Patents by Inventor Jack Bernstein
Jack Bernstein has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 4345096Abstract: Radiolabeled steroid derivatives having the formula ##STR1## wherein St is a des-hydroxy steroid moiety of (i) a hydroxy steroid intended for radioimmunoassay or (ii) a hydroxy containing derivative of a steroid intended for radio-immunoassay, said derivative having a strong affinity for the antibodies of the steroid intended for radioimmunoassay; R is hydrogen or alkyl of 1 to 3 carbon atoms; n is 0, 1, 2, 3 or 4 and the asterisk (*) indicates tagging with a radioisotope, are useful as tracers in radioimmunoassays.Type: GrantFiled: March 10, 1980Date of Patent: August 17, 1982Assignee: E. R. Squibb & Sons, Inc.Inventors: Jack Bernstein, Ravi K. Varma, B. Richard Vogt, Frank L. Weisenborn
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Patent number: 4230621Abstract: Radiolabeled steroid derivatives having the formula ##STR1## wherein St is a des-hydroxy steroid moiety of (i) a hydroxy steroid intended for radioimmunoassay or (ii) a hydroxy containing derivative of a steroid intended for radioimmunoassay, said derivative having a strong affinity for the antibodies of the steroid intended for radioimmunoassay; R is hydrogen or alkyl of 1 to 3 carbon atoms; n is 0, 1, 2, 3 or 4 and the asterisk (*) indicates tagging with a radioisotope, are useful as tracers in radioimmunoassays.Type: GrantFiled: May 1, 1978Date of Patent: October 28, 1980Assignee: E. R. Squibb & Sons, Inc.Inventors: Jack Bernstein, Ravi K. Varma, B. Richard Vogt, Frank L. Weisenborn
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Patent number: 4221725Abstract: Radiolabeled steroid derivatives having the formula ##STR1## wherein St is des-hydroxy steroid moiety of (i) a hydroxy steroid intended for radioimmunoassay or (ii) a hydroxy containing derivative of a steroid intended for radioimmunoassay, said derivative having a strong affinity for the antibodies of the steroid intended for radioimmunoassay; R is hydrogen or alkyl of 1 to 3 carbon atoms; n is 0, 1, 2, 3 or 4 and the asterisk (*) indicates tagging with a radioisotope, are useful as tracers in radioimmunoassays.Type: GrantFiled: January 17, 1979Date of Patent: September 9, 1980Assignee: E. R. Squibb & Sons, Inc.Inventors: Jack Bernstein, Ravi K. Varma, B. Richard Vogt, Frank L. Weisenborn
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Patent number: 4221796Abstract: Imidazolo-pyridine derivatives are provided having the structure ##STR1## wherein R is lower alkyl, lower alkenylalkyl, lower alkynylalkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl or phenylalkyl and R.sup.1 is lower alkyl, phenylalkyl or di-lower alkylaminoalkyl and n is 0, 1 or 2. These compounds are useful as anthelmintic agents administered orally or parenterally.Type: GrantFiled: September 19, 1979Date of Patent: September 9, 1980Assignee: E. R. Squibb & Sons, Inc.Inventors: Peter C. Wade, Jack Bernstein, Rudiger D. Haugwitz
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Patent number: 4209614Abstract: Radiolabeled vitamin B.sub.12 derivatives having the formula ##STR1## wherein R is hydrogen or alkyl of 1 to 3 carbon atoms; n is 0, 1, 2, 3 or 4; and the asterisk (*) indicates tagging with a radioisotope, are useful as tracers in radioassays.Type: GrantFiled: May 30, 1978Date of Patent: June 24, 1980Assignee: E. R. Squibb & Sons, Inc.Inventors: Jack Bernstein, Ravi K. Varma, B. Richard Vogt, Frank L. Weisenborn
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Patent number: 4198509Abstract: The mercaptoacylpiperazine carboxylic acid compounds which have the formula ##STR1## wherein R, R.sub.3 and R.sub.4 each is hydrogen or lower alkyl;R.sub.1 is lower alkyl;R.sub.2 is hydrogen, lower alkanoyl, benzoyl or ##STR2## m is 0, 1 or 2; n is 1, 2 or 3, the sum of m+n being equal to 1, 2 or 3and salts thereof, are useful as hypotensive agents.Type: GrantFiled: October 30, 1978Date of Patent: April 15, 1980Assignee: E. R. Squibb & Sons, Inc.Inventors: Kathryn A. Losee, Jack Bernstein
