Six-membered Ring Consisting Of One Nitrogen And Five Carbons (e.g., Pyridine, Etc.) Patents (Class 544/124)
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Patent number: 7414055Abstract: The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 20, 2004Date of Patent: August 19, 2008Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Craig W. Lindsley, Zhicai Wu, Zhijian Zhao, John C. Hartnett
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Patent number: 7414046Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: May 23, 2003Date of Patent: August 19, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
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Publication number: 20080194816Abstract: A method of producing an o-disubstituted aromatic compound, containing: continuously conducting at least the following steps (a) to (d): (a) a step of mono-lithiating one halogen atom of an o-dihaloaromatic compound, using a first microreactor; (b) a step of making the thus-obtained monolithiated product to react with an electrophilic compound, using a second microreactor, to obtain a monosubstituted-monohaloaromatic compound; (c) a step of lithiating the other halogen atom of the o-dihaloaromatic compound, using a third microreactor; and (d) a step of making the thus-obtained lithiated product successively to react with an electrophilic compound, using a forth microreactor.Type: ApplicationFiled: March 12, 2007Publication date: August 14, 2008Applicant: FUJIFILM CorporationInventors: Jun-ichi Yoshida, Aiichiro Nagaki, Toshiki Nokami
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Patent number: 7410976Abstract: The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.Type: GrantFiled: July 14, 2006Date of Patent: August 12, 2008Assignee: Merck & Co., Inc.Inventors: Takeru Yamakawa, Hideki Jona, Kenji Niiyama, Koji Yamada, Tomoharu Iino, Mitsuru Ohkubo, Hideaki Imamura, Jun Shibata, Jun Kusunoki, Lihu Yang
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Publication number: 20080188474Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 28, 2007Publication date: August 7, 2008Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
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Publication number: 20080176833Abstract: This invention provides novel dihydropyridine derivatives of the formula I having protein tyrosine kinase inhibitory activity, to process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions.Type: ApplicationFiled: December 13, 2007Publication date: July 24, 2008Inventors: Marc Adler, Stefan Baeurle, Judi Bryant, Ming Chen, Yuo-Ling Chou, Paul Hrvatin, Seock-Kyu Khim, Monica Kochanny, Wheeseong Lee, Michael Mamounas, Janet Meurer Ogden, Gary Bruce Phillips, Victor Selchau, Christopher West, Bin Ye, Shendong Yuan, Martin Krueger
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Publication number: 20080176840Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: May 25, 2007Publication date: July 24, 2008Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Przewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
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Patent number: 7396842Abstract: A 5-membered cyclic compound of the formula: wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc., Y1 is a direct bond, substituted or unsubstituted alkylene, —CO(CH2)n—, etc., the wavy line means (E)-configuration or (Z)-configuration, R3 is substituted or unsubstituted aryl, etc., Y2 is substituted or unsubstituted alkylene, etc., R4 is hydrogen, substituted or unsubstituted alkanoyl, substituted or unsubstituted alkyl, etc., R5 is hydrogen, etc., or a salt thereof, these compound being able to inhibit infiltration of leukocytes such as eosinophils and lymphocytes, by which being useful for the treatment of various kinds of inflammation.Type: GrantFiled: April 22, 2005Date of Patent: July 8, 2008Assignee: Dianippon Sumitomo Pharma Co., Ltd.Inventors: Norio Fujiwara, Hitoshi Fujita, Fujio Antoku, Toshinari Sugasawa, Hajime Kawakami
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Publication number: 20080153812Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: December 18, 2007Publication date: June 26, 2008Applicant: ASTRAZENECA ABInventors: David Buttar, Kevin Micheal Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
