The Substituent Nitrogen Is An Amino Nitrogen Attached Indirectly To A Ring By Acyclic Nonionic Bonding Patents (Class 564/164)
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Patent number: 7268147Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: May 6, 2004Date of Patent: September 11, 2007Assignee: Pfizer IncInventors: Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite
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Patent number: 7265220Abstract: Compound of formula (I): wherein: R1 represents aryl, heteroaryl or alkyl which is optionally substituted, or a group of formula —(CO)—CR6R7NR8R9 wherein R6, R7, R8 and R9 are as defined in the description, R2 represents hydrogen or alkyl, R3 represents hydrogen or optionally substituted alkyl, R4 represents a saturated or unsaturated, 7- to 15-membered bicyclic system or optionally substituted alkyl, or R3 and R4, together with the carbon atom carrying them, form a saturated or unsaturated, 3- to 18-membered, mono-, bi- or tri-cyclic system optionally containing one or more hetero atoms selected from O, S and N and optionally substituted, n represents 1 or 2, Ar represents aryl or heteroaryl, R5 represents amino, guanidino, cyano or amidino which is optionally substituted, its optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in pathological conditions involving activated protein C.Type: GrantFiled: February 17, 2003Date of Patent: September 4, 2007Assignee: Les Laboratories ServierInventors: Guillaume De Nanteuil, Philippe Gloanec, Tony Verbeuren, Alain Rupin
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Patent number: 7247748Abstract: Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein.Type: GrantFiled: March 26, 2003Date of Patent: July 24, 2007Assignee: SmithKline CorporationInventors: Scott K. Thompson, James S. Frazee, Lara S. Kallander, Chun Ma, Joseph P. Marino, Michael J. Neeb, Ning Wang
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Patent number: 7244866Abstract: This invention is directed to carboxamido opioid compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder.Type: GrantFiled: May 11, 2005Date of Patent: July 17, 2007Assignee: Janssen Pharmaceutical N.V.Inventors: John R. Carson, Philip M. Pitis
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Patent number: 7227038Abstract: The invention provides compounds of formula in which m, n, R1, R2, R3, R4, and R5, have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: February 19, 2004Date of Patent: June 5, 2007Assignee: AstraZeneca ABInventors: Moya Caffrey, Rhonan Ford, Austen Pimm
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Patent number: 7151195Abstract: The present invention relates to a phthalamide derivative represented by the general formula (I): wherein R1, R2, R3, X, Y, m, and n are as defined in the disclosure, which can be used as the active ingredient in an agricultural or horticultural insecticide that exhibits an excellent insecticidal effect even when used in a small active-ingredient amount.Type: GrantFiled: May 1, 2003Date of Patent: December 19, 2006Assignee: Bayer CropScience LPInventors: Yoshihiro Matsuzaki, Masayuki Morimoto, Shinsuke Fujioka, Masanori Tohnishi
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Patent number: 7144881Abstract: The present invention provides novel arylcyclopropylcarboxylic amides and related derivatives having the general Formula I wherein R, R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said arylcyclopropylcarboxylic amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.Type: GrantFiled: November 21, 2003Date of Patent: December 5, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Alexandre L'Heureux, Li-Qiang Sun
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Patent number: 7132455Abstract: This invention relates to novel phthalamide derivatives of formula (I) wherein R1, R2, R3, R4, and R5 have the meanings given in the disclosure, to processes for their preparation, and to their use as insecticidal agents in agricultural and horticultural field.Type: GrantFiled: June 11, 2003Date of Patent: November 7, 2006Assignee: Bayer Cropscience AGInventors: Katsuaki Wada, Takuya Gomibuchi, Yasushi Yoneta, Yuichi Otsu, Katsuhiko Shibuya, Hanako Okuya, Rüdiger Fischer
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Patent number: 7132457Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy. In formula (I) D represents CH2 or CH2CH2, E represents C(O)NH or NHC(O) and R3 represents a group of formula (I).Type: GrantFiled: March 31, 2004Date of Patent: November 7, 2006Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
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Patent number: 7053211Abstract: The invention relates to a process for the preparation of ?-aminosubstituted carboxylic acid amide compounds and/or their salts comprising reacting a carboxylic acid amide of a primary amine with a nitrosylating agent in the presence of a base followed by hydrolysis to give a hydroxy imino derivative followed by hydrogenation and if necessary converting a base or acid of the ?-aminosubstituted carboxylic acid amide into one of its salts.Type: GrantFiled: December 11, 2001Date of Patent: May 30, 2006Assignee: Merck Patent GmbHInventors: Thorsten Hartig, Steffen Enke
