Patents by Inventor Manuel de Lera Ruiz
Manuel de Lera Ruiz has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 8324213Abstract: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: GrantFiled: October 6, 2009Date of Patent: December 4, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Youngong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
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Publication number: 20110251207Abstract: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: October 6, 2009Publication date: October 13, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Adandan Palani, Michael Y. Berlin, Robert G. Aslanian
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Publication number: 20110190247Abstract: In its many embodiments, the present invention provides a novel class of cyclopropylchromene derivatives as modulators of a2C adrenergic receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the a2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: August 3, 2009Publication date: August 4, 2011Applicant: Schering CorporationInventors: Younong Yu, Manuel De Lera Ruiz, Christopher W. Boyce, Kevin D. McCormick
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Patent number: 7985748Abstract: 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: March 12, 2010Date of Patent: July 26, 2011Assignees: Pharmacopeia Drug Discovery, Inc., Scheeing CorporationInventors: Kevin D. McCormick, Christopher W. Boyce, Neng-Yang Shih, Robert G. Aslanian, Pietro Mangiaracina, Manuel de Lera Ruiz, Younong Yu, Purakkattle Biju, Chia-Yu Huang, Bo Liang, Ruiyan Liu, Rong-Qiang Liu, Lisa Guise-Zawacki
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Publication number: 20110166124Abstract: The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or aired fasting glucose.Type: ApplicationFiled: July 21, 2009Publication date: July 7, 2011Inventors: Kevin D. McCormick, Robert G. Aslanian, Pietro Mangiaracina, Michael Y. Berlin, Manuel De Lera Ruiz, Christopher W. Boyce, Jianhua Chao, Pauline C. Ting, Junying Zheng, Stuart B. Rosenblum
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Publication number: 20110136790Abstract: The present invention relates to novel Tricyclic Heterocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Heterocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R1 is formula (Ia), (Ib) or (Ic); R2 is alkvl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl. any of which can be optionally substituted with R11; M1 is —CH—. —C(halo)- or —N—; Y is —C(O)—, —S—. —S(O)—, —S(O)2—, —CH2— or —O—, such that Y is not —O— when an adjacent atom is N.Type: ApplicationFiled: July 21, 2009Publication date: June 9, 2011Inventors: Manuel De Lera Ruiz, MIchael Y Berlin, Junying Zheng, Robert G. Aslanian, Kenvin D. McCormick, Qingbel Zeng
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Publication number: 20110130385Abstract: The present invention relates to novel bicyclic heterocycle derivatives, pharmaceutical compositions comprising the bicyclic heterocycle derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R1 is: I, Ia, Ib ou Ic. R2 is alkyl, alkenyl, aryl, cycloalkyl.Type: ApplicationFiled: July 21, 2009Publication date: June 2, 2011Inventors: Manuel De Lera Ruiz, Michael Y. Berlin, Junying Zheng, Robert G. Aslanian, Kevin D. Mccormick
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Patent number: 7879880Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein M1 is M2 is N; X is a bond, optionally substituted alkylene, alkenylene, —O—, —CH2N(R12)—, —N(R12)CH2—, —N(R12)—, —NHC(O)—, —OCH2—, —CH2O—, or —S(O)0-2—; and Y is —(CH2)1-2—, —C(?O)—, —C(?NOR13)— or —SO0-2—; or M1 is N; M2 is N or CH; X is a bond, alkylene, alkenylene, —C(O)—, —NHC(O)—, —OC(O)— or —S(O)1-2—; Y is —(CH2)1-2—, —C(?O)— or —SO0-2—; and when M2 is CH, Y is also Y is —O— or —C(?NOR13)—; Z is a bond or optionally substituted alkylene or alkenylene; U and W are CH, or one is CH and one is N; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; and compositions and methods of treating obesity, metabolic syndrome and a cognition deficit disorder, alone or in combinatType: GrantFiled: December 19, 2006Date of Patent: February 1, 2011Assignee: Schering CorporationInventors: Daniel M. Solomon, Robert G. Aslanian, Michael Y. Berlin, Manuel de Lera Ruiz, Kevin D. McCormick, Mwangi W. Mutahi, Wing C. Tom
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Patent number: 7846946Abstract: 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 otheType: GrantFiled: July 22, 2009Date of Patent: December 7, 2010Assignee: Schering Plough CorporationInventors: Robert G. Aslanian, Michael Y. Berlin, Christopher W. Boyce, Jianhua Chao, Manuel de Lera Ruiz, Pietro Mangiaracina, Kevin D. McCormick, Mwangi W. Mutahi, Stuart B. Rosenblum, Neng-Yang Shih, Daniel M. Solomon, Wing C. Tom, Henry A. Vaccaro, Junying Zheng, Xiaohong Zhu