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Patent number: 4179564Abstract: Various 1,5,6,11-tetrahydrobenzo[5,6]cyclohepta[1,2-b]pyrazolo[4,3-e]pyridine derivatives and their salts of the formulas ##STR1## wherein R.sub.1 is lower alkyl, phenyl, or phenyl-lower alkyl; R.sub.2 is hydrogen, lower alkyl or phenyl; R.sub.3 is hydrogen, halogen, or lower alkoxy; R.sub.4 is hydrogen, ##STR2## R.sub.5 is hydrogen or lower alkoxy; R.sub.6 is hydrogen, ##STR3## n is an integer from 2 to 6; R.sub.7 and R.sub.8 are the same or different and each is lower alkyl or R.sub.7 and R.sub.8 taken together with the N-atom form a heterocyclic ring of the formula ##STR4## wherein R.sub.9 is hydrogen or lower alkyl; R.sub.10 and R.sub.11 are the same or different and each is hydrogen or lower alkyl or R.sub.10 and R.sub.11 taken together with the N-atom form a heterocyclic ring of the formula ##STR5## wherein R.sub.9 is as defined above; are disclosed. These compounds possess useful anti-inflammatory activity as well as psychotropic activity.Type: GrantFiled: June 23, 1978Date of Patent: December 18, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Hans Hoehn, Jack Bernstein, Berthold R. Vogt
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Patent number: 4154934Abstract: New mercaptoacyl derivatives of heterocyclic carboxylic acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.Type: GrantFiled: August 11, 1978Date of Patent: May 15, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Jack Bernstein, Kathryn A. Losee
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Patent number: 4128717Abstract: New derivatives of 5,6-dihydrobenzo[5,6]cyclohepta-[1,2-b]pyrazolo[4,3-e]pyridin-11 (1H)-ones and imines, respectively, have the general formula ##STR1## They and the salts thereof are useful as psychotropic and antiinflammatory agents.Type: GrantFiled: July 20, 1977Date of Patent: December 5, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Hans Hoehn, Jack Bernstein, B. Richard Vogt
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Patent number: 4127715Abstract: Compounds of the formulas ##STR1## wherein R.sub.1 is lower alkyl, phenyl, benzyl or phenethyl; R.sub.2 is hydrogen, lower alkyl or phenyl; ##STR2## N IS AN INTEGER FROM 3 TO 6; R.sub.3 and R.sub.4 are each lower alkyl or R.sub.3 and R.sub.4 taken together with the N-atom form a heterocyclic ring of the formula ##STR3## wherein R.sub.5 is hydrogen, lower alkyl, or lower alkoxy; and pharmaceutically acceptable acid addition salts thereof are disclosed. These compounds and their salts possess central nervous system activity and are useful as anti-anxiety agents.Type: GrantFiled: February 27, 1978Date of Patent: November 28, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Hans Hoehn, Jack Bernstein, Berthold R. Vogt
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Patent number: 4111940Abstract: Various 1,5,6,11-tetrahydrobenzo[5,6]cyclohepta[1,2-b]-pyrazolo[4,3-e]pyridine derivatives and their salts of the formulas ##STR1## wherein R.sub.1 is lower alkyl, phenyl, or phenyl-lower alkyl; R.sub.2 is hydrogen, lower alkyl or phenyl; R.sub.3 is hydrogen, halogen, or lower alkoxy; R.sub.4 is hydrogen, ##STR2## ALKYL; R.sub.5 is hydrogen or lower alkoxy; R.sub.6 is hydrogen, ##STR3## n is an integer from 2 to 6; R.sub.7 and R.sub.8 are the same or different and each is lower alkyl or R.sub.7 and R.sub.8 taken together with the N-atom form a heterocyclic ring of the formula ##STR4## wherein R.sub.9 is hydrogen or lower alkyl; R.sub.10 and R.sub.11 are the same or different and each is hydrogen or lower alkyl or R.sub.10 and R.sub.11 taken together with the N-atom form a heterocyclic ring of the formula ##STR5## wherein R.sub.9 is as defined above; are disclosed. These compounds possess useful antiinflammatory activity as well as psychotropic activity.Type: GrantFiled: April 7, 1977Date of Patent: September 5, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Hans Hoehn, Jack Bernstein, Berthold Richard Vogt
