Piperazines (i.e., Fully Hydrogenated 1,4-diazines) Patents (Class 544/358)
  • Patent number: 7388026
    Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.
    Type: Grant
    Filed: September 2, 2005
    Date of Patent: June 17, 2008
    Assignee: Immunogen, Inc.
    Inventors: Robert Yongxin Zhao, Ravi V. J. Chari
  • Patent number: 7381821
    Abstract: The present invention relates to new enantiomerically pure piperazine derivatives of formula (I) wherein Y represents hydroxy or a leaving group and n is 1, 2, 3, 4 or 5, and to their use as synthesis intermediates, especially for the preparation of pharmaceutically active compounds
    Type: Grant
    Filed: January 20, 2004
    Date of Patent: June 3, 2008
    Assignee: UCB, S.A.
    Inventors: Célal Ates, Emile Cavoy, Didier Bouvy
  • Patent number: 7381727
    Abstract: The invention concerns compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds and their therapeutic use.
    Type: Grant
    Filed: January 22, 2007
    Date of Patent: June 3, 2008
    Assignee: Sanofi-Aventis
    Inventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
  • Publication number: 20080125442
    Abstract: This invention relates to a genus of compounds, represented by the formula (I) diagrammed below, wherein the meanings of R1, R2, R3, R4, R5, R6, R7, R8, D and n are indicated therein, which are inhibitors of cathepsin K. These compounds are useful for treating or preventing atherosclerosis and atherosclerotic cardiovascular disease.
    Type: Application
    Filed: January 17, 2006
    Publication date: May 29, 2008
    Inventor: Michael David Percival
  • Patent number: 7371743
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: February 11, 2005
    Date of Patent: May 13, 2008
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
  • Patent number: 7371777
    Abstract: The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. Wherein a, b and c are the same as or different from one another and each represents 0 to 4; R1 to R6 are the same as or different from one another and each represents a hydrogen atom, a hydroxyl group, a cyano group, a halogen atom, etc.; A1 and A2 are the same as or different from each other and each represents a single bond, an oxygen atom, etc.; L, M and T each represent a single bond, an alkylene group having one to six carbon atoms, etc.; W represents a carboxyl group; the partial structure represented by the formula: represents a single bond or a double bond; X represents a single bond, an oxygen atom, —NRx1CQ1O—, etc.; Y represents Y1—Y2— (wherein Y1 represents a 5 to 14-membered aromatic ring having one to four substituents, etc.
    Type: Grant
    Filed: August 16, 2002
    Date of Patent: May 13, 2008
    Assignee: Eisai Co., Ltd.
    Inventors: Richard Clark, Fumiyoshi Matsuura, Eita Emori, Masanobu Shinoda, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Takashi Inoue, Sadakazu Miyashita, Taro Hihara
  • Patent number: 7345168
    Abstract: A simple and economical process for the preparation of polyphosphates of organic bases consists of reacting a mixture of phosphorus pentoxide and at least one organic nitrogen base with at least one compound which releases water accompanied by decomposition under the prevailing conditions in such a molar ratio that upon decomposition of the water-releasing compound at most essentially 2 mol. water are produced per mol. phosphorus pentoxide. Thus-prepared polyphosphates are particularly suitable as flame-protection agents for plastics.
    Type: Grant
    Filed: August 22, 2002
    Date of Patent: March 18, 2008
    Assignee: Chemische Fabrik Budenheim KG
    Inventors: Liselotte Götzmann, legal representative, Hans-Dieter Nagerl, Thomas Futterer, Karl Gotzmann
  • Patent number: 7332495
    Abstract: Arylalkyl ketone piperazine derivatives of the formula: and pharmaceutical compositions comprising the same. Also disclosed are methods for using the compounds as analgesic and sedative agents. The compounds of the present invention have good analgesic and sedative activities but few side effects.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: February 19, 2008
    Assignees: Nhwa Pharma. Corporation, Shanghai Institute of Pharmaceutical Industry
    Inventors: Jianqi Li, Liying Huang, Chunnian Zhang, Xican Tang, Guoyuan Hu
  • Patent number: 7326710
    Abstract: Aralkyl formyl alkyl piperazine derivatives Pharmaceutical compositions comprising the same, and methods of using them as a neuroprotective agent. Pharmaceutical results indicate that these compounds have excellent neuroprotective activities and fewer side effects.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: February 5, 2008
    Assignee: Shanghai Institute of Pharmaceutical Industry
    Inventors: Jianqi Li, Liying Huang, Yang Min, Zhijie Weng, Chunnian Zhang
  • Patent number: 7320978
    Abstract: This invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. The invention further relates to a method for prevention and therapeutic use thereof.
    Type: Grant
    Filed: August 1, 2006
    Date of Patent: January 22, 2008
    Assignee: Sanofi-Aventis
    Inventors: Francis Barth, Joelle Arnaud-Taillades, Christian Congy, Murielle Rinaldi-Carmona
  • Patent number: 7317101
    Abstract: A compound of formula wherein Ac, R1 and R2 have various meanings, a process for a preparation thereof and its use as a pharmaceutical, i.e. as antibacterial agent.
    Type: Grant
    Filed: December 3, 2002
    Date of Patent: January 8, 2008
    Assignee: Sandoz GmbH
    Inventors: Gerd Ascher, Johannes Ludescher
  • Patent number: 7317010
    Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I), wherein: R1, R2, R4, R5, R6, R6a, R7, R8, A and B are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.
    Type: Grant
    Filed: August 18, 2003
    Date of Patent: January 8, 2008
    Assignee: AstraZeneca AB
    Inventor: Jean Claude Arnould
  • Patent number: 7307169
    Abstract: In some embodiments, this invention pertains to isotopically enriched N-substituted piperazines. In some embodiments, this invention pertains to methods for the preparation of isotopically enriched N-substituted piperazines.
    Type: Grant
    Filed: January 5, 2004
    Date of Patent: December 11, 2007
    Assignee: Applera Corporation
    Inventors: Darryl J. C. Pappin, Sasi Pillai, James M. Coull
  • Patent number: 7304155
    Abstract: A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ?Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor ? selective medical treatments.
    Type: Grant
    Filed: December 16, 2002
    Date of Patent: December 4, 2007
    Assignee: N.V. Organon
    Inventor: Hubert Jan Jozef Loozen
  • Patent number: 7297697
    Abstract: A compound of formula I wherein X, Y, X? & Y? are selected from hydrogen, halogen, substituted or unsubstituted alkyl (linear, branched or cyclo), aryl, alkyloxy and haloalkyl group; R1, R2, R3 & R4 are selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: November 20, 2007
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Ajay Sohanlal Midha, Hemant Ashvinbhai Chokshi, Trinadha Rao Chitturi, Rajamannar Thennati
  • Patent number: 7297692
    Abstract: The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
    Type: Grant
    Filed: August 3, 2006
    Date of Patent: November 20, 2007
    Assignee: Sanofi-Aventis
    Inventors: Richard Roux, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
  • Patent number: 7294628
    Abstract: The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4) alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents the aromatic group 1,3-thiazol-2-yl of formula: Preparation process and therapeutic application.
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: November 13, 2007
    Assignee: Sanofi-Aventis
    Inventors: Françoise Bono, Michaël Bosch, Victor Dos Santos, Jean-Marc Herbert, Dino Nisato, Bernard Tonnerre, Jean Wagnon
  • Patent number: 7291633
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia anorexia nervosa or other eating disorders, compulsvie behaviour, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: November 6, 2007
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
  • Patent number: 7271292
    Abstract: The invention relates to a process for continuously, distillatively removing piperazine from an ethylenediamine-piperazine mixture under pressure at elevated temperature, by discharging the ethylenediamine at the top and the piperazine at the bottom of a distillation column. For the purpose of improving the quality of the piperazine, especially its color and color stability, the piperazine is subjected directly to circulation conveying it through an evaporator unit operated at a temperature of from about 160° C. to about 170° C. and returning it into the distillation column. After a residence time of from about 30 min to about 60 min in the circulation system, the piperazine is discharged in vapor form from a side draw in the lower section of the distillation column.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: September 18, 2007
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Jödecke, Ortmund Lang, Gunther van Cauwenberge, Matthias Frauenkron
  • Patent number: 7259186
    Abstract: In one aspect, the present invention relates to a formulation in the form of molecular dispersion comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof and optionally other active substances, ii) a binder component comprising at least one enteric binder, and optionally iii) other physiologically acceptable excipients. In a second aspect, the present invention relates to novel salts of fenofibric acid that are photostable when compared to other salts of fenofibric acid.
    Type: Grant
    Filed: June 30, 2004
    Date of Patent: August 21, 2007
    Assignee: Abbott Laboratories
    Inventors: Russell Drew Cink, Joseph B. Paterson, Jr., Yi Gao, Geoff G. Z. Zhang, Michelle A. Long, John B. Morris, Joerg Rosenberg
  • Patent number: 7244730
    Abstract: A 2-iminopyrrolidine derivative represented by the formula: {wherein ring B represents a benzene ring, pyridine ring, etc.; R101–R103 represent hydrogen, halogen, C1-6 alkyl, etc.; R5 represents hydrogen, C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10—R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc.; and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocyclic ring], etc.}, or a salt thereof.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: July 17, 2007
    Assignee: Eisai Co., Ltd
    Inventors: Shuichi Suzuki, Makoto Kotake, Mitsuaki Miyamoto, Tetsuya Kawahara, Akiharu Kajiwara, Ieharu Hishinuma, Kazuo Okano, Syuhei Miyazawa, Richard Clark, Fumihiro Ozaki, Nobuaki Sato, Masanobu Shinoda, Atsushi Kamada, Itaru Tsukada, Fumiyoshi Matsuura, Yoshimitsu Naoe, Taro Terauchi, Yoshiaki Oohashi, Osamu Ito, Hiroshi Tanaka, Takashi Musya, Motoji Kogushi, Tsutomu Kawada, Toshiyuki Matsuoka, Hiroko Kobayashi, Ken-ichi Chiba, Akifumi Kimura, Naoto Ono
  • Patent number: 7223763
    Abstract: Sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formula II are disclosed and claimed:
    Type: Grant
    Filed: April 30, 2004
    Date of Patent: May 29, 2007
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Pavel Safar, Armin Walser, Stephen James Shimshock
  • Patent number: 7220753
    Abstract: Substituted pyrido[1,2-a]pyrazines of general formula I; wherein Ar and Ar1 represent various carbocyclic and heterocyclic aromatic rings; A represents O, S, SO, SO2, CHOH, C?O, or —(CR3R4); and n is 0–2, as well as precursors thereto, are ligands for dopamine receptor subtypes and serotonin (5HT) within the body and are therefore useful in the treatment of disorders of the dopamine and serotonin systems:
    Type: Grant
    Filed: May 24, 2004
    Date of Patent: May 22, 2007
    Assignee: Pfizer Inc.
    Inventors: Kishor A. Desai, Anton F. Fliri, Mark A. Sanner
  • Patent number: 7217706
    Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.
    Type: Grant
    Filed: February 14, 2002
    Date of Patent: May 15, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
  • Patent number: 7208599
    Abstract: The present invention relates to a process for the preparation of substituted alkanesulfonates by the reaction of an aqueous metal substituted 2-hydroxyethanesulfonate with a nucleophile. 2-Alkylaminoalkanesulfonate is formed when the nucleophile is an amine. The invention also relates to the optimization of reaction conditions to produce an optimum yield.
    Type: Grant
    Filed: October 26, 2004
    Date of Patent: April 24, 2007
    Assignee: Arkema Inc.
    Inventors: Glenn T. Carroll, Gary S. Smith, Gary E. Stringer
  • Patent number: 7202383
    Abstract: There is described compounds of Formula I, and salts, solvates and hydrates thereof: wherein: R1, R2 and R3 are each independently selected from OH, C1-6alkyl, OC1-6alkyl, OC(O)C1-6alkyl, C(O)OC1-6alkyl, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6alkyl), C(O)NHC1-6alkyl, C(O)N(C1-6alkyl)(C1-6alkyl), SH, SC1-6alkyl, NO2, CF3, OCF3 and halogen; and Ar is an aromatic or heteroaromatic group chosen from benzene, naphthalene, quinoline, isoquinoline, indole, pyridine, pyrasine, pyrimidine, imidazole, furan and thiophene, unsubstituted or substituted with 1–4 substituents independently selected from OH, C1-6alkyl, C1-6alkoxy, C1-3alkylenedioxy, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6)(C1-6alkyl), SH, S—C1-6alkyl, NO2, CF3, OCF3 and halogen. The compounds of Formula I are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.
    Type: Grant
    Filed: September 14, 2004
    Date of Patent: April 10, 2007
    Assignee: The Hospital For Sick Children
    Inventors: Chaim Roifman, Peter Demin, Olga Rounova, Tom Grunberger
  • Patent number: 7202244
    Abstract: Disclosed are novel inhibitors of Chk-1 and methods of using the same for therapy.
    Type: Grant
    Filed: May 28, 2003
    Date of Patent: April 10, 2007
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Robert George Boyle, Hassan Julien Imogai, Michael Cherry
  • Patent number: 7193084
    Abstract: The present invention provides a polymorphic form of itraconazole.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: March 20, 2007
    Assignee: Baxter International Inc.
    Inventors: Jane Werling, Mark J. Doty, Christine L. Rebbeck, Joseph Chung Tak Wong, James E. Kipp
  • Patent number: 7189727
    Abstract: Compounds having the general structure III are provided: where D is N or C; W is selected from Z1, Z2, and Z3 are independently selected from CR8 and N; and the other variables have the values described herein. Compounds of formula III have useful properties for controlling diseases related to MC4-R action in humans including obesity and type II diabetes.
    Type: Grant
    Filed: April 5, 2004
    Date of Patent: March 13, 2007
    Assignee: Chiron Corporation
    Inventors: Rustum Boyce, David Duhl
  • Patent number: 7186723
    Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
    Type: Grant
    Filed: August 26, 2002
    Date of Patent: March 6, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Jennifer P. Peckham, William F. Hoffman, Kenneth L. Arrington, Mark E. Fraley, George D. Hartman, Yuntae Kim, Barbara Hanney, Keith L. Spencer
  • Patent number: 7166601
    Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.
    Type: Grant
    Filed: April 26, 2006
    Date of Patent: January 23, 2007
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Sigmond G. Johnson, Ralph A. Rivero
  • Patent number: 7160912
    Abstract: The present invention relates to novel oxazolidinone compounds of formula (I), their stereoisomers, their salts and pharmaceutical compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds, their stereoisomers, their salts and pharmaceutical compositions.
    Type: Grant
    Filed: July 3, 2003
    Date of Patent: January 9, 2007
    Assignees: Dr.Reddy's Laboratories Ltd., Dr. Reddy's Laboratories, Inc.
    Inventors: Natesan Selvakumar, Jagattaran Das, Sanjay Trehan, Javed Iqbal, Magadi Sitaram Kumar, Ramanujam Rajagopalan, Mamidi Naga Venkata Srinivasa Rao
  • Patent number: 7157458
    Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.
    Type: Grant
    Filed: January 31, 2002
    Date of Patent: January 2, 2007
    Assignee: Cryolife, Inc.
    Inventors: Carl W. Gilbert, Eleanor B. McGowan, Kirby S. Black, T. Gregory P. Harper
  • Patent number: 7157585
    Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
    Type: Grant
    Filed: May 11, 2005
    Date of Patent: January 2, 2007
    Assignee: Tularik Limited
    Inventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
  • Patent number: 7153857
    Abstract: Compounds of the formula I useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.
    Type: Grant
    Filed: August 8, 2002
    Date of Patent: December 26, 2006
    Assignee: AstraZeneca AB
    Inventors: Maurice Raymond Verschoyle Finlay, Howard Tucker, David Waterson
  • Patent number: 7148240
    Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.
    Type: Grant
    Filed: August 23, 2001
    Date of Patent: December 12, 2006
    Assignee: Sanofi-Aventis
    Inventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
  • Patent number: 7141573
    Abstract: One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group consisting of D-1 agonists, D-2 agonists, D-3 agonists, D-4 agonists, irreversible monoamine inhibitors, reversible monoamine inhibitors, monoamine transporter inhibitors, COMT inhibitors, MAO inhibitors, and dopamine transporter inhibitors. Moreover, the present invention also relates to combinatorial libraries of polypharmacophoric compounds. Another aspect of the present invention relates to the use of a polypharmacophoric compound in a method of treating a mammal in need thereof. For example, a polypharmacophoric compound of the present invention may be used in a method of treating a mammal afflicted with Alzheimer's Disease, Huntington's Disease, depression, attention deficit disorder, autism, obesity, or inflammation.
    Type: Grant
    Filed: January 11, 2001
    Date of Patent: November 28, 2006
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: Robert N. Hanson, John W. Babich
  • Patent number: 7135472
    Abstract: The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and Het are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said novel 3-heterocyclic benzylamides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: November 14, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Alexandre L'Heureux, Huan He
  • Patent number: 7129240
    Abstract: The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
    Type: Grant
    Filed: April 29, 2004
    Date of Patent: October 31, 2006
    Assignee: Sanofi-Aventis
    Inventors: Richard Roux, Claudine Serradeil-le Gal, Bernard Tonnerre, Jean Wagnon
  • Patent number: 7122567
    Abstract: Heterocyclic amides of formula (1) wherein: Z is CH or nitrogen; R4 and R5 together are either —S—C(R6)?C(R7)— or —C(R7)?C(R6)—S—; R6 and R7 are selected from for example hydrogen, halo, C1-4alkyl, and C1-4alkanoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; r is 1 or 2; Y is —NR2R3 or —OR3; R2 and R3 are selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have va
    Type: Grant
    Filed: March 4, 2003
    Date of Patent: October 17, 2006
    Assignee: AstraZeneca AB
    Inventors: Paul Whittamore, Stuart Norman Lile Bennett, Iain Simpson
  • Patent number: 7112586
    Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.
    Type: Grant
    Filed: February 25, 2005
    Date of Patent: September 26, 2006
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Sigmond G. Johnson, Ralph A. Rivero
  • Patent number: 7112594
    Abstract: Compounds represented by the following general formula (I) wherein ring A is benzene, cyclohexane, pyridine, piperidine, a derivative thereof, imidazole, a derivative thereof, etc.; the ring B represents benzene, cyclohexane, pyrrole or a derivative thereof, furan, thiophene, etc.; R1, R2 and R3 represent each hydrogen, alkyl, halogen, hydroxyl, alkoxy, etc.; W represents hydrogen, alkyl or hydroxycarbonylalkyl; X represents halogen, cyano, nitro, etc.; X? represents hydrogen, halogen, etc.; and Y represents alkyl, hydroxyalkyl, hydroxycarbonylalkyl, aminoalkyl, etc.; salt thereof, and drugs comprising these compounds. Because of having an exellent effect of inhibiting activated lymphocyte proliferation, these compounds are usefull as preventives or remedies for various autoimmune diseases.
    Type: Grant
    Filed: August 9, 2001
    Date of Patent: September 26, 2006
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Hiroyuki Ushio, Youichiro Naito, Naoki Sugiyama, Takafumi Kawaguchi, Makio Ohtsuki, Kenji Chiba
  • Patent number: 7101909
    Abstract: Novel multibinding compounds are disclosed. The compounds of this invention comprise 2–10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel, thereby modulating the biological activities thereof.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: September 5, 2006
    Assignee: Theravance, Inc.
    Inventors: Yu-Hua Ji, Maya Natarajan, John H. Griffin, Thomas E. Jenkins
  • Patent number: 7087604
    Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis, asthma, restinosis, organ transplantation, and cancer.
    Type: Grant
    Filed: March 7, 2003
    Date of Patent: August 8, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventor: Robert J. Cherney
  • Patent number: 7084155
    Abstract: Novel compounds that are useful for targeting chemokine receptors are disclosed. These compounds are complex tertiary amines.
    Type: Grant
    Filed: June 1, 2004
    Date of Patent: August 1, 2006
    Assignee: AnorMED
    Inventors: Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosaria Di Fluri
  • Patent number: 7074794
    Abstract: The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the ?-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: July 11, 2006
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Hiroshi Kitajima, Hiroshi Sakashita, Fumihiko Akahoshi, Yoshiharu Hayashi
  • Patent number: 7067517
    Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: June 27, 2006
    Assignee: Nero Nordisk A/S
    Inventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
  • Patent number: 7049316
    Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.
    Type: Grant
    Filed: October 27, 2003
    Date of Patent: May 23, 2006
    Assignee: Immunogen Inc.
    Inventors: Robert Yongxin Zhao, Ravi V. J. Chari
  • Patent number: 7045520
    Abstract: The invention provides compounds of formula I: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.
    Type: Grant
    Filed: February 7, 2003
    Date of Patent: May 16, 2006
    Assignee: The Curators of the University of Missouri
    Inventors: William J. Welsh, Seong Jae Yu, Anil Nair
  • Patent number: 7030111
    Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: April 18, 2006
    Assignee: Canbas Co., Ltd.
    Inventors: Takumi Kawabe, Hidetaka Kobayashi