Patents in Class 514/210.020

Matches 1 - 50 out of 107

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Match	Document	Document Title
1	7378397	TRH-degrading ectoenzyme inhibitors Peptide derivatives useful as inhibitors of activity of thyrotropin-releasing hormone-degrading ectoenzyme (TRH-DE) are of formula I a : wherein: R 1 is an optionally substituted 4-, 5-...
2	7320972	4-Biarylyl-1-phenylazetidin-2-ones 4-Biarylyl-1-phenylazetidin-2-ones useful for the treatment of hypercholesterolemia are disclosed. The compounds are of the general formula in which represents an aryl or heteroaryl...
3	7268125	β-lactamyl vasopressin V1a antagonists Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism...
4	7229982	Pharmaceutical formulation The instant invention provides a pharmaceutical composition comprised of a cholesterol absorption inhibitor and an HMG-CoA reductase inhibitor, one or more anti-oxidants, microcrystalline...
5	7208486	Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein...
6	7205290	Diphenylazetidinone with improved physiological properties, process for its preparation, medicaments comprising this compound, and its use The invention relates to the compound of the formula 1 and to its physiologically acceptable salts. The compound is suitable, for example, as a hypolipidemic.
7	7176196	Bicyclic heterocycles as HIV integrase inhibitors The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds...
8	7176193	Acid-group-substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use One embodiment of the invention relates to compounds of the formula I: in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification. Other embodiments of the invention relate...
9	7144696	Use of azetidinone compounds The use of azetidinone compounds that are inhibitors of cholesterol absorption as tools for discovering and characterizing proteins involved in trafficking or absorption of cholesterol and/or...
10	7132415	Methods and therapeutic combinations for the treatment of xanthoma using sterol absorption inhibitors The present invention provides therapeutic combinations and methods including at least one sterol or 5α-stanol absorption inhibitor that can be useful for treating xanthomas.
11	7129233	Mandelic acid derivatives and their use as thrombin inhibitors There is provided a compound of formula I wherein R a , R 1 , R 2 , Y and R 3 have meanings given in the description and pharmaceutically-acceptable derivatives (including prodrugs) thereof,...
12	7119083	β-Lactamyl vasopressin V1a Antagonists Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism...
13	7098198	Compositions of ezetimibe and methods for the treatment of cholesterol-associated benign and malignant tumors A method of prevention or treatment of a cholesterol-associated tumor is provided which comprises administering a therapeutically effective amount of an azetidinone-based cholesterol absorption...
14	7094769	2-aminocarbonyl-9H-purine derivatives The present invention relates to compounds of the formula: and pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the...
15	7081453	Compounds for treating impaired fundic relaxation The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharma-ceutically acceptable acid addition salt thereof, wherein —a...
16	7071181	Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors The present invention provides methods of treating diabetes and associated conditions by administering a composition including at least one sterol or 5α-stanol absorption inhibitor or compositions...
17	7056907	Mandelic acid derivatives and their use as thrombin inhibitors There is provided a compound of formula (1) and pharmaceutically-acceptable derivatives (including prodrugs) thereof. Which compound and derivatives are useful as, or are as useful as prodrugs of,...
18	7056906	Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women The present invention provides compositions, therapeutic combinations and methods including: (a) at least one hormone replacement therapy composition; and (b) at least one sterol absorption...
19	7053080	Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors The present invention provides methods for the treatment of obesity using sterol or 5α-stanol absorption inhibitors and compositions and therapeutic combinations including sterol or 5α-stanol...
20	7045515	β-lactam compounds process for reproducing the same and serum cholesterol-lowering agents containing the same Novel β-lactam compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof which are useful as serum cholesterol-lowering agents: (I) wherein A 1 , A 3 and...
21	6982251	Substituted 2-azetidinones useful as hypocholesterolemic agents Hypocholesterolemic substituted 2-azetidinone compounds of the formula: are disclosed, as well as a methods of lowering cholesterol by administering said compounds, pharmaceutical compositions...
22	6933107	Use of azetidinone compounds The use of azetidinone compounds that are inhibitors of cholesterol absorption as tools for discovering and characterizing proteins involved in trafficking or absorption of cholesterol and/or...
23	6894041	Oxazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
24	6890921	Arylsubstituted piperazines useful in the treatment of benign prostatic hyperplasia This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the...
25	6869945	Pyrrolyl-and imidazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
26	6767907	4-aryl-1-(indanmethyl dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl) piperidines tetrahydropyridines or piperazines 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH 2 and...
27	6716834	Thiochromane derivatives and their use as thrombin inhibitors There is provided compounds of formulae I and IA wherein Y, R 1 , R 2 , R 3 , D 1 and D 2 have meanings given in the description which are useful as, or as prodrugs of, competitive inhibitors...
28	6703386	Diphenylazetidinone derivatives, process for their preparation, medicaments comprising these compounds and their use Compounds of the formula I, for example, are disclosed, in which R1, R2, R3, R4, R5, and R6 independently of one another are (C 0 -C 30 )-alkylene-L or are the meanings given in the description,...
29	6610680	Non-peptidyl vasopressin V1A antagonists This invention provides substituted 2-(azetidinon-1-yl) acetic acid derivatives of Formula II for the antagonism of the vasopressin V 1a receptor.
30	6602864	Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from...
31	6599894	Amidinobenzylamine derivatives and their use as thrombin inhibitors There is provided compounds of formula I wherein R 1 , R 2 , Y, R 3 and R 4 have meanings given in the description which are useful as, or as prodrugs of, competitive inhibitors of...
32	6569847	Substituted azetidin-2-ones as cysteine protease inhibitors This invention relates to substituted azetidin-2-ones and to pharmaceutical compositions containing such compounds. Their use in medicine as inhibitors of cysteine proteases, particularly the...
33	6559140	Cyclic and bicyclic diamino histamine-3 receptor antagonists Compounds of formula (I) compounds of formula (II) compounds of formula (III) and compounds of formula (IV) or pharmaceutically acceptable salts thereof are useful as H 3 receptor...
34	6514962	Stabilized preparations of β-lactam antibiotic Stabilized preparations which contain a β-lactam antibiotic having an esterified carboxyl group attached directly to the mother nucleus, an oil and a phosphate.
35	6509359	Pyrrolidin-2-one compounds and their use as neuraminidase inhibitors A compound having the formula: wherein all variables are as defined in the specification, for use as a neuramninidase inhibitor.
36	6451785	Beta lactams as antiproliferative agents A method of inhibiting or reducing cell proliferation in a human or mammal is disclosed. This method involves administering to a human or mammal an effective amount of CoA-independent transacylase...
37	RE37721	Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar 1 and Ar 2 are aryl or R 4 -substituted aryl; Ar 3 is aryl...
38	6335324	Beta lactam compounds and their use as inhibitors of tryptase Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents...
39	6242439	Azetidinone derivatives for the treatment of HCMV infections A compound of formula I ##STR1## wherein R 1 is hydrogen, methyl, ethyl, methoxy or methylthio; R 2 and R 3 each independently is hydrogen or lower alkyl; R 4 is hydrogen, lower alkyl, methoxy,...
40	6239125	Azetidinone derivatives for the treatment of HCMV infections A compound of formula 1: ##STR1## wherein Y is S or O; R 1 is C 1 -6 alkyl; (C 0 -6 alkyl)aryl; (C 0 -6 alkyl)Het; or R 1 is an amino acid analog or dipeptide analog of the formula:...
41	6221860	Beta-lactam inhibitors of CoA-IT This invention relates to methods for treating diseases or disorders mediated by lipid inflammatory mediators, arachidonic acid, its metabolites and/or platelet activating factor (PAF), which...
42	6071899	Azetidinone derivatives for the treatment of atherosclerosis Azetidinone derivatives of formula (I) in which R 1 and R 2 , which may be the same or different, is each selected from hydrogen or C (1-8) alkyl; R 3 is C (1-8) alkyl or C (3-8) cycloalkyl each...
43	6040317	Sulfonamide fibrinogen receptor antagonists A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases...
44	6034077	4-substituted-3-(2-amino-2-cycloalkyl methyl)-acetamido azetidin-2-one derivatives as cysteine proteinase regulators In accordance with the present invention, there are provided 4-substituted-3-(2-amino-2-cycloalkyl methyl)-acetamido azetidin-2-one derivatives of the formula: ##STR1## wherein n is 1, 2 or 3; in...
45	6025353	Method of using cyclooxygenase-2 inhibitors as anti-angiogenic agents This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating angiogenic disorders.
46	5990102	Substituted azetidin-2-ones for treatment of atherosclerosis Compounds of formula (I) in which R 1 and R 2 , which may be the same or different, is each selected from hydrogen, halogen or C (1-8) alkyl; R 3 is aryl or aryl C (1-4) alkyl which may be...
47	5968923	(Azetidin-1-ylalkyl) lactams as tachykinin antagonists The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C 3 -C 7 cycloalkyl, aryl or C 1 -C 6 alkyl, said C 1 -C 6 alkyl, said...
48	5965576	Cyclic amide derivatives for treating asthma Compounds of formula I ##STR1## wherein Q 1 , Q 2 , Q 3 , and Q 4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide...
49	5952322	Method of reducing tissue damage associated with non-cardiac ischemia using glycogen phosphorylase inhibitors A method of preventing non-cardiac tissue damage resulting from ischemia and/or hypoxia, comprising administering to a patient in need of such treatment an effective amount of an glycogen...
50	5952321	Substituted azetidinones as anti-inflammatory and antidegenerative agents New substituted azetidinones of the general Formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described,...

Matches 1 - 50 out of 107

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