Darkes; Paul R. - US Patent Attorneys and Agents

Attorney: Darkes; Paul R.

Number of patents: 42
Last date: August 17, 2010

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Number	Title	Issue Date
7777041	2-acylamino-4-phenylthiazole derivatives, preparation thereof and therapeutic application thereof The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): pharmaceutically acceptable acid-addition salts thereof, hydrates or solvates of such derivatives or such pharmaceutically acceptable...	08/17/2010
7759379	Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors The invention relates to compounds of formula (I): in which R1, R2, L1, X, R3, A, R4, R4′, R4″, R4″′, R5, Y and L2 are as herein defined, salts and prodrugs the...	07/20/2010
7667054	Cytotoxic agents comprising new taxanes The invention relates to novel cytotoxic agents comprising taxanes and their therapeutic use as a result of delivering the taxanes to a specific cell population in a targeted fashion by chemically linking the taxane to a cell binding agent. ...	02/23/2010
7632952	Benzothiazoles and the use thereof as medicaments The invention especially relates to novel chemical compounds, especially novel benzothiazole derivatives, to compositions containing said compounds, and to the use thereof as medicaments. ...	12/15/2009
7524887	2-amino-1,3-propanediol compounds for the treatment of acute pain The present invention relates to a method for the prophylaxis or treatment of pain using compounds of formula I, in which R, R2, R3, R4 and R5 have the meanings indicated in the specification. ...	04/28/2009
7504511	2-acylamino-4-phenylthiazole derivatives, preparation thereof and therapeutic application thereof The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): pharmaceutically acceptable acid-addition salts thereof, hydrates or solvates of such derivatives or such pharmaceutically acceptable...	03/17/2009
7462725	Chloromethylation of thiophene The process according to the invention relates to the preparation of 2-chloromethyl-thiophene of the formula (I). During this process thiophene is chloromethylated in the presence of one or more compounds containing keto group and optionally it is transformed into t...	12/09/2008
7442708	1,2,3-substituted indolizine derivatives, inhibitors of fgfs, method for making same and pharmaceutical compositions containing same Compounds of formula I or salts thereof: in which R1 represents —OH, (C1-C5)alkoxy, carboxyl, (C2-C6)alkoxycarbonyl, —NR5R6, —N...	10/28/2008
7435820	Substituted tetrahydro-1-pyrazolo [3,4-]pyridines compositions comprising them, and use Substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines, compositions comprising them and use. The present invention relates in particular to novel substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines having therapeutic activity, which can be used in particular in oncology...	10/14/2008
7381835	Resolution process for (R)-(-)-2-hydroxy-2-(2-chlorophenyl) acetic acid The subject of the present invention is the preparation of the (R)-(−)-2-hydroxy-2-(2-chlorophenyl)acetic acid of the formula (I) by the resolution of the corresponding racemic compound by using the compounds of the general formula (II). ...	06/03/2008
7354933	Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use...	04/08/2008
7322352	Inhaler Provided herein are dry powder inhalers for the delivery of metered doses of medicament, counters associated with the inhalers for counting and displaying the number of doses administered or remaining within the inhaler, and methods of use thereof. ...	01/29/2008
7241907	Acetone solvate of dimethoxy docetaxel and its process of preparation This invention discloses and claims an acetone solvate of dimethoxydocetaxel or 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-7β,10β-dimethoxy-9-oxotax-11-en-13α-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and its preparation by crystalli...	07/10/2007
7214212	Cap for injection devices The present invention concerns a cap suitable for injection devices having an exchangeable needle assembly, which serves as a mounting/demounting tool of the said needle assembly. ...	05/08/2007
7179816	Chemical derivatives and their application as antitelomerase agents The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which inhibits telomerase. It also relates to novel chemical compounds as well as their therapeutic application in humans. ...	02/20/2007
7160895	Use of pyridoindolone derivatives for the preparation of medicinal products The invention relates to a novel use of compounds of formula: for the preparation of medicinal products that are useful as anticancer agents. ...	01/09/2007
7025205	Method and packaging for pressurized containers A method for maintaining the enclosed volume of a sealed package at about ambient pressure, wherein the package contains a pressurized container comprising a drug, and an HFA (hydrofluoroalkane) propellant selected from the group consisting of HFA 134a and HFA p227,...	04/11/2006
6916838	1-benzylpyrazole-3-carboxylic acid tricyclic derivatives as cannabinoid receptor antagonists Tricyclic derivatives of 1-benzylpyrazole-3-carboxylic acid which are antagonists of the cannabinoid CB2 receptors; their method of preparation and pharmaceutical compositions containing them. ...	07/12/2005
6884895	Process for the preparation of spiro[(4-cyclohexanone)-[3]indol]-2′[1′H]-one derivatives The invention relates to a process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives of the general formula I wherein R1 and R2 independently stand for hydrogen...	04/26/2005
6716853	Cyclic N-substituted alpha-imino carboxylic acids for selective inhibition of collogenase The invention is related to compounds of formula I to pharmaceutical compositions comprising such compounds, to processes for the preparation of such compounds, and to methods of prevention and treatment of disorders, th...	04/06/2004
