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Class 514/327 - Chalcogen bonded directly to ring carbon of the piperidine ring


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein chalcogen (i.e., oxygen, sulfur,
No. of patents: 562
Last issue date: 04/16/2013


1                      
NumberTitleIssue Date
8420674Method of providing pirfenidone therapy to a patient
The invention relates to methods for decreasing adverse events associated with pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) therapy. The invention discloses an optimized dose escalation scheme that results in the patient having increased tolerance to adverse even...
04/16/2013
8410139Prodrugs of a piperidinyl derivative as modulators of chemokine receptor activity
The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma ...
04/02/2013
83620404-phenylpiperidine derivatives as renin inhibitors
Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coro...
01/29/2013
8334306Nitroxide free radical synergized antineoplastic agents
Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivat...
12/18/2012
8299098Piperidinyl derivative as a modulator of chemokine receptor activity
The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic...
10/30/2012
8258159Inhibitors of the α2β1/GPIa-IIa integrin
Novel compounds inhibiting the integrin α2β1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of int...
09/04/2012
8247434Fexofenadine polymorphs and processes of preparing the same
Anhydrous crystalline fexofenadine hydrochloride Form C, crystalline fexofenadine acetate monohydrate Form D, crystalline fexofenadine acetate dihydrate Form E and crystalline fexofenadine free base monohydrate Form F, processes of preparing the same, pharmaceutical...
08/21/2012
8222277Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of non...
07/17/2012
8211916N- and O-substituted 4-[2-(diphenylmethoxy)-ethyl]-1-[(phenyl)methyl]piperidine analogs and methods of treating CNS disorders therewith
N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl] piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and S...
07/03/2012
8129414Non-competitive NMDA receptor antagonists
Disclosed herein are non-competitive NMDA receptor antagonists having chemical structures similar to that of phencyclidine (PCP). These antagonists contain a polycyclic ring structure in place of the cycloalkyl ring of PCP. The antagonists also differ from PCP in th...
03/06/2012
7994198Piperidinetriol derivatives as inhibitors of glycosylceramidsynthase
Compounds of formula (I); wherein R represents various substituent groups, are useful as inhibitors of glucosylceramide synthase. ...
08/09/2011
7910609Inhibitors of integrin alpha2beta1 with modified urea moiety
Novel compounds inhibiting the integrin α2β1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of int...
03/22/2011
7910608Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as define...
03/22/2011
7910607Nitroxide free radical synergized antineoplastic agents
Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivat...
03/22/2011
78120354-substituted piperidines, and methods of use thereof
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine tra...
10/12/2010
7700628Aromatic ether derivatives useful as thrombin inhibitors
This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process fo...
04/20/2010
7662838Use of a deoxynojirimycin derivative or a pharmaceutically salt thereof
The invention relates to the use of a deoxynojirimycin derivative, or pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of insulin resistance, hyperpigmentation and/or inflammatory processes in the skin, a fungal disease...
02/16/2010
7635707Pirfenidone treatment for patients with atypical liver function
Methods are provided for administering pirfenidone to a patient that has exhibited abnormal biomarkers of liver function in response to pirfenidone administration. The methods include administering to a patient pirfenidone at doses lower than the full target dosage ...
12/22/2009
7625928Nitroxide radioprotector formulations and methods of use
Pharmaceutical compositions useful in preventing and treating negative side effects accompanying radiotherapy are disclosed. More particularly, new formulations that can be applied to the skin and mucous membranes of patients undergoing radiotherapy and methods of u...
12/01/2009
7595331N-and O-substituted 4-[2-(diphenylmethoxy)-ethyl]-1-[(phenyl)methyl]piperidine analogs and methods of treating CNS disorders therewith
N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SE...
09/29/2009
7582655Antineoplastic compounds
The present invention relates to 4-piperidone derivatives represented by the following formula (I) and the acid addition salts thereof. The method of preparation and antineoplastic activity of the said compounds are disclos...
09/01/2009
7569588Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. Th...
08/04/2009
7566729Modifying pirfenidone treatment for patients with atypical liver function
Methods are provided for administering pirfenidone to a patient that has exhibited abnormal biomarkers of liver function in response to pirfenidone administration. The methods include administering to a patient pirfenidone at doses lower than the full target dosage ...
07/28/2009
7531555Compositions and methods for selective inhibition of nicotine acetylcholine receptors
The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotinic acetylcholine receptors by administering 2,2,6,6-tetramethylpiperidin-4-yl heptanoate (TMPH), or a pharmaceutically acceptable salt the...
05/12/2009
7501442Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. Th...
03/10/2009
7456199Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 are as defined in t...
11/25/2008
7442711Amelioration of the development of cataracts and other ophthalmic diseases
Ophthalmically acceptable compositions used in arresting the development of cataracts or macular degeneration comprising a pharmaceutically acceptable carrier or diluent and a compound having the formula: where R1
10/28/2008
7439257Aryloxyalkylcarbamate-type derivatives, preparation method thereof and use of same in therapeutics
The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.
10/21/2008
74357465-thiopiperdinyl prostaglandin E analogs
A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. Y and R are described in detail herein A compound having an ω chain comprising ...
10/14/2008
7411093Aminocycloalkanes as DPP-IV inhibitors
The present invention relates to compounds of formula (I) wherein R1 is as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or p...
08/12/2008
7407973Use of pirfenidone in therapeutic regimens
The present invention provides methods for treating a disorder, and methods for inhibiting a stress-activated protein kinase (SAPK) in a cell in an individual, the methods generally involving administering to an individual in need thereof an effective amount of pirf...
08/05/2008
7393873Arylsulfonamide derivatives
N-aryl arylsulfonamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. ...
07/01/2008
7378446Compound having anti-HCV activity and process for producing the same
The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its having a high degree of replication inhibitory activity against HCV,...
05/27/2008
7375230Fermentation and purification of migrastatin and analog
Migrastatin and a migrastatin analog can be produced by fermentation of Streptomyces platensis NRRL 18993 and used in pharmaceutical formulations to treat cancer and/or inhibit metastasis of cancer cells. ...
05/20/2008
73684432,6-disubstituted piperidines and piperazine compounds
The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: which are used to treat diseases of the central nervous system, drug abuse, and withdrawal there...
05/06/2008
7361666Heterocyclic analgesic compounds and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-couple...
04/22/2008
7348341Chemical compounds
The invention concerns compounds of formula (I), and their use in therapy, particularly in the modulation of CCR3 activity. ...
03/25/2008
73389653,4-disubstituted, 3,5-disubstituted and 3,4,5-substituted piperidines
The invention relates to substituted piperidine, piperazine, morpholine and thiomorpholine compounds useful in the treatment of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precu...
03/04/2008
7338962Spirocyclic heterocyclic derivatives and methods of their use
Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be us...
03/04/2008
7326716Treatment of inflammatory bowel disease
The present invention provides a method of treating inflammatory bowel disease which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a piperidinyl prostaglandin E analog. ...
02/05/2008
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