CAS: 107761-42-2; Amyloid|a-Peptide (1-42) (Human)

专利信息

专利号:US-8546532-B2
优先权日:2008-04-17
标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
发明人：BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

专利号:US-7759492-B2
优先权日:2004-08-20
标 题:Enantioselective synthesis of 13-oxotricyclo[8.2.1.0.3,8] trideca-3(8),4,6-triene-5-carboxylates
发明人：KEEN STEPHEN PHILIP; OLIVER STEVEN FRASER; STEWART GAVIN WILLIAM
权利人:MERCK SHARP & DOHME
摘要:An enantioselective route to compounds of formula I is disclosed: n n n n n n n n n n The compounds of formula I are key intermediates in the synthesis of compounds useful in treatment of Alzheimer's disease.

专利号:US-9662347-B2
优先权日:2010-05-11
标题 :Method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of age-albumin in cells of the mononuclear phagocyte system
发明人：LEE BONG HEE; BYUN KYUNG HEE
权利人:LEE BONG HEE; BYUN KYUNG HEE; GACHON UNIV OF INDUSTRY-ACADEMIC COOP FOUND
摘要:The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc.

专利号:US-10323010-B2
优先权日:2015-07-20
标题 :Methods of chemical synthesis of substituted 10H-phenothiazine-3,7-diamine compounds
发明人：STOREY JOHN MERVYN DAVID; LARCH CHRISTOPHER PAUL; KEMP STEVEN JOHN; CLUNAS SCOTT; NICOLL SARAH LOUISE; GIBBARD HELEN SARAH; SIMPSON MICHAEL; SINCLAIR JAMES PETER; MARSHALL COLIN
权利人:WISTA LAB LTD
摘要:The present invention pertains generally to the field of chemical synthesis, and more particularly to methods of chemical synthesis which include the step of preparing a substituted 10H-phenothiazine-3,7-diamine compound of Formula (1) by a step of selective alkylation by reductive amination, in which the corresponding unsubstituted diamine of Formula (4) is reacted with aldehyde/ketone, under reductive amination conditions. The present invention also relates to such methods which incorporate additional subsequent and/or preceding steps, for example, to prepare compounds of Formulae (2) and (3) from compounds of Formula (1), and to prepare compounds of Formula (4) from, for example, compounds of Formulae (5), (6), (7), (8), and (9). Compounds of Formula (1), Formula (2), and Formula (3) are useful, for example, in the treatment of diseases of protein aggregation, such as Alzheimer's disease.

专利号:US-8703812-B2
优先权日:2005-07-29
标 题 :Protein synthesis required for long-term memory is induced by PKC activation on days preceding associative learning
发明人：ALKON DANIEL L
权利人:ALKON DANIEL L; BRNI NEUROSCIENCES INST
摘要:The present invention provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.

专利号:US-8440844-B2
优先权日:2011-06-21
标题 :Process for the preparation of β-amino alcohol
发明人：RAWAT VARUN; CHOUTHAIWALE PANDURANG VILASRAO; CHAVAN VILAS BHIKU; SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM
权利人:RAWAT VARUN; CHOUTHAIWALE PANDURANG VILASRAO; CHAVAN VILAS BHIKU; SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM; COUNCIL SCIENT IND RES
摘要:A high-yielding enantioselective synthesis of the bioactive (S)—N-(5-chlorothiophene-2-sulfonyl)-β,β-diethylalaniol (7.b.2), a Notch-1-sparing γ-secretase inhibitor metabolite (with EC 50 =28 nM) effective in reduction of Aβ production in vivo, has been realized starting from readily available 3-pentanone. The key steps of the synthesis are proline-catalyzed α-aminooxylation and α-amination of aldehyde; the latter contributing an overall yield of 50-75% and 90-99% enantiomeric excess.