Nitrogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/316)
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Patent number: 6984643Abstract: Compounds of Formula (I): wherein Ar1 is aryl; Ar2 is hydrogen, cycloalkyl, aryl or heteroaryl; Z is —C(?O) or a single bond; R1, R2, R3, R4 and R5 are independently hydrogen or alkyl optionally substituted with hydroxy; alk is an alkylene chain of one to six carbon atoms; X is —O—, —NRh (where Rh is hydrogen or alkyl), (CR6R7)m(where R6 and R7 are independently in each occurrence hydrogen or alkyl and m is an integer from 0 to 3), or —S(O)n (wherein n is an integer from 0 to 2); or prodrugs thereof, and pharmaceutically acceptable salts thereof, are inhibitors of CCR3 useful for treating eosinophil induced diseases such as asthma.Type: GrantFiled: July 1, 2003Date of Patent: January 10, 2006Assignee: Roche Palo Alto LLCInventors: Daisy Joe Du Bois, Long Mao, Daniel Harry Rogers, John Patrick Williams
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Patent number: 6949649Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.Type: GrantFiled: October 29, 2003Date of Patent: September 27, 2005Assignee: 3M Innovative Properties Co.Inventors: Jason D. Bonk, Joseph F. Dellaria, Bryon A. Merrill, Matthew R. Radmer
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Patent number: 6909003Abstract: The invention relates to a process for the manufacture of a compound of formula or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the element represents —CH2—CH2— or —CH?CH— and R represents a cyclic radical.Type: GrantFiled: May 2, 2003Date of Patent: June 21, 2005Assignee: Novartis AGInventor: Thomas Storz
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Patent number: 6903117Abstract: A compound of formula (I): or a salt thereof, or a solvate thereof, wherein Ra represents a group R5 which is hydrogen, alkyl or optionally substituted aryl and Rb represents a moiety of formula (a): wherein X represents a hydroxy or an alkoxy group wherein the alkyl group may be substitued or unsubstituted or X represents a group NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclic group; R1 represents an alkyl or a substituted or unsubstituted aryl group; and R2, R3 and R4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R6 and R7 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamiType: GrantFiled: November 20, 2002Date of Patent: June 7, 2005Assignee: Nikem Research S.R.L.Inventors: Carlo Farina, Stefania Gagliardi, Guy Marguerite Marie Gerard Nadler
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Patent number: 6900214Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds induce mitotic arrest thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inducing mitotic arrest.Type: GrantFiled: March 22, 2002Date of Patent: May 31, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Louis J. Lombardo, Laurence I. Wu
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Patent number: 6900210Abstract: The present invention provides novel heterocyclic amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A, B and Z 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 heterocyclic 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: May 31, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Li-Qiang Sun, Jie Chen, Huan He
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Patent number: 6900222Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is aType: GrantFiled: May 23, 2000Date of Patent: May 31, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 6878717Abstract: This invention concerns the use of compounds of formula: the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=-a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally subsType: GrantFiled: November 1, 1999Date of Patent: April 12, 2005Inventors: Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Patent number: 6867210Abstract: This invention relates aryl substituted pyridines, pyrimidines, pyrazines and triazines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A1, A2, A3, R1-R4, X and Y are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: March 12, 2001Date of Patent: March 15, 2005Assignee: Euro-Celtique S.A.Inventors: Derk J. Hogenkamp, Phong Nguyen, Bin Shao
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Patent number: 6864252Abstract: The present invention relates to hydrazinyl and nitrogen oxide pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, X, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.Type: GrantFiled: November 1, 2002Date of Patent: March 8, 2005Assignee: Pfizer, Inc.Inventors: Subas M. Sakya, Bryson Rast
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Patent number: 6864263Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.Type: GrantFiled: April 12, 2002Date of Patent: March 8, 2005Assignees: Berlex Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Patent number: 6864369Abstract: New crystalline forms of lopinavir are disclosed.Type: GrantFiled: March 12, 2003Date of Patent: March 8, 2005Assignee: Abbott LaboratoriesInventors: Daniel A. Dickman, Sanjay Chemburkar, James J. Fort, Rodger F. Henry, David Lechuga-Ballesteros, Yuping Niu, William Porter
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Patent number: 6855716Abstract: Dihydropyrimidine derivatives of the following formula or analogs thereof have selective N-type calcium channel antagonistic activity, and they are used as therapeutic agents for various diseases participating in the N-type calcium channels.Type: GrantFiled: December 26, 2001Date of Patent: February 15, 2005Assignee: Ajinomoto Co., Inc.Inventors: Seiji Ohno, Akiko Okajima, Seiji Niwa, Morikazu Kito, Akira Takahara, Yukitsugu Ono, Yuki Kajigaya, Tomoko Takeda, Hajime Koganei
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Patent number: 6849634Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: December 7, 2001Date of Patent: February 1, 2005Assignee: ICAgenInventors: Serge Beaudoin, Aimee D. Reed, Michael F. Gross
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Patent number: 6846828Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.Type: GrantFiled: November 6, 2002Date of Patent: January 25, 2005Assignee: Roche Palo Alto LLCInventors: Ronald Charles Hawley, Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
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Patent number: 6846928Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: March 14, 2003Date of Patent: January 25, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard, Albert C. Pierce
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Patent number: 6846829Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.Type: GrantFiled: April 12, 2002Date of Patent: January 25, 2005Assignees: Berlex Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Patent number: 6838458Abstract: The present invention relates to 5-(alkylidene-cycloalkyl)-pyrazoles and 5-(alkylidene-heterocyclyl)-pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, B, ring G, R1 through R7 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.Type: GrantFiled: November 1, 2002Date of Patent: January 4, 2005Assignee: Pfizer, Inc.Inventor: Subas M. Sakya
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Patent number: 6833370Abstract: Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3 I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: April 26, 2000Date of Patent: December 21, 2004Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, Jerome F. Daanen, Keith Brian Ryther, Jianguo Ji
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Patent number: 6833378Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.Type: GrantFiled: January 17, 2001Date of Patent: December 21, 2004Assignee: Pfizer IncInventor: Yuhpyng L. Chen
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Patent number: 6828338Abstract: The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.Type: GrantFiled: June 19, 2003Date of Patent: December 7, 2004Assignee: Pharmacia CorporationInventors: Michael J. South, Brenda Case, Danny J. Garland, Michael J. Hayes, Horng-Chih Huang, Wei Huang, Darin E. Jones, William L. Neumann, John J. Parlow, David B. Reitz, Melvin L. Rueppel, Rondald K. Webber
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Publication number: 20040242928Abstract: Reverse hydroxamic acid derivatives having specific structure represented by a general formula (Ia): 1Type: ApplicationFiled: March 4, 2004Publication date: December 2, 2004Inventors: Masanao Shimano, Noriyuki Kamei, Tomohiro Tanaka, Tatsuhiro Harada, Makoto Haino, Akihiko Okuyama, Yoshio Arakawa, Yoshiko Murakami
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Publication number: 20040242609Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: April 15, 2004Publication date: December 2, 2004Applicant: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, John Wetzel, John E. Deleon, Bharat Lagu, Charles Gluchowski, Stewart Noble, Dhanapalan Nagarathnam