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Publication number: 20080153809Abstract: The present invention relates to compounds of formula (I-VII) or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R6, R7 and R8 are defined herein. The present invention also relates to methods of treating pain using these compounds and pharmaceutical compositions including these compounds.Type: ApplicationFiled: February 19, 2008Publication date: June 26, 2008Applicant: ABBOTT LABORATORIESInventors: CHIH-HUNG LEE, Erol K. Bayburt, Stanley DiDomenico, Irene Drizin, Arthur R. Gomtsyan, John R. Koenig, Richard J. Perner, Robert G. Schmidt, Sean C. Turner, Tammie K. White, Guo Zhu Zheng
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Publication number: 20080146564Abstract: Novel 1,3-dihydro-benzimidazol-2-ylidene amine derivatives of formula the addition salts and stereochemically isomeric forms wherein each Alk is C1-6alkanediyl; Q is hydrogen; C1-6alkyl substituted with one or two Ar2 radicals; CI1-6alkyl substituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; —CO—Ar2; or Q is a radical of formula wherein t is 1, 2 or 3; R4 is amino, mono- or di(C1-6alkyl)amino; R1 is Ar2, —CO—Ar2 or a monocyclic or bicyclic heterocycle which may optionally be substituted; R2 is as R1 and additionally can be hydrogen; where Q is other than hydrogen, R3 is hydrogen; and where Q is other than hydrogen, R3 is a radical: wherein R6 is hydrogen, C1-6alkyl, substituted C1-6alkyl; R7, R8, R9 are halo, cyano, C1-6alkyl, substituted C1-6alkyl, C2-6alkenyl, cyanoC2-6alkenyl, C2-6alkynyl, cyanoC2 6alkynyl, Ar1, R10a—0—, R10a —S—, —N(R5aR5b), R10a—O—C(?O)—, N(R5aR5b)—C(?O)—, R10a—C(?O)—NR5b1', R10b—C(?O)—O—; and R8 and/or R9 may also beType: ApplicationFiled: March 17, 2006Publication date: June 19, 2008Inventors: Jean-Francois Bonfanti, Jerome Michel Claude Portin, Ismet Dorange
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Publication number: 20080139561Abstract: This invention relates to novel compounds having the Formula (I) to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.Type: ApplicationFiled: February 1, 2006Publication date: June 12, 2008Applicant: ASTRAZENECA ABInventors: Audrey Davies, Michelle Lamb, Paul Lyne, Tao Wang, Dingwei Yu, Peter Mohr, Bin Wang
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Publication number: 20080139555Abstract: This invention is directed to Arylthiobenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention.Type: ApplicationFiled: February 8, 2008Publication date: June 12, 2008Applicant: H. Lundbeck A/SInventors: Mohammad R. Marzabadi, Yu Jiang, Chien-An Chen, Kai Lu, Kim Andersen
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Publication number: 20080132507Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.Type: ApplicationFiled: October 13, 2005Publication date: June 5, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Richard Clark, Shinsuke Hirota, Hiroshi Azuma, Kazunobu Kira, Nobuhisa Watanabe, Tadashi Nagakura, Tatsuo Horizoe
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Publication number: 20080132502Abstract: The invention provides thiazole derivatives of formula (I), or pharmaceutically acceptable salts thereof in which Ring A, R1, R2 and R3 are as defined in the specification; a processes for their preparation; pharmaceutical compositions containing them; and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.Type: ApplicationFiled: November 7, 2005Publication date: June 5, 2008Inventors: Malena Bengtsson, Joakim Larsson, Grigorios Nikitidis, Peter Storm, John Peter Bailey, Edward Jolyon Griffen, Jean-Claude Arnould, Thomas Geoffrey Colerick Bird
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Publication number: 20080125429Abstract: A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided. The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.Type: ApplicationFiled: November 1, 2005Publication date: May 29, 2008Applicant: BANYU PHARMACEUTICAL CO., LTD.Inventors: Noriaki Hashimoto, Keiji Takahashi, Chisato Nakama, Yoshio Ogino, Fumiko Sakai, Teruyuki Nishimura, Jun-ichi Eiki
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Publication number: 20080113988Abstract: The present invention relates to novel isoxazoline-indole derivatives according to Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, with a binding affinity towards dopamine receptors, in particular towards dopamine D2 and/or D3 receptors, with selective serotonin reuptake inhibition (SSRI) properties and showing an affinity for the 5-HT1A receptor, pharmaceutical compositions comprising the compounds according to the invention, the use thereof for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic disorders, most in particular schizophrenia and processes for their production, wherein the variables are further defined in the application.Type: ApplicationFiled: November 25, 2005Publication date: May 15, 2008Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Jose Ignacio Andres-Gil, Jose Manuel Bartolome-Nebreda, Manuel Jesus Alcazar-Vaca, Maria de las Mercedes Garcia-Martin, Antonius Adrianus Hendrikus Petrus Megens