6559313	Compounds having antihypertensive, cardioprotective anti-ischemic and antilipolytic properties This invention is directed to intermediates of the formula ##STR1## wherein Z is 4-trifluoromethylpyridin-2-yl or 5-trifluoromethylpyridin-2-yl which are useful in the preparation of compounds useful as antihypertensive, anti-ischemic, cardioprotective, a...	05/06/2003
6291446	Therapeutic treatment for cytomegalovirus infection A method for treating CMV infection and disease conditions associated therewith is disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N,N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bis -(3,3'-indolyl)]-1(H)-pyrr...	09/18/2001
6288053	Use of protein kinase C inhibitors to enhance the clinical efficacy of radiation therapy A method for treating neoplasms is disclosed, particularly using the ଲ-isozyme selective PKC inhibitor, (S)-3,4-[N,N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N -dimethylamino)butane)-bis-(3,3'-indolyl)]-1(H)-pyrrole-2,5-dione or one of its salts, such ...	09/11/2001
6284751	Therapeutic treatment for VEGF related diseases A method for inhibiting VEGF stimulated endothelial cell growth, such as associated with neoplasia, and VEGF stimulated capillary permeability, such as associated with pulmonary edema are disclosed, particularly using the ଲ-isozyme selective PKC inh...	09/04/2001
6225301	Therapeutic treatment for renal dysfunction A method for treating renal dysfunctions is disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N, N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bis-(3,3'-indo lyl) ]-1(H)-pyrrole-2,5-dionehydrochloridesalt....	05/01/2001
6133452	Synthesis of bisindolylmalimides The present invention provides for the reaction of optionally substituted indole-3-acetamides with optionally substituted methyl indole-3-glyoxyl reagent to prepare potent PKC inhibitors. The reaction is very efficient and robust macrocyclization methodol...	10/17/2000
6107327	Therapeutic treatment for HIV infection A method for treating HIV infection is disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N, N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bis-(3,3'-indo lyl)]-1(H)-pyrrole-2,5-dione or its acid salt....	08/22/2000
6103713	Therapeutic treatment for autoimmune diseases Methods for inhibiting activation and/or proliferation of T cells and B cells and for treating autoimmune diseases and/or disease manifestations are disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N, N'-1,1'-((2"-ethoxy)-3...	08/15/2000
6103712	Therapeutic treatment for asthma A method for treating asthma and disease conditions associated therewith is disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N,N'-1,1'-((2"-ethoxy)-3'"-(O)-4'"-(N,N-dimethylamino)-butane)-bi s-(3,3'-indoly1)]-1 (H)-pyrrole-2,5-di...	08/15/2000
6093709	Therapeutic treatment for sexual dysfunctions A method for treating sexual dysfunctions is disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N,N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bis -(3,3'-indoly1)]-1(H)-pyrrole-2,5-dione, particularly its hydrochlori...	07/25/2000
6093740	Therapeutic treatment for skin disorders A method for reducing or inhibiting vascular permeability especially the increased vascular permeability associated with VPF/VEGF, and dermal edema exhibited with bullous phemigoid, erythema multiforme, dermatitis herpetiformis, contact dermatitis/delayed...	07/25/2000
6069247	Process for preparing substituted acrylamides by reaction of propiolamides and aromatic rings The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides....	05/30/2000
6015807	Protein kinase C inhibitor This invention provides novel bis-indolylmaleimide macrocycle derivatives of the formula: and solvates thereof. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals....	01/18/2000
5990319	Synthesis of bisindolylmaleimides The present invention provides for the reaction of optionally substituted indole-3-acetamides with optionally substituted methyl indole-3-glyoxyl reagent to prepare potent PKC inhibitors. The reaction is a very efficient and robust macrocyclization method...	11/23/1999
5962446	Therapetutic treatment for human T cell lymphotrophic virus type 1 infection A method for treating human T cell lymphotrophic virus type 1 infection using an isozyme selective PKC inhibitor, particularly using the isozyme selective PKC inhibitor, (S)-3,4-N,N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bis -(3,3...	10/05/1999
5948907	Synthesis of bisindolylmaleimides The present invention provides for the reaction of optionally substituted indole-3-acetamides with optionally substituted methyl indole-3-glyoxyl reagent to prepare potent PKC inhibitors....	09/07/1999
5843942	Aromatic amino ethers as pain relieving agents The present invention relates to compounds of formula (I), ##STR1## wherein A is an optionally substituted phenyl naphthyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidyl, thienyl, thiazolyl, oxazolyl, thiadiazolyl having at least two adjacent ring carbo...	12/01/1998
5834468	Substituted aryl and heteroaryl compounds as E-type prostaglandin antagonists This invention relates to substituted and unsubstituted (aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of ...	11/10/1998
5811459	Ortho substituted aromatic compounds useful as antagonists of the pain enhancing effects of E-type prostaglandins The invention relates to compounds of the formula (I): ##STR1## wherein A, B and D are various ring systems such as phenyl, R1 includes carboxy, R3 is hydrogen or C1-4 alkyl and Z is a linking group such as --(CH(R	09/22/1998
5807897	Aminotetralin derivative and compositions and method of use thereof The invention relates to aminotetralin derivatives of the formula I: ##STR1## wherein: R1 is methyl or ethyl; R2 is hydrogen, halogen, lower-alkoxy or thiolower-alkyl; R3 is hydrogen, halogen, lower-alkoxy or lower-al...	09/15/1998

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Attorney: Darkes; Paul R.