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Patent number: 6821971Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; R2a and R2b units are each independently hydrogen, ethers, amines, amides, carboxylates, or said units can form a double bond, a carbonyl, or R2a and R2b can be taken together to form a substituted or unsubstituted ring comprising from 4 to 8 atoms, said ring selected from the group consisting of: i) carbocyclic; ii) heterocyclic; iii) aryl; iv) heteroaryl; v) bicyclic; and vi) heterobicyclic.Type: GrantFiled: September 18, 2002Date of Patent: November 23, 2004Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Matthew John Laufersweiler, Jane Far-Jine Djung, Biswanath De
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Patent number: 6818648Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.Type: GrantFiled: March 17, 2003Date of Patent: November 16, 2004Assignee: Bristol-Myers Squibb PharmaInventors: Robert John Chorvat, Parthasarathi Rajagopalan
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Patent number: 6812229Abstract: It is to provide a novel fungicide having high controlling effects on plant diseases particularly on wheat powdery mildew and cucumber gray mold, without ill effects on crops. A carbamate derivative represented by the general formula [I] {wherein X is a halogen atom, a C1-C6 alkyl group or the like, n is 0 or an integer of from 1 to 4, R1 is a C1-C6 alkyl group, R2 is a hydrogen atom, a C1-C6 alkyl group or the like, R3 is a hydrogen atom or a C1-C6 alkyl group, G is an oxygen atom, a sulfur atom or the like, Y is a hydrogen atom, a C1-C10 alkyl group, C2-C10 alkenyl group or the like, and Q is a hydrogen atom, a C1-C6 haloalkyl group, a phenyl group or the like} and an agricultural/horticultural fungicide containing the same as the active ingredient.Type: GrantFiled: February 5, 2002Date of Patent: November 2, 2004Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masami Ozaki, Shunichiro Fukumoto, Ryuji Tamai, Kazuhiro Ikegaya, Norihisa Yonekura, Takahiro Kawashima, Junetsu Sakai, Norimichi Muramatsu, Makikazu Takagaki, Kouzou Nagayama
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Patent number: 6809102Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds induce mitotic arrest thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inducing mitotic arrest.Type: GrantFiled: March 22, 2002Date of Patent: October 26, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Spencer David Kimball, Louis J. Lombardo, David B. Rawlins, Hai-Yun Xiao, Robert J. Schmidt, David K. Williams
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Publication number: 20040209883Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.Type: ApplicationFiled: March 4, 2004Publication date: October 21, 2004Inventors: Mark James Bamford, David Kenneth Dean, Antoinette Naylor, Andrew Kenneth Takle, David Matthew Wilson
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Patent number: 6800590Abstract: This invention relates to new 2-pyrimidinyloxy-N-aryl-benzylamine derivatives, their preparation processes and uses as chemical herbicides in agriculture. The compound has the following structure: wherein, D or E is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl or C1-C4 haloalkoxy; R1 is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy; R2 is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 carbamyl, C1-C4 alkoxycarbonyl, C1-C4 haloalkyl, cyano, nitro, carboxy or its alkali metal, alkali earth metal and organoammonium salts, C1-C4 alkylamido, C1-C4 haloalkylamido, heterocyclic amido, benzamido or substituted benzamido, benzo or substituted benzo compounds; R3 is hydrogen, C1-C4 alkanoyl, C1-C4 haloalkanoyl, benzoyl or C1-C4 alkoxyacetyl; X is CH or N; n=1-3.Type: GrantFiled: April 9, 2003Date of Patent: October 5, 2004Assignees: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Zheijiang Chemical Industry Research InstituteInventors: Long Lü, Jie Chen, Jun Wu, Wen Ling, Lisheng Mao, Mingzhi Li, Xian Cai, Weili Peng, Yong Wu, Shenggan Wu, Hongjun Wang, Guochao Wang, Hu Cui, Shidong Han, Weilian Qiu, Yonghua Wang
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Publication number: 20040176348Abstract: Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.Type: ApplicationFiled: March 5, 2003Publication date: September 9, 2004Applicants: Aventis Pharma S.A., Targacept, Inc.Inventors: Jeffrey Daniel Schmitt, Gary Maurice Dull, Arielle Genevois-Borella, Marc Capet, Michel Cheve
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Patent number: 6787555Abstract: The present invention relates to 4-aryl triazoles having the formula: wherein R1 is independently selected from the group consisting of: lower alkyl, lower alkenyl, lower alkynyl, lower heteroalkyl, lower heteroalkenyl, lower heteroalkynyl, heterocycloalkyl, heteroaryl, halo, CN, OR4, SR4, S(O)R4, S(O)2R4, and NR4R5; and Q is has the general formula: said compounds are useful in treating diseases associated with unwanted cytokine activity, inter alia, interleukin-1 (IL-1) and tumor necrosis factor (TNF) from cells.Type: GrantFiled: April 24, 2002Date of Patent: September 7, 2004Assignee: The Procter & Gamble CompanyInventors: Joshua Spector Tullis, John Charles Van Rens, Michael Philip Clark, Benjamin Eric Blass, Michael George Natchus, Biswanath De
