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Class 544/237 - Phthalazines (including hydrogenated)


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system has the following
No. of patents: 375
Last issue date: 03/29/2011


1                    
NumberTitleIssue Date
7915410Acyclic Iinhibitors
A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein. ...
03/29/2011
7807830Manufacture of pure hydralazine salts
The present invention provides an improved process of preparing hydralazine hydrochloride, which involves the preparation of 1-chlorophthalazine salt and further reacting with hydrazine followed by purification of hydralazine hydrochloride, which is free of phosphat...
10/05/2010
7728133Stable pharmaceutical compositions
Pharmaceutical compounds having the general formula: or compounds having the formula: where R1 and R2 are independently H, branched or straight chain alkyl h...
06/01/2010
7692006Phthalazinone derivatives
4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A. ...
04/06/2010
7560551Aurora kinase modulators and method of use
The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R1-8 are defined herein, a...
07/14/2009
7531653Manufacture of pure hydralazine salts
The present invention provides an improved process of preparing hydralazine hydrochloride, which involves the preparation of 1-chlorophthalazine salt and further reacting with hydrazine followed by purification of hydralazine hydrochloride, which is free of phosphat...
05/12/2009
7432263Amino-phthalazinone derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
Compounds which are amino-phthalazinone derivatives according to formula 1 and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or compostions are useful in the treatment of diseases ...
10/07/2008
74230301-amino-phthalazine derivatives, the preparation and the therapeutic use thereof
A 1-amino-phthalazine derivative of general formula (I) wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such method and medical treatments u...
09/09/2008
74079558-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs t...
08/05/2008
7407957Phthalazinone derivatives
A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, wherein: A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or C...
08/05/2008
7405215Indole acetic acids exhibiting CRTH2 receptor antagonism and uses thereof
The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metab...
07/29/2008
7402580Fused pyridazine derivative compounds and drugs containing these compounds as the active ingredient
Fused pyridazine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof (wherein each symbol has the meaning as defined in the specification.). Because of inhibiting poly(ADP-ribose)polymerase, ...
07/22/2008
7388006Non-steroidal progesting
The present invention relates to non-steroidal progestins of the general formula (I) wherein R1 and R2 are independently of each other —H or —F, R3 is —CH
06/17/2008
7329659Substituted-1-phthalazinamines as vr-1 antagonists
The present invention provides a compound of formula (I): in which Ar and R1 are phenyl or a heteroaromatic group, R2 is generally hydrogen, R3 is hydrogen or alkyl and X, Y and Z are generally CH or N as VR-1 antagonists; or a pharm...
02/12/2008
7329660Phthalazine derivatives for treating inflammatory diseases
The invention relates to the treatment of leukemias with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specificatio...
02/12/2008
73122141, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors
The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa. ...
12/25/2007
7265115Diazabicyclic CNS active agents
Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals. ...
09/04/2007
7232826Tyrosine kinase inhibitors
The present invention provides compounds of Formula I or II that are useful as anti-cancer agents and other diseases that can be treated by inhibiting tyrosine kinase enzymes ...
06/19/2007
7226923Phthalazinone derivatives
Compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates are disclosed. Also disclosed are methods for the preparation of the above-mentioned compounds, p...
06/05/2007
7220858Synthesis of hydrazine and chlorinated derivatives of bicyclic pyridazines
The present invention relates to both a novel method of preparing hydralazine hydrochloride and to a novel method of preparing hydrazine derivatives of compounds containing a pyridazine ring, including, for example, pyridazines, phthalazines and other compounds cont...
05/22/2007
7220746Pyrrolidinedione substituted piperidine-phthalazones as PDE4 inhibitors
The compounds of formula I in which the substituents have the meanings as indicated in the description, are novel effective PDE4 inhibitors. ...
05/22/2007
7196085Phthalazinone derivatives
A compound of formula: or an isomer, salt, solvate, chemically protected form, or prodrug thereof, wherein A and B together represent an optionally substituted, fused aromatic ring; RL is ...
03/27/2007
7186720Tetrahydropyridyl-alkyl-heterocycles, method for preparing the same and pharmaceutical compositions containing the same
The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; R2 and R3 independent...
03/06/2007
7186710Phthalazinones
The compounds of formula I in which R1, R2, R3, R4 and R5 have the meanings as given in the description are PDE4/7 inhibitors. ...
03/06/2007
7179810Phthalazinone-piperidino-derivatives as PDE4 inhibitors
The compounds of formula I in which the given substituents have the meanings as given in the description, are novel effective PDE4 inhibitors. ...
02/20/2007
7176312Kinase inhibitor scaffolds and methods for their preparation
General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, bor...
02/13/2007
7153859Condensed polycyclic compounds
The present invention provides a novel a condensed polycyclic compound useful as a phosphodiesterase 4 inhibitor, which is shown by the formula [I]: or a pharmaceutically acceptable salt thereof and a pharmaceuti...
12/26/2006
7151102Phthalazinone derivatives
A method of treatment of a disease of the human or animal body mediated by PARP comprising administering to such a subject a therapeutically effective amount of a compound of formula: or an isomer, salt, solvate,...
12/19/2006
7135471Aryl oximes
Aryl oxime derivatives of the formula (I), in which R1, R2, R3, X and B are as defined in claim 1, act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosi...
11/14/2006
7132418Peptidyl heterocyclic ketones useful as tryptase inhibitors
The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particul...
11/07/2006
7125863Inhibitors of dipeptidyl peptidase IV
Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of t...
10/24/2006
7122544Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6
10/17/2006
7115646Cyclic diamines and derivatives as factor Xa inhibitors
The present application describes cyclic diamino compounds, derivatives thereof, and pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa. ...
10/03/2006
7091209Dihydroxypyridmidine carboxylic acids as viral polymerase inhibitors
A class of 2-aryl-4,5-dihydroxy-6-carboxypyrimidines of formula (I): wherein Ar is an optionally substituted aryl or heterocyclicgroup; as well as compounds of formula (I) which are derivatized at one or more of the 4-hydroxy, 5-hydroxy or 6-carboxy groups; and taut...
08/15/2006
7053093Bicyclic and tricyclic hetroaromatic compounds
Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high aff...
05/30/2006
70455228-Azabicyclo[3.2.1]oct-2-ene and -octane derivatives technical field
The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful ...
05/16/2006
7037880Ethylene derivatives and pesticides containing said derivatives
Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent su...
05/02/2006
7030239Compounds to treat Alzheimer's disease
The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases. ...
04/18/2006
7030120Nitrogen-containing heterocyclic compounds and benzamide compounds and drugs containing the same
Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitor...
04/18/2006
7022696Piperazino-derivatives and their use as PDE4 inhibitor
The compounds of formula I in which R1, R2, R3, A, X, s and R9 have the meanings as given in the description are novel effective PDE4 inhibitors. ...
04/04/2006
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