomas F. Buckley, III
IPC分类号： C10L1/192 , C07C271/10 , C07C271/20 , C08F20060101 , C08G65/32 , C10L1/18 , C10L1/198 , C10L1/22 , C10L1/234 , C10L1/238 , C10L10/08 , C10M133/56 , C10M145/26 , C10M149/00 , C10N30/04 , C10N40/25 , F02B3/06
CPC分类号： C10L1/238 , F02B3/06
摘要： Disclosed is a fuel composition comprising a hydrocarbon boiling in the gasoline or diesel range and from about 30 to about 5,000 parts per million of a fuel soluble alkylphenyl poly(oxyalkylene) aminocarbamate having at least one basic nitrogen and an average molecular weight of about 800 to 6,000 and wherein the alkyl group contains at least 40 carbon atoms. The instant invention is based on the discovery that use of the unique hydrocarbyl gorup, i.e., an alkylphenyl group wherein the alkyl group contains at least 40 carbon atoms provides for improved lubricating oil compatibility.
摘要翻译：公开了一种燃料组合物，其包含在汽油或柴油范围内沸腾的烃和约30至约5,000ppm的燃料可溶性烷基苯基聚（氧亚烷基）氨基氨基甲酸酯，其具有至少一个碱性氮和平均分子量为约800至 6,000，其中烷基含有至少40个碳原子。本发明基于以下发现：使用独特的烃基gorup，即其中烷基含有至少40个碳原子的烷基苯基提供改善的润滑油相容性。

30. 发明授权

US4788329A Preparation of cyclohexyl mono- and diurethanes and isocyanates derived therefrom by addition of methylcarbamate to limonene, process and compositions 失效
标题翻译：通过向柠檬烯中加入甲基氨基甲酸酯，方法和组合物制备环己基单和二氨基甲酸酯和衍生自其的异氰酸酯
公开(公告)号：US4788329A
公开(公告)日：1988-11-29
申请号：US926068
申请日：1986-11-03
申请人： Laurence J. Nummy
发明人： Laurence J. Nummy
IPC分类号： C07C271/10 , B01J31/10 , B01J31/14 , B01J31/20 , C07B61/00 , C07C67/00 , C07C239/00 , C07C241/00 , C07C263/04 , C07C265/10 , C07C265/14 , C07C269/00 , C07C271/06 , C07C271/24 , C08G18/72 , C07C119/045
CPC分类号： C07C265/10 , C07C265/00 , C08G18/728
摘要： A process is disclosed whereby mono- and diurethane cyclohexyl derivatives are obtained corresponding to the Lewis acid-catalyzed addition reaction of dipentene and methyl carbamate at a temperature of from about 40.degree. to about 150.degree.C. The mono- and diurethane cyclohexyl derivatives are pyrolytically converted to other corresponding mono- and diisocyanate cyclohexyl derivatives. Novel vinyl unsaturated monoisocyanate cyclohexyl derivatives useful as reactants for polyfunctional compounds to produce cured compositions are disclosed.
摘要翻译：公开了一种方法，其中相应于二烯和甲基氨基甲酸酯的路易斯酸催化的加成反应在约40至约150℃的温度下获得单 - 和二 - 氨基甲酸酯环己基衍生物。单 - 和二 - 氨基甲酸酯环己基衍生物是热解的转化为其它相应的单和二异氰酸酯环己基衍生物。公开了可用作多官能化合物反应物的新型乙烯基不饱和单异氰酸酯环己基衍生物，用于生产固化组合物。

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