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Class 548/468 - The additional hetero ring and the bicyclo ring system are attached directly to the same acyclic carbon or acyclic carbon chain


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system and the additional
No. of patents: 239
Last issue date: 04/23/2013


1            
NumberTitleIssue Date
8426612Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole
The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletrip...
04/23/2013
7572924Pyrrole substituted 2-indolinone protein kinase inhibitors
The present invention relates to pyrrole substituted-2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related c...
08/11/2009
7402606Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss
Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle ...
07/22/2008
73998684-(Heteroaryl-methyl and substituted heteroaryl-methyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists
Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B
07/15/2008
7368072Photochromic contact lenses and methods of manufacturing
Described are contact lenses having photochromic materials within the central or pupillary area of the lens and methods for manufacturing such lenses. In one method, a photochromic amount of at least one photochromic material is added to the pupillary region of a ca...
05/06/2008
7361682Indole derivatives as H3 inverse agonists
The present invention relates to compounds of formula I: wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable ...
04/22/2008
7320826Photochromic articles with reduced temperature dependency and methods for preparation
Described are photochromic articles that include a substrate, a temperature dependent reducing amount of at least one organic photochromic material (b) that changes from more absorbing to less absorbing of radiation in its activating spectral absorbance as the tempe...
01/22/2008
7261843Photochromic optical article
Describes a photochromic article, e.g., an ophthalmic photochromic plastic article, such as a lens, in which the article includes (1) a rigid substrate, e.g., a transparent substrate such as a glass or organic polymeric substrate, as for example, a thermoset or ther...
08/28/2007
7262295Indeno-fused photochromic naphthopyrans, naphthols and photochromic articles
Described are photochromic materials of indeno [2′,3′:3,4]naphtho[1,2-b]pyran structure, characterized in that they have a nitrogen or sulfur containing substituent at the 11-position ring atom, are substantially free of spiro-substituents at the 13-position and...
08/28/2007
7238723Indole derivatives
The present invention provides eletriptan hydrobromide monohydrate of the formula (I): together with processes for preparing, uses of, and compositions containing, said monohydrate. ...
07/03/2007
7202265Indolinone combinatorial libraries and related products and methods for the treatment of disease
The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including ce...
04/10/2007
7186709Dihydropyrancarboxamides and uses thereof
The present invention provides novel dihydropyrancarboxamide compounds of formula (I): and collections of these compounds, and provides methods for the synthesis of these compounds; wherein R1–R...
03/06/2007
71799103-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors
The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related c...
02/20/2007
7173048Indolyl derivatives as liver-X-receptor (LXR) modulators
The invention relates to compounds of formula (I): and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, wherein R1, R2, R3, R4, R5...
02/06/2007
7166357Photochromic articles that activate behind ultraviolet radiation blocking transparencies and methods for preparation
Described are photochromic articles that include a substrate and a photochromic amount of at least one organic photochromic material (b) represented by graphic formula XIII adapted to change from an unactivated state to an activated state by exposure to radiation su...
01/23/2007
7164030Process
The present invention provides an improved process for the preparation of α-polymorphic eletriptan hydrobromide. ...
01/16/2007
71575775-sulfonamido-substituted indolinone compounds as protein kinase inhibitors
The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions ...
01/02/2007
7148249Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments
The present invention relates to heterocyclically substituted indolinones of general formula wherein R1 to R5 and X are defined as in claim 1, the tautomers, the diastereomers, ...
12/12/2006
7147889Organic photochromic compositions of improved kinetic performance
Described are imbibition compositions that incorporate kinetic enhancing additive(s) into photochromic polymeric host material. Kinetic enhancing additives include organic polyol(s), epoxy-containing compound(s) or a mixture thereof that improves the performance of ...
12/12/2006
7125905Pyrrole substituted 2-indolinone protein kinase inhibitors
The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related c...
10/24/2006
7119209Process for preparing indolinone derivatives
The present invention refers to a process for preparing indolinone derivatives of the general formula (VI) as defined in the specification and intermediates of that process. ...
10/10/2006
7119090Pyrrole substituted 2-indolinone protein kinase inhibitors
The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of prot...
10/10/2006
7112603Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to a...
09/26/2006
7105563Indolinone derivatives and their use in treating disease-states such as cancer
Indolinone derivatives, such as compounds of the formula (I): wherein A, m, n, R1, R2, R3, R5 and R6 are described herein, are discl...
09/12/2006
7094368Pyrano-quinolines, pyrano-quinolinones, combinations thereof, photochromic compositions and articles
Described are compositions of at least one material represented by a pyrano[3,2-c]quinoline structure, a pyrano[3,2-c]quinolinone structure or mixtures thereof. The pyrano[3,2-c]quinoline structure is characterized by having a nitrogen atom at the 6-position ring at...
08/22/2006
7091220Substituted indole Mannich bases
The present invention relates to substituted indole Mannich bases, processes of preparing substituted indole Mannich base, a medicament containing the same, and a pharmaceutical composition containing the same. ...
08/15/2006
7053113Mannich base prodrugs of 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives
The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases ...
05/30/2006
7030214Ureins derived from α, ω, diamino acids and process for their preparation
Ureins are obtained by reaction, in basic medium, between an Nω-(aryloxycarbonyl)diamino acid and a compound containing a free amino group. The chirality of the compounds is outstandingly well preserved. ...
04/18/2006
70089431-(Pyrrolidin-1-ylmethyl)-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
The present invention is directed to 1-pyrrolidin-1-ylmethyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related t...
03/07/2006
6939565Protease inhibitors of the coagulation cascade isolated from Dysidea sponges
The present invention is directed toward a composition comprising a compound isolated from Dysidea species sponges that is capable of inhibiting serine proteases of the coagulation cascade. In particular, this composition inhibits the TF/VIIa complex of the c...
09/06/2005
6930124Compounds derived from oxindoles and their therapeutic application in cancer treatment
The invention relates to compounds of formula (I) in which R5 is chosen from the group consisting of: in which R2 is a C1-C3 a...
08/16/2005
6914145Acylation process
The present invention is concerned with the acylation of indoles, specifically the preparation of 3-acylated indoles which may be further treated to provide indoles having an alternative substituent at the 3-position. ...
07/05/2005
6906093Indolinone combinatorial libraries and related products and methods for the treatment of disease
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. ...
06/14/2005
6852751Difluorobutyric acid metalloprotease inhibitors
Compounds according to the following Formula (I): are effective in treating conditions characterized by excess metalloprotease activity. ...
02/08/2005
6846818Selective inhibitors of cyclooxygenase-2
The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I: pharmaceutical compositions containing them, to their medicinal use, and to their preparations. The compounds of the inventio...
01/25/2005
6797725Prodrugs of a 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related c...
09/28/2004
678416717-beta-hydroxysteroid dehydrogenase-II inhibitors
17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R4)(R6)Y are oriented cis to each other; W represents O or S; R...
08/31/2004
6750240Methods of using bis-indolylquinones
The present invention relates to novel synthetic methods for the preparation of indolylquinones. The methods of the present invention are directed to synthetic reactions involving indoles and halo-quinones in solvent and in the presence of a metal carbonate. The inv...
06/15/2004
6716837Heterocyclic compounds for the treatment of migraine
Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with th...
04/06/2004
6716869Protease inhibitors of the coagulation cascade isolated from Dysidea sponges
The present invention is directed toward a composition comprising a compound isolated from Dysidea species sponges that is capable of inhibiting serine proteases of the coagulation cascade. In particular, this composition inhibits the TF/VIIa complex of the coagulat...
04/06/2004
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