Basel, Switzerland

Hoffmann-La Roche

www.roche.com
Basel, Switzerland

F. Hoffmann-La Roche Ltd. is a Swiss global health-care company that operates worldwide under two divisions: Pharmaceuticals and Diagnostics. Its holding company, Roche Holding AG, has shares listed on the SIX Swiss Exchange. Wikipedia.


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The present invention relates to compounds TAAR receptor antagonists of formula I wherein X, R, L, Ar and R^(1 )are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I.


Patent
Hoffmann-La Roche | Date: 2017-01-26

The present invention relates to compounds of formula of formula I wherein X, L and R^(1 )are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric, metabolic, cardiovascular or sleep disorders with compounds of formula I.


Patent
Hoffmann-La Roche | Date: 2017-04-05

One aspect as reported herein is using a method comprising the step of immunizing an experimental animal, three times with primary cynomolgus PBLs, whereby the PBLs are optionally enriched for T cells without using primary human PBLs as immunogen and without using a denaturing agent for producing a human cynomolgus cross-reactive antibody specifically binding to human CD3 epsilon of SEQ ID NO: 02 and specifically binding to a polypeptide of SEQ ID NO: 01, wherein the human cynomolgus cross-reactive antibody specifically binds to human and cynomolgus T cells, activates human T cells and does not bind to the same epitope as the antibody OKT3, the antibody UCHT1 and/or antibody the SP34.


Patent
Hoffmann-La Roche | Date: 2017-04-26

Provided are novel, non-naturally occurring chagasin scaffold proteins derived from chagasin or chagasin-like protease inhibitor proteins. Also provided are libraries of non-naturally occurring chagasin scaffold proteins and methods of using such libraries to generate non-naturally occurring chagasin scaffold proteins that specifically bind to a target ligand. The present invention further provides methods of using non-naturally occurring chagasin protein scaffold that bind to a target ligand, including diagnostic and therapeutic compositions and methods. The invention also provides novel non-naturally occurring chagasin scaffold proteins that specifically bind low density lipoprotein receptor-related protein 6 (LRP6) and novel non-naturally occurring chagasin scaffold proteins that specifically bind vascular endothelial growth factor (VEGF).


The invention relates to compounds of formula (I) wherein.....C.....is -CH2- or -CH2-CH2-; X is -NH-, -C(0)NH- or -NHC(0)NH-; Ar is phenyl or a 5 or 6-membered heteroaryl group containing one or two N atoms; R1 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by cycloalkyl, lower alkoxy substituted by halogen or is cycloalkyl; -( )- is -CH2-; n is 0 or 1; m is 0, 1 or 2; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinsons disease, neurodegenerative disorders, Alzheimers disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.


Methods of treating patients having HER2 -positive, operable, locally advanced or inflammatory breast cancer with the antibody-drug conjugate Trastuzumab-MCC-DMl and Pertuzumab are provided.


Patent
Hoffmann-La Roche | Date: 2017-01-25

The invention provides novel compounds having the general formula (I) and tautomers and pharmaceutically acceptable salts thereof, wherein A1, A2, A3, A4, R1, R4, R5, R6, R7 and R8 are as defined herein, compositions including the compounds and methods of using the compounds.


Patent
Hoffmann-La Roche and Hoffmann-La Roche | Date: 2017-05-17

Disclosed is a transfilling device (1) for transfilling a liquid drug from a cartridge (3) to a flexible reservoir (4). The transfilling device (1) includes a support unit (111) and a plunger (113), the support unit (111) configured to receive the cartridge (3), the plunger (113) being insertable into the cartridge (3), wherein the plunger (113) is displaceable relative to the support unit (111) along an advancement direction (2) between a plunger retracted position, where the plunger (113) is in a most distal position relative to the support unit (111), and a plunger advanced position, where the plunger (113) is in a most proximal position relative to the support unit (111), wherein the plunger (113) is configured to push a piston (32) of the cartridge (3) from a piston retracted position to a piston advanced position by displacing the plunger (113). The transfilling device (1) further includes a transfer cannula (12, 12), wherein the transfer cannula (12, 12) is configured to penetrate a flexible reservoir septum (41) with a cannula outlet end (122) and to penetrate a cartridge septum (31) with a cannula inlet end (121) and thereby to fluidly couple the flexible reservoir (4) with the cartridge (3). The transfilling device further includes a reservoir locking unit (13), wherein the reservoir locking unit () is configured to releasably mechanically couple the support unit (111) to the flexible reservoir (4) and wherein the coupling of the reservoir locking unit (13) is designed such that the coupling is released in the plunger advanced position.


A laboratory sample distribution system is presented. The laboratory sample distribution system comprises a number of container carriers. The container carriers each comprise at least one magnetically active device such as, for example, at least one permanent magnet, and carry a sample container. The system further comprises a transport plane to carry the container carriers and a number of electro-magnetic actuators being stationary arranged below the transport plane. The electro-magnetic actuators move a container carrier on top of the transport plane by applying a magnetic force to the container carrier.


Patent
Hoffmann-La Roche | Date: 2017-01-04

The present invention relates to compounds of formula I, wherein Y is N or C-R1; R1 is hydrogen or F; R1 is hydrogen, halogen or lower alkyl substituted by halogen; R2 is hydrogen or lower alkyl; or R2 forms together with R4 a 6 membered heterocyclic ring containing -CH2-CH2-O-CH2- or -CH2-CH2-NR-C(O)-; R is hydrogen, lower alkyl, phenyl or benzyl; R3 is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be in different positions; R4 is hydrogen, lower alkyl or lower alkoxyalkyl; R4 is hydrogen, lower alkyl, phenyl optionally substituted by halogen or lower alkoxy, or is cycloalkyl, or is pyridinyl optionally substituted by halogen, lower alkyl, lower alkoxy or =0, or is pyrimidinyl optionally substituted by lower alkyl, lower alkoxy or =0, or is 1 -lower alkyl-pyridinyl, or is pyrazinyl, or is pyridazinyl optionally substituted by lower alkyl, lower alkoxy or =0, or is l-methylpyrrolo[2,3-b]pyridine-5-yl, or is 6-imidazo[l,2- b]pyridazin-6-yl; or R4 forms together with R4 a 4, 5 or 6 membered heterocyclic ring containing -(CH2)5-, -CH2-CH2-O-CH2-CH2-, -CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-, -CH2-O-CH2-CH2- or CH2-CH2-CH2-O-CH2; R5 and R5 are hydrogen or lower alkyl; or R4 forms together with R5 a saturated 5- membered ring containing -CH2-CH2-CH2-; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Parkinsons disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.

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