Amgen Inc.

Colin V Gegg

Fei Xiong

Kenneth William Walker

Olaf B Kinstler

Karen C Sitney

Thomas Charles Boone

Shaw-Fen Sylvia Hu

Leslie Phillip Miranda

Chadwick Terence King

Hsieng Sen Lu

David W Brankow

Licheng Shi

Yue-Sheng Li

Qi Huang

Benny C Askew

Chuan-Fa Liu

John Kevin Sullivan

Aimee Freeman

Jeonghoon Sun

Mark Leo Michaels

Derin C D'amico

Hosung Min

Randy Ira Hecht

Cen Xu

Edward John Belouski

Hung Q Nguyen

Gordon Ng

Yuelie Lu

Thomas Storz

Mark A Jarosinski

Mei-Mei Tsai

Jerry Ryan Holder

Joseph G McGivern

Stefan I McDonough

Jing Xu

Francesco Galimi

Eileen J Johnson

Marie E Wright

Murielle M Ellison

Jr Benny C Askew

Liu Chuan-Fa

Olaf Boris Kinstler

Antigen binding proteins that bind to human CGRP receptor (CGRP R) are provided. Nucleic acids encoding the antigen binding protein, vectors, and cells encoding the same are also provided. The antigen binding proteins can inhibit binding of CGRP R to CGRP, and are useful in a number of CGRP R related disorders, including the treatment and/or prevention of migraine headaches.

Human CGRP receptor binding proteins

Disclosed is a process for preparing a pharmacologically active compound, in which at least one internal conjugation site of an Fc domain sequence is selected that is amenable to conjugation of an additional functional moiety by a defined conjugation chemistry through the side chain of an amino acid residue at the conjugation site. An appropriate amino acid residue for conjugation may be present in a native Fc domain at the conjugation site or may be added by insertion (i.e., between amino acids in the native Fc domain) or by replacement (i.e., removing amino acids and substituting different amino acids). In the latter case, the number of amino acids added need not correspond to the number of amino acids removed from the previously existing Fc domain. This technology may be used to produce useful compositions of matter and pharmaceutical compositions containing them. A DNA encoding the inventive composition of matter, an expression vector containing the DNA, and a host cell containing the expression vector are also disclosed.

Modified Fc molecules

Disclosed is a DNA encoding a composition of matter of the formula(X)&#x2014;(F)&#x2014;(X)&#x2014;(F)&#x2014;(X)&#x2003;&#x2003;(I)and multimers thereof, in which Fand Fare half-life extending moieties, and d and e are each independently 0 or 1, provided that at least one of d and e is 1; X, X, and Xare each independently -(L)-P-(L)-, and f and g are each independently 0 or 1; P is a ShK peptide analog of no more than about 80 amino acid residues in length; L is an optional linker; and a, b, and c are each independently 0 or 1, provided that at least one of a, b and c is 1. A DNA encoding the ShK peptide analog is disclosed. Also disclosed are an expression vector comprising the DNA, and a host cell comprising the expression vector.

Toxin peptide therapeutic agents

The invention relates to the field of compounds, especially peptides or polypeptides, that have thrombopoietic activity. The peptides and polypeptides of the invention may be used to increase platelets or platelet precursors (e.g., megakaryocytes) in a mammal.

Thrombopoietic compounds

The present invention relates to composition of matter involving bradykinin B1 receptor antagonist peptides conjugated to a univalent vehicle, including peptides conjugated to univalent PEG. These compositions can be used as therapeutics or prophylactics against diseases or conditions, such as inflammation or pain, linked to the bradykinin B1 receptor.

Antagonists of the bradykinin B1 receptor

The present invention relates to composition of matter involving bradykinin B1 receptor antagonist peptides conjugated to a multivalent vehicle, including peptides conjugated to multivalent PEG. These compositions can be used as therapeutics or prophylactics against diseases or conditions, such as inflammation or pain, linked to the bradykinin B1 receptor.

Disclosed is a composition of matter of the formula(X)&#x2014;(F)&#x2014;(X)&#x2014;(F)&#x2014;(X)&#x2003;&#x2003;(I)and multimers thereof, in which Fand Fare half-life extending moieties, and d and e are each independently 0 or 1, provided that at least one of d and e is 1; X, X, and Xare each independently -(L)-P-(L)-, and f and g are each independently 0 or 1; P is a toxin peptide of no more than about 80 amino acid residues in length, comprising at least two intrapeptide disulfide bonds; L is an optional linker; and a, b, and c are each independently 0 or 1, provided that at least one of a, b and c is 1. Linkage to the half-life extending moiety or moieties increases the in vivo half-life of the toxin peptide, which otherwise would be quickly degraded. A pharmaceutical composition comprises the composition and a pharmaceutically acceptable carrier. Also disclosed are a DNA encoding the inventive composition of matter, an expression vector comprising the DNA, and a host cell comprising the expression vector. Methods of treating an autoimmune disorder, such as, but not limited to, multiple sclerosis, type 1 diabetes, psoriasis, inflammatory bowel disease, contact-mediated dermatitis, rheumatoid arthritis, psoriatic arthritis, asthma, allergy, restinosis, systemic sclerosis, fibrosis, scleroderma, glomerulonephritis, Sjogren syndrome, inflammatory bone resorption, transplant rejection, graft-versus-host disease, and lupus and of preventing or mitigating a relapse of a symptom of multiple sclerosis are also disclosed.

The present invention concerns compositions of matter, for example, but not limited to, modified antibodies, in which one or more biologically active peptides are incorporated into a loop region of a non-terminal domain of an immunoglobulin Fc domain.

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Camarillo, CA, United States of America

Colin V Gegg