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Publication number: 20080108600Abstract: The present invention provides a genus of polycyclic pyridines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.Type: ApplicationFiled: April 13, 2005Publication date: May 8, 2008Applicants: Icagen, Inc., Astellas Parma Inc.Inventors: Xiaodong Wang, Kerry L. Spear, Alan B. Fulp, Darrick Seconi, Takeshi Suzuki, Takahiro Ishii, Ayako Moritomo, Hideki Kubota, Jun-ichi Kazami
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Patent number: 7365068Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.Type: GrantFiled: May 17, 2005Date of Patent: April 29, 2008Assignee: Achillion Pharmaceuticals, Inc.Inventors: Avinash Phadke, Dawei Chen, Milind Deshpande, Andrew Thurkauf, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Patent number: 7365067Abstract: The present invention provides a compound having the following general formula (I) which is useful as a neurokinin receptor antagonist: (wherein, R1, R2: optionally substituted (hetero)aryl, R3: —CO—R4, —CO—O—R4, etc., R4: alkyl, cycloalkyl, etc., A: CH2, CO, SO2, B: a single bond, etc., D: oxygen, CH2, E: alkylene, alkenylene, n: 1 to 3).Type: GrantFiled: February 24, 2005Date of Patent: April 29, 2008Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Toshiyasu Takemoto, Takuya Ikeda, Kiyoshi Morimoto
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Patent number: 7361682Abstract: The present invention relates to compounds of formula I: wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: June 20, 2005Date of Patent: April 22, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Silvia Gatti McArthur, Cornelia Hertel, Matthias Heinrich Nettekoven, Susanne Raab, Olivier Roche, Rosa Maria Rodriguez-Sarmiento, Franz Schuler, Jean-Marc Plancher
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Patent number: 7351713Abstract: Compounds of formula I wherein R1, R2, R3, R4 and R5 are as defined herein, or pharmaceutically acceptable salts, hydrates or solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity.Type: GrantFiled: September 10, 2004Date of Patent: April 1, 2008Assignee: Viro Chem Pharma, Inc.Inventors: Laval Chan Chun Kong, Ming-Qiang Zhang, Christophe Moinet, Marc Courchesne, Thumkunta Jagadeeswar Reddy, Melanie Proulx
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Publication number: 20080064682Abstract: A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrType: ApplicationFiled: July 1, 2005Publication date: March 13, 2008Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Naoaki Kanaya, Takashi Ishiyama, Ryo Muto, Toshiyuki Watanabe, Yuichi Ochiai
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Publication number: 20080064872Abstract: A novel compound having agonist activity at the S1P3 receptor which is represented by the formula I wherein X is selected from the group consisting of CR3, N and NO; Y is selected from the group consisting of CR3, N and NO; Z is selected from the group consisting of CR3, N and NO; and at least one of X, Y and Z is N or NO; V is O or NOR4 R1 is an aryl group; R2 is an aryl group; R3 is selected from the group consisting of H and alkyl; and 2 of said R3 groups may together form a cyclic alkyl ring having from 3 to 6 carbon atoms; R4 is selected from the group consisting of H and alkyl; a is 0 or an integer of from 1 to 6; b is 0 or 1; c is 0 or 1; f is 0 or an integer of 1 or 2; x is 0 or 1; y is 0 or an integer of from 1 to 3; and z is 0 or an integer of from 1 to 3.Type: ApplicationFiled: September 6, 2007Publication date: March 13, 2008Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Xiaoxia Liu
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Patent number: 7342013Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: May 26, 2006Date of Patent: March 11, 2008Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Patent number: 7338951Abstract: This invention features compounds of formula (I): pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12-related diseases and disorders.Type: GrantFiled: November 10, 2004Date of Patent: March 4, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Mitsunori Ono, Lijun Sun, Yumiko Wada, Teresa Przewloka, Hao Li, Howard P. Ng, Zachary Demko
