Compounds of formula (I), wherein n is 0, 1 or 2; R1 is hydrogen; R2 is selected from hydrogen, halogen, cyano, OR4, -(CH2)m-(C=O)NR5R6, -(CH2)m-SO2NR5R6, -(CH2)m-NR7(C=O)R8, -(CH2)m-NR7SO2R8, -(CH2)m-S(O)xR8, -(CH2)m-NR7(C=O)NR5R6, -(CH2)m-NR7(C=O)OR9, and -CH=CH(CH2)yR10; R3 is selected from hydrogen and C1 to C6 linear or branched alkyl; R4 is selected from hydrogen, C1 to C6 alkyl, and aryl; R5 and R6 are independently selected from hydrogen, C1 to C6 alkyl, aryl, and C1 to C3 alkyl-aryl or R5 and R6 taken together to form a 4, 5, or 6 membered ring; R7 and R8 are independently selected from hydrogen, C1 to C6 alkyl, aryl, and C1 to C3 alkyl-aryl; R9 is selected from hydrogen, C1 to C6 alkyl, aryl, and C1 to C3 alkyl-aryl R10 is selected from -(C=O)NR5R6 and -SO2NR5R6, wherein R5 and R6 are defined as above, and -NR7(C=O)R8, -NR7SO2R8, -NR7(C=O)NR5R6, -S(O)xR8 and -NR7(C=O)OR9, wherein R7, R8, and R9 are as defined above; y is 0, 1, or 2; x is 1 or 2; m is 0, 1, 2, or 3; and the above aryl groups and the aryl moieties of the above alkylaryl groups are independently selected from phenyl and substituted phenyl, wherein said substituted phenyl may be substituted with one to three groups selected from C1 to C4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, and C1 to C4 alkoxy and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.
Chimeric immunoglobulins specific for p55 TAC protein of the IL-2 receptor
Abstract
Novel methods for designing humanized immunoglobulins having one or more complementary determining regions (CDR’s) from a donor immunoglobulin and a framework region from a human immunoglobulin comprising first comparing the framework or variable region amino acid sequence of the donor immunoglobulin to corresponding sequences in a collection of human immunoglobulin chains, and selecting as the human immunoglobulin one of the more homologous sequences from the collection. Each humanized immunoglobulin chain may comprise about 3 or more amino acids from the donor immunoglobulin in addition to the CDR’s, usually at least one of which is immediately adjacent to a CDR in the donor immunoglobulin. The heavy and light chains may each be designed by using any one or all three additional position criteria. When combined into an intact antibody, the humanized immunoglobulins of the present invention will be substantially non-immunogenic in humans and retain substantially the same affinity as the donor immunoglobulin to the antigen, such as a protein or other compound containing an epitope.
A biodegradable polymer is provided for use in providing syringeable, in-situ forming, solid biodegradable implants for animals. The polymer is placed into the animal in liquid form and cures to form the implant in-situ. A thermoplastic system to form said implant comprises the steps of dissolving a non-reactive polymer in biocompatible solvent to form a liquid, placing the liquid within the animal, and allowing the solvent to dissipate to produce the implant. An alternative, thermosetting system comprises mixing together effective amounts of a liquid acrylic ester terminated, biodegradable prepolymer and a curing agent, placing the liquid mixture within an animal and allowing the prepolymer to cure to form the implant. Both systems provide a syringeable, solid biodegradable delivery system by the addition of an effective level of biologically active agent to the liquid before injection into the body.
[UK] UK High Court approves SPCs for functionally defined products
“On 18 July 2014, the UK High Court applied a liberal interpretation of the law concerning Supplementary Protection Certificates (SPCs) and, in particular, what determines whether a product is “protected by a basic patent”. The Court ruled that a patent with a functional definition only of an active ingredient can be the basis for an SPC. The judgment is of particular relevance to patents relating to antibodies, as well as to other biological products that are typically defined by their mode of action.”
[Bulgaria] A Bulgarian milestone as Supreme Court rules on Atripla application
“In a decision of 8 June 2014 the Court held that the claimed product, consisting of efavirenz, emtricitabine and tenofovir disoproxil fumarate, was not protected by the basic patent BG 62612 and therefore did not meet the requirements of Article 3 of the SPC Regulation.”
[LATAM] The Role of Patents in the Latin American Development: ‘Models of protection’ of Pharmaceutical Patents and Access to Medicines in Brazil, Chile and Venezuela
“This book reviews the strategies or models of protection used in Brazil, Chile and Venezuela to balance both intellectual property rights (pharmaceutical patents) and access to medicines. Each country seems to have shaped their policies in accordance with their national priorities, whether these are motivated by health, political or commercial issues.”
[Africa] Local Production of Pharmaceutical Products in Africa: The WHO approach
“The WHO Global Strategy and Plan of Action mandated the Director General to support transfer of technology and local production of medicines in developing countries. This paper briefly lays out the conditions for local production in Africa and describes the on-going work program of the WHO Department of Public Health, Innovation, Intellectual Property and Trade (PHI) directed at supporting local production efforts.”
[Italy] Italy: new developments in the “Pfizer saga” – a recent judgment provides further guidance on the interaction between antitrust law and patent law in the pharmaceutical sector“The Italian Supreme Administrative Court’s recent judgment in the Pfizer case, which upheld a decision by the Italian Competition Authority (ICA) finding Pfizer in breach of Article 102 of the Treaty on the Functioning of the European Union (TFEU), represents a key development concerning the interaction between antitrust law and patent law in the pharmaceutical sector, as well as a very peculiar use of the notion of “abuse of rights” as a special “genus” of abuse of dominant position. The Supreme Administrative Court overturned the decision by the TAR Lazio (i.e. the Italian administrative court of first instance with jurisdiction over antitrust cases), which had annulled the ICA’s decision.”
[Europe] Clear and safe extensions – CJ rules safeners eligible for SPC protection“In a recent decision (case C-13/11), the Court of Justice of the European Union (CJ) has ruled that a supplementary protection certificate (SPC) can be granted for a safener. The decision is welcome news for applicants and much clearer than recent SPC decisions which have raised more questions than answers”.