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序号	专利名	申请号	申请日	公开（公告）号	公开（公告）日	发明人
161	Alkylolamides of iodizable amino acids and immune test reagents containing them	US782868	1977-03-30	US4202873A	1980-05-13	Hans-Georg Batz; Klaus Stellner; Hans-Ralf Linke; Gunter Weimann
Novel alkylolamides of iodizable amino acids of the formula ##STR1## wherein, R.sup.1 is hydroxybenzyl, dihydroxybenzyl or imidazol-4-yl-methyl andR.sup.2 is monohydroxy-alkyl of 1 or 2 carbon atoms or dihydroxy-alkyl of up to 4 carbon atoms,and the water-soluble salts thereof are provided; these materials are useful as components of radioiodizable immune test reagents.
162	2,3-Disubstituted-1-indanones	US139281	1971-04-30	US3992450A	1976-11-16	John Fred Neumer
Compounds of the general formula: ##SPC1##Wherein m = 0 or 1;Ar is an arylene or lower alkyl substituted arylene radical;R.sub.1 and R.sub.2, which may be the same or different, are lower alkyl or hydroxyalkyl groups, or ##EQU1## R.sub.3 is H, lower alkyl, benzyl, R.sub.4, or ##EQU2## R.sub.4 is ##SPC2##Alkyl group, an aryl group, ##EQU3## wherein n=2-6; and R.sub.6 is a lower alkyl group or an aryl group. Where m = 1, the formula represents a colorless leuco compound; where m = 0, the formula represents the yellow dye derivative of the leuco. These compounds are particularly useful in photosensitive compositions.
163	1-Carboxyalkyl derivatives of imidazoles	US483826	1974-06-27	US3952005A	1976-04-20	Dan Jorgensen
Imidazole derivatives substituted in the 1-position by a carboxyalkyl group or an ester of a such and the acid addition salts thereof, and where possible the alkali metal and alkaline earth metal salts thereof possess good antiphlogistic and analgesic activities. Such compounds are prepared, for example, by introducing the carboxyalkyl group or an ester of a such into the 1-position of a corresponding imidazole derivative unsubstituted in the 1-position. Alternatively such compounds are prepared by reacting an appropriate keto-oxime with an appropriate amino compound and an appropriate aldehyde or acetal and optionally reducing the imidazole derivative thus obtained.
164	Herbicidal aliphatic oxaalkyl-2,4,5-trihalogeno-imidazoles	US13144871	1971-04-05	US3813235A	1974-05-28	RUTZ H; GUBLER K
2,4,5,-TRIHALOGENO-IMIDAZOLES SUBSTITUTED IN 1-POSITION AT THE INIDAZOL NUCLEUS BY A GROUP OF THE FORMULA R-O-A WHEREIN R REPRESENTS AN OPTIONALLY SUBSTITUTED ALIPHATIC HYDROCATBON RADICAL AND A REPRESENTS AN ALKYLENE GROUP ARE DESCRIBED, WHICH IMIDAZOLES ARE HERBICADIALLY ACTIVE AND USEFUL IN THE CONTROL OF WEEDS AND THE LIKE UNDESIRABLE PLANT GROWTH; HERICIDAL COMPOSITIONS CONTAINING SUCH INIDAZOLES AS ACTIVE INGREDIENTS AND METHOD OF CONTROLLING UNDESIRABLE PLANT GROWTH WITH THE AID OF SUCH COMPOUDS AE ALSO DISCLOSED.
165	Imidazole synthesis	US3715365D	1971-02-08	US3715365A	1973-02-06	SCHULZE H
An improved process for preparing imidazoles by contacting glyoxal or methyl substituted derivatives thereof, formaldehyde, and an ammonium salt of an acid having an ionization constant greater than 1 X 10 3.
166	Preparation of substituted imidazoles	US16142761	1961-12-22	US3177223A	1965-04-06	ERNER WILLIAM E

167	아미도-치환된 시클로헥산 유도체	KR20177034653	2016-05-02	KR20180002748A	2018-01-08
본발명은화학식 (I)의아미도-치환된시클로헥산화합물, 상기화합물의제조방법, 상기화합물의제조에유용한중간체화합물, 및상기화합물을포함하는제약조성물및 조합물, 및단독작용제로서의또는다른활성성분과조합된, 질환, 특히신생물의치료또는예방을위한제약조성물을제조하기위한상기화합물의용도에관한것이다.여기서 A, R, R, R, R, R, R및 R은본원에정의된바와같다.
168	Illudin analogs useful as antitumor agents	US241172	1999-02-01	US6069283A	2000-05-30	Trevor C. McMorris; Michael J. Kelner
The present invention provides illudin analogs of the general formula (I): ##STR1## where R.sub.1 is (CH.sub.2).sub.n --X--Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C.sub.1 -C.sub.8)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.6 -C.sub.10)aryl(C.sub.1 -C.sub.4)alkyl or cyclo(C.sub.3 -C.sub.6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4;R.sub.2 is absent; or R.sub.1 and R.sub.2 together comprise a 5-7 membered cyclic ring;R.sub.3 is (C.sub.1 -C.sub.4)alkyl or H; R.sub.4 is H, SCH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl, O--(C.sub.5 -C.sub.12)aryl or --S--(C.sub.5 -C.sub.12)aryl; R.sub.5 is H, OH or absent; R.sub.6 is (C.sub.1 -C.sub.4)alkyl or absent; R.sub.7 is OH or OSi((C.sub.1 -C.sub.4)alkyl).sub.3 ; orR.sub.6 and R.sub.7 together are ethylenedioxy;R.sub.8 is optionally substituted (C.sub.1 -C.sub.4)alkyl; andthe bonds represented by ----- are individually present or absent. The invention further provides dimers comprising analogs of formula (I).
169	Inhibitors of farnesyl-protein transferase	US117260	1998-07-27	US6066738A	2000-05-23	Christopher J. Dinsmore; George D. Hartman
The present invention is directed to compounds which inhibit farnesyl -protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
170	Processes for producing 1-substituted-2-cyanoimidazole compounds	US962648	1997-11-03	US5869683A	1999-02-09	Hisayoshi Jonishi; Tokiya Kimura; Fumio Kanamori; Shigehisa Kanbayashi; Tooru Wakabayashi; Fumihiro Fukui; Akimasa Takenaka; Noriyuki Horiuchi
A process for producing 1-substituted-2-cyanoimidazole compounds is described, which comprises (1) undergoing a reaction of a compound represented by formula (IV), hydroxylamine or a mineral acid salt thereof, and glyoxal or glyoxime to produce a compound represented by formula (III), (2) undergoing a reaction of the compound represented by formula (III) with thionyl chloride or thionyl bromide in the presence of N,N-dialkylamide to produce a reaction mixture, and then reacting the produced reaction mixture with sulfur chloride to produce a 2-cyanoimidazole compound represented by formula (II), and (3) undergoing a sulfamoylation reaction and an isomerization reaction of the 2-cyanoimidazole compound represented by formula (II) and a compound represented by formula (V) in the presence of at least one base selected from carbonates of alkali metals and bicarbonates of alkali metals and a polar solvent to produce a 1-substituted-2-cyanoimidazole compound represented by formula (I-b). The formulae and substituents formulae are specifically defined in the specification. ##STR1##
171	N-protected/N-substituted-beta-amino hydroxy sulfonates	US747825	1996-11-13	US5847201A	1998-12-08	Joseph J. Wieczorek
N-protected/N-substituted alpha-amino aldehydes, which are useful as pharmaceuticals and pharmaceutical intermediates, can be stored and shipped in a more stable form as N-protected/N-substituted-beta-amino hydroxy sulfonates which can be readily converted back into the aldehyde under mild conditions. The present invention relates to N-protected/N-substituted-beta-amino hydroxy sulfonates and their preparation and use.
172	Modulators of proteins with phosphotryrosine recognition units	US766114	1996-12-16	US5753687A	1998-05-19	Adnan Mjalli; Sepehr Sarshar; Xiaodong Cao; Farid Bakir
Y--X--C(R').dbd.C(R")COOR'" (A1) The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryoic cells, whole animals and human beings. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.
173	Process for carrying out gas/liquid reactions under avoidance of a continuous gas phase	US620940	1996-03-22	US5726321A	1998-03-10	Klaus Bittins; Marc Heider; Martin Schmidt-Radde; Jochen Kellenbenz; Kurt Josef Wagner; Peter Zehner; Stefan Berg
Process for carrying out gas/liquid reactions at from (-50.degree.) to 300.degree. C. and from 0.1 to 100 bar by carrying out the reaction in the absence of a continuous gas phase, and, as a special case, a process for the batchwise reaction of acetylene in the liquid phase at from 0.degree. to 300.degree. C. and from 2 to 30 bar, in which acetylene is introduced a) in the absence of a continuous gas phase and b) under isobaric conditions to a degree of saturation of from 5 to 100%.
174	Intermediate for synthesis and production of amino acid derivative	US360683	1995-01-03	US5523410A	1996-06-04	Kooji Kagara; Nobutaka Kawai; Koji Machiya; Tetsuo Furutera; Takashi Nakamura; Hiroki Omori
The present invention relates to synthetic intermediates useful for preparing amino acid derivatives possessing renin-inhibitory activity, and to processes for preparing the amino acid derivatives using the synthetic intermediates.
175	Process for the preparation of imidazoles useful in angiotensin II antagonism	US869971	1992-04-16	US5294722A	1994-03-15	Kyoung S. Kim
Imidazoles of the formula ##STR1## are prepared by treating a ketone ##STR2## with a nitrogenic acid, nitrite or nitrate in the presence of an acid to form a hydroxynitrile ##STR3## which is treated with R.sup.2 --CHO and an ammonium to form an N-hydroxyimidazole ##STR4## which is reduced in the presence of a buffer. In these compounds, R.sup.1 is hydrogen, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl;R.sup.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, or --(CH.sub.2).sub.m Z(CH.sub.2).sub.n R.sup.3, each of which is optionally substituted with F or --CO.sub.2 R.sup.1 ; or aryl or aralkyl, each of which is optionally substituted with 1 or 2 groups selected from halogen, lower alkoxy, lower alkyl, or nitro;R.sup.3 is hydrogen, alkyl, cycloalkyl, lower alkenyl, or lower alkynyl;and the remaining symbols are as defined in the specification.
176	Light-sensitive quinone diazide compound containing an alkylimidazole group and method of forming a photoresist using said compound	US443409	1989-11-30	US5099007A	1992-03-24	Masayuki Iwasaki
A light-sensitive compound is described, containing a quinonediazido group and an alkylimidazole group in the same molecule and which is solubilizable in an aqueous alkali solution upon irradiation with light, and a method of forming a photoresist using the light-sensitive compound. The compound is useful, for example, in production of print substrates and in chemical milling.
177	Aromatic derivatives and their use as antimicrobial agents	US469166	1990-01-24	US5089251A	1992-02-18	Madeleine Mosse; Vincenzo Proietto
The present invention relates to aromatic derivatives of the formula: ##STR1## in which: n represents an integer between 2 and 10;R.sub.1 and R.sub.2 are identical or different and represent a cycloalkyl containing 3 to 6 carbon atoms or an alkyl containing from 1 to 6 carbon atoms which is unsubstituted or substituted by a phenyl or benzyl group; orR.sub.1 and R.sub.2, together with the nitrogen atom to which they are bonded, form a heterocycle selected from pyrrolidin-1-yl, piperidino, azepin-1-yl, hexamethyleneimino, 4-methylpiperidino, 4-benzylpiperidino, 4-phenylpiperidino, 1,2,3,4-tetrahydroisoquinol-2-yl, morpholino and imidazol-1-yl groups;R.sub.3 represents a hydrogen, a halogen, a methyl or a phenyl;R.sub.4 represents a hydrogen, a halogen or a methyl; or R.sub.3 and R.sub.4, taken together with the benzene ring to which they are bonded, form a naphth-1-yl or naphth-2-yl group;Y represents a direct bond, a methyleneoxy group, a methylenethio group or a vinylene group; andR.sub.5 represents an alkyl containing from 5 to 18 carbon atoms, a cycloalkyl containing from 3 to 8 carbon atoms, an adamantyl, naphth-1-yl or naphth-2-yl group, an unsubstituted phenyl group or a phenyl group substituted by one or 2 substituents selected from halogen atoms, the trifluoromethyl group, the nitro group and the phenyl group;and to their salts with mineral or organic acids.Application: antimicrobial agents.