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Patent number: 4087433Abstract: Compounds of the formulas ##STR1## wherein R.sub.1 is lower alkyl, phenyl, benzyl or phenethyl; R.sub.2 is hydrogen, lower alkyl or phenyl; R is ##STR2## N IS AN INTEGER FROM 3 TO 6; R.sub.3 and R.sub.4 are each lower alkyl or R.sub.3 and R.sub.4 taken together with the N-atom form a heterocyclic ring of the formula ##STR3## wherein R.sub.5 is hydrogen, lower alkyl, or lower alkoxy; and pharmaceutically acceptable acid addition salts thereof are disclosed. These compounds and their salts possess central nervous system activity and are useful as anti-anxiety agents.Type: GrantFiled: March 28, 1977Date of Patent: May 2, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Hans Hoehn, Jack Bernstein, Berthold Richard Vogt
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Patent number: 4062858Abstract: New derivatives of 5,6-dihydrobenzo[5,6]cyclohepta[1,2-b]pyrazolo[4,3-e]pyridin-11(1H)-ones and imines, respectively, have the general formula ##STR1## They and the salts thereof are useful as psychotropic and antiinflammatory agents.SUMMARY OF THE INVENTIONThis invention relates to new derivatives of 5,6-dihydrobenzo[5,6]cyclohepta[1,2-b]pyrazolo[4,3-e]-pyridin-11(1H)-ones and imines and salts thereof. These new compounds have the general formula ##STR2## R.sup.1 is lower alkyl, phenyl or phenyl-lower alkyl; R.sup.2 is hydrogen, lower alkyl or phenyl;R.sup.3 is hydroxy, lower alkoxy, halogen or an amine group.The amine group is either an acyclic group ##STR3## wherein R.sup.5 and R.sup.6 each is hydrogen, lower alkyl or phenyl or R.sup.5 and R.sup.6 taken together with the nitrogen form a monocyclic nitrogen heterocyclic of 5 or 6 members in which an additional nitrogen, oxygen or sulfur may be present.R.sup.4 is oxygen (.dbd.O) or substituted imine (.dbd.NR)R is lower alkyl or phenyl.Type: GrantFiled: December 22, 1976Date of Patent: December 13, 1977Assignee: E. R. Squibb & Sons, Inc.Inventors: Hans Hoehn, Jack Bernstein, B. Richard Vogt
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Patent number: 4033970Abstract: Compounds of the formulas wherein R.sub.1 is lower alkyl, phenyl, benzyl or phenethyl; R.sub.2 is hydrogen, lower alkyl or phenyl; R is ##STR1## N IS AN INTEGER FROM 3 TO 6; R.sub.3 and R.sub.4 are each lower alkyl or R.sub.3 and R.sub.4 taken together with the N-atom form a heterocyclic ring of the formula ##STR2## wherein R.sub.5 is hydrogen, lower alkyl, or lower alkoxy; and pharmaceutically acceptable acid addition salts thereof are disclosed. These compounds and their salts possess central nervous system activity and are useful as anti-anxiety agents.Type: GrantFiled: June 23, 1976Date of Patent: July 5, 1977Assignee: E. R. Squibb & Sons, Inc.Inventors: Hans Hoehn, Jack Bernstein, Berthold Richard Vogt
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Patent number: 4018779Abstract: New derivatives of 10,11-dihydrobenzo[4,5]cyclohepta[1,2-b]pyrazolo[4,3-e]pyridin-5(1H)ones have the general formula ##STR1## They and salts thereof are useful as psychotropic agents.Type: GrantFiled: March 25, 1976Date of Patent: April 19, 1977Assignee: E. R. Squibb & Sons, Inc.Inventors: Hans Hoehn, Jack Bernstein, B. Richard Vogt
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Patent number: 3985746Abstract: New 7-(.alpha.-cyanomethylthio)acetamido-3-cephem carboxylates which have the formula ##EQU1## have antimicrobial activity.Type: GrantFiled: March 25, 1975Date of Patent: October 12, 1976Assignee: E. R. Squibb & Sons, Inc.Inventors: William Henry Koster, William A. Slusarchyk, Jack Bernstein
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Patent number: 3968249Abstract: This invention relates to pharmaceutical preparations and the method of utilizing them in the treatment of malignant neoplastic diseases. The administration of hydroxyurea or 1-ethyl-1-hydroxyurea has been found to be effective for the amelioration of the symptoms of various forms of leukemia, carcinoma or sarcoma in various organs of the body.Type: GrantFiled: May 15, 1968Date of Patent: July 6, 1976Assignee: E. R. Squibb & Sons, Inc.Inventors: Jack Bernstein, Barbara Stearns