Patents by Inventor Cedric H. Hassall
Cedric H. Hassall 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: 4826980Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl, as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.Type: GrantFiled: July 12, 1988Date of Patent: May 2, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Cedric H. Hassall, Geoffrey Lawton, Sally Redshaw
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Patent number: 4808713Abstract: Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula ##STR2## , R.sup.3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group, R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.Type: GrantFiled: June 10, 1988Date of Patent: February 28, 1989Assignee: Hoffman-La Roche Inc.Inventors: Michael R. Attwood, Cedric H. Hassall, Robert W. Lambert, Geoffrey Lawton, Sally Redshaw
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Patent number: 4785093Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --or--N(R.sup.6)--in which R.sup.6 is hydrogen, alkyl or aralkyl, as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.Type: GrantFiled: May 11, 1987Date of Patent: November 15, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Cedric H. Hassall, Geoffrey Lawton, Sally Redshaw
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Patent number: 4772701Abstract: Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonyl-amino-alkly or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl carbonyl group or a group of the formula ##STR2## R.sup.3 represents a carboxyl, alkoxycarbonyl or aralykoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group; R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.Type: GrantFiled: November 28, 1986Date of Patent: September 20, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Michael R. Attwood, Cedric H. Hassall, Robert W. Lambert, Geoffrey Lawton, Sally Redshaw
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Patent number: 4762924Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl,as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.Type: GrantFiled: June 15, 1987Date of Patent: August 9, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Cedric H. Hassall, Geoffrey Lawton, Sally Redshaw
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Patent number: 4692438Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl,as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.Type: GrantFiled: August 12, 1985Date of Patent: September 8, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Cedric H. Hassall, Geoffrey Lawton, Sally Redshaw
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Patent number: 4658024Abstract: Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula ##STR2## R.sup.3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group, R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.Type: GrantFiled: February 1, 1985Date of Patent: April 14, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Michael R. Attwood, Cedric H. Hassall, Robert W. Lambert, Geoffrey Lawton, Sally Redshaw
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Patent number: 4623639Abstract: The present invention provides for peptide derivatives, a process for their manufacture and pharmaceutical preparations containing the same. The invention is also concerned with novel intermediates used in the manufacture of said derivatives.Type: GrantFiled: July 5, 1984Date of Patent: November 18, 1986Assignee: Hoffmann-La Roche Inc.Inventors: Cedric H. Hassall, William H. Johnson, Noel A. Roberts
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Patent number: 4591636Abstract: The invention relates to compounds of the formula ##STR1## wherein R is lower alkyl or a carboxy group or a group of the formula--(CH.sub.2).sub.n --OY ain which n stands for 1 or 2 and Y is hydrogen or alkyl and R.sup.Y and R.sup.z each are hydrogen or one of R.sup.Y and R.sup.z is hydrogen and the other is hydroxy,and pharmaceutically acceptable acid addition salts thereof.These compounds and salts possess antibiotic and antitumor activity and can be used as medicaments in the form of pharmaceutical preparations.Type: GrantFiled: December 17, 1984Date of Patent: May 27, 1986Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Cedric H. Hassall, Gareth J. Thomas
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Patent number: 4526960Abstract: This invention relates to compounds of the formula ##STR1## wherein R is a hydrogen atom, a lower alkyl, aryl or aryl-(lower alkyl) group, a 5-membered or 6-membered heteroaromatic group in which the hetero atom is nitrogen, oxygen or sulphur or a group of the formula ##STR2## wherein R' is a hydroxy, lower alkoxy, amino, lower alkylamino, di-(lower alkyl)amino or arylamino group, n stands for an integer of 1 to 4, n' stands for an integer of 2 to 10, R.sup.1 and R.sup.2 each are a hydrogen atom or one of R.sup.1 and R.sup.2 is a hydrogen atom and the other is a hydroxy, lower alkoxy or benzyloxy group and X is a group of the formula ##STR3## and pharmaceutically acceptable acid addition salts thereof, a process for their manufacture and medicaments containing them. These compounds and salts possess antitumor activity.Type: GrantFiled: September 26, 1983Date of Patent: July 2, 1985Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Cedric H. Hassall, Gareth J. Thomas
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Patent number: 4518784Abstract: There is presented a process for the manufacture of hexahydronaphthacene derivatives of the general formula ##STR1## wherein one of R.sup.1 and R.sup.2 represents a hydrogen atom and the other represents a hydrogen atom or a hydroxy group of R.sup.1 and R.sup.2 together represent a protected oxo group, R.sup.3 represents a hydrogen atom or a hydroxy or acyloxy group and R.sup.4 represents a lower alkyl or esterified carboxy group or a group of the formula ##STR2## wherein R.sup.5 and R.sup.6 together form an oxo group or a protected oxo group and X represents a hydrogen atom or a hydroxy or acyloxy group or ##STR3## in which n stands for 1 or 2 and Y represents a hydrogen atom or an alkyl or acyl group.Also presented are certain of the novel derivatives per se and various novel intermediates in the process.Type: GrantFiled: February 23, 1984Date of Patent: May 21, 1985Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Cedric H. Hassall, Gareth J. Thomas
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Patent number: 4515969Abstract: There is presented a process for the manufacture of hexahydronaphthacene derivatives of the general formula ##STR1## wherein one of R.sup.1 and R.sup.2 represents a hydrogen atom and the other represents a hydrogen atom or a hydroxy group or R.sup.1 and R.sup.2 together represent a protected oxo group, R.sup.3 represents a hydrogen atom or a hydroxy or acyloxy group and R.sup.4 represents a lower alkyl or esterified carboxy group or a group of the formula ##STR2## wherein R.sup.5 and R.sup.6 together form an oxo group or a protected oxo group and X represents a hydrogen atom or a hydroxy or acyloxy group or ##STR3## in which n stands for 1 or 2 and Y represents a hydrogen atom or an alkyl or acyl group.Also presented are certain of the novel derivatives per se and various novel intermediates in the process.Type: GrantFiled: January 23, 1984Date of Patent: May 7, 1985Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Cedric H. Hassall, Gareth J. Thomas
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Patent number: 4512924Abstract: Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylaminoalkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula ##STR2## R.sup.3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group, R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.Type: GrantFiled: May 12, 1983Date of Patent: April 23, 1985Assignee: Hoffmann-La Roche Inc.Inventors: Michael R. Attwood, Cedric H. Hassall, Robert W. Lambert, Geoffrey Lawton, Sally Redshaw
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Patent number: 4487929Abstract: Intermediates of the formula ##STR1## wherein A is methylene, ethylene or propylene which may be substituted by lower alkyl, Y is halogen, R.sup.3 is hydrogen, lower alkyl, aryl or aryl-(lower alkyl)--, R.sup.20 l is lower alkoxy and R.sup.42 is hydrogen, lower alkyl, aryl or aryl-(lower alkyl) or a group of the formula --A--Y in which A and Y are as above, are described.Type: GrantFiled: April 25, 1983Date of Patent: December 11, 1984Assignee: Hoffmann-La Roche, Inc.Inventors: Cedric H. Hassall, Geoffrey Lawton, Christopher J. Moody
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Patent number: 4409391Abstract: There is presented a process for the manufacture of hexahydronaphthacene derivatives of the general formula ##STR1## wherein one of R.sup.1 and R.sup.2 represents a hydrogen atom and the other represents a hydrogen atom or a hydroxy group or R.sup.1 and R.sup.2 together represent a protected oxo group, R.sup.3 represents a hydrogen atom or a hydroxy or acyloxy group and R.sup.4 represents a lower alkyl or esterified carboxy group or a group of the formula ##STR2## wherein R.sup.5 and R.sup.6 together form an oxo group or a protected oxo group and X represents a hydrogen atom or a hydroxy or acyloxy group or--(CH.sub.2).sub.n --OY bin which n stands for 1 or 2 and Y represents a hydrogen atom or an alkyl or acyl group.Also presented are certain of the novel derivatives per se and various novel intermediates in the process.Type: GrantFiled: November 5, 1981Date of Patent: October 11, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Cedric H. Hassall, Gareth J. Thomas
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Patent number: 4399136Abstract: Compounds of the formula ##STR1## wherein A is methylene, ethylene or propylene which may be substituted by lower alkyl, B is carbonyl or methylene, R.sup.1 is halogen, carboxyl, lower alkoxycarbonyl, hydroxyaminocarbonyl, mercapto, lower alkanoylthio or aryl(lower alkylthio)--, R.sup.2 is hydroxy, lower alkoxy or amino, R.sup.3 is hydrogen, lower alkyl, aryl or aryl(lower alkyl)--, R.sup.4 is hydrogen, lower alkyl, aryl, aryl-(lower alkyl)-- or a group of the formula --A-R.sup.1 wherein A and R.sup.1 are as described above and the broken line denotes an optional carbon-carbon bond which can be present only when B is carbonyl,and salts of the acids of formula I with pharmaceutically acceptable bases, a process for the manufacture thereof and pharmaceutical preparations containing same, are described. The compounds of formula I and their salts are useful as antihypertensive agents.Type: GrantFiled: June 10, 1981Date of Patent: August 16, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Cedric H. Hassall, Geoffrey Lawton, Christopher J. Moody
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Patent number: 4393221Abstract: There is presented a process for the manufacture of hexahydronaphthacene derivatives of the general formula ##STR1## wherein one of R.sup.1 and R.sup.2 represents a hydrogen atom and the other represents a hydrogen atom or a hydroxy group or R.sup.1 and R.sup.2 together represent a protected oxo group, R.sup.3 represents a hydrogen atom or a hydroxy or acyloxy group and R.sup.4 represents a lower alkyl or esterified carboxy group or a group of the formula ##STR2## wherein R.sup.5 and R.sup.6 together form an oxo group or a protected oxo group and X represents a hydrogen atom or a hydroxy or acyloxy groupor ##STR3## in which n stands for 1 or 2 and Y represents a hydrogen atom or an alkyl or acyl group.Also presented are certain of the novel derivatives per se and various novel intermediates in the process.Type: GrantFiled: November 4, 1981Date of Patent: July 12, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Cedric H. Hassall, Gareth J. Thomas
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Patent number: 4341781Abstract: The present invention relates to pyridazopyridazine derivatives, a process for the preparation thereof, pharmaceutical preparations containing said derivatives and the use of said derivatives as antihypertensive agents.Type: GrantFiled: September 11, 1980Date of Patent: July 27, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Cedric H. Hassall, Christopher J. Moody
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Patent number: 4316985Abstract: There is presented a process for the manufacture of hexahydronaphthacene derivatives of the general formula ##STR1## wherein one of R.sup.1 and R.sup.2 represents a hydrogen atom and the other represents a hydrogen atom or a hydroxy group or R.sup.1 and R.sup.2 together represent a protected oxo group, R.sup.3 represents a hydrogen atom or a hydroxy or acyloxy group and R.sup.4 represents a lower alkyl or esterified carboxy group or a group of the formula ##STR2## wherein R.sup.5 and R.sup.6 together form an oxo group or a protected oxo group and X represents a hydrogen atom or a hydroxy or acyloxy group or ##STR3## in which n stands for 1 or 2 and Y represents a hydrogen atom or an alkyl or acyl group.Also presented are certain of the novel derivatives per se and various novel intermediates in the process.Type: GrantFiled: January 11, 1980Date of Patent: February 23, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Cedric H. Hassall, Gareth J. Thomas
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Patent number: 4307094Abstract: The present disclosure is directed to 1-substituted or unsubstituted lower alkylene, 5-carboxy, alkanoyloxy or carbamoyloxy triazolopyridazine derivatives, salts of the acids and pharmaceutically-acceptable bases thereof. The triazolopyridazine derivatives provided by the present invention are useful as angiotensin-related antihypertensive agents.Type: GrantFiled: July 17, 1980Date of Patent: December 22, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Cedric H. Hassall, Christopher J. Moody