Christopher M. Cimarusti Patents

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Christopher M. Cimarusti Patents

Inventor:

Cimarusti; Christopher M.

Address:

Millstone, NJ

No. of patents:

Patents:

1 2

Patent Number	Title Of Patent	Date Issued
5194604	Process and intermediates for beta-lactams having aminothiazole(iminooxyacetic acid)acetic acid	March 16, 1993
Disclosed herein are processes for preparing a compound of the formula ##STR1## in which a novel compound of the formula ##STR2## is reacted with a beta lactam of the formula ##STR3## by treatment with a base, wherein the symbols are as defined in the specification.
4937355	Process for preparing (trans)-4-substituted-dl-proline derivatives	June 26, 1990
A process is provided for preparing (trans)-4-phenyl-DL-proline derivatives, which are useful in preparing certain angiotensin converting enzyme inhibitors, which process involves reacting an ester of the structure ##STR1## wherein X is a leaving group such as tosylate, R.sup.3 i
4912230	Process for stereochemically inverting a hydroxy function of an ester by a modified Mitsunobu re	March 27, 1990
A process is provided for inverting a hydroxy function of a L-trans-hydroxy proline derivative to the corresponding L-cis-hydroxy proline sulfonate by a Modified Mitsunobu reaction process.
4775670	2-oxo-1-azetidinesulfonic acid salts	October 4, 1988
Antibacterial activity is exhibited by .beta.-lactams having a sulfonic acid salt substituent in the 1-position and an amino or acylamino substituent in the 3-position.
4704457	Process for the preparation of (3S)-3-[[[2-(protected amino)-4-thiazolyl]-oxoacetyl]amino]-2-oxo	November 3, 1987
A compund having the formula ##STR1## can be prepared by coupling a compound having the formula ##STR2## or a salt thereof, with a compound having the formula ##STR3## to yield a compound having the formula ##STR4## and oxidizing that compound to yield the desired com
4625022	Process for preparing (s)-3-amino-2-oxo-1-azetidinesulfonic acid salts	November 25, 1986
The process of this invention provides for the conversion of amino acid amides having the formula ##STR1## to 3-amino-2-oxo-1-azetidinesulfonic acid salts having the formula ##STR2## wherein one of R.sub.2 and R.sub.3 is hydrogen and the other is hydrogen, alkyl, cycloalkyl,
4529698	Process for preparing a 2-oxo-1-azetidinesulfonic acid salt	July 16, 1985
A pharmaceutically acceptable salt of (R)-3-(acetylamino)-3-methoxy-2-oxo-1-azetidinesulfonic acid can be prepared by culturing Chromobacterium violaceum A.T.C.C. No. 31532 at about 25.degree. C. under submerged aerobic conditions on an aqueous nutrient medium containing an assimilab
4483797	(S)-3-Isocyanato-2-oxo-1-azetidinesulfonic acids	November 20, 1984
3-Isocyanato-2-oxo-1-azetidinesulfonic acid salts are novel intermediates which are useful in processes for the preparation of 3-amino-2-oxo-1-azetidinesulfonic acid salts and 3-acylamino-2-oxo-1-azetidinesulfonic acid salts.
4478749	2-Oxo-1-(substituted phosphorous)azetidines	October 23, 1984
Antibacterial activity is exhibited by .beta.-lactams having a phosphinic or phosphonic substituent in the 1-position and an acylamino substituent in the 3-position.
4474702	[16,17-a]Cyclopentano pregnenes	October 2, 1984
Antiinflammatory activity is exhibited by pregnenes having the structural formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy, halogen, or acyloxy;R.sub.2 and R.sub.3 are each hydrogen, R.sub.2 and R.sub.3 are each methyl, R.sub.2 and R.sub.3 are each alkylthio, R.sub.2 is hydrogen
4443374	Process for preparing (3S)-3-[[(2-amino-4-thiazolyl)[(1-carboxy-1-methylethoxy)imino]-acetyl]a	April 17, 1984
Disclosed herein is a process for preparing a compound having the formula ##STR1## which comprises coupling a compound having the formula ##STR2## or a salt thereof, with a compound having the formula ##STR3## to obtain a compound having the formula ##STR4## reacting
4421686	4-Norbornyl-sulfonyl azetidinone intermediates and process for preparing (S)-3-acylamino-4-subst	December 20, 1983
Compounds having the formula ##STR1## can be prepared by reacting a compound having the formula ##STR2## with a Grignard reagent having the formulawherein R.sub.1 is phenylacetyl or phenoxyacetyl;R.sub.2 is a not readily enolyzable alkyl group, aryl or norbornyl;R.sub.3 is alkyl, alk
4386034	Sulfamated amino acid amides	May 31, 1983
The process of this invention provides for the conversion of amino acid amides having the formula ##STR1## to 3-amino-2-oxo-1-azetidinesulfonic acid salts having the formula ##STR2## wherein one of R.sub.2 and R.sub.3 is hydrogen and the other is hydrogen, alkyl, cycloalkyl,
4267373	5,6,7,8-Tetrahydronaphthalene hypotensive agents	May 12, 1981
5,6,7,8-Tetrahydronaphthalenes having the structure ##STR1## and the pharmaceutically acceptable salts thereof, are useful as blood pressure lowering agents. In the above formula R.sub.1 can be hydrogen or alkyl; R.sub.2 is alkyl; R.sub.3 and R.sub.4 can each be hydrogen, hydroxy
4252973	Process for chemically removing the acyl sidechain from cephalosporins and penicillins	February 24, 1981
A process for removing the acyl sidechain from penicillins and cephalosporins which comprises chlorinating the acyl compound and treating the resulting iminochloride with an o-aminothiophenol to obtain the corresponding 6.beta.-aminopenicillin or 7.beta.-aminocephalosporin.
4237128	7-[2-(2-Amino-4-thiazolyl)-2-[(1-carboxy-1, 1-dialkyl)alkoxyimino]acetamido]cephem sulfoxides	December 2, 1980
Compounds of the formula ##STR1## wherein R is hydrogen, sodium, potassium, or certain ester groups; R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy; R.sub.2 and R.sub.3 are independently selected from methyl, ethyl, i-propyl, and n-propyl; R.sub.4 is hydrogen,
4206218	Phthalidyl esters of the acetone adduct of epicillin	June 3, 1980
Penicillin esters and their acid addition salts of the formula ##STR1## wherein X is hydrogen, methyl, methoxy, chloro, or bromo and n is an integer from 1 to 3 provided that n is 2 or 3 only when X is hydrogen or methoxy; are disclosed. Upon oral administration, these esters provide
4156789	5,6,7,8-Tetrahydro-1,6,7-naphthalenetriols	May 29, 1979
5,6,7,8-Tetrahydro-1,6,7-naphthalenetriols having the formula ##STR1## wherein R.sup.8, R.sup.9 and R.sup.10 are the same or different and are hydrogen, lower alkyl, monocyclic aryl-lower alkyl, lower alkoxy, carboxy, or monocyclic cycloalkyl, are intermediates useful in the preparat
4155917	Process for preparing D-homo oxasteroids	May 22, 1979
A steroid having the formula ##STR1## or the 1,2-dehydro derivative thereof, can be prepared by reacting the corresponding steroid having the formula ##STR2## or the 1,2-dehydro derivative thereof, with ozone and an alkanol having the formula R.sub.3 --OH and then treating th
4127589	4,5-Seco-steroids	November 28, 1978
Novel 4,5-seco-steroids having anti-inflammatory activity are disclosed herein.
4127578	Diene intermediates for indantetrols	November 28, 1978
Diene intermediates for indantetrols are provided having the structure ##STR1## wherein X is a single bond or a straight or branched chain alkylene group containing from 1 to 10 carbons, Y is ##STR2## wherein R.sub.7 is hydrogen, lower alkyl, arylalkyl or lower alkoxy and ##S
4116978	D-Homo oxasteroids	September 26, 1978
Steroids having the formula ##STR1## or the 1,2-dehydro derivative thereof, wherein R.sub.1 is hydrogen, acyloxy, halogen, or hydroxy; R.sub.2 is hydrogen or alkyl; R.sub.3 is alkyl; R.sub.4 is carbonyl, .beta.-hydroxymethylene, .beta.-chloromethylene or .beta.-bromomethylene; R.
4113722	Steroidal[16.alpha.,17-b]benzodioxins	September 12, 1978
Steroids having the formula ##STR1## wherein R.sub.1 is hydrogen, acyloxy, halogen or alkoxy of 1 to 10 carbons; R.sub.2 is halogen or cyano; R.sub.3 is hydrogen or halogen; R.sub.4 is carbonyl, .beta.-hydroxymethylene or .beta.-acetyloxymethylene; and R.sub.5 is hydrogen or fluo
4092318	Indantetrol derivatives	May 30, 1978
Compounds are provided having the structure ##STR1## WHEREIN N IS 1, 2 OR 3, M AND M' ARE 0, 1 OR 2, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and can be hydrogen, lower alkyl, halolower alkyl, acyl, lower alkoxy-carbonyl ##STR2## or lower alkoxyalkyl
4091216	4-Thio substituted-.DELTA..sup.2 cephalosporin intermediates	May 23, 1978
Cephalosporin intermediates of the formulas ##STR1## wherein R is lower alkyl, 2,2,2-trichloroethyl, diphenylmethyl, p-methoxybenzyl, or p-nitrobenzyl; R.sub.1 is lower alkyl or phenyl; R.sub.2 is hydrogen or acetoxy; R.sub.4 is methyl or ethyl; and R.sub.5 is hydrogen, methyl, o
4076843	5,6,7,8-Tetrahydronaphthalene hypotensive agents	February 28, 1978
5,6,7,8-Tetrahydronaphthalenes having the structure ##STR1## and the pharmaceutically acceptable salts thereof, are useful as blood pressure lowering agents. In the above formula R.sub.1 can be hydrogen or alkyl; R.sub.2 is alkyl; R.sub.3 and R.sub.4 can each be hydrogen, hydroxy
4053596	Indanpentol derivatives	October 11, 1977
Compounds are provided having the structure ##STR1## wherein n is 1, 2 or 3, m is 0, 1 or 2, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and can be hydrogen, lower alkyl, halo-lower alkyl, acyl, lower alkoxy-carbonyl ##STR2## amido ##STR3##
4052422	4,5-Secopregnane derivatives	October 4, 1977
Novel 4,5-seco-steroids having anti-inflammatory activity are disclosed herein.
4044040	4,7-Dihydroindanyl alkanols, analogues thereof and their corresponding tosylates	August 23, 1977
Compounds are provided having the structure ##STR1## WHEREIN N IS 1, 2 OR 3, M AND M' ARE 0, 1, OR 2, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and can be hydrogen, lower alkyl, halolower alkyl, acyl, lower alkoxy-carbonyl ##STR2## or lower alkoxyalky
4039537	Thio-.beta.-lactam cephalosporins	August 2, 1977
Thio-.beta.-lactam cephalosporins of the general formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal; R.sub.1 is hydrogen, lower alkyl, cycloalkyl, phenyl, phenoxy, phenyl-lower alkyl or certain heterocyclic
4039534	4-Thio substituted-.DELTA..sup.2 -cephalosporin intermediates	August 2, 1977
Cephalosporin intermediates of the formulas ##STR1## wherein R is lower alkyl, 2,2,2-trichloroethyl, diphenylmethyl, p-methoxybenzyl, or p-nitrobenzyl; R.sub.1 is lower alkyl or phenyl; R.sub.2 is hydrogen or acetoxy; R.sub.4 is methyl or ethyl; and R.sub.5 is hydrogen, methyl, o
4029676	Esters of tetrahydronaphthyloxy-aminopropanols	June 14, 1977
Compounds having the formula ##STR1## wherein R.sup.1 is lower alkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are the same or different and are hydrogen or lower alkyl; R.sup.8, R.sup.9, and R.sup.10 are the same or different and are hydrogen, lower alkyl, lower alkoxy or
4029645	Mercury intermediates useful in the preparation of 2-alkoxy cephalosporins	June 14, 1977
Compounds of the formula ##STR1## WHEREIN R.sub.1 is lower alkyl, diphenylmethyl, 2,2,2-trichloro-ethyl, p-methoxybenzyl, or p-nitrobenzyl; R.sub.2 is hydrogen or acetoxy; R.sub.5 is lower alkyl; and R.sub.4 is ##STR2## wherein R.sub.3 is a heterocyclic group, lower alkyl, cy
4018774	Steroidal [16.alpha.,17-d]isoxazolidines	April 19, 1977
Novel steroids having the structure ##STR1## and the 1,2-dehydro derivatives thereof, wherein R.sub.1 is hydrogen, hydroxy, alkanoyloxy, fluorine, chlorine, or bromine; R.sub.2 is alkyl or aryl; R.sub.3 is alkyl, aryl, alkanoyl, aroyl, alkoxycarbonyl, or cyano; R.sub.4 is hydroge
4018761	Thio-.beta.-lactam cephalosporins	April 19, 1977
New intermediates of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal and X is lower alkylthiadiazolylthio or lower alkyltetrazolylthio are useful for the production of antimicrobially active acyl deri
4018760	Thio-.beta.-lactam cephalosporins	April 19, 1977
Thio-.beta.-lactam cephalosporins of the general formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal; R.sub.1 is hydrogen, lower alkyl, cycloalkyl, phenyl, phenoxy, phenyl-lower alkyl or certain heterocyclic
4018757	Steroidal[16.alpha.,17-c][2H]pyrroles	April 19, 1977
Steroids having the structure ##STR1## and the 1,2-dehydro derivatives thereof, wherein R.sub.1 is hydrogen, hydroxy, ##STR2## fluorine, chlorine, or bromine; R.sub.2 is alkyl or aryl; R.sub.3 is aryl, cyano, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, a
