Having Chalcogen Or Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/362.5)
-
Publication number: 20090088576Abstract: A process for the synthesis of an alcohol of formula (I), using as intermediate a compound of formula (V).Type: ApplicationFiled: January 29, 2007Publication date: April 2, 2009Inventors: Peter Herold, Stefan Stutz, Robert Mah, Aleksandar Stojanovic, Isabelle Lyothier, Dirk Behnke, Felix Spindler, Erhard Bappert
-
Publication number: 20090082395Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.Type: ApplicationFiled: September 9, 2008Publication date: March 26, 2009Inventor: Richard D. Gless, JR.
-
Publication number: 20090082372Abstract: The present invention relates to arylmethylene substituted N-Acyl-?-amino alcohols of the formula I in which Y is selected from the aryl or heteroaryl groups: and R1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.Type: ApplicationFiled: July 24, 2008Publication date: March 26, 2009Inventors: Lars WORTMANN, Marcus Koppitz, Bernd Menzenbach, Dirk Kosemund, Norbert Schmees, Hans-Peter Muhn, Thomas Frenzel, Florian Peter Liesener, Anna Schrey, Ronald Kuehne
-
Publication number: 20090054431Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.Type: ApplicationFiled: October 12, 2006Publication date: February 26, 2009Inventors: Kevin Karl Barvian, Jason Daniel Speake, David John Cowan, Andrew Lamont Larkin, Jerzy Ryszard Szewczyk
-
Publication number: 20090054397Abstract: The present invention provides a novel compound having an excellent JNK inhibitory effect. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 designates —(CO)h—(NRa)j—(CRb?CRc)k—Ar (wherein Ra, Rb and Rc each independently designate a hydrogen atom, a halogen atom, hydroxyl group, an optionally substituted C1-6 alkyl group or the like; Cy designates a 5- or 6-membered heteroaryl; and V each independently designate the formula -L-X—Y (wherein L designates a single bond, an optionally substituted C1-6 alkylene group or the like; X designates a single bond or the formula -A- (wherein A designates NR2, O, CO, S, SO or SO2) and so on; and Y designates a hydrogen atom, a halogen atom, nitro group or the like).Type: ApplicationFiled: April 29, 2008Publication date: February 26, 2009Inventors: Norihito Ohi, Nobuaki Sato, Motohiro Soejima, Takashi Doko, Taro Terauchi, Yoshimitsu Naoe, Takafumi Motoki
-
Patent number: 7491741Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.Type: GrantFiled: February 8, 2007Date of Patent: February 17, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
-
Publication number: 20090042820Abstract: Novel tubulin binding compounds and hypoxia activated prodrugs of novel and known tubulin binding compounds useful for treating cancer and other hyperproliferative diseases are disclosed.Type: ApplicationFiled: November 17, 2005Publication date: February 12, 2009Applicant: Threshold Pharmaceuticals, Inc.Inventors: Mark Matteucci, Jian-Xin Duan, Xiaohong Cai
-
Patent number: 7482342Abstract: Compound corresponding to general formula (I): in which, R1 represents a hydrogen or halogen atom, an NH2, NHR2, NHCOR2, NO2, CN, CH2NH2 and CH2NHR2; or alternatively R1 represents an optionally substituted phenyl or an optionally substituted heteroaromatic group; Ar represents an optionally substituted phenyl group or an optionally substituted heteroaromatic group; n represents 0, 1, 2 or 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Application in therapy.Type: GrantFiled: April 1, 2005Date of Patent: January 27, 2009Assignee: sanofi-aventisInventors: Hugues D'Orchymont, Luc Van Hijfte, Andre Zimmermann
-
Patent number: 7482461Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: GrantFiled: April 4, 2007Date of Patent: January 27, 2009Assignee: WyethInventors: Kevin Liu, Albert Jean Robichaud, Jennifer Rebecca Lo, Hassan Mahmoud Elokdah
-
Publication number: 20090023795Abstract: The compound of Formula (I) and pharmaceutically acceptable salts and prodrugs thereof are useful in the treatment and prevention of various disorders mediated by kinases.Type: ApplicationFiled: January 26, 2007Publication date: January 22, 2009Inventors: Robert Groneberg, Laurence E. Burgess, Darren Harvey, Ellen Laird, Mark C. Munson, James P. Rizzi, Martha Rodriguez, Charles Todd Eary, Daniel John Watson
-
Publication number: 20090023718Abstract: The present invention relates to a novel class of hydroxamic acid derivatives having a diamine or iminodiacetic acid backbone. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively including terminal differentiation, arresting cell growth and/or apoptosis of neo-plastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compound of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: November 23, 2004Publication date: January 22, 2009Applicant: Aton Pharma, Inc.Inventors: Thomas A. Miller, David J. Witter, Sandro Belvedere
-
Publication number: 20090023779Abstract: The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.Type: ApplicationFiled: October 14, 2005Publication date: January 22, 2009Applicant: Laboratoire TheramexInventors: Benoit Rondot, Jean Lafay, Paule Bonnet, Thierry Clerc, Igor Duc, Eric Duranti, Francois Puccio, Jacqueline Shields, Christian Blot, Philippe Maillos
-
Publication number: 20090005417Abstract: The present invention relates to substituted indazolyl sulfonamide and 2,3-dihydroindolyl sulfonamide compounds of general formula I, a process for their preparation, medicaments comprising said substituted indazolyl sulfonamide and 2,3-dihydro-indolyl sulfonamide compounds as well as the use of said substituted indazolyl sulfonamide and 2,3-dihydro-indolyl sulfonamide compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.Type: ApplicationFiled: December 29, 2005Publication date: January 1, 2009Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: Ramon Merce Vidal, Xavier Codony-Soler, Alberto Dordal-Zueras
-
Patent number: 7470717Abstract: The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents aType: GrantFiled: July 30, 2004Date of Patent: December 30, 2008Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoshihisa Ohta, Fumihiko Kanai, Shinji Nara, Yutaka Kanda, Hiroshi Umehara, Yukimasa Shiotsu, Tomoki Naoe, Hitoshi Kiyoi, Keiko Kawashima, Hiromi Ando, Motoki Miyama
-
Publication number: 20080300243Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 24, 2006Publication date: December 4, 2008Inventors: Michael G. Kelly, John Kincaid, Matthew Duncton, Kiran Sahasrabudhe, Satyanarayana Janagani, Ravindra B. Upasani, Guoxian Wu, YunFeng Fang, Zhi-Liang Wei, Carl Kaub, Jianhua He
-
Publication number: 20080287676Abstract: The present invention discloses novel compounds of general formula (I) or a pharmaceutically acceptable salt or prodrug thereof (in which X1-X5, R5-R8b, Z1-Z2 and Ar1 are defined herein), a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain in mammals, and pharmaceutical compositions including those compounds and a process for making those compounds.Type: ApplicationFiled: April 30, 2008Publication date: November 20, 2008Applicant: Abbott LaboratoriesInventors: Arthur R. Gomtsyan, Erol K. Bayburt, Chih-Hung Lee, John R. Koenig, Robert G. Schmidt, Kirill A. Lukin, Gilles Chambournier, Margaret Chi-Ping Hsu, Robert M. Leanna, Russell D. Cink
-
Patent number: 7449586Abstract: The invention relates to novel processes for the preparation of small molecule antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”) and intermediates thereof.Type: GrantFiled: December 1, 2005Date of Patent: November 11, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Xiaojan Han, Xiang-Jun J. Jiang
-
Publication number: 20080275062Abstract: There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: wherein R1 is hydrogen or C1-6alkyl; n is 1, 2, 3 or 4; R2 is aryl, optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy, C1-4alkoxycarbonyl, C1-4alkylsulfonyl and a group R3R4NSO2 (wherein R3 and R4 are independently hydrogen or C1-4alkyl) and a 5- or 6-membered heteroaryl group; or n is 0 and R1 and R2, together with the nitrogen atom to which they are joined, form a 5- or 6-membered monocyclic heterocyclic ring or a 9- or 10-membered bicyclic heterocyclic ring wherein at least the ring which contains the nitrogen atom to which R1 and R2 are joined is non-aromatic, and wherein the 5- or 6-membered monocyclic heterocyclic ring or the 9- or 10-membered bicyclic heterocyclic ring is optionally substituted by one or two groups selected from the group consistinType: ApplicationFiled: January 28, 2005Publication date: November 6, 2008Inventors: David Harold Drewry, David Kendall Jung, James Andrew Linn, Robert Neil Hunter, Dennis Lee, Robert A. Stavenger, Clark Sehon
-
Publication number: 20080275097Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein V, W, X, Y, Z, R1, R2, R4, R5, R6, ring A, ring B, j and k are defined herein. The compounds of Formula I, and the pharmaceutically acceptable salts and prodrugs thereof, are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: December 6, 2007Publication date: November 6, 2008Inventors: Neville J. Anthony, Robert Gomez, Samson M. Jolly, Dai-Shi Su, John Lim
-
Publication number: 20080269211Abstract: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, A and m are each as described herein and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 agonistic activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome.Type: ApplicationFiled: July 14, 2006Publication date: October 30, 2008Inventors: Asako Ishibashi, Tomoki Kato, Kiyoshi Kawamura, Sachiko Mihara, Mikio Morita
-
Publication number: 20080227820Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: ApplicationFiled: October 31, 2007Publication date: September 18, 2008Inventors: Markus Berger, Hartmut Rehwinkel, Heike Schaecke, Matti Lepisto, Karl Edmann
-
Patent number: 7419989Abstract: The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: December 21, 2005Date of Patent: September 2, 2008Assignee: Theravance, Inc.Inventors: Paul Fatheree, Roland Gendron, Adam A Goldblum, Daniel D Long, Daniel Marquess, S. Derek Turner, Seok-Ki Choi
-
Publication number: 20080188666Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: ApplicationFiled: November 7, 2007Publication date: August 7, 2008Inventors: Markus Berger, Hartmut Rehwinkel, Heike Schaecke, Matti Lepisto, Karl Edmann
-
Patent number: 7402606Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.Type: GrantFiled: April 1, 2003Date of Patent: July 22, 2008Assignee: SmithKline Beecham CorporationInventors: David Gene Barrett, John G. Catalano, David Norman Deaton, Aaron Bayne Miller, John A. Ray, Vicente Samano
-
Patent number: 7399765Abstract: Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: September 16, 2004Date of Patent: July 15, 2008Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
-
Publication number: 20080167361Abstract: Compounds of the formula I: wherein m, n, Ar, R1 and R2 are as defined herein. Methods of making the compounds and using the compounds are disclosed.Type: ApplicationFiled: November 8, 2007Publication date: July 10, 2008Inventors: Francisco Javier Lopez-Tapia, Lee Edwin Lowrie, Dov Nitzan
-
Patent number: 7396833Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: GrantFiled: December 22, 2004Date of Patent: July 8, 2008Assignee: Memory Pharmaceuticals CorporationInventors: Wenge Xie, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
-
Publication number: 20080146808Abstract: The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: X1 and X2 are independently O or S; L is a bond or —C(X3)—, —C(X3)NR12, —C(X3)O— wherein X3 is O or S and R12 is H or R1; R1 is alkyl, a carbocycle, carbocycle-substituted alkyl, a heterocycle or heterocycle-substituted alkyl, wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, haloalkyl, alkoxy, alkylsulfonyl, amino, nitro, aryl and heteroaryl; R2 is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, a heterocycle or heterocyclylalkyl; R3 is H or alkyl; R4 and R4? are independently H, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, or heteroaralkyl wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, alkoxy, amino and nitro; R5, and R5? are each independently H or alkyl; R6 is H or alkyl; and salts and solvates thereof.Type: ApplicationFiled: January 24, 2008Publication date: June 19, 2008Applicant: Genentech, Inc.Inventors: Frederick Cohen, Wayne Fairbrother, John Flygare, Stephen Franz Keteltas, Vickie Hsiao-Wei Tsui
-
Publication number: 20080119648Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.Type: ApplicationFiled: October 31, 2007Publication date: May 22, 2008Inventors: Jerome C. Bressi, Anthony R. Gangloff, Lily Kwok
-
Publication number: 20080103182Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.Type: ApplicationFiled: October 19, 2007Publication date: May 1, 2008Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