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Patent number: 7049271Abstract: The present invention relates to novel phenyl-substituted 2-enamino-ketonitriles of the formula (I): in which Ar, X, Z, Y and K are each as defined in the description, to a plurality of processes for their preparation and to their use as herbicides and pesticides.Type: GrantFiled: April 25, 2001Date of Patent: May 23, 2006Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Jutta Böhmer, Ralf Wischnat, Mark Wilhelm Drewes, Peter Dahmen, Rolf Pontzen, Peter Lösel, Christoph Erdelen, Dieter Feucht
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Patent number: 7041844Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.Type: GrantFiled: November 18, 2002Date of Patent: May 9, 2006Assignee: The University Of Tennessee Research CorporationInventors: Duane D. Miller, Leonid I. Kirkovsky, James T. Dalton, Arnab Mukherjee
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Patent number: 7038085Abstract: The present invention relates generally to the enantiomers of para-hydroxy-milnacipran or congeners thereof. Biological assays revealed that racemic para-hydroxy-milnacipran is approximately equipotent in inhibiting serotonin and norepinephrine uptake (IC50=28.6 nM for norepinephrine, IC50=21.7 nM for serotonin). Interestingly, (+)-para-hydroxy-milnacipran is a more potent inhibitor of norepinephrine uptake than serotonin uptake (IC50=10.3 nM for norepinephrine, IC50=22 nM for serotonin). In contrast, (?)-para-hydroxy-milnacipran is a more potent inhibitor of serotonin uptake compared to norepinephrin uptake (IC50=88.5 nM for norepinephrine, IC50=40.3 nM for serotonin). The invention also relates to salts and prodrug forms of the aforementioned compounds. In certain embodiments, the compounds of the present invention and a pharmaceutically acceptable excipient are combined to prepare a formulation for administration to a patient.Type: GrantFiled: October 22, 2003Date of Patent: May 2, 2006Assignee: Collegium Pharmaceutical, Inc.Inventors: Roman V. Rariy, Michael Heffernan, Stephen L. Buchwald, Timothy M. Swager
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Patent number: 7005546Abstract: A group of benzamide compounds are disclosed which are useful for treating neurodegenerative disorders. Methods for making these compounds are provided. These materials are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from conditions such as Parkinson's disease which can exhibit themselves as progressive loss of central nervous system function. The compounds can arrest or slow the progressive loss of function.Type: GrantFiled: June 22, 2004Date of Patent: February 28, 2006Assignee: Renovis, Inc.Inventors: William Flitter, William Garland, Richard Paylor, Allan Wilcox
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Patent number: 6995269Abstract: Compounds of formula IIA and IIB are novel guanidine compounds where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.Type: GrantFiled: March 4, 2003Date of Patent: February 7, 2006Assignee: Chiron CorporationInventors: Paul A. Renhowe, Daniel Chu, Rustum S. Boyce, David Duhl
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Patent number: 6995284Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: October 22, 2002Date of Patent: February 7, 2006Assignee: The University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Yali He, Donghua Yin
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Patent number: 6949658Abstract: The present invention provides a process for efficiently producing an optically active ?-amino acid and an optically active ?-amino acid amide. After contacting with cells or processed cells thereof having an ability to asymmetrically hydrolyse, a water solvent is substituted with at least one solvent selected from the group consisting of linear, branched, or cyclic alcohol having 3 or more carbon atoms and the optically active ?-amino acid is preferentially precipitated from the alcohol solution. The addition of basic compounds, particularly potassium compounds to the alcohol solution containing the optically active ?-amino acid amide, which is obtained after the separation of the optically active ?-amino acid, enables the purification of the amide without the inclusion of amino acid into amino acid amide. Thus, the amide is subjected to the step of racemization and then recycled.Type: GrantFiled: May 18, 2001Date of Patent: September 27, 2005Assignee: Mitsubishi Rayon Co., Ltd.Inventors: Osamu Katoh, Toshitaka Uragaki, Tetsuji Nakamura
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Patent number: 6946489Abstract: The invention relates to compounds of the formula I in which R1, R2, R3, R4 and X have the meaning indicated in the text. The compounds act as inhibitors of factors Xa and VIIa and can therefore be employed for the control and prevention of thromboembolic conditions such as thrombosis, myocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.Type: GrantFiled: March 23, 2001Date of Patent: September 20, 2005Assignee: Merck Patent GmbHInventors: Horst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Bames, Johannes Gleitz