4003930	2,3-Trans-5-[3-(amino)-2-hydroxy-propoxy]-1,2,3,4-tetrahydro-3-(or 2)-amino-2-(or 3)-hydroxy-nap	January 18, 1977
This invention relates to novel cyclic polymethylene phenoxy-aminopropanols having the structure ##STR1## and the pharmaceutically acceptable salts of said compounds, wherein R.sup.1, R.sup.2, R.sup.8 and R.sup.9 are each independently selected from hydrogen, lower alkyl and aryl
3994935	Steroidal 16.beta.-alkyl[16.alpha.,17-b]naphthalenes	November 30, 1976
Novel steroids having the structure ##SPC1##And the 1,2-dehydro derivatives thereof, wherein R.sub.1 is chlorine, fluorine, or hydroxy and R'.sub.1 is hydrogen or R.sub.1 and R'.sub.1 together are =O; R.sub.2 is hydrogen or halogen; R.sub.3 is hydrogen, methyl, or fluorine; R.sub.4 i
3984474	4,5-Secoandrostanes	October 5, 1976
4,5-Secoandrostanes having the formula ##SPC1##Have useful anti-inflammatory activity wherein R.sub.1 is hydrogen and R.sub.2 is hydroxyl, R.sub.1 is hydroxyl and R.sub.2 is hydrogen, R.sub.1 and R.sub.2 are each hydrogen, or together R.sub.1 and R.sub.2 are =0; R.sub.3 is hydrogen a
3984407	Diene intermediates for indantetrol derivatives	October 5, 1976
Compounds are provided having the structure ##SPC1##Wherein n is 1, 2 or 3, m and m' are 0, 1 or 2, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and can be hydrogen, lower alkyl, halolower alkyl, acyl, lower alkoxy-carbonyl ##EQU1## amido ##EQU2## or
3982021	Compositions for the treatment of coronary diseases containing tetrahydronaphthyloxy-aminopropan	September 21, 1976
This invention relates to pharmaceutical compositions for the treatment of coronary diseases comprising a compound having the formula ##SPC1##Wherein R.sup.1 is lower alkyl, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are the same or different and are hydrogen or lower alkyl, and
3979417	1 H-androsta(16,17)cyclopentene-3-ones	September 7, 1976
Steroids having the formula ##SPC1##And the 1,2-dehydro derivatives thereof, wherein R.sub.1 is phenyl, naphthyl, or substituted phenyl or naphthyl, have useful anti-inflammatory activity.
3976638	16.alpha.-ARYLCARBONYLPREGNENES	August 24, 1976
Topical and systemic anti-inflammatory activity is exhibited by steroids having the formula ##SPC1##And the 1,2-dehydro derivatives thereof, wherein R.sub.1 is phenyl, naphthyl, or substituted phenyl or naphthyl.
3976637	3,20-Diketopregnenes having an 11.beta.-acetal group	August 24, 1976
3,20-Diketopregnenes having in the 11.beta.-position a group of the formula ##SPC1##Wherein R.sub.1 is alkyl and R.sub.2 is hydrogen, alkyl, alkoxy, or halogen, and having a cyclic 16,17-acetal or ketal group, have useful anti-inflammatory activity.
3971780	Thio-.beta.-lactam cephalosporins	July 27, 1976
Thio-.beta.-lactam cephalosporins of the general formula ##SPC1##Wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal; R.sub.1 is hydrogen, lower alkyl, cycloalkyl, phenyl, phenoxy, phenyl-lower alkyl or certain heterocyclic group
3971776	Thio-.beta.-lactam penicillins	July 27, 1976
Thio-.beta.-lactam penicillins of the general formula ##EQU1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, trihaloethyl, alkali metal or alkaline earth metal; R.sub.1 is hydrogen, lower alkyl, cycloalkyl, phenyl, lower alkoxyphenyl, phenoxy, phenyl-lower alkyl or cert
3971773	Steroidal 9,11-dihalo-[16.alpha.,17-b]1,4-dioxanes	July 27, 1976
A series of novel steroidal 9,11.beta.-dihalo-[16.alpha.,17-b]-1,4-dioxanes is disclosed herein. These compounds are useful as anti-inflammatory agents.
3971772	Steroidal[16.alpha.,17-b]1,4-dioxanes and Steroidal[16.alpha.,17-b]1,4-dioxins	July 27, 1976
A series of novel steroidal [[16.alpha.,17-b]1,4-dioxanes and steroidal [ 16.alpha.,17-b]1,4-dioxins having useful anti-inflammatory properties is disclosed herein.
3945997	Steroidal bicyclic dioxanes	March 23, 1976
Steroids having the structure ##SPC1##Wherein P is hydrogen, methyl or chloro; Q is hydrogen, methyl or fluoro; X is hydrogen or halogen; Y is hydrogen and Y' is hydroxyl or together Y and Y' can be =O; and R can be hydrogen, alkyl or aryl; have useful anti-inflammatory activity.