181 |
Metal chelating compounds having an SNNN donor set |
US917476 |
1997-08-26 |
US6004531A |
1999-12-21 |
Colin Mill Archer; Gary Robert Bower; Harjit Kaur Gill; Anthony Leonard Mark Riley; Anthony Eamon Storey; Lewis Reuben Canning; David Vaughan Griffiths |
Ligands for radiopharmaceutical use are capable of chelating radiometal species and of being bound to biological targeting molecules. The ligands have formula (a) and (b), where A, A'=--SZ or Y, B.dbd.O or S, Y.dbd. (c), Z.dbd.H or a thiol protecting group, m=2 or 3, n=2 or 3, q=0 or 1, R.dbd.H or unsubstituted or substituted hydrocarbon and pharmaceutically acceptable salts, provided that at least one CR.sub.2 group represents CO and forms, together with an adjacent N atom, a --CONR-- amide group. ##STR1## |
182 |
Process for making gemcitabine hydrochloride |
US209398 |
1998-12-10 |
US6001994A |
1999-12-14 |
John A. Weigel |
An improved process to make gemcitabine hydrocrhloride, the improvement consisting essentially of making the lactone intermediate, 2-deoxy-2,2-difluoro-D-erythro-pentafuranose-1 ulose-3,5-dibenzoate: ##STR1## from D-erythro-2-Deoxy-2,2-difluoro 4,5-O-(1-ethylpropyl)-idene) pentoic acid tert Butyl ester wherein, the D-erythro-2-deoxy-2,2 difluoro-4,5-O-(1-ethylproyl)-ideno) pentoic acid tert-Butyl ester is prepared by the process of reacting S-tert-butyl difluoroethane thioate with 2,3-O (1-ethylpropylidene)-D-glyceraldehyde, in a solvent and in the presence of a strong base; with the proviso that the process is conducted in the absence of a catalyst and in the absence of a silyl containing compound. |
183 |
Dihalopropene compounds, insecticides containing them as active
ingredients, and intermediates for their production |
US913879 |
1997-09-24 |
US5952386A |
1999-09-14 |
Sanshiro Matsuo; Taro Hirose; Keiichi Izumi; Masaya Suzuki; Noriyasu Sakamoto; Kazunori Tsushima; Shigeru Saito; Hirotaka Takano |
The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects. |
184 |
Thioether-containing metal chelating compounds |
US888398 |
1997-07-07 |
US5932707A |
1999-08-03 |
Colin Mill Archer; Gary Robert Bower; Harjit Kaur Gill; Anthony Leonard Mark Riley; Anthony Eamon Storey; Lewis Reuben Canning; David Vaughan Griffiths |
Ligands for radiopharmaceutical use are capable of chelating radiometal species and of being bound to biological targeting molecules. The ligands have the formula (a) and (b), where A, A'=--SZ or Y, B=O or S, Y=(c), Z=H or a thiol protecting group, m=2 or 3, n=2 or 3, q=0 or 1, R=H or unsubstituted or substituted hydrocarbon and pharmaceutically acceptable salts, provided that at least one CR.sub.2 group represents CO and forms, together with an adjacent N atom; a --CONR-- amide group. ##STR1## |
185 |
Enzyme inhibitors |
US750679 |
1996-12-27 |
US5889056A |
1999-03-30 |
Harold Francis Hodson; Richard Michael John Palmer; David Alan Sawyer; Richard Graham Knowles; Karl Witold Franzmann; Martin James Drysdale; Patricia Ifeyinwa Davies; Helen Alice Rebecca Clark; Barry George Shearer; Steven Smith |
A compound of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group, each optionally substituted by one to three groups independently selected from: --CN; --NO.sub.2 ; a group --COR.sup.2 wherein R.sup.2 is hydrogen, C.sub.1-6 alkyl, --OR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-6 alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently selected from hydrogen or C.sub.1-6 alkyl; a group --S(O).sub.m R.sup.6 wherein m is 0, 1 or 2, R.sup.6 is hydrogen, C.sub.1-6 alkyl, hydroxy or NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 are independently hydrogen or C.sub.1-6 alkyl; a group PO(OR.sup.9).sub.2 wherein R.sup.9 is hydrogen or C.sub.1-6 alkyl; a group NR.sup.10 R.sup.11 wherein R.sup.10 and R.sup.11 are independently selected from hydrogen, C.sub.1-6 alkyl, --COR.sup.12 wherein R.sup.12 is hydrogen or C.sub.1-6 alkyl, or --S(O).sub.m' R.sup.13 wherein m' is 0, 1 or 2 and R.sup.13 is hydrogen or C.sub.1-6 alkyl; halo; or a group --OR.sup.14 wherein R.sup.14 is hydrogen, C.sub.1-6 alkyl optionally substituted by one to three halo atoms, C.sub.6-10 aryl or --COR.sup.15 wherein R.sup.15 is hydrogen or C.sub.1-6 alkyl; p is 2 or 3, q is 1 or 2 and n is 0 or 1 and all salts, esters, amides and physiologically acceptable prodrugs thereof; pharmaceutical uses and formulations therefor; and processes for their preparation are disclosed. |
186 |
Process to make .alpha.,.alpha.-difluoro-.beta.-hydroxyl thiol esters |
US762622 |
1996-12-09 |
US5756775A |
1998-05-26 |
John A. Weigel |
A process to make .alpha.,.alpha.-difluoro-.beta.-hydroxy thiol esters of formula (IIIA) ##STR1## comprising reacting a difluoroethanethioate of formula (IVA) ##STR2## with a second reactant selected from the group consisting of aldehydes, ketones, acid halides and esters; in a solvent and in the presence of a strong base; with the proviso that the process is conducted in the absence of a catalyst and in the absence of a silyl containing compound. These thiol esters are useful as intermediates in organic syntheses of pharmaceutical products. |
187 |
Process for producing optically active .beta.-hydroxyketone |
US208379 |
1994-03-10 |
US5434289A |
1995-07-18 |
Koichi Mikami; Satoru Matsukawa; Masaki Shimizu; Masahiro Terada; Noboru Sayo |
A process for producing an optically active .beta.-hydroxyketone represented by formula (I): ##STR1## by catalytic asymmetrical aldol reaction is disclosed, comprising reacting a silyl-enol ether represented by formula (II): ##STR2## with a substituted aldehyde represented by formula (III):R.sup.5 CHO (III)in the presence of a binaphthol-titanium complex represented by formula (IV): ##STR3## An optically active .beta.-hydroxyketone is efficiently produced with diastereo-specificity and enantio-specificity. |
188 |
Trifluoromethyl mercaptan and mercaptoacyl derivatives and method of
using same |
US38207 |
1993-03-26 |
US5414017A |
1995-05-09 |
Norma G. Delaney; George C. Rovnyak; Melanie J. Loots |
Compounds of the formula ##STR1## wherein m is zero or 1; n is zero, 1 or 2; p is zero or 1 to 6 provided that m and p are not both zero; R.sub.3 is hydrogen, acyl, or benzyl; and R.sub.1 is hydrogen, alkyl, phenyl, substituted phenyl, phenyl-alkylene, heterocyclic-alkylene, etc. These compounds are useful as cardiovascular agents. |
189 |
Electroactive compounds, compositions and devices and methods of making
the same |
US629781 |
1990-12-17 |
US5334333A |
1994-08-02 |
Frederick J. Goetz |
The present invention relates to electroactive compounds capable of undergoing a change in light absorption and refraction due to an applied electric field and a permanent change in refraction due to exposure to predetermined bands of optical radiation. The present invention also relates to electroactive compositions containing such electroactive compounds, electrooptical components comprised of such electroactive compositions and electrooptical devices comprised of such electrooptical components, as well as novel processes of making the same. |
190 |
Benzophenone oxime ether compounds, pharmaceutical compositions and
treatment methods |
US518816 |
1990-05-04 |
US5064848A |
1991-11-12 |
Youji Yamagishi; Kozo Akasaka; Takeshi Suzuki; Mitsuaki Miyamoto; Kouji Nakamoto; Kazuo Okano; Shinya Abe; Hironori Ikuta; Kenji Hayashi; Hiroyuki Yoshimura; Tohru Fujimori; Koukichi Harada; Isao Yamatsu |
A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.NOR14)--CH2--COOR15, R15 being hydrogen or a lower alkyl, R14 being a lower alkyl, --CH(CN)--(CH2)q--COOR16, R16 being hydrogen or a lower alkyl, q being an integer of 1 to 3, or --(CH2)p--Z, Z being --SH, --SCN or a monovalent group derived from a five- or six-membered ring which may be substituted by a ring having one or more sulfur atoms in the ring, p being 1 or 2. |
191 |
Diphenylethylene derivative and pharmaceutical use |
US364710 |
1989-06-09 |
US4978767A |
1990-12-18 |
Youji Yamagishi; Kozo Akasaka; Takeshi Suzuki; Mitsuaki Miyamoto; Kouji Nakamoto; Kazuo Okano; Shinya Abe; Hironori Ikuta; Kenji Hayashi; Hiroyuki Yoshimura; Tohru Fujimori; Koukichi Harada; Isao Yamatsu |
A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.NOR14)--CH2--COOR15, R15 being hydrogen or a lower alkyl, R14 being a lower alkyl, --CH(CN)--(CH2)q--COOR16, R16 being hydrogen or a lower alkyl, q being an integer of 1 to 3, or --(CH2)p--Z, Z being --SH, --SCN or a monovalent group derived from a five- or six-membered ring which may be substituted by a ring having one or more sulfur atoms in the ring, p being 1 or 2. |
192 |
Diphenyl-methane compounds useful in the treatment of diseases caused by
aggregation of platelets or formation of thrombus |
US24737 |
1987-03-11 |
US4886834A |
1989-12-12 |
Youji Yamagishi; Kozo Akasaka; Takeshi Suzuki; Mitsuaki Miyamoto; Kouji Nakamoto; Kazuo Okano; Shinya Abe; Hironori Ikuta; Kenji Hayashi; Hiroyuki Yoshimura; Tohru Fujimori; Koukichi Harada; Isao Yamatsu |
A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(C.dbd.NOR14)--CH2--COOR15, R15 being hydrogen or a lower alkyl, R14 being a lower alkyl, --CH(CN)--(CH2)q--COOR16, R16 being hydrogen or a lower alkyl, q being an integer of 1 to 3, or --(CH2)p--Z, Z being --SH, --SCN or a monovalent group derived from a five- or six-membered ring which may be substituted by a ring having one or more sulfur atoms in the ring, p being 1 or 2. |
193 |
Substituted 3-hydrazinopropionates |
US628240 |
1984-07-06 |
US4633014A |
1986-12-30 |
Gunar A. Bremanis; Ivars Y. Kalvinsh; Irene B. Antsena; Edmund Y. Lukevits; Maris M. Veveris; Valeryans Y. Kauss; Peter T. Trapentsier; Edvards E. Liepinsh |
Substituted 3-hydrazinopropionates comprising compounds of the general fola: ##STR1## wherein R.sup.1, R.sup.2 =H, an alkyl, a substituted alkyl, hydroxycarbonyl, alkoxycarbonyl, an aryl, an aralkyl, an unsaturated alkyl, a substituted aryl or a substituted aralkyl: ##STR2## wherein R.sup.7, R.sup.8 =H, an alkyl, an unsaturated alkyl, an aralkyl, an aryl, a substituted alkyl,R.sup.9 =OH, an alkoxy, an aralkoxy, an alkyl, an unsaturated alkyl, an aryl, a substituted aryl, an aralkyl;R.sup.4 is --C.tbd.N, --COR.sup.10, wherein R.sup.10 =OR.sup.11, NR.sup.12 R.sup.13, where R.sup.11 is H, an alkyl, an aralkyl and an alkali metal, R.sup.11 and R.sup.12 are each H, an alkyl, an aralkyl, an aryl;R.sup.5, R.sup.6 = an alkyl, an aryl, an aralkyl. |
194 |
4-Phenoxy-2-butene derivatives as plant growth regulators |
US178080 |
1980-08-14 |
US4340765A |
1982-07-20 |
Gary M. Gray; George Schwartzkopf, Jr.; J. T. Baker Chemical Co. |
4-Phenoxy-2-butene derivatives are disclosed as inhibitors of cytokinin plant growth regulatory activity and as possessing seed germination regulatory properties and senescence delaying activity when applied to plants. 4-Phenoxy-2-butene derivatives can also be useful as plant dwarfing agents, agents to retard seedling development or as herbicides. |
195 |
Halogenated 4-trifluoromethyl-4'-nitro-diphenyl-ether |
US686349 |
1976-05-14 |
US4104313A |
1978-08-01 |
Lothar Rohe; Jurgen Schramm; Erich Klauke; Ludwig Eue; Robert Rudolf Schmidt |
Halogenated 4-trifluoromethyl-4'-nitro-diphenyl-ether compounds of the formula ##STR1## in which R is halogen or methylthio, andX is hydrogen or chlorine,Are outstandingly effective as herbicides, particularly as selective herbicides. |
196 |
Tetrafluorodithiosuccinyl difluoride and method of preparing same |
US47631774 |
1974-06-04 |
US3907885A |
1975-09-23 |
MIDDLETON WILLIAM J |
Tetrafluorodithiosuccinyl difluoride is prepared by reacting trifluorovinyl iodide with sulfur in the vapor phase. The product is polymerized by ionic polymerization to polymers which are corrosion resistant and have nonstick surfaces.
|
197 |
Addition product of an alpha beta-unsaturated ester and a thiocarboxylic acid |
US3636033D |
1969-02-27 |
US3636033A |
1972-01-18 |
KLEINER EDUARD K |
ORGANIC MATERIALS, PARTICULARLY SYNTHETIC POLYMERS SUCH AS POLYPROPYLENE, ARE PROTECTED AGAINST OXIDATION IN AIR, THERMAL DEGRADATION OR DETERIORATION BY INCLUDING, IN SUCH SUBSTANCES, A STABILIZING AMOUNT OF AN ANTIOXIDANT. THE ANTIOXIDANT IS OBTAINED BY REACTING (A) AN A,B-UNSATURATED ESTER OF A HINDERED HYDROQUINONE AND (B) A THIO ACID.
|
198 |
Process for preparing carboxylic acid thioanhydrides |
US3476784D |
1968-01-19 |
US3476784A |
1969-11-04 |
GRECO CARL C |
|
199 |
Preparation of carbothiolic acids and corresponding thiolesters |
US26375563 |
1963-03-08 |
US3254106A |
1966-05-31 |
GODFREY JOHN J |
|
200 |
Halothioacyl fluorides and polymers thereof |
US79185959 |
1959-02-09 |
US3069395A |
1962-12-18 |
MIDDLETON WILLIAM J |
|