Abstract:
The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, Rls R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
Abstract:
The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C(=O)-; -C(=O)-C(=O)-; -NRX-C(=O)-; -Z-C(=O)-; -Z-NRX-C(=O)-; -C(=O)-Z-; -NRX-C(=O)-Z-; -C(=S)-; -NRX-C(=S)-; -Z-C(=S)-; -Z-NRX-C(=S)-; - C(=S)-Z-; -NRX-C(=S)-Z-; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents -C(=O)-NRX- or -NRX-C(=O)-; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3- dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (A), (B) are excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.
Abstract:
The present disclosure relates to compounds, which are useful for regulating the expression of apolipoproteiπ A-I (ApoA-l), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
Abstract:
The present invention is directed to cyclic sulfonamide derivatives of formula (I): or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behaviorial disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.
Abstract:
The present invention relates to compounds of the general Formula (I) wherein (A) is a 5 or 6-membered aromatic or heteroaromatic ring; R 1 is cycloalkyl or is aryl or heteroaryl, wherein at least one ring is aromatic in nature, unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, -C(O) -lower alkyl, -S(O) 2 -lower alkyl, nitro or cyano; R 2 is hydrogen or lower alkyl; R 3 is hydrogen or lower alkyl; R 4 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or nitro; R 5 is hydrogen, halogen, lower alkyl or lower alkyl substituted by halogen; X is a bond, -(CH 2 ) m -, -CH 2 O- or -CH 2 NH-; The dotted line denotes a bond or not; n is 1 or 2; m is 1, 2 or 3; and pharmaceutically acceptable acid addition salts thereof and their use in the treatment of neurological and neuropsychiatric disorders.
Abstract translation:本发明涉及通式(I)的化合物,其中(A)是5或6元芳族或杂芳族环; R 1是环烷基或芳基或杂芳基,其中至少一个环在本质上是芳族的,未被取代或被1至3个选自以下的取代基取代:卤素,低级烷基,被 卤素,低级烷氧基,被卤素取代的低级烷氧基,-C(O) - 低级烷基,-S(O)2 - 低级烷基,硝基或氰基; R 2是氢或低级烷基; R 3是氢或低级烷基; R 4是卤素,低级烷基,被卤素取代的低级烷基,低级烷氧基,被卤素或硝基取代的低级烷氧基; R 5是氢,卤素,被卤素取代的低级烷基或低级烷基; X是一个键, - (CH 2)2 - , - CH 2 O-或-CH 2 - NH-; 虚线表示不是键; n为1或2; m为1,2或3; 及其药学上可接受的酸加成盐及其在治疗神经和神经精神障碍中的用途。
Abstract:
The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
Abstract:
The invention concerns compounds of formulae (Ia) or (Ib) wherein M: represents a molecule for use in the treatment or diagnosis of pathologies affecting the cartilage; R1, R2, R3 represent an alkyl group, or R1, R 2, R3 together with the nitrogen atom which bears them form a heterocycle; X represents a C1-C6 alkyl chain wherein one or several -CH2- groups are optionally substituted by a sulphur, an oxygen atom, a -NR, -CO-, -CO-NH-, -CO2-, SO- or SO2- group; n represents 0 or 1; Hal represents a halogen atom, or the formula (Ib); R4 represents an alkyl group; Hal represents a halogen atom. General formula (F1) represents a molecule for use in the treatment or diagnosis of pathologies affecting the cartilage, provided that the nitrogen atom can optionally be included in a saturated or unsaturated nitrogenous heterocyclic system, or involved in a double bond.