-
Patent number: 7365211Abstract: This invention relates to a method for modulating ?2 subtype GABAA receptors with heterocyclic compounds of formula I, and salts, solvates and prodrugs thereof. The invention further relates to said heterocyclic compounds and pharmaceutical compositions containing said compounds.Type: GrantFiled: August 11, 2004Date of Patent: April 29, 2008Assignee: Roche Palo Alto LLCInventors: Xao-Fa Lin, David Garrett Loughhead, Sanja Novakovic, Counde O'Yang, Michael Soth, David George Putman
-
Publication number: 20080058515Abstract: Indazolylacrylamide derivatives, which are useful as SGK-1 inhibitors are described herein. The described invention also includes methods of making such indazolylacrylamide derivatives as well as methods of using the same in the treatment of diseases mediated by inappropriate SGK-1 activity.Type: ApplicationFiled: July 23, 2004Publication date: March 6, 2008Inventors: David Harold Drewry, James Andrew Linn, James Marvin Veal
-
Publication number: 20080045511Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.Type: ApplicationFiled: August 15, 2007Publication date: February 21, 2008Inventors: Joshua Kennedy-Smith, Wylie Solang Palmer, Zachary Kevin Sweeney
-
Patent number: 7332149Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.Type: GrantFiled: June 21, 2000Date of Patent: February 19, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Milind Rajopadhye, John A. Barrett, Alan P. Carpenter, Jr., Edward H. Cheesman, Thomas D. Harris
-
Publication number: 20080033184Abstract: Disclosed is a method of making a 1-alkylindazole comprising reacting a 1-acylindazole with a first reducing agent, and contacting the resulting mixture with an acid anhydride or acyl halide, and with pyridine or a 4-dialkylaminopyridine or a combination of pyridine and a 4-dialkylaminopyridine, to form a hemiaminal ester and reacting the hemiaminal ester with a second reducing agent to form a 1-alkylindazole. Also disclosed are intermediates for the synthesis of 1-alkylindazoles.Type: ApplicationFiled: August 1, 2007Publication date: February 7, 2008Applicant: ALCON MANUFACTURING, LTD.Inventors: Pete Delgado, W. Dennis Dean, Raymond E. Conrow
-
Patent number: 7304060Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: July 6, 2004Date of Patent: December 4, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Han-Cheng Zhang, Bruce Maryanoff, Bruce Conway, Kimberly White, Hong Ye, Leonard Robert Hecker, David F. McComsey
-
Publication number: 20070238765Abstract: The present invention provides a compound of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Y, Ar, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: April 11, 2007Publication date: October 11, 2007Inventors: Xiao-Fa Lin, David Garrett Loughhead, Jason Manka, Counde O'Yang, Michael Soth, Dennis M. Yasuda
-
Patent number: 7271190Abstract: A compound represented by the general formula I: I wherein R1 represents hydrogen, etc. R2 represents NHSO2R3, etc., provided that R3 represents C1-6 alkyl, etc. R5 represents hydrogen, etc. R6 and R7 may be the same or different and each independently represents hydrogen, etc. X represents oxygen, etc. Y represents oxygen, etc. Z1 to Z6 each represents carbon, etc. n is an integer of 0 to 6 and ast1 indicates that the carbon atom is asymmetric, and *2, in the case where R5 is not hydrogen, indicates that the carbon atom is asymmetric or a salt of the compound.Type: GrantFiled: October 25, 2002Date of Patent: September 18, 2007Assignee: Asahi Kasei Pharma CorporationInventors: Shiro Miyoshi, Kohei Ogawa
-
Patent number: 7250436Abstract: The invention relates to compounds of the general formula wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances given in the specification, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.Type: GrantFiled: June 6, 2003Date of Patent: July 31, 2007Assignee: Novartis Animal Health US, Inc.Inventors: Pierre Ducray, Thomas Goebel, Jorg Fruchtel
-
Publication number: 20070142434Abstract: The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.Type: ApplicationFiled: August 3, 2006Publication date: June 21, 2007Applicant: DECODE CHEMISTRY, INC.Inventors: Vincent Sandanayaka, Jasbir Singh, Lei Zhao, Mark E. Gurney