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Patent number: 6784167Abstract: 17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R4)(R6)Y are oriented cis to each other; W represents O or S; R1 represents —H or optionally substituted —(C1-C4)alkyl; n represents 0 or an integer of 1-3; and R2 represents any of a variety of substituents on ring A. R4 generally represents —H but may be a bond terminating at the ortho position of ring A. Y represents fluorine, —OR5, or —SR5, and R5 represents —H, optionally substituted —(C1-C4)alkyl, optionally substituted -phenyl, optionally substituted —(C1-C4)alkyl-phenyl, or optionally substituted —(C1-C4)acyl. R6 represents any of a variety of groups as defined in the specification and claims, including heteroaryl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, alkynyl, arylalkynyl, heteroarylalkynyl, aryl, and indolyl.Type: GrantFiled: September 28, 2001Date of Patent: August 31, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Jill E. Wood, Jeremy L. Baryza, Catherine R. Brennan, Soongyu Choi, James H. Cook, Brian R. Dixon, Paul P. Ehrlich, David E. Gunn, Ian McAlexander, Peiying Liu, Derek B. Lowe, Anikó M. Redman, William J. Scott, Yamin Wang
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Patent number: 6784171Abstract: The invention concerns a process for the manufacture of tert-butyl (E)-(6-[2-4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]vinyl)-(4R, 6S)-2,2-dimethyl(1,3-dioxan-4-yl) acetate, the novel starting material used in said process and the use of the process in the manufacture of a pharmaceutical.Type: GrantFiled: July 2, 2003Date of Patent: August 31, 2004Assignee: AstraZenecaInventors: Nigel P Taylor, Loius J Diorazio, Haruo Koike, Mikio Kabaki
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Publication number: 20040167334Abstract: Heterocyclic acylsulfimides, processes for their preparation, compositions comprising them and their use as pesticidesType: ApplicationFiled: February 5, 2004Publication date: August 26, 2004Inventors: Yuriy Grigorievich Shermolovich, Pavel Petrovich Kornuta, Nataliya Olezandrivna Komuta, Uwe Doller, Oswald Ort, Wolfgang Schaper, Daniela Jans, Ulrich Sanft, Maria-Theresia Thonessen, Marion Beckmann, Jutta Maria Waibel, Sergiy Pazenok
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Patent number: 6780868Abstract: Compounds of formula (I): wherein: V represents a single bond or a linear or branched (C1-C6)alkylene chain, M represents a single bond or a linear or branched (C1-C6)alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i): X represents carbonyl, G1 represents a linear C3 alkylene chain optionally containing a double bond and/or being optionally substituted by a hydroxyl group, their isomers, their hydrates, their solvates, and additional salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.Type: GrantFiled: February 20, 2003Date of Patent: August 24, 2004Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
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Patent number: 6753332Abstract: The present invention relates to compounds of the formula wherein R1, R3, R5 and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).Type: GrantFiled: July 3, 2002Date of Patent: June 22, 2004Assignee: Pfizer, Inc.Inventors: Subas M. Sakya, Andrei Shavnya, Bryson Rast
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Patent number: 6743798Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.Type: GrantFiled: April 11, 2001Date of Patent: June 1, 2004Assignee: Bayer AktiengesellschaftInventors: Alexander Straub, Achim Feurer, Cristina Alonso-Alija, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hütter, Klaus Dembowsky, Elke Stahl
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Publication number: 20040092402Abstract: The present invention provides a pyrimidine derivative represented by the formula: 1Type: ApplicationFiled: June 26, 2003Publication date: May 13, 2004Inventors: Takashi Kuragano, Yasushi Tanaka