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Patent number: 6924391Abstract: Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula wherein X, Z, X1, R1, R2, Ra, Rb, R3, R4 and Y are as defined in the specification.Type: GrantFiled: May 3, 2001Date of Patent: August 2, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Jacques Banville, Roger Remillard, Neelakantan Balasubramanian, Gilles Bouthillier, Alain Martel
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Patent number: 6921774Abstract: The invention provides novel compounds of the formula I below: wherein the meaning of each substituent is defined in the application. The compounds are useful as inhibitors of the glycine transporter and useful in the treatment of diseases responsive to the inhibition of the glycine transporter. The invention provides a pharmaceutical composition comprising a compound of Formula I as defined above and the use of compounds as above for the manufacture of medicaments for treatment of diseases responsive to ligands of the glycine transporter.Type: GrantFiled: January 17, 2003Date of Patent: July 26, 2005Assignee: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Paul Garrick Smith, Christian Krog-Jensen, Klaus Peter Bøgesø
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Patent number: 6916957Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: December 13, 2000Date of Patent: July 12, 2005Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
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Patent number: 6846955Abstract: The invention relates to a process for racemising an enantiomer-enriched Schiff base of a primary amino acid amide with a strong base that is chemically reactive towards water. The reaction is conducted in an organic solvent. Preferably a metal alkoxide, a metal alkyl, a metal amide, or a metal hydride, in particular a metal alkoxide is applied as the strong base. As the Schiff base preferably N-benzylidene primary amino acid amide is used, with the primary amino acid amide preferably being derived from an aliphatic primary amino acid amide, for example tertiary-leucine amide. As organic solvent use is preferably made of an aromatic hydrocarbon, a cyclic, aliphatic hydrocarbon or a ether, in particular an aromatic hydrocarbon is applied. The invention may also be applied for the racemisation of an enantiomer-enriched primary amino acid amide.Type: GrantFiled: June 22, 2001Date of Patent: January 25, 2005Assignee: DSM N.V.Inventors: Robert Patrick Hof, Petrus Johannes Hermsen, Ronus de Bode
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Patent number: 6831197Abstract: The present application relates to a plurality of novel processes for preparing 2-(2-hydroxyphenyl)-2-(alkoxyimino)-N-methylacetamide derivatives, to novel intermediates for their preparation, and to processes for preparing these intermediates.Type: GrantFiled: January 14, 2004Date of Patent: December 14, 2004Assignee: Bayer AktiengesellschaftInventors: Walter Hübsch, Bernd Gallenkamp, Herbert Gayer, Lubbertus Mulder, Thorsten Müh, Reinhard Lantzsch, Holger Weintritt
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Publication number: 20040229904Abstract: The invention relates to compounds of formula (1) 1Type: ApplicationFiled: May 6, 2004Publication date: November 18, 2004Applicant: Pfizer IncInventors: Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite
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Publication number: 20040229910Abstract: The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.Type: ApplicationFiled: November 19, 2003Publication date: November 18, 2004Inventors: Fredericus Antonius Dijcks, Dirk Leysen, Joannes Theodorus Maria Linders, Gerardus Stephanus Franciscus Ruigt, Ian Craig Carlyle, Simon James Anthony Grove, Duncan Robertson Rae, Simon N. Thorn
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Patent number: 6803378Abstract: Novel diketoacid compounds of Formula I are provided which are useful as HIV integrase inhibitors and for the treatment of AIDS or ARC.Type: GrantFiled: September 25, 2002Date of Patent: October 12, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Timothy D. Johnson, Nicholas A. Meanwell, Jacque Banville
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Patent number: 6794542Abstract: Process for the preparation of a diasteromerically enriched phenylglycine amide derivative in which an enantiomerically enriched phenylglycine amide is converted into the corresponding Schiff base with the aid of compound R2—C(O)—R3, and the Schiff base obtained is subsequently converted into the diastereomerically enriched phenyglycine amide derivative with the aid of a cyanide source, a reducing agent or an allyl organometallic compound. The phenylglycine amide derivatives obtained are interesting starting materials for the preparation of for example enantiomerically enriched &agr;- and or &bgr;-amino acids and derivatives thereof, such as amides and esters, and amines.Type: GrantFiled: October 9, 2002Date of Patent: September 21, 2004Assignee: DSM N.V.Inventors: Wilhelmus Hubertus Joseph Boesten, Harold Monro Moody, Bernardus Kaptein, Johannes Paulus Gerardus Seerden, Marcelles Van Der Sluis, Ben Lange De, Quirinus Bernardus Broxterman