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Publication number: 20100197562Abstract: In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: February 11, 2008Publication date: August 5, 2010Applicants: SCHERING CORPORATION AND PHARMACOPEIA, LLC, PHARMACOPEIA, INC.Inventors: Manuel De lera Ruiz, Kevin D. McCormick, Christopher W. Boyce, Robert G. Aslanian, Younong Yu, Pietro Mangiaracina, Junying Zheng, Michael Y. Berlin, Stephanie L. Ciesla, Chia-yu Huang, Bo Liang
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Publication number: 20100173823Abstract: 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: ApplicationFiled: March 12, 2010Publication date: July 8, 2010Inventors: Kevin D. McCormick, Christopher W. Boyce, Neng-Yang Shih, Robert G. Aslanian, Pietro Mangiaracina, Manuel de Lera Ruiz, Younong Yu, Purakkattle Biju, Chia-Yu Huang, Bo Liang, Ruiyan Liu, Rong-Qiang Liu, Lisa Guise-Zawacki
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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: 7638531Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(?O)—, —C(?NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combinatioType: GrantFiled: December 19, 2006Date of Patent: December 29, 2009Assignee: Schering CorporationInventors: Mwangi W. Mutahi, Robert G. Aslanian, Michael Y. Berlin, Christopher W. Boyce, Manuel de Lera Ruiz, Kevin D. McCormick, Daniel M. Solomon, Henry A. Vaccaro, Junying Zheng, Purakkattle Biju, Younong Yu, Wei Zhou, Xiaohong Zhu
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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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HETEROATOM-LINKED SUBSTITUTED PIPERIDINES AND DERIVATIVES THEREOF USEFUL AS HISTAMINE H3 ANTAGONISTS
Publication number: 20090286830Abstract: 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 otheType: ApplicationFiled: July 22, 2009Publication date: November 19, 2009Inventors: 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 -
Patent number: 7531660Abstract: The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its use in treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease. The invention also relates to the use of a combination of the Compound of Formula I with additional therapeutic agents for treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease.Type: GrantFiled: August 10, 2007Date of Patent: May 12, 2009Assignee: Schering CorporationInventors: Manuel de Lera Ruiz, Robert G. Aslanian, Michael Y. Berlin, Kevin D. McCormick, Chander S. Celly
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Publication number: 20080058370Abstract: The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its use in treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease. The invention also relates to the use of a combination of the Compound of Formula I with additional therapeutic agents for treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease.Type: ApplicationFiled: August 10, 2007Publication date: March 6, 2008Inventors: Manuel de Lera Ruiz, Robert Aslanian, Michael Berlin, Kevin McCormick, Chander Celly
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Patent number: 7332604Abstract: The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its use in treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease. The invention also relates to the use of a combination of the Compound of Formula I with additional therapeutic agents for treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease.Type: GrantFiled: September 19, 2006Date of Patent: February 19, 2008Assignee: Schering CorporationInventors: Manuel de Lera Ruiz, Robert G. Aslanian, Michael Y. Berlin, Kevin D. McCormick
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Publication number: 20080039439Abstract: 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: ApplicationFiled: February 13, 2007Publication date: February 14, 2008Inventors: Kevin McCormick, Christopher Boyce, Neng-Yang Shih, Chia-Yu Huang, Robert 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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Publication number: 20070167435Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(?O)—, —C(?NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combinatType: ApplicationFiled: December 19, 2006Publication date: July 19, 2007Inventors: Mwangi Mutahi, Robert Aslanian, Michael Berlin, Christopher Boyce, Manuel de Lera Ruiz, Kevin McCormick, Daniel Solomon, Henry Vaccaro, Junying Zheng, Purakkattle Biju, Younong Yu, Wei Zhou, Xiaohong Zhu