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Class 544/361 - The additional six-membered hetero ring is one of the cyclos in a polycyclo ring system


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional six-membered hetero ring
No. of patents: 500
Last issue date: 11/03/2009


1                      
NumberTitleIssue Date
7612205Crystals of quinolinecarboxylic acid derivative solvate
A main object is to provide a crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)-methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid acetonitrile solvate (Compound B) which is an intermediate for producing preferentially ...
11/03/2009
7435726Compositions and methods for the treatment of cancer
This invention relates to compositions comprising thalidomide and another anti-cancer drug which can be used in the treatment or prevention of cancer. Preferred anti-cancer drugs are topoisomerase inhibitors. A particular composition comprises thalidomide, or a phar...
10/14/2008
7432276ABCA1 elevating compounds
The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The inve...
10/07/2008
7423045ABCA1 elevating compounds
The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The inve...
09/09/2008
7388016Dibenzonaphthyridine derivatives and methods of use thereof
The present invention relates to Dibenzonaphthyridine Derivatives, compositions comprising an effective amount of a Dibenzonaphthyridine Derivative and methods for treating or preventing a proliferative disorder, comprising administering to a subject in need thereof...
06/17/2008
7384939Process for preparation of pyridine derivatives of NK-1 receptor antagonist
The present invention provides a process for preparing a pyridine compound of the formula: wherein R1, R2, R3 and a are those defined herein. ...
06/10/2008
7354918Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol and applications thereof
The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I) in which R represents a radical —AR′ wherein A represents a heteroatom and R′ represents a group selected fr...
04/08/2008
7351830Pancratistatin cyclic phosphate prodrugs and phenpanstatin cyclic phosphate prodrugs
Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexyl-carbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient mute to a new series (3
04/01/2008
7342016Farnesyl protein transferase inhibitors as antitumor agents
Disclosed are novel tricyclic compounds represented by the formula (1.0): and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are p...
03/11/2008
7320984Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group
The invention provides a morphinan derivative of the Formula (I): wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y ...
01/22/2008
7320989Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use. ...
01/22/2008
7312209Acridone inhibitors of IMPDH enzyme
Compounds having the formula (I), wherein R3 is selected from H, OH and NH2; R30 is selected from ═O and ═S; W is —C(═O)—, —S(═O)—, or —S(O)2—; or W...
12/25/2007
7273873Camptothecins with a modified lactone ring
Compounds of formula (I) or (II) are described: where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said co...
09/25/2007
7265103Substituted amino isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart o...
09/04/2007
7247642Antibacterial optically pure benzoquinolizine carboxylic acids, processes, compositions and methods of treatment
The present invention relates to optically pure S-(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(+)-isomers, to processes for preparation of the optically pure S-(...
07/24/2007
7247641Compounds, derivatives, compositions, preparation and uses
This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP. ...
07/24/2007
RE39707Camptothecin derivatives
(20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an oxyalkanoic acid and camptothecin, which is are optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating canc...
06/26/2007
72301059-aminoacridine derivatives and process for the preparation thereof
The present invention relates to a new 9-aminoacridine derivative which exhibits prominent antitumor activity and low toxicity. ...
06/12/2007
7226928Methods for the treatment of periodontal disease
The disclosure provides methods for the treatment and prevention of periodontal disease. In preferred embodiments, the invention provides for local treatment of periodontal tissues with a pharmaceutical composition including an immune response modifier (IRM) selecte...
06/05/2007
7217714CCR5 modulators
Compounds of Formula 1 [Region α]−[Region β]−[Region γ]−[Region δ]   (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
05/15/2007
7211417Antibiotic P175-A and semisynthetic derivatives thereof
This invention relates to a new antibiotic designated P175-A, to production of fermentation of Micromonospora echinospora NRRL 30633, to methods for recovery and concentration from the crude solutions, and to a process for purification and to semisynthetic es...
05/01/2007
71991288-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents
The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and ...
04/03/2007
7186724Heterocyclic substituted carbonyl derivatives and their use as dopamine Dreceptor ligands
The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine...
03/06/2007
7176214Imidazo-fused oxazolo[4,5-β]pyridine and imidazo-fused thiazolo[4,5-β]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I), wherein R1, R2, R3, R4, R5 and R6 are as descr...
02/13/2007
7169786Isoxazoline derivatives as anti-depressants
The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piper...
01/30/2007
7153849Antidepressant arylpiperazine derivatives of hetrocycle-fused benzodioxans
Compounds of the formula I: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress ...
12/26/2006
7135480Substituted 1-benzoyl-3-cyano-pyrrolo [1,2-a] quinolines and analogs as activators of caspases and inducers of apoptosis
The present invention is directed to substituted 1-benzoyl-3-cyano-pyrrolo[1,2-α]quinolines and analogs thereof, represented by the general Formula I: wherein R1–R8, L, Q, dash line and A...
11/14/2006
7132541Crystalline fluoroquinolone arginine salt form
The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]qui...
11/07/2006
7122553Liposomal formulation of irinotecan
The present invention is for novel compositions and methods for treating cancer, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the present invention include liposome entrapped irinotecan in which the li...
10/17/2006
7115621Chemical compounds
Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disorders ...
10/03/2006
RE39265Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compound...
09/05/2006
7098219Inhibitors of cellular efflux pumps of microbes
Compounds are described which are efflux pump inhibitors of cellular efflux pumps of microbes. Also described are methods of preparing such compounds, methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds....
08/29/2006
70676667-substituted camptothecin and camptothecin analogs and methods for producing the same
Methods of forming camptothecin compounds which are effective anti-tumor compounds are disclosed. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated topoisomerase I-DNA cleavable complex. ...
06/27/2006
705309117 β-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing...
05/30/2006
6989390Amonafide salts
Disclosed is a salt of amonafide or amonafide analogs represented Structural Formula (I): R1 is —(CH2)nN+HR3R4 X− or R1 is —(CH2)
01/24/2006
6964966Generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, their preparation, compositions and use as medicaments
This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydr...
11/15/2005
6956035Isoquinoline derivatives and methods of use thereof
The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described. ...
10/18/2005
6943168Calcium channel inhibitors comprising benzhydril spaced from piperazine
Certain piperazine substituted compounds are described which are useful in altering calcium channel activity. ...
09/13/2005
6943199Spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines
Substituted spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines capable of modulating NPY5 receptor activity are provided. Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are part...
09/13/2005
6936615Heteroaryl derivatives and their use as medicaments
The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors. ...
08/30/2005
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