Patent classifications
A61P13/08
ANTI-CXCR4 ANTIBODIES AND ANTIBODY-DRUG CONJUGATES
The present invention provides antibodies and related molecules that bind to chemokine receptor 4 (CXCR4). The invention further provides antibody-drug conjugates comprising such antibodies, antibody encoding nucleic acids, and methods of obtaining such antibodies. The invention further relates to therapeutic methods for use of these antibodies and anti-CXCR4 antibody-drug conjugates for the treatment of a disorder associated with CXCR4 function or expression (e.g., cancer), such as colon, RCC, esophageal, gastric, head and neck, lung, ovarian, pancreatic cancer or hematological cancers.
IMIDAZOPYRIDAZINE DERIVATIVES AS PI3KB INHIBITORS
- Laurence Anne Mevellec ,
- Lieven Meerpoel ,
- Sophie Coupa ,
- Virginie Sophie Poncelet ,
- Isabelle Noelle Constance Pilatte ,
- Elisabeth Therese Jeanne Pasquier ,
- Didier Jean-Claude Berthelot ,
- Olivier Alexis Georges Querolle ,
- Christophe Meyer ,
- Patrick Rene Angibaud ,
- Christophe Gabriel Marcel Demestre ,
- Guillaume Jean Maurice Mercey
The present invention relates to substituted imidazopyridazine derivatives of Formula (I)
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wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ inhibitors. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
TARGETED TGFß INHIBITION
This invention relates generally to bifunctional molecules including (a) a TGFβRII or fragment thereof capable of binding TGFβ and (b) an antibody, or antigen binding fragment thereof, that binds to an immune checkpoint protein, such as Programmed Death Ligand 1 (PD-L1), uses of such molecules (e.g., for treating cancer), and methods of making such molecules.
PROCESSES FOR THE PREPARATION OF A DIARYLTHIOHYDANTOIN COMPOUND
Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.
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SYNTHESIS OF HETEROCYCLIC COMPOUNDS
Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I):
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or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P.sup.1 and P.sup.2 are as defined in this disclosure.
Novel Forms of [R-(R*,R*)]-2-(4-Fluorophenyl)-Beta, Gamma-Dihydroxy-5-(1-Methylethyl)-3-Phenyl-4-[(Phenylamino)carbonyl]-1H-Pyrrole-1-Heptanoic Acid Calcium Salt (2:1)
Novel forms of [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptatonic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease.
NOVEL CRYSTALLINE FORM OF ATORVASTATIN HEMI-CALCIUM SALT, HYDRATE THEREOF, AND METHOD OF PRODUCING THE SAME
The present invention provides a novel crystalline form of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-heptanoic acid hemi-calcium salt (atorvastatin hemi-calcium salt) of the following formula 1, which is known to be useful as a drug, a hydrate thereof and a preparation method thereof:
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COMBINATION THERAPY WITH AN ANTITUMOR ALKALOID
The present invention relates to the combination of PM01183 with several anticancer drugs, in particular other anticancer drugs selected from antitumor platinum coordination complexes, antimetabolites, mitotic inhibitors, anticancer antibiotics, topoisomerase I and/or II inhibitors, proteasome inhibitors, histone deacetylase inhibitors, nitrogen mustard alkylating agents, nitrosourea alkylating agents, nonclassical alkylating agents, estrogen antagonists, androgen antagonists, mTOR inhibitors, tyrosine kinase inhibitors, and other agents selected from aplidine, ET-743, PM02734 and PM00104, and the use of these combinations in the treatment of cancer.
LIGNEOUS PLANT-DERIVED HETEROPOLYSACCHARIDES FOR USE IN TREATMENT OF UROLOGIC SYMPTOMS AND DISEASES
The present invention relates to preventing and/or treating urologic diseases and symptoms in humans or domestic animals. The present invention relates also to preventing and/or treating pain in the pelvic area. The invention relates to use of a heteropolysaccharide composition isolated from ligneous plants and comprising hemicelluloses, mainly glucomannans, but also xylans and pectic polysaccharides, as well as fractions, subgroups or mixtures of these, as pharmaceutical preparations, food additives and food products.
METHODS TO INDUCE TARGETED PROTEIN DEGRADATION THROUGH BIFUNCTIONAL MOLECULES
The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.