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Drug, Bio-affecting And Body Treating Compositions > Designated Organic Active Ingredient Containing (doai) > Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai > Hetero Ring Is Four-membered And Includes At Least One Ring Nitrogen > Additional Hetero Ring Attached Directly Or Indirectly To The Four-membered Hetero Ring By Nonionic Bonding > The Additional Hetero Ring Contains Ring Nitrogen > Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos

Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos

Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos patent applications listed are from June 2005 to current and include Date, Patent Application Number, Patent Title, Patent Abstract summary and are linked to the corresponding patent application page.

01/25/07 - 20070021407 - Substituted quinolines as antitumor agents
(v) a group of the formula —X1—C1-3alkyl-CO—NR18NR18—R20 where R18 is as defined above and R20 is selected from hydrogen or C1-5alkoxycarbonyl; or (vi) a heterocyclic ring. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) and ...

01/25/07 - 20070021406 - New neurokinin antagonists for use as medicaments
The present application relates to internally cyclized naphthamide compounds of the formula Ia (wherein R1a, R1b, R1c, R2, R3, R4, R5, R6, R7, R8, X1, X2, Y, Z, and n are as defined herein), which are useful, for example, for antagonizing the pharmacological actions of the neurokinin 1 (NK1) receptor. ...

01/18/07 - 20070015744 - Benzimidazolone and dihydroindolone derivatives and uses thereof
or pharmaceutically acceptable salts thereof wherein m, n, X, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I. ...

01/18/07 - 20070015743 - Quinazoline derivatives as antitumor agents
A quinazoline derivative of the formula (I): (A chemical formula should be inserted here—please see paper copy enclosed) Formula I wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 ...

01/04/07 - 20070004703 - Novel 1,3-dihydro-2h-indol-2-one derivatives, process for preparing them and pharmaceutical compositions containing them
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. ...

12/28/06 - 20060293304 - Process for preparing triazole substituted azaindoleoxoacetic piperazine derivatives and novel salt forms produced therein
A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoloxoacetic piperazine derivatives and processes for producing such novel forms are also provided. ...

12/28/06 - 20060293303 - Antiprotozoal imidazopyridine compounds
Compounds described by the Formula (I) or (II): or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination ...

12/28/06 - 20060293302 - Imidazopyridine-derivatives as inducible no-synthase inhibitors
in which R1, R2, R3, R4, R5 and A have the meanings as given in the description are novel effective iNOS inhibitors. ...

12/21/06 - 20060287292 - Naphthyridine compounds
Certain naphthyridine compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases. ...

12/07/06 - 20060276450 - Isoquinoline potassium channel inhibitors
The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like. ...

12/07/06 - 20060276449 - 1,3-dihydro-2h-indol-2-one derivative
A 1,3-dihydro-2H-indol-2-one derivative expressed by Formula 1 (wherein R1 is a halogen atom, a C1 to C4 alkyl group, etc., and R2 is a hydrogen atom, a halogen atom, etc., or R2 is in the 6-position of the indol-2-one and R1 and R2 join together to form a C3 to ...

11/30/06 - 20060270655 - Combination therapy for treating obesity or maintaining weight loss
Combination therapies for treating obesity or related eating disorders and/or reducing food consumption are described herein which comprises administering a therapeutically effective amount of a cannabinoid-1 (CB-1) receptor antagonist and an intestinal-acting microsomal triglyceride transfer protein inhibitor (MTPi) to an animal in need of such treatment. The CB-1 receptor antagonist ...

11/30/06 - 20060270654 - 1,6-dihydro-1,3,5,6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same
wherein R1, R2, R5, R6, R7, and R8 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases. ...

11/23/06 - 20060264416 - Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such ...

10/12/06 - 20060229289 - 1h-benzimidazole-4-carboxamides substituted with a quaternary carbon at the 2-position are potent parp inhibitors
inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I). ...

10/12/06 - 20060229288 - Inhibitors of phosphodiesterases in infertility
The present invention is directed to methods of increasing oocyte production in a mammal. More specifically, the specification describes methods and compositions for inducing follicular maturation using a PDE inhibitor. The inhibitor may be used alone at high doses. Alternatively, the follicular maturation is achieved by combining a low dose ...

09/21/06 - 20060211678 - Aryl-amino substituted pyrrolopyrimidine multi-kinase inhibiting compounds
or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mek1, PDK-1, GSK3β, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-1R, Ron, Ret, and KDR kinases in animals, including humans, for the treatment and/or prevention of various ...

09/21/06 - 20060211677 - Diphenyl substituted cycloalkanes, compositions containing such compounds and methods of use
The instant invention provides compounds of formula: (I) which are 5-lipoxygenase activating protein inhibitors: formula (I). Compounds of formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cyto-protective agents. ...

08/31/06 - 20060194782 - Pharmacologically active imidazo[4,5-c] pyridines
in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties. ...

08/24/06 - 20060189593 - Aryl spirohydantoin cgrp receptor antagonists
The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the ...

08/10/06 - 20060178358 - Antiprotozoal imidazopyridine compounds
Compounds described by the Formula (I): (I) or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with ...

08/03/06 - 20060172989 - Aminoalkoxyphenyl indolone derivatives
This invention is directed to aminoalkoxyphenyl indolone derivatives which are ligands at the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective ...

07/27/06 - 20060166963 - Processes for producing 4-aminoquinazolines
or suitable salts thereof useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also relates to methods for preparing intermediates related thereto. ...

07/13/06 - 20060154913 - Respiratory syncytial virus replication inhibitors
This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH═CH—CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—CH═N—wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8). G is a direct bond or C1-10alkanediyl; ...

06/29/06 - 20060142262 - Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity. ...

06/15/06 - 20060128686 - Preparation of pyridonecarboxylic acid antibacterials
A process for making 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, and therapeutically acceptable salts thereof, and intermediates used in the process are disclosed. ...

06/08/06 - 20060122167 - C6-and c9-substituted isoxazoline derivatives and their use as anti-depressants
wherein X═CH2, N—R7, S or O, R1, R2, R14 and R15 are certain specific substituents, with the proviso that at least one of R14 and R15 is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring ...

05/25/06 - 20060111338 - 2-amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1, R2, X and Z are defined herein. ...

05/25/06 - 20060111337 - Substituted biaryl quinolin-4-ylamine analogues
Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat ...

05/04/06 - 20060094704 - Treatment of premature ejaculation
This invention relates to the use of cyclic guanosine 3′,5′-monophosphate phosphodiesterase type five inhibitors, including in particular the compound sildenafil, for the treatment of premature ejaculation in patients with normal erectile function. ...

04/27/06 - 20060089345 - Indole derivatives, method for preparating same and pharmaceutical compositions containing same
and also provides their preparation and the pharmaceutical compositions comprising them. These compounds are ligands of CB2 cannabinoid receptors. ...

04/13/06 - 20060079498 - Therapeutic compounds
or a pharmaceutically acceptable salt of said compound, or a solvate of said compound or salt, wherein R1, R2, R3, HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof including treating Type 2 diabetes. ...

04/13/06 - 20060079497 - Lavendamycin analogues and methods of synthesizing and using lavendamycin analogues
Lavendamycin analogues, methods for their synthesis, and methods for their use in the treatment of diseases such as cancer and HIV infection are described. ...

03/16/06 - 20060058284 - Pyrrolidine and azetidine compounds as ccr5 antagonists
The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency ...

03/09/06 - 20060052359 - 7-amino alkylidenyl-heterocyclic quinolones and naphthyridones
or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof. ...

02/02/06 - 20060025403 - Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same
X is N or CH, W is —NR16R17, —NR16C(═O)R22, —NR16CO2R22, —OR23, or a heteroaryl or heterocyclo group as defined in the specification, and R1 through R12, R16, R17, R22, R23, x, y, and z are as defined in the specification, are useful as modulaters of melanocortin receptors, particularly MC-1R and ...

02/02/06 - 20060025402 - Benzimidazolidinone derivatives as muscarinic agents
Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed. ...

12/01/05 - 20050267096 - New indazole and indolone derivatives and their use pharmaceuticals
which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; ...

11/24/05 - 20050261272 - Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants. ...

11/10/05 - 20050250760 - 1-[(indol-3-yl)carbonyl]piperazine derivatives
or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said 1-[(indol-3-yl)carbonyl]piperazine derivatives, and to the use of these derivatives in the treatment of pain, such as peri-operative pain, chronic pain neuropathic pain, cancer pain, and pain and spasticity associated with multiple sclerosis. ...

11/03/05 - 20050245500 - Beta-ketoamide compounds with mch antagonistic activity
wherein the groups and residues A, B, b, X, Y, Z, R1, R2, R3, R5a and R5b have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one amide according to the invention. As a result of their MCH-receptor antagonistic activity the pharmaceutical ...

10/20/05 - 20050234037 - Compounds, compositions, and methods
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed. ...

10/20/05 - 20050234036 - Thioxanthine derivatives as myeloperoxidase inhibitors
There is disclosed the use of a compound of formula (Ia) or (Ib) wherein R1, R2, R3, R4, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition ...

10/13/05 - 20050227960 - Substituted bicycloalkylamine derivatives as modulators of chemokine receptor activity
or stereoisomers or pharmaceutically acceptable salts thereof, wherein X, Z, a, b, c, d, n, R1, R2, R3, R4, R5, R10, R10a, and R12, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as ...

09/22/05 - 20050209213 - Quinoline compound
may further have substituents, and when ring B further has a substituent, the substituent may be linked to R1 to form a ring, or a salt thereof, or a prodrug thereof, is provided. ...

08/25/05 - 20050187209 - 1h-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors
Thieno[2,3-c]pyrazole derivatives of formula (1) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. ...

08/11/05 - 20050176698 - Neuropeptide y antagonists
Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity. ...

08/04/05 - 20050171086 - Compositions for treating cns disorders
An aminomethylpyridyloxymethyl/benzisoxazole substituted azabicyclic compound, a pharmaceutical composition comprising same, and a method of treating one or more CNS or other disorders, including concurrent treatment of disorders such as schizophrenia and depression. ...

08/04/05 - 20050171085 - Lactam-containing compounds and derivatives thereof as factor xa inhibitors
or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa. ...

08/04/05 - 20050171084 - Methods of treatment with lxr modulators
Disclosed are methods of using compounds that modulate LXR. ...

07/28/05 - 20050165001 - Quinazolinone and benzoxazinone derivatives and uses thereof
and pharmaceutically acceptable salts or prodrugs thereof, wherein m, n, p, q, X, Y, Z, A, R1, R2, R4, R5, R6, R7, R8, R9 and R10 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I. ...

07/28/05 - 20050165000 - Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant
and a nonionic surfactant; wherein R1, R2, R3 and Q1 are defined herein. Compounds of Formula (I) are HIV integrase inhibitors, and the pharmaceutical compositions are useful for preventing or treating HIV infection or for preventing, treating, or delaying the onset of AIDS. The pharmaceutical compositions are typically administered orally, ...

06/30/05 - 20050143367 - Process for the preparation of pyrazolo[4,3-d]pyrimidin-7-one compounds and intermediates thereof
A process is provided for the preparation of compounds of formula (I) herein comprising reacting a compound of formula (II), (III), (IV) or (V) in the presence of −OR3 and a hydroxide trapping agent or in the case of compounds of formula (IV) reacting in the presence of an auxiliary ...

06/16/05 - 20050130954 - Akt protein kinase inhibitors
where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer. ...

06/09/05 - 20050124599 - Novel benzoimidazole derivatives useful as antiproliferative agents
and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, and R4 are as defined herein. The invention also relates to methods of treating abnormal cell growth, such as cancer, in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders ...



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