Abstract: A pyrrolesulfonamide derivative having the following formula (I):
is provided wherein P, A, Y, l, Z1 and Z2 are as described herein, wherein the derivative has strong serotonin-2 receptor antagonistic action, low toxicity and fewer side effects, and its use as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.
Abstract: An enantiomeric-resolving process for obtaining (1R,2S)-1-amino-2-vinylcyclopropyl carboxylic acid methyl ester by use of an esterase, and especially Alcalase®, is disclosed.
Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula
wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.
Type:
Grant
Filed:
May 20, 1999
Date of Patent:
July 24, 2001
Assignee:
Bristol-Myers Squibb Company
Inventors:
Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
Abstract: Novel aromatic polycyclic retinoid-type derivatives of general formula (I),
wherein groupings R3 and R4 attached to the double bond between carbons 11 and 12 are cis groupings, and pharmaceutical and cosmetic compositions containing same, are disclosed.
Type:
Grant
Filed:
July 15, 1998
Date of Patent:
July 24, 2001
Assignee:
Centre Europeen de Bioprospective-Ceb
Inventors:
Bertrand Leblond, Francis Darro, Abdallah Devine, Véronique Sales-Sallans, Pierre Duhamel, Robert Kiss, Alain-René Schoofs, Pierre Germain, Bernard Pourrias
Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1):
where X and Y are selected from groups that include O, S, and NH; and Ar1, Ar2 and Ar3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteroaryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.
Type:
Grant
Filed:
June 8, 1999
Date of Patent:
July 24, 2001
Assignee:
Texas Biotechnology Corporation
Inventors:
Ming Fai Chan, Vitukudi Narayanaiyengar Balaji, Rosario Silvestre Castillo, Adam Kois, Bore Gowda Raju, Chengde Wu
Abstract: A process for preparing 1H-indole-3-glyoxamides useful for inhibiting SPLA2 and novel intermediates useful in the preparation of such compounds.
Abstract: Substituted carbamoyltriazoles of the formula I as defined in the specification and the agriculturally useful salts thereof, processes for their preparation and their use as herbicides.
Type:
Grant
Filed:
March 17, 1999
Date of Patent:
July 24, 2001
Assignee:
BASF Aktiengesellschaft
Inventors:
Ernst Baumann, Cyrill Zagar, Uwe Kardorff, Ulf Misslitz, Karl-Otto Westphalen, Helmut Walter, Gerhard Hamprecht
Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovis replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.
Abstract: A series of bioactive analogs of (+)-CC-1065 (1) and the duocarmycins 2 and 3 are synthesized. The bioactive analogs include either iso-CI or iso-CBI (6 and 7) as a DNA alkylation subunit. Conjugated to the DNA alkylating subunits are a variety of DNA binding subunits. The bioactive analogs maintain their DNA selectivity and display enhanced reactivity.
Abstract: New compounds have the formula:
wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.
Type:
Grant
Filed:
February 16, 2000
Date of Patent:
July 17, 2001
Assignee:
Hoffman-La Roche Inc.
Inventors:
Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
Abstract: Compounds, or solvates or salts thereof, of formula (I):
selective delta opioid agonists and antagonists and may be of therapeutic utility as analgesics, immunosuppressants to prevent rejection in organ transplant and skin graft, anti-allergic and anti-inflammatory agents, brain cell protectants, agents for treating drug and alcohol abuse, gastritis, diarrhoea, cardiovascular and respiratory diseases, cough, mental illness, epilepsy and, in general, agents for the treatment of those pathological conditions which, customarily, can be treated with agonists and antagonists of the delta opioid receptor.
Abstract: There is provided compounds of formula I,
wherein R1, R2, R3, Rx, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.
Abstract: This invention describes the new, nonsteroidal gestagens of general formula I
in which A, B, Ar, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.
Type:
Grant
Filed:
May 29, 1998
Date of Patent:
June 12, 2001
Assignee:
Schering Aktiengesellschaft
Inventors:
Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
Abstract: The present invention relates to inhibition of angiogenesis and the treatment of diseases mediated by angiogenesis. Particularly, the invention relates to the inhibition of neovascularization and the treatment of cancer. The invention further relates to the use of cytochalasin derivatives for the inhibition of angiogenesis and the treatment of angiogenesis associated diseases.
Type:
Grant
Filed:
September 28, 1999
Date of Patent:
June 5, 2001
Assignee:
The Children's Medical Center Corp.
Inventors:
Taturo Udagawa, Robert J. D'Amato, Jamshed H. Shah
Abstract: The present invention relates to leukotriene A4 hydrolase inhibitors containing compounds represented by the formula [I] or salts thereof as active ingredients,
wherein R1 represents hydrogen, alkyl, phenylalkyl, alkanoyl or benzoyl; R2 and R3 each represent hydrogen or alkyl; R4 represents hydroxyl, alkoxy, phenylalkoxy, amino, alkylamino or phenylalkylamino; R5 represents phenylalkyl or naphthylalkyl; “Z” represents sulfur or oxygen; “A” represents alkylene; and “n” represents 0, 1 or 2; providing that the phenyl ring in R1 can be substituted by alkyl, alkoxy or halogen, and that the phenyl ring or the naphthyl ring in R5 can be substituted by alkyl, cycloalkyl, alkoxy, alkylthio or halogen.
Abstract: The present invention relates to arylpyrrole particles which are prepared by a process in which the particles are aged and milled, and pesticidal suspension concentrate compositions comprising them. The size of the particles of this invention remains surprisingly stable during storage.
Type:
Grant
Filed:
April 6, 1999
Date of Patent:
June 5, 2001
Assignee:
American Cyanamid Co.
Inventors:
Mimi Yih-Pei Chou Schaaf, Steven Brunt, Jian James Xu, Andrew Evelyn Goldsmith, Anthony Francis Walker, Patrick C. Mowery, Edward S. Donoghue, Srinivasan Rajan
Abstract: Compound of formula (I):
wherein:
R1 and R2 each independently of the other represents hydrogen or alkyl,
A represents alkylene, alkenylene or alkynylene,
G1 represents
wherein R3 and R4 each independently of the other represents hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, optionally substituted aryl or optionally substituted arylalkyl, or G1 represents heterocycloalkyl optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, nitrile, carboxy, alkoxycarbonyl, carbamoyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, and
which medicinal products containing the same/are useful as serotonin-reuptake inhibitors.
Type:
Grant
Filed:
January 25, 2000
Date of Patent:
May 29, 2001
Assignee:
Adir et Compagnie
Inventors:
Gilbert Lavielle, Olivier Muller, Bernard Cimetiere, Mark Millan, Alain Gobert, Jean-Michel Rivet
Abstract: The invention is a process for the preparation of cyclic-sulfur fluorine containing oxazolidinone antibacterial agents which utilizes the important tetrahydrothiopyran-o-fluorinated carbamate of formula (IV)
Abstract: Benzimidazole derivatives of the formula (I):
wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R′ group; R1 is hydrogen or an optionally substituted hydrocarbon residue; R2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R′ is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is —O—, —S(O)m— or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes,