PATENTSCOPE: EN_ALL:nmr AND PA:eisai

SYNTHESIS OF HALICHONDRINS (Fri, 11 Jan 2019)
The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondnn A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A)
>> Read More

FLUORINE-LABELLED HALICHONDRIN DERIVATIVES AND RELATED METHODS OF SYNTHESIS (Fri, 30 Nov 2018)
The invention relates to halichondrin derivatives containing fluorine, e.g., fluorine-18, as well as methods of synthesizing the same.
>> Read More

MACROCYCLIC COMPOUND AND USES THEREOF (Fri, 12 Oct 2018)
The present invention provides novel Compound (1) having tumor vascular remodeling effect and/or anti-CAF (Cancer Associated Fibroblasts) activity, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable and medical uses thereof. Compound (1)
>> Read More

SPLICEOSOME MUTATIONS AND USES THEREOF (Fri, 21 Sep 2018)
Spliceosome mutations are described herein, including mutations in the PHF5A and SF3B1 subunits. This application also describes detecting the presence and/or absence of mutations in the spliceosome, as well as methods of diagnosing responsiveness to splice modulator treatment, methods of treating neoplastic disorders, and methods of monitoring or altering the treatment based on mutation status.
>> Read More

COMPOUNDS (Fri, 27 Jul 2018)
The present invention relates to compounds of Formulae (I) and (II) as defined herein, and salts and solvates thereof. The present invention also relates to pharmaceutical compositions comprising compounds of Formulae (I) and (II), and to the use of compounds of Formulae (I) and (II) in the treatment or prevention of filarial worm infection, as well as other diseases or conditions in which filarial worm infection is implicated.
>> Read More

SALTS OF INDAZOLE DERIVATIVE AND CRYSTALS THEREOF (Fri, 01 Jun 2018)
The present invention provides salts of (E)-N,N-dimethyl-4-((2-((5-((Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)pyridin-2-yl)oxy)ethyl)amino)but-2-enamide represented by the formula I and acids, and crystals thereof, possessing a potential to be used as drug substance in pharmaceuticals.
>> Read More

TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE FOR THE TREATMENT OF BREAST CANCER (Fri, 01 Jun 2018)
Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
>> Read More

TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE (Fri, 01 Jun 2018)
Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
>> Read More

PRINS REACTION AND INTERMEDIATES USEFUL IN THE SYNTHESIS OF HALICHONDRIN MACROLIDES AND ANALOGS THEREOF (Fri, 05 Jan 2018)
The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.
>> Read More

LYSINE CONJUGATED IMMUNOGLOBULINS (Fri, 15 Dec 2017)
Provided herein are conjugated immunoglobulins and methods for generating conjugated immunoglobulins using a microbial transglutaminase.
>> Read More

ERIBULIN-BASED ANTIBODY-DRUG CONJUGATES AND METHODS OF USE (Sat, 09 Sep 2017)
Linker toxins and antibody-drug conjugates that bind to human oncology antigen targets such as folate receptor alpha and/or provide anti-tubulin drug activity are disclosed. The linker toxins and antibody-drug conjugates comprise an eribulin drug moiety and can be internalized into target antigen-expressing cells. The disclosure further relates to methods and compositions for use in the treatment of cancer by administering the antibody-drug conjugates provided herein.
>> Read More

PEPTIDE DRUG CONJUGATES (Fri, 11 Aug 2017)
Embodiments provide protein-drug conjugates for treatment of cancer. Protein-drug conjugates may include protein-drug conjugates of Formula I: Ctx-L-Cp (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: Ctx is chlorotoxin or a chlorotoxin analog; Cp is a cryptophycin amide, and L is a linker wherein the linker is bound to Ctx at an X2 moiety of the linker and at one of a lysine residue and the N-terminus of the chlorotoxin or chlorotoxin analog.
>> Read More

A SOLID STATE FORM OF PLADIENOLIDE PYRIDINE COMPOUNDS AND METHODS OF USE (Sat, 27 May 2017)
The present disclosure provides a novel solid state form of pladienolide pyridine compounds, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.
>> Read More

EP4 ANTAGONISTS (Fri, 21 Apr 2017)
We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.
>> Read More

CHIRAL REAGENTS FOR PREPARATION OF HOMOGENEOUS OLIGOMERS (Fri, 10 Feb 2017)
We provide diastereomerically pure or substantially diastereomerically pure activated phosphoramidochloridate morpholino nucleosides, methods of their preparation, and methods of their use in stereospecific coupling for stereospecific synthesis of diastereomerically pure phosphorodiamidate morpholino oligomers (PMOs).
>> Read More

TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE (Fri, 09 Dec 2016)
Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
>> Read More

TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE (Fri, 09 Dec 2016)
Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
>> Read More

TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE (Fri, 09 Dec 2016)
Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
>> Read More

MACROCYCLIZATION REACTIONS AND INTERMEDIATES AND OTHER FRAGMENTS USEFUL IN THE SYNTHESIS OF HALICHONDRIN MACROLIDES (Fri, 11 Nov 2016)
The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
>> Read More

CRYSTALLINE FGFR4 INHIBITOR COMPOUND AND USES THEREOF (Fri, 21 Oct 2016)
A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also provided.
>> Read More