Abstract: The present invention relates to a parenteral composition comprising a bisphosphonic acid or a pharmaceutically acceptable salt thereof (bisphosphonate) as active component and a pharmaceutically acceptable chelating agent, processes of the preparation of this composition, and methods of their use in the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, hypercalcemia of malignancy, and metabolic bone disease. The compositions are especially useful for improving the local tolerance of the active component when administered parenterally.
Type:
Grant
Filed:
January 11, 2001
Date of Patent:
January 13, 2004
Assignee:
Hoffmann-La Roches Inc.
Inventors:
Anke Diederich, Pierre Goldbach, Thomas Pfister
Abstract: Piperidine derivatives, their manufacture and use as medicaments is described. The compounds are useful for treating diseases associated with restenosis, glaucoma, cardiac infarct, high blood pressure and end organ damage, e.g. cardiac insufficiency and kidney insufficiency.
Type:
Grant
Filed:
December 18, 2001
Date of Patent:
January 6, 2004
Assignee:
Hoffman-La Roche Inc.
Inventors:
Volker Breu, Hans-Peter Märki, Eric Vieira, Wolfgang Wostl
Abstract: The present invention is a pyrimidine, triazine or pyrazine derivative of the formula
or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, X, Y and Z are as defined in the specification. The invention is a pharmaceutical composition containing an effective amount of the compound of formula 1, its preparation and to a method of treatment, control or prevention of acute and/or chronic neurological disorders by administering a therapeutically effective amount of a compound of formula 1.
Type:
Grant
Filed:
May 29, 2002
Date of Patent:
January 6, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Alfred Binggeli, Hans-Peter Maerki, Thierry Masquelin, Vincent Mutel, Maurice Wilhelm, Wolfgang Wostl
Abstract: Disclosed are pyridine amido derivatives of the formula
wherein X, Y, and R1 to R6 are as defined herein. These compounds are selective MAO-B inhibitors and are useful in treating diseases such as, for example, Alzheimer's and senile dementia. Also disclosed are pharmaceutical compositions containing such compounds and a method of preparing such compounds.
Type:
Grant
Filed:
January 14, 2003
Date of Patent:
December 23, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
Abstract: Ready-to-use, aqueous injection solutions containing carvedilol (1-(9H-carbazolyl-4-yloxy)-3-[[(2-(2-methoxyphenoxy)ethyl]-amino]-2-propanol) or its pharmacologically harmless salts which are stable in storage and are well tolerated by veins are disclosed.
Abstract: This invention relates to phthalimido derivatives of the formula
wherein X is —N═ or —CH═, and R1 to R4 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to pharmaceutical compositions containing these compounds, a method of treating a disease by administering a therapeutically effective amount of at least one of these compounds, and a process for their preparation for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.
Type:
Grant
Filed:
March 13, 2003
Date of Patent:
December 9, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
Abstract: The present invention relates to compounds of the general formula
wherein
R1 is C6-10-cycloalkyl, optionally substituted by lower alkyl or —C(O)O-lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.
Type:
Grant
Filed:
June 11, 1999
Date of Patent:
November 4, 2003
Assignee:
Hoffman-La Roche Inc.
Inventors:
Geo Adam, Andrea Cesura, François Jenck, Sabine Kolczewski, Stephan Röver, Jürgen Wichmann
Abstract: The invention relates to compounds of the formula
wherein R1 is optionally substituted phenyl, morpholinyl, piperazinyl, pyrrolidinyl, piperidinyl or is thiomorpholinyl, 1-oxo-thiomorpholinyl or 1,1-dioxothiomorpholinyl. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable in the control or treatment of diseases, related to this receptor.
Type:
Grant
Filed:
January 25, 2002
Date of Patent:
November 4, 2003
Assignee:
Hoffman-La Roche Inc.
Inventors:
Sabine Kolczewski, Stephan Roever, Patrick Schnider
Abstract: Antibody binding to the SEMP1 antigen and characterized in that said antibody binds to SEMP1 in a manner equivalent to an antibody selected from the group of antibodies DSM ACC2458, DSM ACC2459, DSM ACC2461, and DSM ACC2463 is useful for cancer diagnosis and therapy.
Type:
Grant
Filed:
June 21, 2001
Date of Patent:
September 30, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Thorsten Hoevel, Stefan Koch, Manfred Kubbies, Olaf Mundigl, Petra Rueger
Abstract: The invention relates to a solid pharmaceutical form of administration containing a diphosphonic acid or a physiologically compatible salt thereof as the active substance, wherein the active substance is present in granulate form, optionally together with pharmaceutical adjuvants in the inner phase, and the outer phase contains a lubricant in the form of less than 5% by weight of stearic acid relative to the total weight of the form of administration.
Type:
Grant
Filed:
July 20, 2001
Date of Patent:
September 30, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Rolf-Dieter Gabel, Walter Preis, Heinrich Woog
Abstract: The present invention relates to compounds of the formula
wherein R1 and R2 are as defined herewithin. The compounds of formula I have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they are therefore useful in the treatment of diseases, related to this receptor.
Type:
Grant
Filed:
November 15, 2002
Date of Patent:
September 23, 2003
Assignee:
Hoffman-La Roche Inc.
Inventors:
Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
Abstract: The present invention relates to compounds of the formula
wherein R1, A and R are as described within. The compounds of the present invention have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have an affinity to the A2A-receptor and are therefore useful in the treatment of diseases related to this receptor.
Type:
Grant
Filed:
November 5, 2002
Date of Patent:
September 16, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
Abstract: The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity
Type:
Grant
Filed:
December 11, 2002
Date of Patent:
September 9, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Norman Kong, Emily Aijun Liu, Binh Thanh Vu
Abstract: Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.
Type:
Grant
Filed:
December 20, 2001
Date of Patent:
August 26, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
Abstract: The present invention relates to a new process for the preparation of compounds of the formulae
and their pharmaceutically acceptable acid addition salts, which are NMDA (N-methyl-D-aspartate)-receptor-subtype selective blockers.
Type:
Grant
Filed:
March 15, 2001
Date of Patent:
August 12, 2003
Assignee:
Hoffman-La Roche Inc.
Inventors:
Yvo Crameri, Michelangelo Scalone, Pius Waldmeier, Ulrich Widmer
Abstract: New compounds containing bicyclic fused rings, one of which being a phenyl moiety connected by an aliphatic chain to a cycloalkyl or aryl moiety, and pharmaceutically active salts thereof are useful as RAR selective retinoid agonists. Furthermore, such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, are useful for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumors and precancerous changes of the mucous membrane in the mouth, tongue, larynx, esophagus, bladder, cervix and colon.
Type:
Grant
Filed:
April 23, 2001
Date of Patent:
August 5, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Paula Nanette Belloni, Synese Jolidon, Michael Klaus, Jean-Marc Lapierre
Abstract: The present invention relates to compounds of the formula
wherein R is as defined herewithin. The compounds of formula I have a good affinity to the A2A receptor and therefore they may be used in the control or prevention of illnesses based on the modulation of the adenosine system, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or against asthma, allergic responses, hypoxia, ischaemia, seizure and substance abuse. Furthermore, compounds of the present invention may be useful as sedatives, muscle relaxants, antipsychotics, antiepileptics, aniticonvulsants and cardiaprotective agents for disorders such as coronary artery disease and heart failure.
Type:
Grant
Filed:
November 5, 2002
Date of Patent:
July 29, 2003
Assignee:
Hoffman-La Roche Inc.
Inventors:
Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
Abstract: A method and a needleless injection system for administering a medication. In order to simplify as far as possible the handling necessary for loading the injector with medication and thereby eliminate risks caused by a complex handling the method and system according to the invention provide loading of medication into a needleless injector device by means of a syringe prefilled with a medication, this loading step preferably including connecting the syringe to the injector device by means of a suitable coupling member or adapter and operating the syringe for transferring medication prefilled therein into the injector device. After this transfer the syringe and/or the coupling member or adapter are detached from the injector device, which is then ready to be operated for ejecting the loaded dosage of said medication from the injector device and thereby pass the selected dosage through the skin of an injection receiver.
Abstract: The present invention is a series of novel compounds of formula I and a method of treatment or prevention of a mGluR5 receptor mediated disease by administering an therapeutically effective amount of a compound formula
wherein R1 and R2 are selected from hydrogen, (C1-6)-alkyl, halogen, hydroxy, (C1-6)-alkoxy and A is defined the description, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 8, 2002
Date of Patent:
July 22, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann