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Mark Twain (Samuel L. Clemens) received Patent No. 121,992 for "An Improvement in Adjustable and Detachable Straps for Garments." He later received two more patents: one for a self-pasting scrapbook and one for a game to help players remember important historical dates.

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Class 514/254.04 - The additional five-membered hetero ring consists of three ring carbons, and of nitrogen and chalcogen in adjacent ring positions (e.g., isoxazolyl, isothiazolyl, etc.)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein one chalcogen (i.e. oxygen, sulfur,
No. of patents: 231
Last issue date: 04/03/2012


1            
NumberTitleIssue Date
8148379Therapeutic agent for senile dementia
A therapeutic/preventive agent for cognitive dysfunctions, which comprises as an active ingredient an imide derivative of the following formula [1]: wherein Z is a group of the formula [2]: ...
04/03/2012
8088778Benzisoxazole piperazine compounds and methods of use thereof
The invention includes benzisoxazole piperazine compositions and methods of using them for modulating sleep. ...
01/03/2012
7939535Benzo[D]isoxazol-3-yl-piperazin derivatives useful as modulators of dopamine D3 receptors
The present invention provides compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cogn...
05/10/2011
7858630Dand 5-HTreceptor modulators
The present invention provides compounds of the general formula (I) wherein X, n and R1 are as described herein, as well as pharmaceutically acceptable salts and esters thereof, methods for their manufacture, pha...
12/28/2010
7563794Ziprasidone free from colored impurities and a process for its preparation
Ziprasidone base or a pharmaceutically acceptable salt thereof free from colored impurities, in particular those giving the product a “slightly pink to pink” coloration. ...
07/21/2009
7550469Heterocyclic amide derivatives and their use as dopamine D3 receptor ligands
The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D
06/23/2009
7511046Thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives useful as Dantagonists
The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. Th...
03/31/2009
7432254Method for treating glaucoma IC
Provided is a method of treating or ameliorating or preventing glaucoma, decreasing intraocular pressure or improving or amemliorting ocular accommodation in an animal, including a human comprising administering an intraocular pressure decreasing or accommodation im...
10/07/2008
74140484,5-dihydro-isoxazole derivatives and their pharmaceutical use
The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A1=A2-A3=A4- is a pyridinylidene, p...
08/19/2008
7405218Isothiazole derivatives useful as anticancer agents
The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein....
07/29/2008
7348347Substituted 4,5,6,7-tetrahydrobenzthiazol-2-ylamine compounds
Substituted 4,5,6,7-tetrahydrobenzothiazol-2-ylamine compounds, a method for their production; pharmaceutical compositions comprising them, and methods of use for modulating biological functions and/or treating or inhibiting various medical conditions such as, e.g.,...
03/25/2008
7335660Isochroman compounds for treatment of CNS disorders
This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the tre...
02/26/2008
7300949Thiazolopyrazoles and methods of their use
This invention concerns novel thiazolopyrazole compounds and compositions comprising them. Methods of using these compounds for the treatment, prevention and management of various diseases and disorders are also encompassed by the invention. ...
11/27/2007
7265103Substituted amino isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart o...
09/04/2007
7253172Dipeptidyl peptidase inhibitors for the treatment of diabetes
Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (I) are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent d...
08/07/2007
7241761Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups
The present invention relates to compounds of the general formula I wherein R1 is the group and R2, R′, R″, R3...
07/10/2007
72299944(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain anxiety or gastrointestinal disorders
Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; R2 is independently selected from ethyl and isopropyl; R3 is indepen...
06/12/2007
7214679Piperidine/piperazine-type inhibitors of p38 kinase
Compounds of the formula: wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase. ...
05/08/2007
7208169Biphenyl carboxamides
The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality...
04/24/2007
7208505β3 adrenergic agonists
The present invention relates to a β3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful, e.g., for treating Type 2 diabetes and/or obesity...
04/24/2007
7186724Heterocyclic substituted carbonyl derivatives and their use as dopamine Dreceptor ligands
The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine...
03/06/2007
7173035Arylsulfonamide compounds
The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II...
02/06/2007
7169786Isoxazoline derivatives as anti-depressants
The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piper...
01/30/2007
7157464Substituted piperazines
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful ...
01/02/2007
7153858Arylpiperazinyl compounds
The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formulae I: and II, and synthesis and uses of those compounds for treating diseases including those mediated directly or indirectly by 5-HT rec...
12/26/2006
7148219Biaryl heterocyclic compounds and methods of making and using the same
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety th...
12/12/2006
7144883Bicyclic sulfonamide compounds
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obe...
12/05/2006
7141570N-aryl-2-oxazolidinone-5-carboxamides and their derivatives
The present invention provides antibacterial agents having the formula I described herein. ...
11/28/2006
7125903Thienoisoxazolyl-and thienylpyrrazolyl-phenoxy substituted propyl derivatives useful as Dantagonists
The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. Th...
10/24/2006
7125887Pyrrolidine modulators of CCR5 chemokine receptor activity
Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokin...
10/24/2006
7101886Phenylalkyl and pyridylalkyl piperazine derivatives
This invention relates to compounds of the formula 1 wherein R1, R3, R4, X1, and X2 are defined as in the specification, pharmaceutical compositions containi...
09/05/2006
RE39265Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compound...
09/05/2006
7091199Thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives useful as d antagonists
The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These condi...
08/15/2006
7087611Preparation of an anhydrate form of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride (ziprasidone hydrochloride)
The present invention relates to new and useful processes for the preparation of the anhydrate form of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride. ...
08/08/2006
7019009Acyl derivatives of 5-(2-(4-(1,2 benzisothiazole-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2h-indol-2-one having neuroleptic activity
A process for preparing acyl derivatives as prodrugs of 5-(2-(4-(1,2 benzisothiazole-3-yl)-1-piperazinyl)ethyl-6-chloro-1,3-dihydro-2H-indol-2-one and pharmaceutically acceptable acid addition salts and methods of use as an antipsychotic. ...
03/28/2006
6982262Combination of cyamemazine and an atypical neuroleptic
The present invention relates to the combination of cyamemazine and an atypical neuroleptic, or a pharmaceutically acceptable salt thereof, and to the use thereof in the treatment of schizophrenia, and in particular of acute episodes of schizophrenia. ...
01/03/2006
6969713Piperidine and piperazine acetamide derivatives
The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy
11/29/2005
69060742-phenylpiperazine derivatives
A 2-phenylpiperazine derivative represented by the formula (I) or a pharmaceutically acceptable salt, hydrate, or complex thereof: wherein each of X1 and X3 is oxygen or two hydrogen atoms, X...
06/14/2005
6884803Phenylalkynes
Disclosed are substituted phenylalkynes of formula (I), wherein R1, R2, R3, R4, R5 and n are as defined, compositions containing them, and methods of making and us...
04/26/2005
6861432Piperazine derivatives that destabilize androgen receptors
This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R′, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the inventio...
03/01/2005
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