178	Aryl derivatives	US24031	1987-03-10	US5036157A	1991-07-30	Geoffrey Kneen; William P. Jackson; Peter J. Islip; Peter J. Wates
Novel compounds of formula (I)Ar--(L--Ar').sub.q --(X).sub.k --(Y).sub.p --Q (I)wherein:k, p and q are independently 0 or 1;Ar represents either:(i) naphthyl, tetrahydronaphthyl, pyridyl or(ii) phenyl, optionally substituted,L is selected from --(CH.sub.2).sub.r -- (where r is 1-4), --O--, --CH.sub.2 O--, --CH.sub.2 S--, --OCH.sub.2 --, --CONH--, --NHCO--, --CO-- and --CH.sub.2 NH--, and,Ar' represents phenylene, thienylene or pyridylene optionally substituted,X represents oxygen, sulphur or carbonyl,Y is C.sub.1-10 alkylene or C.sub.1-10 alkenylene;Q represents a non-cyclic moiety selected from groups of formula ##STR1## in which one of m and n is 0 and the other is 1, R.sup.1 and R.sup.2 is selected from hydrogen, C.sub.1-4 alkyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.5-7 cycloalkylamino, C.sub.5-7 cycloalkyl (C.sub.1-4 alkyl) amino, anilino, N-C.sub.1-4 alkylanilinoor Q represents a cyclic moiety selected from 1-hydroxy-1,3-dihydroimidazol-2-one and groups of formula ##STR2## in which Z represents a C.sub.2-5 alkylene chain in which one of the carbon atoms may be replaced by a hetero atom; and salts thereof.
179	Acrylamidobenzoic acid derivatives and their use	US393068	1989-08-07	US5006548A	1991-04-09	Toshio Satoh; Hitoshi Matsumoto; Hisao Kakegawa; Yoshiko Kato; Juichi Riku; Junji Yoshinaga; Yoshifumi Kanamoto
Compounds of the general formula: ##STR1## wherein R.sup.1 is heterocyclic group other than pyridyl and which is unsubstituted or substituted with lower alkyl or lower alkoxycarbonyl, R.sup.2 is hydrogen, halogen, or nitro, and R.sup.3 is carboxy group or its functional derivative, with the proviso that when R.sup.1 is an unsubstituted furyl, or furyl mono- or polysubstituted with alkyl and R.sup.2 is hydrogen, then R.sup.3 is functional derivative of carboxy and, where applicable, pharmaceutically acceptable salts thereof are hyaluronidase inhibitors and useful as anti-allergic agent.
180	Aromatic derivatives, their preparation and their use as antimicrobial agents	US178327	1988-04-06	US4916156A	1990-04-10	Madeleine Mosse; Vincenzo Proietto
The present invention relates to aromatic derivatives of the formula: ##STR1## in which: n represents an integer between 2 and 10;R.sub.1 and R.sub.2 are identical or different and represent a cycloalkyl containing 3 to 6 carbon atoms or an alkyl containing from 1 to 6 carbon atoms which is unsubstituted or substituted by a phenyl or benzyl group; orR.sub.1 and R.sub.2, together with the nitrogen atom to which they are bonded, form a heterocycle selected from pyrrolidin-1-yl, piperidino, azepin-1-yl, hexamethyleneimino, 4-methylpiperidino, 4-benzylpiperidino, 4-phenylpiperidino, 1,2,3,4-tetrahydroisoquinol-2-yl, morpholino and imidazol-1-yl groups;R.sub.3 represents a hydrogen, a halogen, a methyl or a phenyl;R.sub.4 represents a hydrogen, a halogen or a methyl; or R.sub.3 and R.sub.4, taken together with the benzene ring to which they are bonded, form a naphth-1-yl or naphth-2-yl group;Y represents a direct bond, a methyleneoxy group, a methylenethio group or a vinylene group; andR.sub.5 represents an alkyl containing from 5 to 18 carbon atoms, a cycloalkyl containing from 3 to 8 carbon atoms, an adamantyl, naphth-1-yl or naphth-2-yl group, an unsubstituted phenyl group or a phenyl group substituted by one or 2 substituents selected from halogen atoms, the trifluoromethyl group, the nitro group and the phenyl group;and to their salts with mineral or organic acids.

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