Abstract:
Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R1, R2, R3, R4, R5, R6, R7; R8, R9 and R10 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HTV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HTV infection and ADDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Abstract:
The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt or stereoisomer thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.
Abstract:
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. They are also useful for treating neurodegenerative diseases, mental retardation, 10 schizophrenia, inflammatory diseases, restenosis, immune disorders, diabetes, cardiovascular disorders and asthma.
Abstract:
The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or stereoisomers thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.
Abstract:
The present invention discloses a compound of formula (I): wherein: R1 is an aryl or heteroaryl ring; R2 is hydroxy, C1-6 alkoxy, C1-6 alkyl, amino, NR′R″ or C1-6 alkyl-NR′R″ where R′ and R″ are independently chosen from hydrogen and C1-4 alkyl and where R′ and R″, together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing 3-7 membered heterocycle optionally containing a further nitrogen atom and optionally substituted by NR′R″ as defined above or R2 is C1-6 alkoxy substituted by NR′R″ as defined above; R3 is hydrogen or C1-6 alkyl; R4 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl or aryl C1-6 alkyl; R5 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl, aryl C1-6 alkyl or C1-6 alkoxycarbonyl; or R4 and R5, together with the nitrogen atom to which they are attached, form a C3-C10 mono- or bicyclic saturated ring; X and Y are independently chosen from hydrogen, hydroxy, nitro, amino, cyano, CF3, halogen and C1-4 alkyl; or a pharmaceutically acceptable salt thereof; as NK-2/NK-3 ligands for treating schizophrenia, COPD, asthma or irritable bowel syndrome.
Abstract:
The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.
Abstract translation:本发明提供治疗患有诸如精神分裂症的受试者的方法,所述疾病包括施用NK-3拮抗剂,其包括向该受试者施用治疗有效量的式I化合物:其中 通常,Q是R 1是苄基,苯基,噻吩或任选被C 1-4烷基或卤素取代的咪唑基,例如甲基,氟或溴; R 2是氢或C 1-4烷基,例如甲基; R 3是苯基; R 4是氢; R 5是氢或C 1-6烷基羰基,例如甲基羰基; X是-SO 2 - 或-C(O)N(R 2)SO 2 - ,其中R 2 O / >优选为氢; Y是键,CH 2或Z 1,其中Z 1是-N(R f), - 其中R 1是C 1-6烷基羰基,例如乙基羰基; R 6是苯基,吡唑基,吡啶基,嘧啶基或苯并咪唑烷基,任选地被一个或两个选自C 1-6烷基和苄基的基团取代,例如甲基,乙基和 苄基; 或其药学上可接受的盐。
Abstract:
A repeat prescription ordering system for allowing patients requiring resupply of medication or medical products to access a server using a portable communications and data processing device such as a smart phone or personal digital assistant. The server supplies to the patient a list of medication and medical products which they are authorized to order. The patient can select the products required, and the order is logged by the server and allocated to a supplier for completion of the order. The server maintains an estimate of the amount of medication or medical product held by the patient, this being based on the prescribed dosage regimen and information entered by the patient on their usage and, optionally, on checks on their own health. The patient may be alerted when the estimate indicates that their supplies are running low. The estimate is allowed to go below zero, this implying a possible departure from the prescribed medication regimen.
Abstract:
The locking mechanism includes a lever handle having a fluted passageway for fitting to an adjacent end of a latch spindle. The passageway allows the handle to turn relatively to the latch spindle in opposite directions through a predetermined angle of movement. At one end of this angle of movement, the handle is in a horizontal rest position and is engageable with the latch spindle for turning the spindle in a direction to withdraw the latch bolt from its latching position, and at the opposite end, the handle is in a lifted locking position and is engageable with the spindle to prohibit turning thereof in the opening direction. At the locking position, a locking member slidably mounted in the handle and controlled by a trigger part, extending behind the lever part of the handle is engageable in one of a pair of retainer holes depending on the handing of the lever handle.
Abstract:
Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.