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Patent number: 6730668Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; each R2 unit is independently selected from the group consisting of: a) hydrogen; b) —(CH2)jO(CH2)nR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —(CH2)jCON(R10)2; g) —(CH2)jOCON(R10)2; h) two R2 units can be taken together to form a carbonyl unit; i) and mixtures thereof; R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 units can be take together to form a carbocyclic or heterocyclic ringType: GrantFiled: September 18, 2002Date of Patent: May 4, 2004Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Matthew John Laufersweiler, Jane Far-Jine Djung, Michael George Natchus, Biswanath De
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Patent number: 6727257Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: wherein A is which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: December 5, 2000Date of Patent: April 27, 2004Assignee: Synaptic Pharmaceutical CorporationInventors: Dhanapalan Nagarathnam, George Chiu, T. G. Murali Dhar, Wai C. Wong, Mohammad R. Marzabadi, Charles Gluchowski, Bharat Lagu, Shou Wu Miao
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Patent number: 6723711Abstract: A compound of the structure A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1(vascular cell adhesion molecule-1) and fibronectin; pharmaceutically active compositions comprising these compounds; and the use of these compounds for the control or prevention of diseases states in which &agr;4&bgr;1 is involved are also disclosed.Type: GrantFiled: October 9, 2001Date of Patent: April 20, 2004Assignee: Texas Biotechnology CorporationInventors: Ronald J. Biediger, Brian Dupre, Linda K. Hamaker, George W. Holland, Jamal M. Kassir, Wen Li, Robert V. Market, Noel Nguyen, Ian L. Scott, Chengde Wu, E. Radford Decker
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Patent number: 6723753Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.Type: GrantFiled: February 7, 2002Date of Patent: April 20, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6720324Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of modifying feeding behavior of a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject.Type: GrantFiled: July 5, 2001Date of Patent: April 13, 2004Assignee: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, John Wetzel, John E. DeLeon, Bharat Lagu, Charles Gluchowski, Stewart Noble, Dhanapalan Nagarathnam
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Publication number: 20040058944Abstract: The present invention relates to 2-(4-fluorophenyl)-3-(2-phenoxy-pyrimidin-4-yl)-6,7-dihydro-5H-pyrazolo-[1,2-a]pyrazol-1-one, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, having the formula: 1Type: ApplicationFiled: September 12, 2003Publication date: March 25, 2004Inventors: Michael Philip Clark, Matthew John Laufersweiler
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Publication number: 20040058942Abstract: The present invention is directed in part towards methods of modulating the function of calcium channels with pyrimidine-based compounds. In addition, the invention describes methods of preventing and treating calcium channel-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyrimidine-based compounds and pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: June 10, 2003Publication date: March 25, 2004Inventors: Phani Kumar Pullela, Paramashivappa Rangappa, Srinivasa Rao Alapati, Pillarisetti V. Subbarao
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Publication number: 20040049032Abstract: The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora-mediated diseases or conditions.Type: ApplicationFiled: June 18, 2003Publication date: March 11, 2004Inventors: Jean-Damien Charrier, Francesca Mazzei, David Kay, Andrew Miller
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Publication number: 20040039005Abstract: This invention concerns the use of compounds of formula 1Type: ApplicationFiled: August 5, 2003Publication date: February 26, 2004Inventors: Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Publication number: 20040034018Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: August 1, 2003Publication date: February 19, 2004Inventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
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Patent number: 6693101Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.Type: GrantFiled: January 23, 2001Date of Patent: February 17, 2004Assignee: Merck & Co., Inc.Inventors: Ben C. Askew, Michael J. Breslin, Mark E. Duggan, John H. Hutchinson, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Michael A. Patane
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Patent number: RE39056Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.Type: GrantFiled: September 11, 1996Date of Patent: April 4, 2006Assignee: Merck & Co, Inc.Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman