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Class 540/455 - Polycyclo ring system which contains the hetero ring as one of the cyclos


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the hetero ring is one of the cyclos
No. of patents: 103
Last issue date: 01/10/2012


1      
NumberTitleIssue Date
8093379Macrocyclic serine protease inhibitors
Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection i...
01/10/2012
7429565Antiviral phosphonate analogs
The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing su...
09/30/2008
7381743Macrocycles for the treatment of cancer
The present invention relates to new macrocycles of the general formula (I) as well as their use for the treatment of cancer diseases ...
06/03/2008
73234557-aryl 1,5-dihydro-4,1-benzoxazepin-2(3)-one derivatives and their use as progesterone receptor modulators
This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof. ...
01/29/2008
7244594Microbial transformation method for the preparation of an epothilone
A microbial method for the preparation of an epothilone containing a terminal hydroxyalkyl group, comprising contacting at least one epothilone having a terminal alkyl group with an enzyme or microorganism capable of catalyzing the selective hydroxylation of said al...
07/17/2007
7176001Manufacture and purification of cyclosporin A
The present invention provides an improved method for the manufacture of Cyclosporin A is disclosed. Cyclosporin A is produced by solid state fermentation of Fusarium solani in a bioreactor under optimal fermentation parameters. The product is extracted and f...
02/13/2007
7176208Quinoxalinyl macrocyclic hepatitis C serine protease inhibitors
The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C v...
02/13/2007
7122662Tricyclic compound having spiro union
This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which e...
10/17/2006
7074961Antidepressants and their analogues as long-acting local anesthetics and analgesics
Methods and compositions of antidepressants and analogs thereof for inducing local long-lasting anesthesia and analgesia are provided. The methods and compositions are useful for alleviating acute and chronic pain, particularly useful for treating a localized pain.
07/11/2006
7030107Fused bicyclic pyridine derivatives as tachykinin receptor antagonists
A novel fused bicyclic pyridine derivative or a salt thereof that acts as a tachykinin receptor antagonist, in particular as an NK1 receptor antagonist, is represented by the following general formula (1): ...
04/18/2006
7012140Selection of coordination geometry to adjust water exchange rates of paramagnetic metal ion-based macrocyclic contrast agents
The present invention is directed, in general, to a contrast agent comprising a tetraazacyclododecane ligand and comprising a macrocyclic ring and a paramagnetic metal ion coordinated to the tetraazacyclododecane ligand. Pendent arms R, R′, R″ and R′″ attach...
03/14/2006
7012166Catalyst composition and method for chlorinating aromatic compounds
Aromatic compounds such as toluene and o-xylene are chlorinated in the presence of a catalyst combination prepared by combining (A) at least one salt comprising a metal selected from the group consisting of a Group 4–12 metal, a lanthanide and an actinide; and a c...
03/14/2006
6995153Fused bicyclic pyrimidine derivatives
A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following general formula (1): wherein...
02/07/2006
6984734Cyclo[n]pyrroles and methods thereto
The present invention provides an oxidative coupling procedure that allows efficient synthesis of novel cyclo[n]pyrrole macrocycles. Therefore, the present invention provides cyclo[n]pyrroles where n is 6, 7, 8, 9, 10, 11, or 12, and derivatives, multimers, isomers,...
01/10/2006
6984635Dimerizing agents, their production and use
Materials and methods are disclosed for regulation of biological events such as target gene transcription and growth, proliferation or differentiation of engineered cells. ...
01/10/2006
6962992Crown ether derivatives
The invention describes crown ether chelators, including crown ethers having the formula and aza-substituted and thia-substituted analogs thereof. These crown ethers are substituted by a dye moiety, a chemically reacti...
11/08/2005
6924277Cyclized benzamide neurokinin antagonists for use in therapy
Compounds having the general formula wherein R1a, R1b, R1c, X1, X2, R2, R3, R4, R5, R6, n, Y and Z are as de...
08/02/2005
6911428Diaryl peptides as NS3-serine protease inhibitors of hepatitis C virus
The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus. A particularly preferred compound is of the formula: ...
06/28/2005
6903129D-proline prodrugs
The invention relates to compounds of formulas wherein R1 and R2 are independently from each other lower alkoxy, lower alkenyloxy, benzyloxy, hydroxy, —OCH(CH3)OC(O)-lowe...
06/07/2005
6846814Neurokinin antagonists for use as medicaments
Compounds having the general formula wherein R1a, R1b, R1c, R2, R3, R4, R5, R6, R7, R8, X1, X
01/25/2005
6841530Semi-synthetic studies toward didemnin analogues
Disclosed are semi-synthetic methods for the preparation of Didemnin Analogs. The compounds of this type are illustrated in Formula (I). ...
01/11/2005
68219634-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors
Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical,...
11/23/2004
6680311Cryptophycin compounds
The present invention provides cryptophycin compounds of Formula I ##STR1## that are useful in the treatment of neoplasms....
01/20/2004
6656930Aralkyl diazabicycloalkane derivatives for CNS disorders
Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions. For example, compounds of interest are of the formula: ##STR1##...
12/02/2003
6632929Avidin derivatives and uses thereof
A covalent conjugate of a 4'-hydroxyazobenzene-2-carboxylic acid derivative (HABA) and an avidin-type molecule, of the formula: ##STR1## wherein A is (CH2)n or --CH.dbd.CH--, wherein n is an integer from 0-10; B is (CH2)
10/14/2003
6608027Macrocyclic peptides active against the hepatitis C virus
The present invention covers macrocyclic compounds of formula I active in-vitro and in cellular assays against the NS3 protease of the hepatitis C virus. ##STR1## wherein W, R21, R22, R3, R4, D and A are as defi...
08/19/2003
65933608a- and 9a-15-membered lactams
The invention relates to novel 15-membered 8a- and 9a-lactams from the class of 6-O-methyl-erythromycin A of general formula (I) ##STR1## their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to intermediates...
07/15/2003
6545038Heterocyclic metalloprotease inhibitors
The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of...
04/08/2003
6489314Epothilone derivatives and methods for making and using the same
The present invention relates to 16-membered macrocyclic compounds. In one aspect of the present invention, compounds of the formula ##STR1## are provided wherein: R1, R2, R3, and R5 are each independently hydrogen, ...
12/03/2002
6468996Substituted hetero-polycyclic compounds as PPAR଱ and PPARγ activators
The present invention relates to compounds of the general formula (I) ##STR1## The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR)....
10/22/2002
6384014Purified form of streptogramines, preparation of same and pharmaceutical compositions containing them
Purified form of streptogramines, characterised in that it contains at least one component from group B streptogramines of general formula (I), wherein R1 is Me or Et, R2 is H or OH, and R3 is substituted benzyl of general...
05/07/2002
6358985Inhibitors of prenyl-protein transferase
The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds...
03/19/2002
6288073Acronycine derivatives, preparation method and pharmaceutical compositions
A compound selected from those of formula (I): ##STR1## in which: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents h...
09/11/2001
6277839Biphenylene lactams as prostaglandin receptor ligands
The present invention relates to biphenylene lactams of Formula II which are ligands at the prostaglandin receptors, as well as a method for treating prostaglandin mediated diseases comprising administration to a patient in need of such a treatment of a n...
08/21/2001
6180619Prenyl transferase inhibitors
A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by the four following formulas ##STR1## Each of the R groups is defined in the disclosure....
01/30/2001
6177551Bridged aromatic substituted amine ligands with donor atoms
The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent oth...
01/23/2001
6147071Cyclic compounds, their production and use
Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.CC
11/14/2000
6124453Macrolides
A novel class of macrolides in which i) positions 2 to 6 inclusive of the macrocyclic ring are provided by a piperidazinyl carboxylic acid residue; and/or ii) positions 7 to 9 inclusive of the macrocyclic ring are provided by an aromatic ଱-amino acid res...
09/26/2000
6107482Nitrogenous macrocyclic compounds
Novel macrocyclic compounds are constructed to include large cyclic structures that are interrupted by at least one ring system. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridges that interconn...
08/22/2000
60691142-amino-4-bicycloamino-1,3,5-Triazines, their preparation, and their use as herbicide and plant growth regulators
Compounds of the formula (I) and their salts ##STR1## in which R1 to R6, Y1, to Y2, Y3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepa...
05/30/2000
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