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Class 544/231 - Spiro diazine


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein at least one of the rings in the spiro
No. of patents: 194
Last issue date: 06/16/2009


1          
NumberTitleIssue Date
7547780Dihydropteridione intermediate compounds
Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specification, the is...
06/16/2009
7429598Spirocondensed quinazolinones and their use as phosphodiesterase inhibitors
The invention relates to compounds of formula (I) wherein R1, R2 and m are as defined in the description, their use as medicament, pharmaceutical compositions containing them and a process for their pr...
09/30/2008
7378411Substituted thienopyrimidinones as a mitotic kinesin inhibitor
The present invention relates to thienopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which ...
05/27/2008
7371753Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and sp...
05/13/2008
7361758Crystals of triazaspiro[5.5]undecane derivative
The present invention relates to a new crystal of triazaspiro[5.5]undecane derivatives. The crystal of a non-solvate of (3R)-1-butyl-2,5-dioxo-3-[(1R)-1-hydroxy-1-cyclohexylmethyl]-9-[4-(4-carboxyphenyloxy)phenylmethyl]-1,4,9-triazaspiro[5.5]undecane hydrochloride h...
04/22/2008
7338954Compounds useful as motilin agonists and method
A method is provided for treating disorders of gastrointestinal motility which include the steps of administering to a patient in need of treatment of a compound having the structure or a pharmaceutically acceptable salt th...
03/04/2008
7332491Dihydropteridione derivatives, process for their manufacture and their use as medicament
Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specificat...
02/19/2008
7294632Substituted 8′-pyridinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a]pyrimidin-6-one and 8′-pyrimidinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a]pyrimidin-6-one derivatives
The invention relates to a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, m, n, p and q are as described herein. The invention relates also...
11/13/2007
7294631Substituted 8′-pyri(MI)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-]pyrimidin-6-one derivatives
The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, o, m, n, p and q are as defined herein. The invention rela...
11/13/2007
72681281,3,5-trisubstituted-5-phenyl and 5-pyridyl pyrazolopyrimidinone derivatives having PDE7 inhibiting action
Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds selectively in...
09/11/2007
7262193Triazaspiro[5.5]undecane derivative and pharmaceutical composition comprising the same as active ingredient
Triazaspiro[5.5]undecane derivatives of the formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R1 is formula (II) or formula (III); R
08/28/2007
72418896-formyl-tetrahydropteridines, process for their manufacture and use thereof as medicaments
Disclosed are 6-formyl-tetrahydropteridines of the formula (I) wherein the groups R1 to R6 have the meanings given in the claims and specification, the isomers thereof, methods of preparing ...
07/10/2007
7238807Process for the manufacture of fused piperazin-2-one derivatives
Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given i...
07/03/2007
7235538Heterocyclic compounds, which are inhibitors of the enzyme DPP-IV
The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I wherein each n is one or two independently and R1, R2, R3
06/26/2007
7214676Spirotricyclic derivatives and their use as phosphodiesterase-7 inhibitors
The invention provides compounds which are PDE7 inhibitors, having the following formula (I), (II) and (III) in which X1, X2, X3, X4, X, Y, Z, A and Z1 are a...
05/08/2007
7176313Anti acid-fast bacterial agent containing pyridonecarboxylic acids as active ingredient
An anti acid-fast bacterial agent containing, as an active ingredient, a pyridonecarboxylic acid derivative represented by the following general formula (1), a salt thereof, or a hydrate thereof, which shows excellent antibacterial activity against Mycobacterium ...
02/13/2007
7129245Aromatic amides
This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor....
10/31/2006
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
7109243Inhibitors of cathepsin S
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present inven...
09/19/2006
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
7067501Aryloxyphenyl and arylsulfanylphenyl derivatives
The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors. ...
06/27/2006
7053090Triazaspiro[5.5]undecane derivatives and drugs containing the same as the active ingredient
Triazaspiro[5.5]undecane derivatives of the formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R1 is formula (II) or formula (III); R
05/30/2006
7008555Epoxy resin curing agents and epoxy resin compositions
A curing agent for epoxy agent having N-phenyl-p-phenylenediamine(4-aminodiphenylamine). An epoxy resin combination having a main agent and a curing agent. The main agent has an epoxy resin. The curing agent has a N-phenyl-p-phenylenediamine(4-aminodiphenylamine).
03/07/2006
6967201Benzofurylpiperazines and benzofurylhomopiperazines: serotonin agonists
The present invention provides serotonergic benzofurylpiperazines of Formula I: where: A is a piperazine of formula: and R, R1...
11/22/2005
6943171Polycyclic guanine derivative phosphodiesterase V inhibitors
A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases:
09/13/2005
6919349Spiro compounds and adhesion molecule inhibitors containing the same as the active ingredient
Disclosed are novel spiro derivatives and their medical uses, especially as adhesion molecule inhibitors useful for therapies of inflammatory diseases. The spiro derivative according to the present invention has the chemical structure, for example, represented by th...
07/19/2005
6916807Triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, G, and W are as ...
07/12/2005
6911452Spiroazacyclic compounds as monoamine receptor modulators
The present invention relates to 1-oxa-3,8-diaza-spiro[4.5]decan-2-one compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease conditio...
06/28/2005
6900201N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, and G...
05/31/2005
6894048Sulfur containing dihydrophthalazine antagonists of excitatory amino acid receptors
Substituted dihydrophthalazine sulfur containing compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of the non-NM...
05/17/2005
6861422Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
The present invention relates to new dihydropteridinones of general formula (I): wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, proces...
03/01/2005
6841671Spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to 5-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said “A” is a 5-7 membered heterocyclic ring as defined in the specification and to pharmaceutica...
01/11/2005
6740636Non-peptide CCR1 receptor antagonists in combination with cyclosporin A for the treatment of heart transplant rejection
This invention is directed to pharmaceutical compositions useful in treating heart transplant rejection in mammals comprising a pharmaceutically acceptable excipient, a therapeutically effective amount of a non-peptide CCR1 receptor antagonist and a sub-nephrotoxic ...
05/25/2004
6703390Sulfur containing dihydrophthalazine antagonists of excitatory amino acid receptors
Substituted dihydrophthalazine sulfur containing compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compositions are useful for treating disorders associated with excessive activation of...
03/09/2004
6677451Preparation of sterically hindered amine ethers
A new process is described for the preparation of a compound of the formula I ##STR1## wherein R1, R2, R3 and R4, independently of each other, are C1 -C8 alkyl or C1 -C5...
01/13/2004
6677336Substituted piperazine compounds
Novel compounds of the general formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subse...
01/13/2004
6649622Tetrahydropyrimidone inhibitors of fatty acid binding protein and method
aP2 inhibiting compounds are provided having the formula ##STR1## wherein A, B, X, and Y are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination ...
11/18/2003
6534506Inhibitors 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...
03/18/2003
6509346Chemokine receptor antagonists and methods of use therefor
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: ##STR1## and ...
01/21/2003
6503926Chemokine receptor antagonists and methods of use therefor
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: ##STR1## and ...
01/07/2003
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