U.S. patents available from 1976 to present.
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...that after Parker Brothers executives turned down the game of Monopoly because it had "52 fundamental errors" (including taking too long to play), a copy of the game wound up in the home of the company president who stayed up until 1 a.m. to finish playing it? He was so impressed by the game that the next day he wrote to inventor Charles Darrow and offered to buy it!

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Class 548/557 - Nitrogen attached directly to the five-membered hetero ring by nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen is attached directly to the five-membered
No. of patents: 330
Last issue date: 11/15/2011


1                  
NumberTitleIssue Date
8058456Optically active 3-amino-2,5-dioxopyrrolidine-3-carboxylate, process for production of the compound, and use of the compound
The present invention provides a compound of the formula (III): wherein R is a C1-6 alkyl group, as a novel optically active intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3′-pyrro...
11/15/2011
76190963-Aminopyrrolidines as inhibitors of monoamine uptake
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active monoamines (serotonin, norepinep...
11/17/2009
7504521Methods for the preparation of pyrrolotriazine compounds
A method for preparing a compound having the formula: including the steps of: (a) cyclizing a compound of formula II:
03/17/2009
7425631Compounds and methods of use
Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for...
09/16/2008
7405307Biphenylcarboxamides useful as lipid lowering agents
Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia...
07/29/2008
7388112Immunomodulation with novel pharmaceutical compositions
The synthesis and use of a novel class of tumor necrosis factor (TNFα) inhibitors and immunomodulators are provided. Examples are those having the structures: wherein a, b and c are integers from 0 to 12, X equals NH or CH...
06/17/2008
73817413-amino-2-phenylpyrrolidine derivatives
3-amino-2-phenylpyrrolidine compounds useful as NK-1 antagonists, with pharmaceutical compositions and methods of treatment comprising same, are disclosed. ...
06/03/2008
7378436Compounds
A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl ...
05/27/2008
7368572Acetylene derivatives as inhibitors of histone deacetylase
The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparin...
05/06/2008
73296851-Phenyl-2-oxo-3-sulfonylamino-pyrrolidine derivatives and related compounds as factor Xa inhibitors for the treatment of acute vascular diseases
The invention relates to compounds of formula (I): wherein substituents are as defined. ...
02/12/2008
7326729CXCR1 and CXCR2 chemokine antagonists
The present invention is directed to a compound having the general structure of formula (1): useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease. ...
02/05/2008
7304167Biphenylcarboxamides useful as lipid lowering agents
Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyp...
12/04/2007
7300934Benzamide nitriles
Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds an...
11/27/2007
7291621Substituted biaryl amides C5a receptor modulators
Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5...
11/06/2007
7291615Cyclic derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and ...
11/06/2007
7271272Process for preparing 4-aminomethyl-3-alkoxyiminopyrrolidine methanesulfonate
The present invention relates to a process for the preparation of 4-aminomethyl-3-alkoxyiminopyrrolidine methane-sulfonate, a key intermediate of quinolone antibiotics. According to the process of the present invention, the total number of steps has been shortened t...
09/18/2007
7268236Method of heightening optical purity of 1-benzyl-3-aminopyrrolidine and salt for used therein
The present invention provides a method to improve the optical purity of 1-benzyl-3-aminopyrrolidine having a low optical purity using an inexpensive agent via a simple procedure. The present invention provides a method for improving the optical purity of 1-benzyl-3...
09/11/2007
7250443Pyrrole based inhibitors of glycogen synthase kinase 3
New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed al...
07/31/2007
7244750Active substance combinations having insecticidal and acaricidal properties
The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties. ...
07/17/2007
7232845Active substance combinations comprising insecticidal and acaricidal properties
The invention relates to novel active compound combinations of certain cyclic ketoenols and certain insecticidally active compounds that together have very good insecticidal and acaricidal properties. ...
06/19/2007
7223788Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have...
05/29/2007
7214701Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ...
05/08/2007
7183298Carbamic acid compounds comprising a sulfonamide linkage as HDAC inhibitors
This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(═O)...
02/27/2007
7179301Dyeing compositions for keratinous fibers containing paraphenylenediamine derivatives with pyrrolidinyl group
The invention concerns novel dyeing compositions for keratinous fibers comprising at least a paraphenylenediamine derivative with pyrrolidinyl group as oxidation base, a dyeing method and a dyeing kit using said composition. ...
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
7148225Substituted biaryl amides as C5A receptor modulators
Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in...
12/12/2006
7132543Para-phenylenediamine derivatives containing a disubstituted pyrrolidinyl group bearing a cationic radical, and use of the same for dyeing keratin fibers
The present disclosure relates to a novel a para-phenylenediamine derivative substituted with a pyrrolidinyl group of formula (I) and the addition salts thereof. The present disclosure also relates to a dyeing composition for keratin fibers comprising the paraphenyl...
11/07/2006
7132534Para-phenylenediamine derivatives containing a pyrrolidyl group, and use of these derivatives for coloring keratin fibers
The invention relates to novel pyrrolidyl-substituted para-phenylenediamine derivatives, to dye compositions containing them and to the process for dyeing keratin fibers using these compositions. The present invention makes it possible in particular to obtain...
11/07/2006
7126010Benzylcycloalkyl amines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic disease...
10/24/2006
7126007Process for preparing pyrrolidinyl-functional para-phenylenediamine derivatives substituted by a nitrogenous radical, and intermediate compounds
A process for synthesizing para-phenylenediamine derivative compounds containing a pyrolidinyl group, and substituted by a nitrogenous radical, wherein the para-phenylenediamine derivative compounds are chosen from those of formula (I):
10/24/2006
7122683Amides useful as monoamine re-uptake inhibitors
A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1, R2, R3 and R20 are ea...
10/17/2006
7115754Pyrrolidine derivatives as oxytocin antagonists
The present invention relates to novel pyrrolidine derivative of formula (I), its geometrical isomers, its optically active forms as enantiomers, diastereomers, mixtures of these and its racemate forms, as well as salts thereof, wherein R1 is selected fro...
10/03/2006
7105546Acyclic and cyclic amine derivatives
The present invention relates to acyclic and cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizin...
09/12/2006
7098225Active compound combinations having insecticidal and acaricidal properties
The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties. ...
08/29/2006
7091233Active substance combinations comprising insecticidal and acaricidal properties
The invention relates to novel active compound combinations of certain cyclic ketoenols and certain insecticidally active compounds that together have very good insecticidal and acaricidal properties. ...
08/15/2006
7084138Active ingredient combinations with insecticidal and acaricidal properties
The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the gro...
08/01/2006
7064218Aromatic compounds and poly(oxyalkylene) containing aromatic compounds possessing antibacterial, antifungal or antitumor activity
The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity. The compounds are of Formula (I): Pharmaceutical compositions c...
06/20/2006
7060692Active ingredient combinations comprising insecticidal and acaricidal properties
The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the gro...
06/13/2006
7045521Cyclic derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and ...
05/16/2006
7045532ACE-2 modulating compounds and methods of use thereof
ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-Λ  (I) Wherein Z is...
05/16/2006
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