Patent classifications
A61K47/641
DIMERIC COLLAGEN HYBRIDIZING PEPTIDES AND METHODS OF USING
Disclosed are peptide conjugates comprising an active agent, a spacer moiety, and a dimeric collagen hybridizing peptide comprising a first and second collagen hybridizing peptide, a linker; and a branch point, wherein the first and second collagen hybridizing peptides comprise the sequence of at least (GXY)n, wherein G is glycine, wherein X and Y are any amino acid, and wherein n is any number between 3 and 12. Also disclosed are methods of detecting denatured collagen in a sample comprising contacting a composition comprising any one of the disclosed peptide conjugates to a sample, wherein the active agent comprises a therapeutic agent, and detecting the presence or absence of binding of the peptide conjugate to denatured collagen, the presence of binding indicating the presence of denatured collagen in the sample. Also disclosed are methods of treating a disease or injury involving collagen damage comprising administering to a subject having a disease or injury involving collagen damage any one of the disclosed peptide conjugates.
SILICON BASED DRUG CONJUGATES AND METHODS OF USING SAME
Described herein are silicon based conjugates capable of delivering one or more payload moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more payload moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core.
Blood cell biomarker for late onset Alzheimer's disease
Described herein are compositions and methods for diagnosing late-onset Alzheimer's disease (LOAD), treating LOAD and assessing efficacy of therapeutic agents used to treat LOAD.
Compositions and Methods of Manufacturing Star Polymers for Ligand Display and/or Drug Delivery
A star polymer of formula O[P1]-([X]-A[P2]-[Z]-[P3])n where O is a core; A is a polymer arm attached to the core; X is a linker molecule between the core and the polymer arm; Z is a linker molecule between the end of the polymer arm and P3; P1, P2 and P3 are each independently one or more pharmaceutically active compounds that act extracellularly or intracellularly, n is an integer number; [ ] denotes that the group is optional; and at least one of P1, P2 or P3 is present.
CONJUGATES OF TUBULYSIN DERIVATIVES AND CELL BINDING MOLECULES AND METHODS OF MAKING
The present invention relates to the conjugates of Tubulysin derivatives (anologs) and cell-binding molecules using branched (side-chain) linkers, and the resulting conjugates have better pharmacokinetic properties, and thus can more accurately target and kill abnormal cells. The invention also relates to the conjugation methods of the Tubulysin derivatives (anologs) to cell-binding molecules, and methods for synthesizing the small molecules, and methods of using the conjugates for targeted therapy for cancers, infections and autoimmune diseases. The conjugates of Tubulysin derivatives with long branched linkers demonstrated increased half-life, minimal exposure to non-targeted cells, tissues or organs in system circulation, leading to reduced off-target toxicity.
OLIGONUCLEOTIDES WITH NUCLEOSIDE ANALOGS
siRNA compositions are provided that contain gemcitabine (GEM) in place of cytosine moieties within the siRNA sequence. Pharmaceuticals compositions containing these siRNA molecules, and methods of using the compositions for treating diseases such as cancer are provided.
Modular self assembly disassembly (SADA) technologies
The present invention relates to compositions and methods employing conjugates that include a self-assembly and disassembly (SADA) polypeptide and a binding domain. The present invention encompasses the recognition that conjugates with a SADA polypeptide have certain improved biological properties. SADA-conjugates are described, along with uses thereof (e.g., as therapeutic or diagnostic agents) and methods of manufacture.
POLYETHYLENE GLYCOL CONJUGATE DRUG, AND PREPARATION METHOD THEREFOR AND USE THEREOF
- Gaoquan LI ,
- Dajun LI ,
- Qian ZHANG ,
- Diedie LI ,
- Chengzhi GAO ,
- Yue LIU ,
- Xiaoling DING ,
- Yusong WEI ,
- Xiangwei YANG ,
- Yongchen PENG ,
- Jia GAO ,
- Qiang LUO ,
- Yanxia HENG ,
- Mei LIU ,
- Yuyang YI ,
- Xiafan ZENG ,
- Tao TU ,
- Xiao TANG ,
- Xi LIU ,
- Jianhuan LI ,
- Zhaojie WANG ,
- Bin WANG ,
- Jinping WAN ,
- Mingyang HOU ,
- Jiao LIU ,
- Huiyu CHEN ,
- Jie LOU ,
- Yue YANG ,
- Yuanqiang WANG
The present invention relates to the technical field of medicines, and relates to a polyethylene glycol conjugated drug, a preparation method therefor and the use thereof. In particular, the present invention relates to a polyethylene glycol conjugated drug as shown in formula I or a pharmaceutically acceptable salt thereof. The present invention also relates to a method for preparing the polyethylene glycol conjugated drug or the pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the polyethylene glycol conjugated drug or the pharmaceutically acceptable salt thereof, and the use thereof in the preparation of a drug.
##STR00001##
TAXOL CONJUGATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME, AND METHODS FOR THEIR USE
Provided herein are Taxol transporter compounds, pharmaceutical compositions, methods of their preparation, and methods of their use in treatment or prevention of a proliferative, dermatological, or ophthalmological disease or disorder.
ASYMMETRICALLY BRANCHED DEGRADABLE POLYETHYLENE GLYCOL DERIVATIVE
A branched degradable polyethylene glycol derivative with a high molecular weight that does not cause vacuolation of cells is provided. A branched degradable polyethylene glycol derivative represented by the following formula (1), containing, in a molecule, an oligopeptide that is degraded in the cells:
##STR00001##
wherein k.sub.1 and k.sub.2 are each independently 1-12, j.sub.1 and j.sub.2 are each independently 45-950, R is a hydrogen atom, a substituted or unsubstituted alkyl group having 1-12 carbon atoms, a substituted aryl group, an aralkyl group or a heteroalkyl group, Z is an oligopeptide that is degraded by enzyme in the cells, X is a functional group capable of reacting with a bio-related substance, and L.sub.1 and L.sub.2 are each independently a single bond or a divalent spacer.