Patents Represented by Attorney Baerbel R. Brown
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Patent number: 7276520Abstract: Certain novel bicyclic N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: March 22, 2004Date of Patent: October 2, 2007Assignee: Merck & Co., Inc.Inventors: Ravi P. Nargund, Zhixiong Ye, Liangqin Guo
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Patent number: 7160886Abstract: Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 27, 2004Date of Patent: January 9, 2007Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Liangqin Guo, Qingmei Hong, Ravi P. Nargund, Patrick G. Pollard, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye
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Patent number: 7115628Abstract: Certain novel bridged piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: July 12, 2002Date of Patent: October 3, 2006Assignee: Merck & Co., Inc.Inventors: Zhixiong Ye, Khaled J. Barakat, Liangqin Guo, Ravi P. Nargund, Iyassu K. Sebhat
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Patent number: 7105526Abstract: The present invention relates to novel benzimidazole derivatives which are useful as neuropeptide Y receptor antagonists.Type: GrantFiled: June 18, 2003Date of Patent: September 12, 2006Assignee: Banyu Pharmaceuticals Co., Ltd.Inventors: Norikazu Otake, Minoru Moriya, Yoshio Ogino, Kenji Matsuda, Yoshikazu Nagae, Akio Kanatani, Takehiro Fukami
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Patent number: 7015235Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 25, 2002Date of Patent: March 21, 2006Assignee: Merck & Co., Inc.Inventors: Mark T. Goulet, Ravi P. Nargund, Iyassu K. Sebhat, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner, Zhixiong Ye, Jonathan R. Young, Raman K. Bakshi
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Patent number: 7012084Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 25, 2002Date of Patent: March 14, 2006Assignee: Merck & Co., Inc.Inventors: Mark T. Goulet, Ravi P. Nargund, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner
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Patent number: 6998488Abstract: A novel process is provided for the preparation of 4-aryl piperidines, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obesity, diabetes, male sexual dysfunction, and female sexual dysfunction.Type: GrantFiled: March 8, 2004Date of Patent: February 14, 2006Assignee: Merck & Co., Inc.Inventors: Genevieve N. Boice, Karen M. Conrad, Edward G. Corley, Louis Matty, Jr., Jerry A. Murry, Cecile G. Savarin
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Patent number: 6939966Abstract: The present invention is directed to radiolabeled neuropeptide Y Y5 receptor antagonists which are useful for the labeling and diagnostic imaging of neuropeptide Y Y5 receptors in mammals.Type: GrantFiled: July 19, 2002Date of Patent: September 6, 2005Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: H. Donald Burns, Raymond E. Gibson, Terence G. Hamill, Takehiro Fukami
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Patent number: 6924291Abstract: This invention relates to a process for making spiro isobenzofuranone compounds by coupling of an aminopyrazine fragment with a spirolactone piece.Type: GrantFiled: January 22, 2002Date of Patent: August 2, 2005Assignee: Merck & Co., Inc.Inventors: Zhiquo Jake Song, Matthew Mangzhu Zhao
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Patent number: 6818658Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 3, 2003Date of Patent: November 16, 2004Assignee: Merck & Co., Inc.Inventors: Feroze Ujjainwalla, Lin Chu, Mark T. Goulet, Bonnie Louridas, Matthew J. Wyvratt, Daniel Warner
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Patent number: 6767915Abstract: Certain novel 4-substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: January 27, 2003Date of Patent: July 27, 2004Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Khaled J. Barakat, Yingjie Lai, Ravi P. Nargund, Brenda L. Palucki, Min K. Park, Iyassu K. Sebhat, Zhixiong Ye, Arthur A. Patchett
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Patent number: 6638942Abstract: Compounds of general structural formula I are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.Type: GrantFiled: August 26, 2002Date of Patent: October 28, 2003Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ying-Duo Gao, Douglas J. MacNeil, Lihu Yang, Nancy R. Morin, Takehiro Fukami, Akio Kanatani, Takahiro Fukuroda, Yasuyuki Ishii, Masaki Ihara
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Patent number: 6605720Abstract: This invention relates to processes for making spirolactone compounds analogous to formula I:Type: GrantFiled: January 23, 2003Date of Patent: August 12, 2003Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Kenji Maeda, Shinji Kato, Takehiko Iida, David M. Tschaen
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Patent number: 6555552Abstract: The present invention relates compounds of the formula (I): wherein X represents hydrogen or a C1-4alkyl group optionally substituted by a hydroxy group; Y represents hydrogen, C1-6alkyl or C3-7cycloalkyl; Z is —CR9R10CH2— or —CH2CR9R10—; R represents hydrogen, fluorine, hydroxy, C1-6alkyl or C1-6alkoxy; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: April 1, 2002Date of Patent: April 29, 2003Assignee: Merck Sharp & Dohme Ltd.Inventors: Janusz Jozef Kulagowski, Piotr Antoni Raubo, Christopher George Thomson
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Patent number: 6495559Abstract: Compounds of general structural formula I such as that shown in structural formula II are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.Type: GrantFiled: June 29, 2001Date of Patent: December 17, 2002Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ying-Duo Gao, Douglas J. MacNeil, Lihu Yang, Nancy R. Morin, Takehiro Fukami, Akio Kanatani, Takahiro Fukuroda, Yasuyuki Ishii, Masaki Ihara
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Patent number: 6436962Abstract: Arylhydantoin derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.Type: GrantFiled: September 27, 2000Date of Patent: August 20, 2002Assignee: Merck & Co., Inc.Inventors: Jacob M. Hoffman, Mark G. Bock, Robert M. DiPardo, Linda S. Payne, Michael A. Patane
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Patent number: 6432931Abstract: The present invention relates to oral compositions and methods for inhibiting bone resoprtion in a mammal while counteracting the occurrence of potentially adverse gastrointestinal effects. The compositions useful herein comprise the combination of a pharmaceutically effective amount of a nitrogen-containing bisphosphonate or a pharmaceutically-acceptable salt thereof and a pharmaceutically effective amount of an isoprenoid compound.Type: GrantFiled: June 21, 1999Date of Patent: August 13, 2002Assignee: Merck & Co., Inc.Inventors: Alfred A. Reszka, Edward S. Scolnick
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Patent number: 6410554Abstract: This invention relates to combination therapy for the treatment of benign prostatic hyperplasia comprising an alpha-1a antagonist and an endothelin antagonist. More specifically, the use of a selective alpha-1a adrenergic receptor antagonist in combination with a subtype non-selective endothelin antagonist provides relief of lower urinary tract symptoms in patients with symptomatic prostatism or benign prostatic hyperplasia. This combination therapy improves lower urinary tract symptoms including increasing urine flow rate, decreasing residual urine volume and improving overall obstructive and irritative symptoms in patients with benign prostatic hyperplasia or symptomatic prostatism.Type: GrantFiled: March 23, 1999Date of Patent: June 25, 2002Assignee: Merck & Co., Inc.Inventors: Theodore P. Broten, Peter K. S. Siegl, Steven A. Nichtberger
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Patent number: 6387893Abstract: Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.Type: GrantFiled: September 27, 2000Date of Patent: May 14, 2002Assignee: Merck & Co., Inc.Inventors: Ben E. Evans, Jacob M. Hoffman, Kevin F. Gilbert, Kenneth E. Rittle
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Patent number: 6372911Abstract: A process for preparing a &bgr;-hydroxy carbamate product is disclosed. The process comprises reacting an olefin compound containing at least one carbon-carbon double bond with a carbamate in an aqueous solvent and in the presence of a base, an osmium catalyst, a co-oxidant selected from a halohydantoin, a haloisocyanuric acid, and an alkali metal salt of a haloisocyanuric acid, and optionally an asymmetric ligand, to form a reaction mixture containing the &bgr;-hydroxy carbamate product. The process optionally further comprises treating the &bgr;-hydroxy carbamate product with additional base to form an oxazolidinone. The oxazolidinones are useful as chiral auxiliary agents and as intermediates for the formation of pharmaceutically active substances such as alpha 1 a adrenergic receptor antagonists. A process for preparing nitrogen-functionalized derivatives of the oxazolidinones is also disclosed.Type: GrantFiled: January 13, 2000Date of Patent: April 16, 2002Assignee: Merck & Co., Inc.Inventors: Nancy Barta, Robert D. Larsen, Daniel R. Sidler, Steven A. Weissman