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Publication number: 20040176446Abstract: The invention relates to compounds of formula (I), to salts and stereoisomers thereof, to their production and to their use for producing medicaments used for treating cardiovascular diseases.Type: ApplicationFiled: April 12, 2004Publication date: September 9, 2004Inventors: Cristina Alonso-Alija, Michael Harter, Michael Hahn, Josef Pernerstorfer, Stefan Weigand, Johannes-Peter Stasch, Frank Wunder
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Patent number: 6787670Abstract: The invention relates to novel gloyoxylic acid amides, to a process for their preparation and to their use for controlling harmful organisms.Type: GrantFiled: May 23, 2002Date of Patent: September 7, 2004Assignee: Bayer AktiengesellschaftInventors: Christiane Boie, Thomas Seitz, Ulrich Heinemann, Reiner Fischer, Martin Vaupel, Ulrike Wachendorff-Neumann, Karl-Heinz Kuck
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Patent number: 6780995Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: November 25, 2002Date of Patent: August 24, 2004Assignee: Isotechnika Inc.Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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Patent number: 6774116Abstract: A prodrug composition containing a cinnamate moiety and a biologically active molecule moiety which can be released by hydrolysis or activated by light is disclosed. The cinnamate moiety can have substituents of various electronically donating or electronically withdrawing groups to modify the cinnamate moiety's electric properties as well as photo reactivities for the purpose of achieving a proper hydrolysis rate of the acyl bond between the biologically active molecule moiety and the cinnamic acid backbone. The biologically active molecule can be any biologically active agent or diagnostic, for example, a chemotherapeutic such as a paclitaxel, campotothecin, doxorubicin, amethopterin, etoposide, or fluconazole. The prodrug composition can be modified to add a carrier moiety on the prodrug composition for targeting or to facilitate uptake of the drug. The prodrug compositions can be activated with an energy source to release the drug at the desired site.Type: GrantFiled: January 31, 2002Date of Patent: August 10, 2004Assignee: Cryolife, Inc.Inventors: Carl W. Gilbert, Eleanor B. McGowan, Kirby S. Black, T. Gregory P. Harper
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Patent number: 6770778Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions, and methods of use thereof.Type: GrantFiled: January 23, 2003Date of Patent: August 3, 2004Assignee: Pfizer IncInventors: Stephen Douglas Barrett, Michael David Kaufman, Gordon William Rewcastle, Julie Ann Spicer
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Publication number: 20040143009Abstract: The present invention relates to novel secondary or tertiary amines useful for smoothing wrinkles and fine lines, in particular expression wrinkles and fine lines.Type: ApplicationFiled: November 6, 2003Publication date: July 22, 2004Applicant: L'OREALInventors: Maria Dalko, Lionel Breton, Christophe Boulle
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Patent number: 6753327Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m, —CH═CH—, —C≡C—, and Y is phenyl, pyridine, pyrimidine and pyrazine and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.Type: GrantFiled: October 11, 2000Date of Patent: June 22, 2004Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
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Publication number: 20040106646Abstract: The present invention provides a visual function disorder improving agent containing a compound having Rho kinase inhibitory activity, particularly (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide, as an effective component. This agent has axon of the retinal ganglion cellal extension promoting action and optic nerve cell regeneration promoting action, and is useful for the treatment of a visual function disorder associated with various eye diseases caused by damage, defects, degeneration and the like in the retinal or optic nerve.Type: ApplicationFiled: November 18, 2003Publication date: June 3, 2004Inventors: Yoshiko Takayama, Yukuo Yoshida, Masayoshi Uehata
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Publication number: 20040106794Abstract: There are disclosed compounds of the formula 1Type: ApplicationFiled: September 11, 2002Publication date: June 3, 2004Applicant: Schering CorporationInventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, Laura L. Rokosz
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Publication number: 20040097407Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.Type: ApplicationFiled: July 1, 2003Publication date: May 20, 2004Inventors: Adnan M.M. Mjalli, Ramesh Gopalaswamy, Kwasi S. Avor, Christopher L. Wysong, Andrew Patron
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Patent number: 6730705Abstract: The invention relates to new alkoximinoacetic acid amides, a process for their preparation and their use as agents for combating pests.Type: GrantFiled: June 30, 2000Date of Patent: May 4, 2004Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Gerd Hänssler, Klaus Stenzel