-
Patent number: 7223772Abstract: The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R0 and R1 are independently selected from the group consisting of H, halogen, C1-6alkyl, C1-6alkoxy, and C1-6alkoxy substituted by one or more fluorine atoms; R2 is selected from the group consisting of H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, and C1-6alkoxy substituted by one or more fluorine atoms; and R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.Type: GrantFiled: November 1, 1999Date of Patent: May 29, 2007Assignee: SmithKline Beecham CorporationInventors: Ian Baxter Campbell, Alan Naylor
-
Patent number: 7217728Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.Type: GrantFiled: September 21, 2004Date of Patent: May 15, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
-
Patent number: 7214699Abstract: This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein R3 is optionally substituted aryl or heteroaryl, R1 and R2 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.Type: GrantFiled: December 1, 2003Date of Patent: May 8, 2007Assignee: Roche Palo Alto LLCInventors: Richard Leo Cournoyer, David Garrett Loughhead, Counde O'Yang
-
Patent number: 7205299Abstract: The invention relates to indole derivatives which are used as drugs for treating tumor diseases, in particular when there is drug resistance against other active compounds and where there is a metastasizing carcinoma.Type: GrantFiled: June 2, 2004Date of Patent: April 17, 2007Assignee: Zentaris GmbHInventors: Matthias Gerlach, Tilmann Schuster, Peter Ernig, Peter Schmidt, Silke Baasner, Eckhard Günther
-
Patent number: 7199147Abstract: A compound represented by the formula (1): wherein R1—X— indicates that 1 to 4 R1—X— groups are present which may be the same or different, the ring A is a saturated or unsaturated 5-membered heterocyclic ring, X is a single bond, a group represented by the formula: —N(R3)—, —O— or —S—, or the like. R1 is a hydrogen atom, a halogen atom, a nitro group, a carboxyl group, a substituted or unsubstituted alkyl group, or the like, R2 is a hydrogen atom, a halogen atom, a nitro group, a carboxyl group, a substituted or unsubstituted alkyl group, or the like, and R3 is a hydrogen atom, a substituted or unsubstituted alkyl group, or the like; a prodrug of said compound, or a pharmaceutically acceptable salt of said compound or prodrug is a useful compound as a therapeutic agent for diseases for which Rho kinase is responsible.Type: GrantFiled: June 6, 2002Date of Patent: April 3, 2007Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Naonori Imazaki, Masafumi Kitano, Naohito Ohashi, Kazuki Matsui
-
Patent number: 7196082Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: October 14, 2003Date of Patent: March 27, 2007Assignee: Merck & Co. Inc.Inventors: James B. Doherty, Meng-Hsin Chen, Luping Liu, Swaminathan R. Natarajan, Robert M. Tynebor
-
Patent number: 7141587Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: November 18, 2004Date of Patent: November 28, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Robert Steven Kania, Steven Lee Bender, Allen J. Borchardt, Stephan James Cripps, Ye Hua, Michael David Johnson, Theodore Otto Johnson, Jr., Hiep The Luu, Cynthia Louise Palmer, Siegfried Heinz Reich, Anna Maria Tempczyk-Russell, Min Teng, Christine Thomas, Michael David Varney, Michael Brennan Wallace, Michael Raymond Collins
-
Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
-
Patent number: 7060841Abstract: The invention provides a process for preparing 1-methylindazole-3-carboxylic acid of formula (I): which comprises reacting a methylating agent with indazole-3-carboxylic acid of formula (VI): in the presence of an alkaline earth metal oxide or alkoxide in an appropriate solvent. Also provided is a process for producing Granisetron, using the method of the present invention for producing 1-methylindazole-3-carboxylic acid.Type: GrantFiled: June 3, 2003Date of Patent: June 13, 2006Assignee: Chemagis Ltd.Inventors: Vladimir Naddaka, Shadi Saeed, Dionne Montviliski, Oded Arad, Joseph Kaspi
-
Patent number: RE39265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 9, 2000Date of Patent: September 5, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley