Abstract: The invention provides chroman compounds having formula 1 wherein R1 is (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl, and independently R1 has a cis-orientation in relation to the exocyclic phenyl group at the 2-position of the skeleton; R4 is H, Hal, CF3, OH or (1C-2C)alkyloxy; R2, R3, and R5are independently H, Hal, CF3, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl and prodrugs thereof for the manufacture of a medicine for estrogen-receptor related treatments.

Abstract: Disclosed is a novel class of steroid compounds based on estradiol, and carrying an 11?-substitution. Said substitution is a hydrocarbon group which may be linear or branched, provided that it comprises, as the longest chain on carbon atom no. 11 of the steroid skeleton, one single linear chain having a length of from 5 to 9 carbon atoms, wherein said chain may be saturated or unsaturated. The resulting compounds have a desirable mixed agonist/antagonist profile for estrogen receptor ? and estrogen receptor ?.

Abstract: Embodiments of the present invention generally relate to novel fed-batch fermentations wherein processes of DO-stat and pH-stat are combined for nutrient feeding control.

Abstract: Disclosed herein are methods for treating energy metabolism disorders by administering a composition containing a therapeutically effective amount of a fatty acid amide hydrolase inhibitor. The composition can also be administered to reduce body fat, body weight, or caloric intake.

Abstract: The invention relates to an isolated polynucleotide sequence comprising a nucleic acid sequence encoding the amino acid sequence of KshA protein or of KshB protein, encoded by nucleotides 499-1695 of SEQ ID NO:1 or by nucleotides 387-1427 of SEQ ID NO:2, respectively, and functional homologues thereof. The polynucleotides of the invention can be used to construct genetically modified microorganisms blocked in 3-ketosteroid 9?-hydroxylase activity, which are useful in the microbial degradation of steroids to accumulate certain steroid products.

Abstract: The present invention relates to spiro[2H-1-benzopyran-2,4?-piperidine] derivatives having general formula (I), or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these spiro[2H-1-benzopyran-2,4?-piperidine] derivatives in therapy, more specifically for the treatment of CNS disorders.

Abstract: The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.

Abstract: A nucleotide acid sequence is provided encoding a peptidylargine deiminase 6. The gene is found to be expressed in gonads only and may be used as target for male and female contraception. Its encoded protein can be used to screen for small molecular weight modulators of the enzyme activity.

Abstract: The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. The alkylcarbamic acid aryl ester of Formula (I), KDS-4103, is a FAAH inhibitor. Described herein is a process for the preparation of the compound of Formula (I), characterization of polymorphs of the FAAH inhibitor, and their uses therof.

Abstract: The invention relates to a pharmaceutical dosage form comprising an analgesic combination for simultaneous or sequential use which comprises a peripherally restricted cannabinoid CB1 receptor agonist having a brain Cmax to plasma Cmax ratio of less than 0.1 and an opioid receptor agonist, as well as to a method for treating pain using said pharmaceutical dosage form.

Abstract: The invention relates to 2-(benzimidazol-1-yl)-acetamide bisaryl derivative having the general Formula I wherein n is 0 or 1; Ar1 represents a diradical derived from a 5- or-6-membered aromatic ring, optionally comprising 1-3 heteroatoms selected from N, O and S, said ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy, halogen, CF3 or cyano; Ar2 represents a 6-membered aryl ring, optionally comprising 1-3 nitrogen atoms, said ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl (optionally substituted with 1 or more halogens), (C1-4)alkyloxy (optionally substituted with 1 or more halogens), di(C1-4)alkylamino, halogen, CF3 or cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-acetamide bisaryl derivatives in the treatment of TRPV1 mediated disorders.

Abstract: The invention provides a process for the preparation of 2-substituted-derivatives of estrone and estradiol. The invention also provides several novel compounds, which can be intermediates in the process, and processes to prepare these novel compounds. The invention also provides 2-alkoxy-estrone, 2-alkoxy-estradiol or mixtures thereof essentially free from other estrogenic intermediates.

Abstract: The invention pertains to a kit for assembling a disposable applicator for inserting an implant, in particular a rod-like implant containing an active substance, under the skin of a human or animal, the kit comprising a first component, in turn comprising a main housing part providing a handle for grasping and maneuvering the applicator, a cannula, and a cannula holder mounted in the main housing part, the main housing part having an opening which allows introduction of an implant into the proximal end of the cannula or the cannula holder, and, a second component for closing said opening, in turn comprising a second housing part and a rod attached to or forming an integral whole with the second housing part and mountable inside the cannula or the cannula holder.

Abstract: The present invention generally relates to non-ethylene diamine like compounds that prevent and/or delay carbamylation of peptides.

Abstract: The present invention relates to i-benzylindole-2-carboxamide derivatives of formula I, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 1-benzylindole-2-carboxamide derivatives and to their use in therapy, particularly for the treatment of obesity or nicotine dependence.

Abstract: The present invention relates to 4-phenyl-5-oxo-1,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R1 is (1-6C)alkyl, (2-6C)alkenyl or (2-6C)aDcynyl; R2, R3 are independently halogen, (1-4C)allyl, (2-4C)alkenyl, (2-4C)-alkynyl, (1-4C)aBcoxy, (3-4C)alkenyloxy or (3-4C)alkynyloxy; R4 is phenyl or (2-5C)-heteroaryl, both substituted with R7 and optionally substituted on the (hetero)aromatic ring with one or more substituents selected from hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (1-4C)alkyl, (1-4C)alkoxy, (1-4C)alkylthio and (di)(1-4C)-alkylamino.

Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4-)alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.

Abstract: The invention provides for a combination comprising an amount of an SSRI, or a pharmaceutically acceptable salt or solvate thereof, and an amount of a GR antagonist, or a pharmaceutically acceptable salt or solvate thereof, optionally in association with one or more pharmaceutically acceptable carriers for use as therapy for depression and related disorders.

Abstract: The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.