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Patent number: 7338950Abstract: 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: GrantFiled: October 7, 2004Date of Patent: March 4, 2008Assignee: Renovis, Inc.Inventors: Michael G. Kelly, Satyanarayana Janagani, Guoxian Wu, John Kincaid
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Publication number: 20080044379Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: August 8, 2007Publication date: February 21, 2008Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
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Publication number: 20080045705Abstract: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.Type: ApplicationFiled: August 17, 2007Publication date: February 21, 2008Inventors: Guenther Huchler, Werner Rall, Uwe Ries
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Patent number: 7332602Abstract: The present invention relates to pyridyl substituted heterocycles and hydro isomers thereof and pharmaceutical compositions thereof that inhibit replication and/or proliferation of HCV virus. The present invention also relates to the use of the pyridyl heterocycles and hydro isomers thereof and/or pharmaceutical compositions comprising the compounds to treat or prevent HCV infections.Type: GrantFiled: November 21, 2006Date of Patent: February 19, 2008Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, John Partridge, Henry H. Lu
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Patent number: 7329656Abstract: This invention is directed to Arylthiobenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention.Type: GrantFiled: September 21, 2005Date of Patent: February 12, 2008Assignee: H. Lundbeck A/SInventors: Mohammad R. Marzabadi, Yu Jiang, Chien-An Chen, Kai Lu, Kim Andersen
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Patent number: 7323462Abstract: Compounds of formula (I), (Ia) and (Ib) useful as a medicament.Type: GrantFiled: December 2, 2003Date of Patent: January 29, 2008Assignee: Pfizer Inc.Inventors: Charlotte Moira Norfor Allerton, Andrew Douglas Baxter, Andrew Simon Cook, David Hepworth, Stephen Kwok-Fung Wong
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Patent number: 7317007Abstract: The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.Type: GrantFiled: September 2, 2005Date of Patent: January 8, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Alexander Flohr, Aubry Kern Miller, Roger David Norcross, Claus Riemer
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Patent number: 7314874Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: September 15, 2004Date of Patent: January 1, 2008Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Wenrong Huang, Robert M. Scarborough, deceased
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Patent number: 7314872Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula I: wherein Q is morpholinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.Type: GrantFiled: August 18, 2004Date of Patent: January 1, 2008Assignee: IRM LLCInventors: Hong Liu, Arnab Chatterjee, David C. Tully, Phillip Alper, Badry Bursulaya, Jianhua Guo, David H. Woodmansee, Daniel Mutnick, Donald S. Karanewsky, Yun He
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Patent number: 7288658Abstract: The present invention relates to a process for the manufacture of compounds of formula wherein the substituents are as described herein which comprises the steps of a) reacting a compound of formula with a compound of formula to form a compound of formula b) converting the OH/?O function of compounds of formula XIV/XIVa into a leaving group P with a reagent containing a leaving group, selected from POCl3, PBr3, MeI and (F3CSO2)2O to form a compound of formula wherein P is halogen or trifluoromethanesulfonate; c) substituting R2 for the leaving group P by reacting compound XV with HR2 to form a compound of formula and d) hydrolyzing the nitrile function in an acidic medium selected from H2SO4, HCl and acetic acid, to form a compound of formula I The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds which have NK-1 antagonist activity.Type: GrantFiled: July 9, 2004Date of Patent: October 30, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Wolfgang Goehring, Peter John Harrington, Lewis M Hodges, David A Johnston, Goesta Rimmler
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Patent number: 7288548Abstract: Compounds of formula I wherein X, Y, Z, W, R1 and R2 as defined herein, or pharmaceutically acceptable salts, hydrates or solvates thereof, are useful for the modulation of CCR5 chemokine receptor activity.Type: GrantFiled: September 10, 2004Date of Patent: October 30, 2007Assignee: ViroChem Pharma, Inc.Inventors: Laval Chan Chun Kong, Ming-Qiang Zhang, Christophe Moinet, Marc Courchesne, Thumkunta Jagadeeswar Reddy
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Patent number: 7282500Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, use as Raf Kinase Inhibitors and treatment methods for neurotraumatic diseases and cancer.Type: GrantFiled: May 20, 2002Date of Patent: October 16, 2007Assignee: SmithKline Beecham P.L.C.Inventors: David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson
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Patent number: 7279491Abstract: Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: GrantFiled: October 23, 2003Date of Patent: October 9, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Richard L. Apodaca, Curt A. Dvorak, Chandravadan R. Shah, Wei Xiao
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Patent number: 7279470Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.Type: GrantFiled: December 13, 2002Date of Patent: October 9, 2007Assignee: Novo Nordisk A/SInventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
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Publication number: 20070213314Abstract: Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.Type: ApplicationFiled: January 3, 2007Publication date: September 13, 2007Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
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Patent number: 7265112Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2 and B are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases in which HGF/SF or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role.Type: GrantFiled: December 29, 2004Date of Patent: September 4, 2007Assignee: Angion Biomedica Corp.Inventors: David E. Zembower, David A. Eiznhamer
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Patent number: 7253192Abstract: This invention is concerned with compounds of the formula I: wherein one of R5, R6 and R7 is and X1, X2, R1 to R12, m, n and o are as defined in the description, and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists.Type: GrantFiled: June 30, 2005Date of Patent: August 7, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer
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Patent number: 7241758Abstract: Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: October 15, 2002Date of Patent: July 10, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Ming-Hong Hao, Sanxing Sun
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Patent number: 7230098Abstract: Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided.Type: GrantFiled: February 26, 2004Date of Patent: June 12, 2007Assignee: Sugen, Inc.Inventors: Jingrong Jean Cui, Dilip Bhumralkar, Iriny Botrous, Ji Yu Chu, Lee A. Funk, Cathleen Elizabeth Hanau, G. Davis Harris, Lei Jia, Joanne Johnson, Stephen A. Kolodziej, Pei-Pei Kung, Xiaoyuan (Sharon) Li, Jason (Qishen) Lin, Jerry Jialun Meng, Mitchell David Nambu, Christopher G. Nelson, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube, Allison Walter, Fang-Jie Zhang, Jennifer Zhang
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Patent number: 7214714Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.Type: GrantFiled: April 26, 2002Date of Patent: May 8, 2007Assignee: Taisho Pharmaceutical Co. Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
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Patent number: 7179806Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, m, and Q have the meanings given in the disclosure, to a plurality of processes for preparing these substances, and to their use for controlling pests.Type: GrantFiled: November 22, 2001Date of Patent: February 20, 2007Assignee: Bayer Cropscience AGInventors: Andrew Plant, Thomas Seitz, Johannes Rudolf Jansen, Christoph Erdelen, Andreas Turberg, Olaf Hansen
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Patent number: 7169779Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: September 8, 2003Date of Patent: January 30, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Guy Bemis, Huai Gao, Ghotas Evindar
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Patent number: 7160877Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower-alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.Type: GrantFiled: June 22, 2004Date of Patent: January 9, 2007Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Patent number: RE40245Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: April 28, 2004Date of Patent: April 15, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul S. Charifson, Dean Stamos, Yusheng Liao, Michael C. Badia, Martin Trudeau