Abstract: Compounds of formula (I) which are optionally substituted 2-(&ohgr;,&ohgr;-diarylalkyl)-4,5-dihydro-1H-imidazoles and 2-(&ohgr;,&ohgr;-diarylalkyl)-1,4,5,6-tetrahydropyrimidines and salts thereof with inorganic and organic acids have interesting pharmacological properties. Thus, the compounds are useful in the treatment of type 2 diabetes.
Type:
Application
Filed:
November 9, 2001
Publication date:
September 19, 2002
Inventors:
Henrik Sune Andersen, Palle Jakobsen, Peter Madsen
Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: 1
Type:
Application
Filed:
January 31, 2002
Publication date:
September 5, 2002
Applicant:
Pfizer Inc.
Inventors:
Anthony Marfat, Michael William McKechney
Abstract: Compositions and methods are described for hydrating terminal alkynes catalytically in anti-Markovnikov fashion. The compositions comprise a transition metal complex including at least one organic ligand having at least two heteroatoms, wherein the heteroatoms are directly bonded or located one atom away. Preferably, at least one of the heteroatoms is nitrogen, which is typically provided as part of a heterocyclic ring. Other preferred heteroatoms include S, P, N, As or Se. A particularly preferred catalyst employs a P-linked imidazole ligand bound to Ru. Such complexes have a controlled adaptable proton transfer ability and/or a hydrogen bonding ability making them particularly useful as chemical reaction facilitators.
Abstract: The present invention discloses novel substituted imidazole compounds which have either or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.
Type:
Application
Filed:
September 18, 2001
Publication date:
August 1, 2002
Inventors:
Robert G. Aslanian, Stuart B. Rosenblum, Mwangi Wa Mutahi, Neng-Yang Shih, John J. Piwinski
Abstract: The present invention provides of method of preparing phenyl-substituted azoles. This method uses an efficient ligand-accelerated Ullmann coupling reaction of anilines with azoles. The coupling products are useful for preparing factor Xa inhibitors.
Type:
Application
Filed:
July 25, 2001
Publication date:
July 25, 2002
Inventors:
Jiacheng Zhou, Pasquale N. Confalone, Hui-Yin Li, Philip Ma, Lynette M. Oh, Lucius T. Rossano, Charles G. Clark, Chris Teleha
Abstract: Compounds and methods of treating or preventing bone disorders including osteoporosis, rheumatoid arthritis, and metastatic bone disease are provided. The inventive compounds comprise a bone targeting moiety and a payload. The payload portion of these inventive compounds inhibit the proton pump of osteoclasts, thereby, reducing bone resorption.
Type:
Grant
Filed:
December 18, 2000
Date of Patent:
July 16, 2002
Assignee:
Ariad Pharmaceuticals, Inc.
Inventors:
Manfred Weigele, David C. Dalgarno, John Iuliucci, Terence P. Keenan, Tomi K. Sawyer
Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor antagonists, and which are represented by Formula I: 1
Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment of cardiovascular or related diseases and in the treatment of symptoms thereof.
Abstract: There is provided a stereospecific process for the preparation of essentially enantiomerically pure imidazolinone herbicides having the R-configuration via (R)2-amino-2, 3-dimethylbutyronitrile.
Abstract: The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I):
that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H.
This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
Type:
Grant
Filed:
December 6, 2000
Date of Patent:
June 18, 2002
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
David A. Nugiel, David J. Carini, Susan V. Di Meo, Eddy W. Yue
Abstract: Neuroprotective agents are disclosed having the following structure:
wherein R1, R2, R3, R4 and R5 are as defined herein. Such compounds have utility in the treatment of conditions which benefit from administration of neuroprotective agents generally, including treatment of central and peripheral nervous condition as well as for promoting nerve cell differentiation. Methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more of the compounds of this invention.
Type:
Grant
Filed:
November 27, 2000
Date of Patent:
June 4, 2002
Assignee:
Nippon Kayaku Co., Ltd.
Inventors:
Moorthy S. S. Palanki, Shripad S. Bhagwat, Hiroshi Sato, Paul E. Erdman, Mary Doubleday
Abstract: 1 The present invention relates to compound of formula (1), wherein Ar1 represents (A), or (B), or (C); R12 and R13 are independently hydrogen or C1-4 alkyl; Ar2 is phenyl or heteroaryl; p is 0 or 1; Ar3 is phenyl, pyridinyl, pyridazinyl, pyrimidyl or pyrazynyl the ring being substituted on ring carbon atoms by R2 and (CH2)nR3 and wherein Ar3 is attached to Ar1C(R12)R13CH(Ar2)O— by a ring carbon atoms; R2 is a group of formula (2), or R2 represents a lactone of formula (3), the group of formula (2) or (3) having L or D configuration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R3 is phenyl or heteroaryl; and R5-R9, m and n are as defined in the specification; or a pharmaceutically acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use is in cancer therapy.
Abstract: This invention relates to peptide-containing &agr;-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.
Type:
Application
Filed:
June 12, 2001
Publication date:
May 9, 2002
Applicant:
Cephalon, Inc.
Inventors:
Sankar Chatterjee, John P. Mallamo, Ron Bihovsky, Gregory J. Wells
Abstract: Derivatives of tetrahydropyridines (or 4-hydroxypiperidines)-butylazols of formula (I), wherein R1, R2 and R3, which are similar or different, represent each of them hydrogen, halogen, alkyl C1-C4, trifluoromethyl, hydroxyl, alkoxyl, or two adjacent radicals can form a ring; A is a C atom and the dotted line represents an additional bond, or A is a C atom joined to a hydroxyl group and the dotted line represents absence of additional bond; Z1 is N or CR4; Z2 is N or CR5; Z4 is N or CR7; and R4, R5, R6 and R7, which different, represent hydrogen, halogen, alkyl C1-C4, aryl or substituted aryl, or two adjacent radicals can form part of another ring. These derivatives are useful for the treatment of acute pain, neuropathic pain or nociceptive pain in mammals, including human beings.
Type:
Grant
Filed:
February 13, 2001
Date of Patent:
May 7, 2002
Assignee:
Laboratorios Del Dr. Esteves, S.A.
Inventors:
Ramon Merce-Vidal, Jordi Frigola-Constansa
Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
Type:
Application
Filed:
December 12, 2000
Publication date:
December 20, 2001
Inventors:
Jinhua J. Song, Nathan K. Yee, Suresh R. Kapadia
Abstract: A method for the prophylaxis or treatment of conditions for which 5-HT1-like agonists are indicated comprising the administration of therapeutically-effective amount of compounds of formula (I) 1
Type:
Application
Filed:
January 12, 2001
Publication date:
December 13, 2001
Inventors:
Robert John Blade, Yih Sang Pang, David Lawrence Selwood
Abstract: A compound represented by the formula (I):
wherein R1 is an optionally substituted heterocyclic group; R2 is optionally substituted aryl or heterocyclic group; R3 is hydrogen, alkyl, alkenyl, or alkynyl; R4 is hydrogen, alkyl, alkoxy, halogen, nitro, cyano, or halogenated alkyl; M is oxygen, S(O)i wherein i is 0, 1, or 2, NR5 wherein R5 is hydrogen, alkyl, or acyl, —Q—N═C(R6)—, —B—C(R8)═N—, —CH═N—N═C(R9)—, or —CH═N—A—(CR10R11)m—; and n is 0, 1, or 2, an intermediate for producing the same and an agrochemical composition containing the same as an active ingredient.
Abstract: This invention provides a compound of the following formula:
or the pharmaceutically acceptable salts thereof, wherein
Ar is heteroaryl; X1 and X2 are independently selected from halo, C1-C4 alkyl, hydroxy, C1-C4 alkoxy, amino, C1-C4 alkanoyl, carboxy, carbamoyl, cyano, nitro, mercapto, (C1-C4 alkyl)thio, (C1-C4 alkyl)sulfinyl, (C1-C4 alkyl)sulfonyl, aminosulfonyl, or the like; R1 is selected from hydrogen, straight or branched C1-C4 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, phenyl , heteroaryl and the like; R2 and R3 are independently selected from hydrogen, halo, C1-C4 alkyl, phenyl and the like; or R1 and R2 can form, together with the carbon atom to which they are attached, a C5-C7 cycloalkyl ring; and m and n are independently 0, 1, 2 or 3.
These compounds and pharmaceutical compositions containing such compounds are useful as analgesics and anti-inflammatory agents.
Type:
Grant
Filed:
February 5, 1999
Date of Patent:
October 30, 2001
Assignee:
Pfizer Inc.
Inventors:
Yoshiyuki Okumura, Yoshinori Murata, Takashi Mano
Abstract: Disclosed are aryl and heteroaryl substitated pyridino compounds. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
Type:
Grant
Filed:
June 15, 2000
Date of Patent:
October 2, 2001
Assignee:
Neurogen Corporation
Inventors:
Guolin Cai, Gang Liu, Pamela A. Albaugh
Abstract: This invention is directed to a compound of formula I which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
Abstract: A compound represented by general formula (I) or a salt thereof, a process for producing the same, an intermediate for the production thereof, and a bactericide (fungicide) containing the same as the active ingredient wherein R1 represent optionally substituted aryl, optionally substituted heterocycle, mono- or di-substituted methyleneamino, optionally substituted (substituted imino)methyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, substituted carbonyl or substituted sulfonyl; R2 represents alkyl, alkenyl, alkynyl or cycloalkyl; R3 represents optionally substituted heterocycle; R4 represents hydrogen, alkyl, alkoxy, halogen, nitro, cyano or haloalkyl; M represents oxygen, S(O)i (i being 0, 1 or 2), NR16 (R16 being hydrogen, alkyl or acyl) or a single bond; n represents 0 or 1, provided n represent 1 when R3 represents imidazol-1-yl or 1H-1,2,4-triazol-1-yl; and the symbol˜represents the E form, Z form or a mixture thereof.
Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae:
wherein Z1, Z2, R1, R2, R3, R4, R5, R6, and R7 are defined herein. These compounds are useful as anti-coagulants.
Abstract: Compounds of general formula (1) are described:
wherein
═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—;
L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1;
Z is a group (A), (B), (C) or (D):
wherein
Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms;
Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12
Type:
Grant
Filed:
June 20, 1995
Date of Patent:
June 12, 2001
Assignee:
Celltech Therapeutics Limited
Inventors:
Graham John Warrellow, Ewan Campbell Boyd, Rikki Peter Alexander
Abstract: The present invention relates to the compounds of general formula
used as medicaments possessing therapeutic activity for the treatment of anxiety, psychosis, epilepsy, convulsion, motoricity problems, amnesia, cerebrovascular diseases or senile dementia.
Type:
Grant
Filed:
February 26, 1998
Date of Patent:
May 15, 2001
Assignee:
Laboratorios Del Dr. Esteve, S.A.
Inventors:
Ramon Merce-Vidal, Jordi Frigola-Constansa
Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
Type:
Grant
Filed:
January 11, 2000
Date of Patent:
April 24, 2001
Assignee:
Berlex Laboratories, Inc.
Inventors:
Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
Type:
Grant
Filed:
October 22, 1998
Date of Patent:
March 6, 2001
Assignee:
Idun Pharmaceuticals, Inc.
Inventors:
Donald S. Karanewsky, Robert J. Ternansky
Abstract: A dye represented by the following formula (1);
Formula (1)
wherein A represents an acidic nucleus, L1, L2 and L3 represent a methine group, n represents 0, 1 or 2, Z represents a nonmetalic atom group necessary to form a heterocyclic group by bonding with a nitrogen atom included in the above formula (1), Y represents a substituent represented by the following formula (2) or a heterocyclic group;
Formula (2)
wherein R1 and R2 represent an alkyl group, and R1 and R2 may form a ring by bonding with each other, R3 represents a hydrogen atom or an electron withdrawing group: said dye represented by the above formula (1) has at least one carboxy group or one alkylsulfonamide group in an aromatic ring portion of its molecular structure.
Abstract: A compound selected from the group consisting of a compound of the formula
wherein the substituents are defined as in the specification having antagonist properties to histamine H3-receptors.
Type:
Grant
Filed:
April 6, 2000
Date of Patent:
July 31, 2001
Assignees:
Institut National del la Sante et de la Recherche
Medicale, Societe Civile Bioprojet
Inventors:
Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Jeanne-Marie Lecomte, Charon R. Ganellin, Abdellatif Fkyerat, Wasyl Tertiuk, Walter Schunack, Ralph Lipp, Holger Stark, Katja Purand