Patents Represented by Attorney, Agent or Law Firm Mark W. Russell
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Patent number: 8329905Abstract: This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.Type: GrantFiled: February 5, 2010Date of Patent: December 11, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Kelvin H. Yong, Ilia A. Zavialov, Jianguo Yin, Xiaoyong Fu, Thiruvettipuram K. Thiruvengadam
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Patent number: 8273790Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.Type: GrantFiled: February 10, 2012Date of Patent: September 25, 2012Assignee: Schering CorporationInventors: Tiruvettipuram K. Thiruvengadam, Anantha Sudhakar, Ngiap Kie Lim, Daw-Iong Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green
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Patent number: 8258319Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.Type: GrantFiled: June 24, 2011Date of Patent: September 4, 2012Assignee: Schering CorporationInventors: George G. Wu, Anantha Sudhakar, Tao Wang, Ji Xie, Frank X. Chen, Marc Poirier, Mingsheng Huang, Vijay Sabesan, Daw-long Kwok, Jian Cui, Xiaojing Yang, Tiruvettipuram K. Thiruvengadam, Jing Liao, Ilia Zavialov, Hoa N. Nguyen, Ngiap Kie. Lim
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Patent number: 8153664Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: GrantFiled: October 2, 2007Date of Patent: April 10, 2012Assignee: Schering CorporationInventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Patent number: 8138180Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.Type: GrantFiled: June 30, 2010Date of Patent: March 20, 2012Assignee: Schering CorporationInventors: Tiruvettipuram K. Thiruvengadam, Anantha Sudhakar, Ngiap Kie Lim, Daw-long Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green
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Patent number: 8022088Abstract: Substituted bicyclic and tricyclic modified himbacine derivative of the formula: or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein En, Fn, Gn, Zn, Jn, X, R3, R9, R10, R11, R32, R33, B and Het are herein defined are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other agents is also claimed.Type: GrantFiled: June 27, 2007Date of Patent: September 20, 2011Assignee: Schering CorporationInventors: Mariappan V. Chelliah, Samuel Chackalamannil, Yan Xia
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Patent number: 8003803Abstract: Fused-ring, heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein ? represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: GrantFiled: April 11, 2007Date of Patent: August 23, 2011Assignee: Schering CorporationInventors: Yan Xia, Samuel Chackalamannil
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Patent number: 7989653Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.Type: GrantFiled: July 17, 2009Date of Patent: August 2, 2011Assignee: Schering CorporationInventors: George G. Wu, Anantha Sudhakar, Tao Wang, Ji Xie, Frank X. Chen, Marc Poirier, Mingsheng Huang, Vijay Sabesan, Daw-Iong Kwok, Jian Cui, Xiaojing Yang, Tiruvettipuram K. Thiruvengadam, Jing Liao, Ilia Zavialov, Hoa N. Nguyen, Ngiap Kie Lim
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Patent number: 7888377Abstract: Monocyclic and bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein Gn, Jn, R3, R8, R9, R10, R11, R32, R33, B and Het are herein defined are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other agents is also claimed.Type: GrantFiled: March 27, 2007Date of Patent: February 15, 2011Assignee: Schering CorporationInventors: Mariappan V. Chelliah, Samuel Chackalamannil, Yan Xia
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Patent number: 7888369Abstract: This application provides for oxazolisoquinoline derivatives of the formula or a pharmaceutically acceptable salt of said compound wherein: B is —CH?CH—; M is —C(R1)(R2)—; and the remaining substituents are as defined in the specification as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. This application also provides for combination therapy with the compounds of Ib or pharmaceutically acceptable salts thereof with other cardiovascular agents.Type: GrantFiled: December 20, 2006Date of Patent: February 15, 2011Assignee: Schering CorporationInventors: Samuel Chackalamannil, Yuguang Wang
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Patent number: 7776889Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein An, En, Mn, Un, Gn, Jn, Kn, R9, R10, R11, R32, R33, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: GrantFiled: March 29, 2006Date of Patent: August 17, 2010Assignee: Schering CorporationInventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia
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Patent number: 7741289Abstract: The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating atherosclerosis, hypercholesterolemia, or sitosterolemia, and for lowering plasma levels of sterols and/or stanols.Type: GrantFiled: April 22, 2008Date of Patent: June 22, 2010Assignee: Schering CorporationInventors: Duane A. Burnett, John W. Clader, Wayne Vaccaro
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Patent number: 7732413Abstract: The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating atherosclerosis, hypercholesterolemia, or sitosterolemia, and for lowering plasma levels of sterols and/or stanols.Type: GrantFiled: April 24, 2008Date of Patent: June 8, 2010Assignee: Schering CorporationInventors: Duane A. Burnett, John W. Clader
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Patent number: 7700592Abstract: In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as ?2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the ?2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.Type: GrantFiled: February 13, 2007Date of Patent: April 20, 2010Assignee: Schering CorporationInventors: Kevin D. McCormick, Christopher W. Boyce, Neng-Yang Shih, Chia-Yu Huang, Robert G. Aslanian, Salem Fevrier, Bo Liang, Rong-qiang Liu, Ruiyan Liu, Pietro Mangiaracina, Manuel de Lera Ruiz, Younong Yu, Lisa Guise-Zawacki, Junying Zheng
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Patent number: 7635705Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(?O)—, —C(?S)—, —(CH2)q—, —C(?NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula: where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, —C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with othType: GrantFiled: June 19, 2006Date of Patent: December 22, 2009Assignee: Schering CorporationInventors: Robert G. Aslanian, Michael Y. Berlin, Christopher W. Boyce, Jianhua Chao, Manuel de Lera Ruiz, Pietro Mangiaracina, Kevin D. McCormick, Stuart B. Rosenblum, Neng-Yang Shih, Daniel M. Solomon, Wing C. Tom, Henry A. Vaccaro, Junying Zheng, Xiaohong Zhu, Mwangi W. Mutahi
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Patent number: 7612058Abstract: The present invention provides compositions, therapeutic combinations and methods including: (a) at least one peroxisome proliferator-activated receptor activator; and (b) at least one substituted azetidinone or substituted ?-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols.Type: GrantFiled: November 29, 2004Date of Patent: November 3, 2009Assignee: Schering CorporationInventor: Wing-Kee Philip Cho
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Patent number: 7560449Abstract: The present invention provides methods for treating demyelination and associated conditions by administering at least one sterol absorption inhibitor and compositions, therapeutic combinations and methods including: (a) at least one sterol absorption inhibitor; and (b) at least one demyelination treatment which can be useful for preventing or treating demyelination and associated conditions, such as multiple sclerosis.Type: GrantFiled: November 4, 2003Date of Patent: July 14, 2009Assignee: Schering CorporationInventors: Jay S. Fine, Eric McFee Parker
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Patent number: 7531544Abstract: A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:Type: GrantFiled: September 10, 2007Date of Patent: May 12, 2009Assignee: Schering CorporationInventors: Samuel Chackalamannil, Yuguang Wang, Craig D. Boyle, Andrew W. Stamford
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Patent number: 7482468Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: n is 2-5; R is R3-aryl, R3-heteroaryl, R3-cycloalkyl, R3-heterocycloalkyl, alkyl, haloalkyl, —OR4, —SR4 or —S(O)1-2R5; R1 and R2 are H or optionally substituted phenyl or optionally substituted and X is —O— or —S—; or R1 and R2, together with the carbon atoms to which they are attached form optionally substituted and X is —O—, —S— or —NR7—; Z is and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I; also disclosed are methods of treating allergy, allergy-induced airway responses, congestion, obesity and metabolic syndrome using the compounds of Formula I, as well as combinations with other drugs useful for treating those diseases.Type: GrantFiled: January 19, 2006Date of Patent: January 27, 2009Assignee: Schering CorporationInventors: Robert G. Aslanian, Wing C. Tom, Xiaohong Zhu
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Patent number: 7459442Abstract: The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating atherosclerosis, hypercholesterolemia, or sitosterolemia, and for lowering plasma levels of sterols and/or stanols.Type: GrantFiled: April 24, 2008Date of Patent: December 2, 2008Assignee: Schering CorporationInventors: Duane A. Burnett, John W. Clader