Patents by Inventor Michael J. Broadhurst
Michael J. Broadhurst 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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Publication number: 20020052513Abstract: Disclosed are compounds of the general formula 1Type: ApplicationFiled: February 8, 2001Publication date: May 2, 2002Inventors: Michael J. Broadhurst, Christopher H. Hill, David N. Hurst, Philip S. Jones, Paul B. Kay, Ian R. Kilford, Robert M. McKinnell
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Patent number: 5614625Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino, carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.Type: GrantFiled: April 5, 1995Date of Patent: March 25, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson
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Patent number: 5447929Abstract: Hydroxamic acid derivatives of the fdrrnula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases, such as, rheumatoid arthritis and ostecarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis, are described. Said compounds can be prepared either by hyclroxamidating a corresponding carboxylic acid or deprotecting a corresponding benzyloxycarbamoyl compound.Type: GrantFiled: March 17, 1994Date of Patent: September 5, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
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Patent number: 5318964Abstract: Hydroxamic acid derivatives of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases, such as, rheumatoid arthritis and osteoarthritis or for the treatment of invasive tumors, atherosclerosis or multiple sclerosis, are described. Said compounds can be prepared either by hydroxamidating a corresponding carboxylic acid or deprotecting a corresponding benzyloxycarbamoyl compound.Type: GrantFiled: May 24, 1993Date of Patent: June 7, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
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Patent number: 5304549Abstract: Compounds of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is hydrogen, amino, protected amino, acylamino or lower alkyl optionally substituted by aryl, hydroxy, protected hydroxy, amino, protected amino, acylamino, maleimido, succinimido, naphthalimido, 2,3-dihydro-1,3-dioxo-1H-benz[d,e]isoquinol-2-yl, carboxy, protected carboxy, carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, carboxy-lower alkanoylamino, pyrrolidino or morpholino; R.sup.2 is hydrogen or lower alkyl optionally substituted by aryl, amino, protected amino, di(lower alkyl)- amino, guanidino, carboxyl, protected carboxyl, carbamoyl, mono(lower alkyl) carbamoyl, di(lower alkyl)carbamoyl, di(lower alkoxy)phosphinyl, dihydroxyphosphinyl, pyrrolidino, piperidino or morpholino; R.sup.3 is hydrogen or lower alkyl optionally substituted by hydroxy, protected hydroxy, amino or protected amino; R.sup.4 is hydrogen, hydroxy, lower alkoxy or benzyloxy; and R.sup.Type: GrantFiled: January 21, 1992Date of Patent: April 19, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
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Patent number: 5006651Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.Type: GrantFiled: September 22, 1989Date of Patent: April 9, 1991Assignee: Hoffman-La Roche Inc.Inventors: Michael J. Broadhurst, Balraj K. Handa, William H. Johnson, Geoffrey Lawton, Peter J. Machin
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Patent number: 4885283Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.Type: GrantFiled: December 1, 1987Date of Patent: December 5, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Balraj K. Handa, William H. Johnson, Geoffrey Lawton, Peter J. Machin
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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: 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: 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: 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: 4302398Abstract: The present invention relates to naphthacene derivatives. More particularly, the invention is concerned with a process for the manufacture of hexahydronaphthacene derivatives and with certain of said derivatives per se. The invention is also concerned with novel intermediates occurring in said process and with the preparation thereof.There are presented hexahydronaphthacene derivatives of the formula ##STR1## wherein R.sup.1 represents a lower alkyl or esterified carboxy group or a group of the formula ##STR2## , in which R.sup.2 and R.sup.3 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 intermediates and a process to produce the compounds of formula I.Type: GrantFiled: August 6, 1980Date of Patent: November 24, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Cedric H. Hassall, Michael J. Broadhurst, Gareth J. Thomas