Patents Represented by Attorney Patricia A. Shatynski
-
Patent number: 8338472Abstract: The present invention is directed to hexahydrocyclopentylf]imidazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: February 16, 2009Date of Patent: December 25, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: William P. Dankulich, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
-
Patent number: 8309544Abstract: The present invention relates to spiroindalone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: GrantFiled: May 12, 2008Date of Patent: November 13, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Joan M. Fletcher, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
-
Patent number: 8299048Abstract: The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: February 24, 2009Date of Patent: October 30, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
-
Patent number: 8278304Abstract: The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: GrantFiled: March 12, 2009Date of Patent: October 2, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina B. Madsen-Duggan, Thomas F. Walsh
-
Patent number: 8247415Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: April 2, 2009Date of Patent: August 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
-
Patent number: 8207221Abstract: The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.Type: GrantFiled: July 16, 2008Date of Patent: June 26, 2012Assignee: Schering CorporationInventors: Mengwei Hu, Younong Yu, Michael P. Dwyer, Arthur G. Taveras, Agnes Kim-Meade, Jianguo Yin, Xiaoyong Fu, Timothy L. McAllister, Shuyi Zhang, Kevin Klopfer
-
Patent number: 7994189Abstract: The present invention relates to dihydropyridine derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, phenyl, (1-5C)heteroaryl R2, R3 are independently (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkoxy, (24C)alkenyloxy, (2-4C)alkynyloxy, halogen X is SO2, CH2, C(O) or X is absent R4 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-6C)cycloalkyl, (3-6C)cycloalkenyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl, (2-6C)heterocycloalkyl(14C)alkyl, (6-1 OC)aryl, (6-10C)aryl(1-4C)alkyl, (1-9C)heteroaryl or (1-9C)heteroaryl(14C)alkyl. The compounds are useful for the treatment of fertility disorders.Type: GrantFiled: May 4, 2005Date of Patent: August 9, 2011Assignee: N.V. OrganonInventors: Nicole Corine Renee Van Straten, Gerritdina Geziena Gerritsma, Lars Anders Van Der Veen
-
Process and intermediates for the synthesis of 2-(quinolin-5-yl)-4,5 disubstituted-azole derivatives
Patent number: 7985860Abstract: This application discloses a novel process to synthesize 2-(Quinolin-5yo)-4,5-Disubstituted-Azole derivatives, which may be used, for example, as PDE IV inhibitor compounds in pharmaceutical preparations.Type: GrantFiled: August 10, 2007Date of Patent: July 26, 2011Assignee: Schering CorporationInventors: Timothy D. Cutarelli, Xiaoyong Fu, Timothy L. McAllister, Michael R. Reeder, Jianguo Yin, Kelvin H. Yong, Shuyi Zhang -
Patent number: 7956189Abstract: Disclosed are maleate, tosylate, fumarate, and oxalate salts of the compound 5-(1(S)-Amino-2-Hydroxyethyl)-N-[(2,4-Difluorophenyl)-Methyl]-2-[8-Methoxy-2-(Trifluoromethyl)-5-Quinoline]-4-Oxazolecarboxamide, represented by Formula I, and methods of preparing the same.Type: GrantFiled: August 10, 2007Date of Patent: June 7, 2011Assignee: Schering CorporationInventors: Xiaoming Chen, Xiao Chen, Jianguo Yin, Xiaoyong Fu, David J. Blythin, Rongze Kuang, Ho-Jane Shue, Scott Trzaska, Chee-Wah Tang, Vincenzo Liotta, Zaher Shabani
-
Patent number: 7919505Abstract: The present invention relates to the compound of the formula To methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.Type: GrantFiled: July 10, 2007Date of Patent: April 5, 2011Assignee: Schering CorporationInventors: Pauline C. Ting, Joe F. Lee, Kung-I Feng, Michael R. Reeder, Scott T. Trzaska, Man Zhu, Chen Mao, Dimitar L. Filipov, Dimitrios N. Zarkadas
-
Patent number: 7351698Abstract: Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue.Type: GrantFiled: May 3, 2004Date of Patent: April 1, 2008Assignee: Merck & Co., Inc.Inventors: Robert S. Meissner, James J. Perkins
-
Patent number: 7268153Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.Type: GrantFiled: June 3, 2005Date of Patent: September 11, 2007Assignee: Merck & Co., Inc.Inventors: Barbara Hanney, Yuntae Kim, Michael R. Krout, Robert S. Meissner, Helen J. Mitchell, Jeffrey Musselman, James J. Perkins, Jiabing Wang
-
Patent number: 7217720Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient.Type: GrantFiled: September 2, 2004Date of Patent: May 15, 2007Assignee: Merck & Co., Inc.Inventors: Robert S. Meissner, Helen J. Mitchell
-
Patent number: 7196076Abstract: Compounds of structural formula (I) are disclosed as useful for modulating the androgen receptor (AR) in a tissue selective manner in a patient in need of such modulation, and in particular for antagonizing AR in the prostate of a male patient or in the uterus of a female patient and agonizing AR in bone and/or muscle tissue. These compounds are useful in the treating conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.Type: GrantFiled: October 15, 2002Date of Patent: March 27, 2007Assignee: Merck & Co., Inc.Inventors: Paul J. Coleman, Lou Anne Neilson
-
Patent number: 7186838Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, cancer cachexia, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.Type: GrantFiled: March 7, 2003Date of Patent: March 6, 2007Assignee: Merck & Co., Inc.Inventors: Robert S. Meissner, James J. Perkins
-
Patent number: 7153862Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as ?v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ?v?3 and/or ?v?5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.Type: GrantFiled: July 10, 2003Date of Patent: December 26, 2006Assignee: Merck & Co., Inc.Inventors: Ben C. Askew, Michael J. Breslin, Mark E. Duggan, John H. Hutchinson, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Michael A. Patane
-
Patent number: 7109191Abstract: The present invention relates to novel benzazepinone derivatives, their synthesis, and their use as ?v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ?v?3 and ?v?5 and are therefore useful for inhibiting bone resorption, treating and/or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.Type: GrantFiled: April 29, 2002Date of Patent: September 19, 2006Assignee: Merck & Co., Inc.Inventors: Robert S. Meissner, Paul J. Coleman, Mark E. Duggan, George D. Hartman, Jiabing Wang, John H. Hutchinson
-
Patent number: 7074930Abstract: Amine salts of 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3-(6-methoxy-pyridin-3-yl)propionic acid are potent antagonists of the integrin ?v?3 receptor and are useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salts as well as pharmaceutical compositions containing the salts and methods of using the salts.Type: GrantFiled: November 1, 2002Date of Patent: July 11, 2006Assignee: Merck & Co., IncInventors: Kenneth M. Wells, Nobuyoshi Yasuda, Yaling Wang
-
Patent number: 7056909Abstract: The present invention relates to novel chain-fluorinated alkanoic acid derivatives thereof, their synthesis, and their use as ?v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ?v?3 and/or ?v?5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.Type: GrantFiled: July 20, 2001Date of Patent: June 6, 2006Assignee: Merck & Co., Inc.Inventor: Jiabing Wang
-
Patent number: RE39056Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.Type: GrantFiled: September 11, 1996Date of Patent: April 4, 2006Assignee: Merck & Co, Inc.Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman