Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/476)
  • Patent number: 7569325
    Abstract: A photoresist monomer having a sulfonyl group, a polymer thereof and a photoresist composition containing the same are disclosed. The photoresist monomer is represented by following Formula. wherein, R* is a hydrogen atom or a methyl group, R1 and R2 are independently a C1˜C20 alkyl group, a C4˜C20 cycloalkyl group, a C6˜C20 aryl group or a C7˜C20 arylalkyl group, one of R1 and R2 may not exist, and R1 and R2 can be connected to form a ring.
    Type: Grant
    Filed: October 24, 2007
    Date of Patent: August 4, 2009
    Assignee: Dongjin Semichem Co., Ltd.
    Inventors: Jung-Youl Lee, Geun-Jong Yu, Sang-Jung Kim, Jae-Woo Lee, Deog-Bae Kim, Jae-Hyun Kim
  • Patent number: 7563890
    Abstract: Certain amphiphilic modules comprising 3-24 synthons are provided herein. Each synthon is independently selected from aryl, heteroaryl, alicyclic, and heteroalicyclic substituents, wherein each synthon selected is bonded to the next through a linker to form a closed ring that defines a nanopore. One or more lipophilic moieties and one or more hydrophilic moieties are bonded to one or more of the synthons, resulting in the formation of the desired amphiphilic modules. Those modules may be subsequently linked to one another to form two-dimensional close-packed planar arrays, referred to as nanomembranes. Nanomembranes may be useful in filtering certain ionic species from a solution. Selective passage of particular species is determined, in part, by the size of the module's nanopore and the nature of the lipophilic/hydrophobic species attached thereto. Also provided are methods of making and using amphiphilic modules and nanomembranes.
    Type: Grant
    Filed: August 18, 2005
    Date of Patent: July 21, 2009
    Assignee: Covalent Partners, LLC
    Inventors: Timothy B. Karpishin, Josh Kriesel, Grant Merrill, Donald B. Bivin, Thomas H. Smith, Martin Stuart Edelstein
  • Publication number: 20090131500
    Abstract: The present invention relates to novel porphyrin derivates of formula (I), especially to porphyrins which carry substituted phenyl moieties in meso-position. The porphyrin derivates of the invention are useful as photosensitizers in photodynamic therapy (PDT), especially in photodynamic tumor therapy. Due to their excellent photophysical properties the compounds of formula I are extremely efficient in photodynamic treatment.
    Type: Application
    Filed: March 9, 2007
    Publication date: May 21, 2009
    Inventors: Beate Roeder, Eugeny Ermilov, Norbert Jux, Stefan Jasinski
  • Publication number: 20090069294
    Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.
    Type: Application
    Filed: June 6, 2006
    Publication date: March 12, 2009
    Inventors: Zhuoliang Chen, Mark G. Palermo, Sushil K. Sharma, Troy Smith, Christopher S. Straub, Run-Ming D. Wang, Yaping Wang, Leigh Zawel
  • Patent number: 7485630
    Abstract: Embodiments of this invention provide novel peptidomimetics that contain a macrocycle. Such compounds are neuroprotective and have utility as therapeutic agents for treatment of diseases, injuries and other conditions characterised by neuronal degeneration and/or death. Compounds are also useful for manufacture of medicaments useful for treatment of such conditions.
    Type: Grant
    Filed: March 16, 2004
    Date of Patent: February 3, 2009
    Assignee: Neuren Pharmaceuticals Limited
    Inventors: Paul William Richard Harris, Margaret Anne Brimble
  • Publication number: 20080318905
    Abstract: Prodrugs of parent drugs and methods of making and using the same are described. The prodrugs comprise an amine-containing parent drug moiety and a prodrug moiety, such as methoxyphosphonic acid or ethoxyphosphonic acid. The prodrugs may be employed in therapy for the treatment of various indications, such as pain, and in methods of decreasing the abuse potential of abuse-prone drugs and/or delaying the onset of parent drug activity and/or prolonging parent drug activity as compared to administration of a parent drug.
    Type: Application
    Filed: December 5, 2007
    Publication date: December 25, 2008
    Inventors: Naweed Muhammad, Keith R. Bley
  • Publication number: 20080261938
    Abstract: The present invention relates to tetracyclic indole compounds of formula (I); wherein R1, R2, R14, R15, A, Ar, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
    Type: Application
    Filed: October 25, 2005
    Publication date: October 23, 2008
    Inventors: Caterina Ercolani, Joerg Habermann, Frank Narjes, Simona Ponzi, Michael Rowley, Ian Stansfield
  • Patent number: 7414045
    Abstract: Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: August 19, 2008
    Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Benedetta Crescenzi, Olaf Kinzel, Ester Muraglia, Federica Orvieto, Giovanna Pescatore, Michael Rowley, Vincenzo Summa
  • Publication number: 20080188454
    Abstract: Bicyclic aryl substituted triazoles or heteroaryl 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: Application
    Filed: December 28, 2007
    Publication date: August 7, 2008
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Thilo J. Heckrodt, Joane Litvak
  • Patent number: 7378426
    Abstract: Disclosed are fused heterotricyclic compounds of the following formula I, or an enantiomer, diastereomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of A ring or C ring is a 5-7 membered unsaturated heterocyclic ring. The disclosed compounds are useful as inhibitors of 17?-hydroxysteroid dehydrogenase 3 (17?-HSD3). Also disclosed are methods of using such compounds in the treatment of hormone sensitive diseases such as prostate cancer, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: February 25, 2005
    Date of Patent: May 27, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashvinikumar V. Gavai, Derek J. Norris, Wen-Ching Han, Gregory D. Vite, Brian E. Fink, John S. Tokarski
  • Patent number: 7371772
    Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
    Type: Grant
    Filed: August 7, 2002
    Date of Patent: May 13, 2008
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Mitsuru Shiraishi, Masanori Baba, Katsuji Aikawa, Naoyuki Kanzaki, Masaki Seto, Yuji Iizawa
  • Patent number: 7335677
    Abstract: Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3)2 or CH(CN), and b is 1 or 2. G1 is H or a group according to the formula —CH2—X2—(CH2)a-G3 and G2 is H or a group according to the formula —CH2—(CH29a-G3, provided that one of G1 and G2 is H and the other is not H. X2 is O, S, or CH2, and a is 0, 1 or 2, provided that when a is 1 then X2 is CH2. G3 is a group according to one of general formulae 2-4, where the variables have meaning given in the description. The compounds are useful in the treatment of i.a.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: February 26, 2008
    Assignee: Ferring B.V.
    Inventors: David M. Evans, Doreen M. Ashworth
  • Patent number: 7199248
    Abstract: The present invention relates to a process for preparing a pharmaceutical starting compound compound by hydrolyzing a compound of the general formula (II): Wherein R1 is protected carboxy, R2 is lower alkoxy or higher alkoxy, A1 is an aromatic bivalent group, heterocyclic bivalent group or cyclo (lower) alkane bivalent group, and A2 is an aromatic bivalent group, heterocyclic bivalent group or cyclo (lower) alkane bivalent group, with aqueous potassium hydroxide and by treating with hydrochloric acid.
    Type: Grant
    Filed: August 4, 2003
    Date of Patent: April 3, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyuki Tsuboi, Atsushi Ohigashi, Yoshitaka Shimojo
  • Patent number: 7179802
    Abstract: Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11?-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidernia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: February 20, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Steven H. Olson, James M. Balkovec, Yuping Zhu
  • Patent number: 7148215
    Abstract: The present invention concerns compounds of general formula (I): in which the substituents are as described herein.
    Type: Grant
    Filed: March 18, 2004
    Date of Patent: December 12, 2006
    Assignee: Aventis Pharma S.A.
    Inventors: Andrew James Ratcliffe, Roger John Aitchison Walsh, Tahir Nadeem Majid, Sukanthini Thurairatnam, Shelley Amendola, David John Aldous, John Edward Souness, Conception Nemecek, Sylvie Wentzler, Corinne Venot
  • Patent number: 7122534
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.
    Type: Grant
    Filed: January 23, 2004
    Date of Patent: October 17, 2006
    Assignee: Pfizer Inc
    Inventor: Jotham Wadsworth Coe
  • Patent number: 7105667
    Abstract: Fused heterocylic compounds of the following Formula wherein R1, R2, R5, Z, J1 and J2 are described herein which are useful in treating leukocyte activation-associated disorders.
    Type: Grant
    Filed: November 6, 2002
    Date of Patent: September 12, 2006
    Assignee: Bristol-Myers Squibb Co.
    Inventors: William J. Pitts, Joseph Barbosa, Junqing Guo
  • Patent number: 7087749
    Abstract: Certain 4-aryl-piperidine compounds, including N-substituted 9?-substituted-5-(3-substituted-phenyl)morphans and N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines, pharmaceutical compositions, and methods of their use, inter alia, as opioid antagonists are disclosed.
    Type: Grant
    Filed: March 11, 2004
    Date of Patent: August 8, 2006
    Assignee: Adolor Corporation
    Inventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
  • Patent number: 6984734
    Abstract: The present invention provides an oxidative coupling procedure that allows efficient synthesis of novel cyclo[n]pyrrole macrocycles. Therefore, the present invention provides cyclo[n]pyrroles where n is 6, 7, 8, 9, 10, 11, or 12, and derivatives, multimers, isomers, and ion and neutral molecule complexes thereof as new compositions of matter. A protonated form of cyclo[n]pyrrole displays a gap of up to 700 nm between strong Soret and Q-like absorption bands in the electronic spectrum, demonstrating no significant ground state absorption in the visible portion of the electronic spectrum. Uses of cyclo[n]pyrroles as separation media, nonlinear optical materials, information storage media and infrared filters are provided.
    Type: Grant
    Filed: February 26, 2003
    Date of Patent: January 10, 2006
    Assignee: Board of Regents, The University of Texas System
    Inventors: Jonathan L. Sessler, Daniel Seidel, Frederic R. Bolze, Thomas Koehler
  • Patent number: 6951850
    Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: October 4, 2005
    Assignee: Pfizer, Inc.
    Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
  • Patent number: 6864367
    Abstract: A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a compound represented by the formula: {wherein Z represents an electron-attracting group; W represents optionally substituted ethylene or optionally substituted vinylene; R3 represents hydrogen or an optionally substituted hydrocarbon group; and X represents a divalent group [provided that when W represents optionally substituted vinylene, then —X—CH2—Z is not —X1—X2—CH2—Z (wherein X1 represents sulfur or optionally substituted nitrogen and X2 represents optionally substituted ethylene)]} or a salt thereof, is characterized by subjecting a compound represented by the formula (II) or a salt thereof: (wherein the symbols have the same meanings as the above) to a ring closure reaction in a solvent containing a carbonic diester.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: March 8, 2005
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tomomi Ikemoto, Tatsuya Ito, Kiminori Tomimatsu
  • Patent number: 6858624
    Abstract: This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of nicotine addiction/withdrawal and CNS disorders.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: February 22, 2005
    Assignees: Pfizer, Inc., Pfizer Products, Inc.
    Inventors: Anne E. Hagen, R. Scott Obach
  • Patent number: 6852854
    Abstract: The present invention is directed, in general, to a method for making high yields of functionalized cyclic or acyclic tertiary amine-containing compounds, termed active esters, the functionalized compounds themselves, and diagnostic or therapeutic systems incorporating such compounds. Ester groups are attached to all but one of its Nitrogen atoms of the tertiary amine-containing compound. Therefore, an active agent, in the presence of coupling agent, attaches to the remaining amine via a carboxylate group attached to the amine, to produce high yields of the active ester. The active ester is then combined with a biomolecule, to produce high yields of a bioconjugated product. A metal ion may be chelated to the bioconjugated product to produce a chelating agent for use in either diagnostic or therapeutic applications.
    Type: Grant
    Filed: October 1, 2002
    Date of Patent: February 8, 2005
    Assignee: PsiloQuest Inc.
    Inventors: Zoltan Kovacs, Dhurjati S. Mudigonda, A. Dean Sherry
  • Patent number: 6838557
    Abstract: The present invention is directed, in general, to a method for making high yields of functionalized cyclic or acyclic tertiary amine-containing compounds, termed active esters, the functionalized compounds themselves, and diagnostic or therapeutic systems incorporating such compounds. Ester groups are attached to all but one of its Nitrogen atoms of the tertiary amine-containing compound. Therefore, an active agent, in the presence of coupling agent, attaches to the remaining amine via a carboxylate group attached to the amine, to produce high yields of the active ester. The active ester is then combined with a biomolecule, to produce high yields of a bioconjugated product. A metal ion may be chelated to the bioconjugated product to produce a chelating agent for use in either diagnostic or therapeutic applications.
    Type: Grant
    Filed: October 1, 2002
    Date of Patent: January 4, 2005
    Assignee: Board of Regents The University of Texas System
    Inventors: Zoltan Kovacs, Dhurjati S. Mudigonda, A. Dean Sherry
  • Patent number: 6706702
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.
    Type: Grant
    Filed: August 13, 2002
    Date of Patent: March 16, 2004
    Assignee: Pfizer Inc.
    Inventor: Jotham Wadsworth Coe
  • Publication number: 20040034217
    Abstract: Intermediates A, which are important in the whole synthesis of vindoline; and a method of synthesizing intermediates respectively represented by the general formulae B and C. By the method, the target intermediates are effectively synthesized with satisfactory reproducibility. This synthesis method is especially suitable for mass production.
    Type: Application
    Filed: March 19, 2003
    Publication date: February 19, 2004
    Inventors: Tohru Fukuyama, Hidetoshi Tokuyama
  • Publication number: 20040014753
    Abstract: The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula: 1
    Type: Application
    Filed: June 9, 2003
    Publication date: January 22, 2004
    Applicant: The Procter & Gamble Company
    Inventors: Steven Victor O'Neil, Michael Christopher Laufersweiler, Yili Wang, Kofi Abeka Oppong, David Lindsey Soper, John August Wos, Biswanath De, Thomas Prosser Demuth
  • Publication number: 20030166925
    Abstract: The present invention provides a novel compound having a superior acetylcholinesterase inhibitory action.
    Type: Application
    Filed: November 25, 2002
    Publication date: September 4, 2003
    Inventors: Yoichi Iimura, Takashi Kosasa
  • Patent number: 6482825
    Abstract: This invention provides compounds of formula I and pharmaceutically-acceptable salts thereof, where the substituents are defined in the specification, which are growth hormone secretogogues useful for treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength , mobility, maintenance of skin thickness, metabolic homeostatis or renal homeostasis. Compounds of formula I in combination with: a bisphosphonate such as alendronate; estrogen, estrogens, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions thereof are useful in treating osteoporosis.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: November 19, 2002
    Assignee: Pfizer Inc.
    Inventors: Philip A Carpino, Paul A DaSilva-Jardine, Bruce A Lefker, John A Ragan
  • Patent number: 6472402
    Abstract: Disclosed are compounds of the formula: wherein Ar, R1, W, X and m are substituents as defined herein.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: October 29, 2002
    Assignee: Neurogen Corporation
    Inventors: Raymond F. Horvath, James W. Darrow, George D. Maynard
  • Patent number: 6462035
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.
    Type: Grant
    Filed: August 7, 2000
    Date of Patent: October 8, 2002
    Assignee: Pfizer Inc.
    Inventor: Jotham Wadsworth Coe
  • Patent number: 6444808
    Abstract: Improved synthesis of a macropolycycle, more particularly, of a cross-bridged tetraazamacrocycle.
    Type: Grant
    Filed: April 11, 2001
    Date of Patent: September 3, 2002
    Assignee: The Procter & Gamble Company
    Inventors: George Douglas Hiler, II, Christopher Mark Perkins
  • Publication number: 20020091256
    Abstract: The azepine compound capable of emitting a light by light-irradiation or action of an electric field is represented by the following formula (I) or (II): 1
    Type: Application
    Filed: November 7, 2001
    Publication date: July 11, 2002
    Inventors: Masaru Matsuoka, Kazuko Shirai, Toru Kitaguchi, Shigeki Kambara
  • Patent number: 6410556
    Abstract: Disclosed are novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP, wherein n, m, X, R1, R2, R3, R4, R5, R6, and R7 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
    Type: Grant
    Filed: September 11, 2000
    Date of Patent: June 25, 2002
    Assignees: Novo Nordisk A/S, Ontogen Corporation
    Inventors: Henrik Sune Andersen, Thomas Kruse Hansen, Jesper Lau, Niels Peter Hundahl Møller, Ole Hvilsted Olsen, Frank Urban Axe, Yu Ge, Daniel Dale Holsworth, Todd Kevin Jones, Luke Milburn Judge, Wiliam Charles Ripka, Barry Zvi Shapira, Roy Teruyuki Uyeda
  • Patent number: 6410534
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: June 25, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Ian M. Bell, Douglas C. Beshore, Theresa M. Williams
  • Patent number: 6403561
    Abstract: A compound of formula wherein the substituents are defined as in the specification and salts or hydrates thereof is disclosed as well as a method of treating disorders associated with the inactivation or excessive degradation of cholecystokinin.
    Type: Grant
    Filed: February 19, 1998
    Date of Patent: June 11, 2002
    Assignee: Institut National de la Sante et de la Recherche Medicale (Inserm)
    Inventors: Christiane Rose, Froylan Vargas, Pierre Bourgeat, Jean-Charles Schwartz, Paul Beaumont Bishop, Ramesh B. Bambal, Charon Robin Ganellin, Bertrand Leblond, Andrew N. J. Moore, Lihua Zhao, Suzanne Chan
  • Publication number: 20020058652
    Abstract: The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacyclic compounds, including pyridyl olefinic cycloalkylamines and pyridyl acetylenic cycloalkylamines. The present invention also relates to prodrug derivatives of the compounds of the present invention.
    Type: Application
    Filed: April 30, 2001
    Publication date: May 16, 2002
    Inventors: Gary Maurice Dull, Jeffrey Daniel Schmitt, Balwinder Singh Bhatti, Craig Harrison Miller
  • Patent number: 6376664
    Abstract: Cyclic bis benzimidazole ligands of the following formula are formed by contacting a (2-aminophenyl)-benzimidazole-4-carboxaldehyde ethylene acetal or a (2-nitrophenyl)-benzimidazole-4-benzaldehyde with an acid optionally in the presence of a metal or a metal salt. wherein R1 and R2 may be the same or different and are selected from H, an alkyl having 1 to 10 carbon atoms, a benzyl group, a substituted 2-ethylphenyl group, a carbonyl group, a phenyl substituent, a tosyl group, and an alkylsulfonate group; R3 and R4 may be the same or different and are selected from H, methyl, and ethyl; and R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, and R18 may be the same or different and are selected from H, alkyl having 1 to 10 carbon atoms, fluoride, chloride, bromide, iodide, nitro, amino, a carboxylate, an ester, and a phenyl group.
    Type: Grant
    Filed: March 17, 2000
    Date of Patent: April 23, 2002
    Assignee: The Ohio State University
    Inventors: Michael K. Chan, Wai H. Kwok, Huichang Zhang, Maosheng Duan
  • Patent number: 6362186
    Abstract: Disclosed are compounds of the formula: wherein Ar, R1, W and X are substituents as defined herein, which compounds are (1) antagonists at CRF1 receptors and are, therefore, useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety; and (2) are neuropeptide Y1, receptor antagonists, and are therefore useful in the treatment of a variety of clinical conditions which are characterized by the presence of an excess of neuropeptide Y.
    Type: Grant
    Filed: November 6, 2000
    Date of Patent: March 26, 2002
    Assignee: Neurogen Corporation
    Inventors: Raymond F. Horvath, James W. Darrow, George D. Maynard
  • Patent number: 6350760
    Abstract: Certain novel 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. Also provided are methods of treating sexual dysfunction with a compound that is a selective agonist of MC-4R over any other human melanocortin receptor.
    Type: Grant
    Filed: June 1, 2000
    Date of Patent: February 26, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, Khaled J. Barakat, Ravi P. Nargund, Brenda L. Palucki, Arthur A. Patchett, Iyassu Sebhat, Zhixiong Ye, Leonardus H. T. Van Der Ploeg
  • Publication number: 20010056088
    Abstract: Hydroxamic acids having the formula 1
    Type: Application
    Filed: June 14, 2001
    Publication date: December 27, 2001
    Applicant: American Cyanamid Company
    Inventors: Jeremy I. Levin, James M. Chen
  • Patent number: 6303543
    Abstract: A compound represented by the formula (I) or its salt and herbicidal and desiccant use thereof: wherein X, Y are independently hydrogen, halogen, cyano, nito, or (C1-6)haloalkyl; Z is oxygen or sulfur; and
    Type: Grant
    Filed: May 15, 2000
    Date of Patent: October 16, 2001
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: David A. Pulman, Bai-Ping Ying, Shao-Yong Wu, Sandeep Gupta, Masamitsu Tsukamoto, Takahiro Haga
  • Patent number: 6225464
    Abstract: Improved synthesis of a macropolycycle, more particularly, of a cross-bridged tetraazamacrocycle.
    Type: Grant
    Filed: September 7, 1999
    Date of Patent: May 1, 2001
    Assignee: The Procter & Gamble Company
    Inventors: George Douglas Hiler, II, Christopher Mark Perkins
  • Patent number: 6191272
    Abstract: The invention relates to a process for the preparation of endo-nortropine using 8-benzyl-nortropan-3-one perchlorate, as well as the latter product. Endo-nortropine is the key product for the production of important azonia-spironortropanol esters, which are used as pharmaceuticals, particularly spasmolytics. There are three different synthesis methods for the preparation of said intermediate, which lead to different disadvantages. These problems are obviated by the present invention through the two-stage treatment of 8-benzyl-nortropan-3-one perchlorate with catalytically activated hydrogen, the starting product initially being prehydrogenated in aqueous suspension and at atmospheric pressure and ambient pressure with a palladium catalyst, at the end of the reaction the catalyst is recovered by filtration, the filtrate is passed over an anion exchanger and the now alkaline reacting solution is rendered turbulent at 1000 to 1500 r.p.m.
    Type: Grant
    Filed: January 19, 2000
    Date of Patent: February 20, 2001
    Assignee: Dr. Robert Pfleger Chemische Fabrik, GmbH
    Inventors: Rolf Sachse, Albert Schaupp
  • Patent number: 6147085
    Abstract: Disclosed are compounds of the formula: ##STR1## wherein Ar, R.sup.1, W and X are substituents as defined herein, which compounds are (1) antagonists at CRF.sub.1 receptors and are, therefore, useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety; and (2) are neuropeptide Y.sub.1 receptor antagonists, and are therefore useful in the treatment of a variety of clinical conditions which are characterized by the presence of an excess of neuropeptide Y.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: November 14, 2000
    Assignee: Neurogen Corporation
    Inventors: Raymond F. Horvath, James W. Darrow, George D. Maynard
  • Patent number: 6140317
    Abstract: There are described compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are as defined in the description, Q is heterocyclyl boned via a ring nitrogen atom and having the formula IA ##STR2## wherein R.sub.3 and R.sub.4 and m and n are as defined in the description, the ring marked A is a heterocyclyl having 5 to 9 ring atoms and having at least one saturated bond, it being possible for a further ring hetero atom selected from O and S to be present in addition to the bonding nitrogen atom, the ring system marked B is a free or benzo-, thieno-, furo-, pyrrolo- or dihydropyrrolo-fused carbocyclic ring having from 5 to 9 carbon atoms that is fused to the ring A and may be unsaturated, partially saturated or fully saturated, and the bond marked by a parallel dotted line between the ring systems marked A and B is either a single bond or a double bond, and a salt thereof where at least one salt-forming group is present.
    Type: Grant
    Filed: July 22, 1998
    Date of Patent: October 31, 2000
    Assignee: Novartis AG
    Inventors: Peter Traxler, Jorg Frei, Guido Bold
  • Patent number: 6084098
    Abstract: Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH;R.sub.1, R.sub.2 and R.sub.3 independently represent organic or inorganic substituents;R.sub.4 and R.sub.4 ' independently represent hydrogen, alkyl or form a ring with the atom to which they are attached;R.sub.5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R.sub.6 represents hydrogen or alkyl; or R.sub.5 and R.sub.6 form a ring together with the atoms to which they are attached; andR.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 independently represent hydrogen or alkyl,which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
    Type: Grant
    Filed: February 26, 1999
    Date of Patent: July 4, 2000
    Assignee: Neurogen Corporation
    Inventors: Renata Xavier Kover, Silva Terdjanian, Jennifer Tran, Andrew Thurkauf
  • Patent number: 6048980
    Abstract: The present invention relates to the novel compound, 1,4,7,10-tetraazabicyclo[8.2.2]tetradecan-2-one of formula (I), its preparation and the use thereof for the preparation of tetraazamacrocycles.
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: April 11, 2000
    Assignee: Dibra S.p.A
    Inventors: Maria Argese, Giorgio Ripa
  • Patent number: 6030964
    Abstract: Compounds of the formula and compounds of the formula ##STR1## or their salts have the potent ability to bind to retinoic acid receptors thus useful in treating psoriasis and rheumatoid arthritis.
    Type: Grant
    Filed: June 29, 1998
    Date of Patent: February 29, 2000
    Assignee: Eisai Co., Ltd.
    Inventors: Shigeki Hibi, Kouichi Kikuchi, Hiroyuki Yoshimura, Mitsuo Nagai, Katsuya Tagami, Shinya Abe, Ieharu Hishinuma, Junichi Nagakawa, Norimasa Miyamoto, Takayuki Hida, Aichi Ogasawara, Seiko Higashi, Kenji Tai, Takashi Yamanaka, Makoto Asada
  • Patent number: 5889022
    Abstract: Novel indole, indoline and quinoline derivatives of formula (I) processes for their preparation, pharmaceutical compositions containing them, and their use in medicine is disclosed. A structurally distinct class of compounds have now been discovered and have been found to exhibit 5HT.sub.1-D antagonist activity. In a first aspect, the present invention therefore provides a compound of formula (I) or a salt thereof, in which P is a 5-7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, A, B, m, R.sup.1 -R.sup.8 are defined in the application.
    Type: Grant
    Filed: June 20, 1996
    Date of Patent: March 30, 1999
    Assignee: SmithKline Beecham, p.l.c.
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman