Patents Assigned to Merckle GmbH
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Patent number: 8034837Abstract: The present invention relates to a new crystalline modification of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,S-dihydro-1H-pyrrolizin-S-ylacetic acid which is referred to as polymorph B. It has a peak in the solid state 13C-NMR spectrum (with adamantane as external reference standard; CH group d=29.45 ppm) in the range from 179.8 to 180.2 ppm and can be processed directly to a pharmaceutical formulation.Type: GrantFiled: March 20, 2006Date of Patent: October 11, 2011Assignee: Merckle GmbHInventors: Wolfgang Albrecht, Thomas Kammermeier, Hans-Gunter Striegel, Philipp Merckle, Stefan Laufer
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Publication number: 20100099730Abstract: The present invention relates to the use of annellated pyrrole compounds and in particular ML3000 (licofelone), salts or derivatives thereof, for cancer management, and in general to the use of a compound of Formula (I): wherein the variables have the meanings given in the present description, for the prevention and/or treatment of neoplasia, in particular neoplasia selected from the group consisting of papilloma, carcinoma, adenoma and adenocarcinoma, e.g. human airway or colorectal carcinoma, preferably fast-growing, multidrug resistant and/or COX-2 negative neoplasia. The invention further relates to pharmaceutical compositions for the aforesaid purposes, comprising annellated pyrrole compounds and in particular ML3000 (licofelone), optical isomers, salts or derivatives thereof, as well as to a method of treating and/or preventing neoplasia and/or restoring the ability to undergo apoptosis in a cell having lost the same.Type: ApplicationFiled: July 30, 2007Publication date: April 22, 2010Applicant: MERCKLE GMBHInventors: Stefan Laufer, Tiziana Guarnieri, Simona Tavolari, Vittorio Tomasi, Ernesto Palazzini, Miriam Barbanti
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Patent number: 7608633Abstract: The invention relates to novel heteroaryl substituted acetone derivatives which inhibit the enzyme phospholipase A2, pharmaceutical preparations containing these compounds and a method of producing these compounds.Type: GrantFiled: February 6, 2004Date of Patent: October 27, 2009Assignee: Merckle GmbHInventors: Matthias Lehr, Joachim Ludwig
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Publication number: 20090221697Abstract: The present invention relates to macrolide conjugates of pyrrolizine and indolizine derivatives with macrocyclic antibiotics and derivatives thereof. The macrolide conjugates are potent inhibitors of 5-lipoxygenase and cyclooxygenase and are therefore suitable to treat disorders of the rheumatic type and to prevent allergically induced diseases. The macrolide conjugates have significantly enhanced potency and efficacy.Type: ApplicationFiled: July 26, 2006Publication date: September 3, 2009Applicant: MERCKLE GMBHInventors: Stefan Laufer, Wolfgang Albrecht, Michael Burnet, Hans-Jürgen Gutke
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Publication number: 20090105327Abstract: The present invention relates to compounds of the formula I in which R1, R2, R3, R4, X and Y have the meanings indicated in the description. These compounds have immunomodulating effects, as well as an inhibiting or regulating effect on the release of IL-1? and/or TNF-?. They can therefore be used for the treatment of diseases associated with a disturbance of the immune system.Type: ApplicationFiled: May 12, 2006Publication date: April 23, 2009Applicant: Merckle GMBHInventors: Stefan Laufer, Wolfgang Albrecht, Cornelia Greim, Hans-Guenter Striegel, Karola Tollmann
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Patent number: 7442713Abstract: The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R1, R2, R3, R4 and p are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.Type: GrantFiled: May 16, 2003Date of Patent: October 28, 2008Assignee: Merckle GmbHInventors: Stefan Laufer, Hans-Guenter Striegel, Wolfgang Albrecht, Karola Tollmann
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Patent number: 7425573Abstract: Treating or preventing degeneration or destruction of articular cartilage and/or subchondral bone in the affected joint of a mammal is accomplished by administering a compound of formula (I), wherein the variables have the meanings given in the present description. A preferred compound of formula (I) is formula (II).Type: GrantFiled: August 29, 2002Date of Patent: September 16, 2008Assignees: Merckle GmbH, Ascentia Pharma Inc.Inventors: Jean-Pierre Pelletier, Johanne Martel-Pelletier
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Patent number: 7271154Abstract: This invention features a compound of the following formula: wherein T is a transportophore, L is a bond or linker, and C is an antibiotic therapeutic agent, the transportophore is covalently bonded to the antibiotic therapeutic agent via the bond or the linker, and the transportophore is an azithromycin derivative or crown ether derivative.Type: GrantFiled: February 14, 2003Date of Patent: September 18, 2007Assignee: Merckle GmbHInventors: Michael Burnet, Jan-Hinrich Guse, Gene Kim
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Patent number: 7253191Abstract: The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R1, R2, R3 and R4 are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.Type: GrantFiled: February 19, 2002Date of Patent: August 7, 2007Assignee: Merckle GmbHInventors: Stefan Laufer, Dunja Kotschenreuther, Philipp Merckle, Karola Tollmann, Hans-Guenter Striegel
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Publication number: 20060235054Abstract: The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R1, R2 R3 and m are as defined in the description. The compounds according to the invention have immunomodulating and/or cytokine-release-inhibiting action and are therefore suitable for treating disorders associated with a disturbed immune system.Type: ApplicationFiled: August 20, 2003Publication date: October 19, 2006Applicant: MERCKLE-GMBHInventors: Stefan Laufer, Hans-Gunter Striegel, Karola Tollmann, Wolfgang Albrecht
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Patent number: 7078535Abstract: The invention relates to a process for the preparation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-ylacetic acid, in which 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole is reacted with ?-bromo-4-chloroacetophenone with formation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizine and the acetic acid group is introduced into the 5-position, 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole being obtained by hydrogenation of 2,2-dimethyl-4-oxo-5-phenylvaleronitrile or a ketal thereof. The invention also relates to processes for the preparation of intermediates occurring in the above process.Type: GrantFiled: August 21, 2002Date of Patent: July 18, 2006Assignee: Merckle GmbHInventors: Gerd Dannhardt, Thomas Kammermeier, Philipp Merckle, Hans-Günter Striegel, Stefan Laufer
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Publication number: 20060142366Abstract: The invention relates to novel heteroaryl substituted acetone derivatives which inhibit the enzyme phospholipase A2, pharmaceutical preparations containing these compounds and a method of producing these compounds.Type: ApplicationFiled: February 6, 2004Publication date: June 29, 2006Applicant: MERCKLE GMBHInventors: Matthias Lehr, Joachim Ludwig
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Publication number: 20060128759Abstract: The invention relates to substituted isoxazole derivatives of formula (I), wherein the radicals R1, R2 and R3 have the meanings as cited in the description.Type: ApplicationFiled: August 19, 2003Publication date: June 15, 2006Applicant: MERCKLE GMBHInventors: Stefan Laufer, Hans-Gunter Striegel, Wolfgang Albrecht, Karola Tollmann
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Publication number: 20060040945Abstract: Inhibiting gastric proton pump in a mammal is accomplished by the use of a compound of formula (1) wherein the variables have the meaning given in the present description. A preferred compound of formula (2) is this treatment ameliorates, diminishes, actively treats, reverses or prevents any injury, damage or lesions of gastric mucosa, e.g. gastric mucosal lesions and ulceration.Type: ApplicationFiled: May 16, 2003Publication date: February 23, 2006Applicant: MERCKLE GMBHInventors: Adams Smolka, Charles Hammond, Sandeep Gupta
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Patent number: 6936632Abstract: The present invention relates to fused pyrrole compounds of the formula 1. in which at least one of the radicals R1, R2, R3 is 4-sulphur-substituted phenyl. These compounds are in particular pyrrolizines, indolizines and heteroanalogues having selective inhibitory action on isoenzyme-2 of prostaglandin H synthase (COX-2). The invention also relates to pharmaceutical compositions which contain these compounds; and the use of these compounds for the treatment of disorders of the rheumatic type.Type: GrantFiled: January 12, 2001Date of Patent: August 30, 2005Assignee: Merckle GmbHInventors: Hans-Guenter Striegel, Stefan Laufer, Karola Tollmann, Susanne Tries
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Patent number: 6930094Abstract: The present invention relates to the use of tissue factor for influencing blood vessel formation, particularly for activating blood vessel formation, above all for wound healing.Type: GrantFiled: May 8, 1998Date of Patent: August 16, 2005Assignee: Merckle GmbHInventors: Peter Nawroth, Katsumi Nakagawa, Youming Zhang
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Patent number: 6878738Abstract: The present invention relates to compounds of the formula I in which one of the radicals R8 and R9 is a hydrogen atom or an alkyl group and the other is hydroxyl, alkoxy or acyloxy or where R8 and R9, together with the carbon atom to which they are bonded, are a carbonyl group and the radicals R1 to R7 have the meanings indicated in the description. The compounds inhibit the release of various mediators of the arachidonic acid cascade and can thus be used for the prevention of allergically induced disorders or for the treatment of disorders of the rheumatic type.Type: GrantFiled: November 23, 1999Date of Patent: April 12, 2005Assignee: Merckle GmbHInventors: Stefan Laufer, Karola Tollmann, Hans-Guenter Striegel
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Patent number: 6867211Abstract: The present invention relates to 4-pyridyl- and 2,4-pyrimidinyl-substituted pyrrole derivatives and their use in pharmacy, of the formula 1: in which the variables have the meanings indicated in the description. The compounds according to the invention have immunomodulating and/or cytokine release-inhibiting action and are therefore utilizable for the treatment of disorders which are connected with a disturbance of the immune system.Type: GrantFiled: January 31, 2001Date of Patent: March 15, 2005Assignee: Merckle GmbHInventors: Hans-Guenter Striegel, Stefan Laufer, Karola Tollmann, Susanne Tries
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Patent number: 6627200Abstract: The invention relates to the utilization of monocytes growth factor CD137 or of a functional analogue thereof in order to produce a medicament for promoting the proliferation of peripheral monocytes of a mammal. The invention especially relates to the utilization of the growth factor for treating pathological conditions.Type: GrantFiled: November 30, 2000Date of Patent: September 30, 2003Assignee: Merckle GmbHInventors: Herbert Schwarz, Joachim Langstein
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Patent number: 6544775Abstract: The invention relates to a device and to a process for the automatic synthesis of macromolecules on a tape-like substrate material (11). The device has at least one synthesis module (12) which can be sealed from the outside and comprises reaction chambers (15) and fluid lines (18, 19) for filling and emptying the reaction chambers (15) with and of reaction media, it being possible to introduce the substrate material (11) into the synthesis module (12) and bring it into contact with the reaction chambers (15). Transport means (20-26) which are intended to move the substrate material (11) through a particular distance and can be actuated by a control device are furthermore provided. The invention also relates to the use of such a device for the synthesis of oligonucleotides bound on a functionalized substrate material, in particular the production of oligonucleotide libraries.Type: GrantFiled: November 8, 1999Date of Patent: April 8, 2003Assignee: Merckle GmbHInventors: Hermann Brugger, Christian Rembe, Raoul Bader, Eberhard P. Hofer, Hartmut Seliger