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Publication number: 20040072868Abstract: 1Type: ApplicationFiled: March 18, 2003Publication date: April 15, 2004Inventors: Jon Loren Collins, Adam M. Fivush, Patrick Reed Maloney, Eugene L. Stewart, Timothy Mark Willson
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Patent number: 6720452Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: June 10, 2002Date of Patent: April 13, 2004Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber, Timothy Luker, Michael Mortimore, Philip Thorne
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Patent number: 6706765Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: February 6, 2003Date of Patent: March 16, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Publication number: 20040048907Abstract: One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke.Type: ApplicationFiled: May 15, 2003Publication date: March 11, 2004Inventors: Brian M. Aquila, Seth C. Hopkins, Curtis A. Lockshin, Fengjiang Wang
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Patent number: 6700017Abstract: The present invention provides processes for preparing 2-(2-hydroxyphenyl)-2-(alkoxyimino)-N-methylacetamides, to intermediates for this preparation, and to processes for preparing those intermediates.Type: GrantFiled: May 20, 2002Date of Patent: March 2, 2004Assignee: Bayer AktiengesellschaftInventors: Walter Hübsch, Bernd Gallenkamp, Herbert Gayer, Lubbertus Mulder, Thorsten Müh, Reinhard Lantzsch, Holger Weintritt
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Patent number: 6699463Abstract: Compounds of Formula I Each R is independently linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy or one R is H and the other R is linear or branched C1 to C8 alkyl, or linear or branched C1 to C8 alkoxy; R1 is selected from the group consisting of COCH3, CO2R3, CONH2, CONH(R4)2, CN, COX(CH2)n-N—(R2)(R4)(R3), and the quaternized salt form of the formula COX(CH2)n-N—(R2)(R4)(R3)+Y−; X is O or NH; n is an integer of 1 to 5; Y is an anion; and R2, R3 and R4 are independently linear or branched C1 to C20. Hair care formulations and other compounds containing compounds of Formula I, and methods for protecting hair and substrates such as polymers, textiles, fabrics, leathers and paints using the compounds herein.Type: GrantFiled: April 10, 2002Date of Patent: March 2, 2004Assignee: EM IndustriesInventor: Ratan K. Chaudhuri
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Publication number: 20040039034Abstract: The present invention relates to compounds of formula (I): 1Type: ApplicationFiled: April 30, 2003Publication date: February 26, 2004Inventors: John A. Tucker, Brian A. Sherer, Ying Zi Xu, Louis Brogley, Shon R. Pulley, Jon S. Jacobs, James P. Beck, Varghese John
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Publication number: 20040034080Abstract: The invention relates to a novel method for producing 3,3-diarylpropylamines of formula (I), wherein A represents a substituted or unsubstituted aryl radical, X represents H, OH or OR3 and Y, R1, R2 and R3 have the meanings given in the description, by hydroformylation/hydrocarbonylation and subsequent reductive amination using a transition metal catalyst.Type: ApplicationFiled: July 14, 2003Publication date: February 19, 2004Inventors: Martin Donsbach, Peter Eilbracht, Christian Buss, Andreas Schmidt
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Publication number: 20040014969Abstract: The invention relates to compound of formula (I): 1Type: ApplicationFiled: March 14, 2003Publication date: January 22, 2004Inventors: Carole Descamps-Francois, Said Yous, Daniel Lesieur, Gerald Guillaumet, Marie-Claude Viaud, Herve Da Costa, Caroline Bennejean, Philippe Delagranes, Pierre Renard
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Patent number: 6677369Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: April 25, 2002Date of Patent: January 13, 2004Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6673794Abstract: A substituted aminomethyl-phenyl-cyclohexane derivative of formula I or Ia, and their a diastereomer, enantiomer, or of a salt formed with a physiologically tolerated acid. Also disclosed are method for preparing the substituted aminomethyl-phenyl-cyclohexane derivative, pharmaceutical compositions comprising the same and method of using the same for treating pain, urinary incontinence, itching, diarrhea, inflammatory and allergic reactions, depression, drug or alcohol abuse, gastritis, cardiovascular diseases, respiratory tract diseases, coughing, mental illnesses and epilepsy.Type: GrantFiled: July 5, 2002Date of Patent: January 6, 2004Assignee: Gruenenthal GmbHInventors: Claudia Puetz, Wolfgang Strassburger, Babette-Yvonne Koegel
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Publication number: 20030225040Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: ApplicationFiled: October 16, 2002Publication date: December 4, 2003Inventors: James T. Dalton, Duane D. Miller, Yali He, Donghua Yin