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Assignee: Hoffman-La Roche Inc.


Location: Nutley, NJ
No. of patents: 404

1                      
NumberTitleIssue Date
8178689Tricyclic compounds
The present invention provides novel compounds of formula I, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the tre...
05/15/2012
8163793Proline derivatives
The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament. ...
04/24/2012
8163781Bi-aryl aminotetralines
The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R1-R5, A, B, Q, W, and X are defined in the detailed description and claims...
04/24/2012
8153815Pseudoproline dipeptides
Disclosed is a process for the manufacture of pseudo proline dipeptides of the formula wherein R1 is a side chain of an alpha amino acid, R2 is an amino protecting group and R3 and R4
04/10/2012
8143273Quinolizidine and indolizidine derivatives
The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid add...
03/27/2012
8138189Substituted benzene compounds as modulators of the glucocorticoid receptor
The present invention relates to compounds of formula I wherein R.sup.1a to R.sup.1e and R.sup.2 to R.sup.5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are gluc...
03/20/2012
8129423Imidazolone and imidazoloidinone derivatives as 11b-HSD1 inhibitors
Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositio...
03/06/2012
8110187Purification and characterization of cytotoxic lymphocyte maturation factor and monoclonal antibodies thereto
The present invention is a novel cytokine protein called IL-12 or Cytotoxic Lymphocyte Maturation Factor (CLMF) which is produced and synthesized by human NC-37 B lymphoblastoid cells (American Type Culture Collection, Rockville, Md.). CLMF synergistically induces w...
02/07/2012
8088936Leukotriene B4 inhibitors
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositi...
01/03/2012
8088815Spiroindolinone pyrrolidines
There are provided compounds of the formula wherein X, Y and R1 to R8 are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as ...
01/03/2012
8084609Spiropiperidine derivatives
The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. The compoun...
12/27/2011
8076360Indoles
The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are usefu...
12/13/2011
8071622Indoles
The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the t...
12/06/2011
8071571Orlistat compositions
A pharmaceutical combination or composition containing a lipase inhibitor, preferably orlistat, and a bile acid sequestrant is useful for treating obesity. ...
12/06/2011
8067599Imidazo [4,5-B] pyridine and pyrrolo [2,3-B] pyridine protein kinase inhibitors
Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments cont...
11/29/2011
8067598Heterofused piperidines as orexin antagonists
The present invention relates to compounds of formula wherein R1, R2, R3, and R4 are as defined herein and hetaryl is a one or two ring-membered heteroaromatic ring s...
11/29/2011
8058269Oxindole derivatives
There is provided compounds of the formula wherein R6, V, W, X, Y, Q and n are as described. The compounds exhibit activity as anticancer agents. ...
11/15/2011
80440475-substituted benzoxazines
The present invention is concerned with 5-substituted benzoxazine derivatives of formula (I) wherein X, R1 and R2 are as described herein, as well as their manufacture, pharmaceutical compositions cont...
10/25/2011
8039624Azaspiro derivatives
The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other...
10/18/2011
8039495Biphenyl carboxylic acids and bioisosteres as glycogen synthase activators
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositi...
10/18/2011
80263654,4-disubstituted piperidine derivatives
This invention relates to 4,4-disubstituted piperidine derivatives of the formula wherein A and R1 to R5 are as defined in the specification, and pharmaceutically acceptable salts thereof. The inventio...
09/27/2011
8026255Substituted piperidines as somatostatin receptor subtype 5 (SSTR5) antagonists
This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their prepara...
09/27/2011
79894494,5-dihydro-oxazol-2-yl amine derivatives
The present invention relates to a compounds of formula I wherein R1, R1′, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceuticall...
08/02/2011
7973051Aminothiazoles as FBPase inhibitors for diabetes
Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in claim 1 and which can be used in the form of pharmaceuti...
07/05/2011
7968554Pyrazolo[3,4-d]pyrimidine derivatives
Disclosed are novel pyrazolo[3,4-d]pyrimidine derivatives that are inhibitors of Raf kinase. These compounds and their pharmaceutically-acceptable salts and esters are anti-proliferative agents useful in the treatment or control of proliferative disorders such as so...
06/28/2011
7956201Process for the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one
The present invention relates to a process of the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one of the formula by employing a dialkylmalonate of the formula wherein R...
06/07/2011
7956074Aryl-isoxazolo-4-yl-oxadiazole derivatives
The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula wherein R1, R2, and R3, are as defined in the specification and...
06/07/2011
79518244-aryl-pyridine-2-carboxyamide derivatives
The present invention relates to novel pyridine-2-carboxyamide derivatives of formula (I) useful as metabotropic glutamate receptor antagonists: wherein Y, Z, R1, R2 and R3 are as defined in...
05/31/2011
7939661Pyridine, quinoline and pyrimidine derivatives
This invention is concerned with compounds of the formula wherein A, R1 to R5 are as defined in the specification and G is a pyridine, quinoline or pyrimidine group as defined in the specification, and...
05/10/2011
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
7935707Imidazole derivatives
The invention is concerned with novel imidazole derivatives of formula (I), wherein m, E, R1, R2, R3, R4, R5, R6 ...
05/03/2011
7932390Substituted thieno[3,2-C]pyridine carboxylic acid derivatives
There are provided compounds of the formula wherein R1, R2, R3, X, ring A and ring B are as described. The compounds exhibit anticancer properties. ...
04/26/2011
7928248Benzopyran and benzoxepin PI3K inhibitor compounds and methods of use
Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms ...
04/19/2011
7923028High dose oral formulation of bisphosphonate and a process for making thereof
The invention relates to a high dose oral formulation of bisphosphonates and to a process for the preparation of such formulations. ...
04/12/2011
7893278CIS-imidazolines
The present invention relates to compounds of the formula and the pharmaceutically acceptable salts and esters thereof, a process for their manufacture, medicaments containing them as well as the use of these compounds as p...
02/22/2011
7893099Cyclopentane derivatives
The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. ...
02/22/2011
7846896PEG conjugates of NK4
The present invention provides a conjugate consisting essentially of a NK4 molecule and a polyethylene glycol group having a molecular weight of from about 20 to about 40 kDa. The invention also provides a composition in which the monoPEGylated conjugates comprise a...
12/07/2010
7875645Method for the treatment of CNS disorders with substituted 2-imidazoles or imidazole derivatives
The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neu...
01/25/2011
78586532-imidazoles
The present invention relates to compounds of formula I, wherein X is —CH2— or —NH—; Y is —CH(lower alkoxy)-, —CH(lower alkyl)-, —O—, —S—, —S(O)—, —S(O)2
12/28/2010
7812161Synthesis of GlyT-1 inhibitors
The present invention relates to a process for preparation of a compound of formula I wherein Het, R1, R2, R3, and n are as defined herein and pharmaceutic...
10/12/2010
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