Patent classifications
C07D209/60
Method for the synthesis of monoprotected bifunctional prodrugs and antibody drug conjugates based thereon as well as a method for preparing antibody drug conjugates
The present invention relates to a method for the synthesis of compounds useful in the preparation of antibody drug conjugates (ADC), namely, monoprotected dimeric bifunctional prodrugs based on duocarmycin analogs. In a further aspect, compounds obtained by the method according to the present invention are provided. The monoprotected bifunctional prodrug is used for preparing antibody drug conjugates composed of an antibody moiety and the monoprotected bifunctional prodrug. The antibody compound conjugates thus obtained are provided. Further, a method of preparing an antibody drug conjugate composed of two identical or two different antibody moieties is provided as well as the antibody compound conjugate containing two different antibody moieties accordingly. These conjugates can be used in pharmaceutical compositions, in particular, for use in treatment of tumors, e.g. for use in ADC therapy.
Tosylacetate based compounds and derivatives thereof as PHGDH inhibitors
The present invention encompasses compounds of formula (I), wherein the groups R.sup.1 to R, A.sup.1 to A.sup.4 and n have the meanings given in the claims and specification, their use as inhibitors of PHGDH, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases. ##STR00001##
Tosylacetate based compounds and derivatives thereof as PHGDH inhibitors
The present invention encompasses compounds of formula (I), wherein the groups R.sup.1 to R, A.sup.1 to A.sup.4 and n have the meanings given in the claims and specification, their use as inhibitors of PHGDH, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases. ##STR00001##
TOSYLACETATE BASED COMPOUNDS AND DERIVATIVES THEREOF AS PHGDH INHIBITORS
The present invention encompasses compounds of formula (I), wherein the groups R.sup.1 to R, A.sup.1 to A.sup.4 and n have the meanings given in the claims and specification, their use as inhibitors of PHGDH, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
##STR00001##
TOSYLACETATE BASED COMPOUNDS AND DERIVATIVES THEREOF AS PHGDH INHIBITORS
The present invention encompasses compounds of formula (I), wherein the groups R.sup.1 to R, A.sup.1 to A.sup.4 and n have the meanings given in the claims and specification, their use as inhibitors of PHGDH, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
##STR00001##
Naphthalocyanine compound, method for producing same, and use thereof
Provided are a novel naphthalocyanine compound, which has strong absorption in a near-infrared range, extremely weak absorption in a visible range, and high resistance such as light resistance and heat resistance, and exhibits excellent solubility in an organic solvent or a resin, a heat ray shielding material, and uses of the naphthalocyanine compound such as a heat ray shielding material and the like. The naphthalocyanine compound is represented by General Formula (1). ##STR00001## wherein, in Formula (1), M represents two hydrogen atoms, a divalent metal, or a derivative of a trivalent or tetravalent metal, R.sub.1 to R.sub.3 each independently represent a hydrogen atom, a halogen atom, or a linear, branched, or cyclic alkyl group, A represents Formula (2), and B represents Formula (3), ##STR00002## wherein, in Formula (2), R.sub.4 to R.sub.8 each independently represent a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an alkylthio group, an aryloxy group, or an arylthio group, and ##STR00003## wherein, in Formula (3), X represents an oxygen atom, a sulfur atom, and or an imino group, R.sub.9 to R.sub.13 each independently represent a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an ester group, an amide group, or a sulfonamide group.
CARBONIC ANHYDRASE TARGETING AGENTS AND METHODS OF USING SAME
The invention provides agents that target carbonic anhydrase, which can be used as imaging agents or therapeutic agents. The agents can be used to image tumor hypoxia as well as other physiological processes in a subject.
AGONISTS OF ROR GAMMAt
The present invention is directed to compounds of the formula wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
AGONISTS OF ROR GAMMAt
The present invention is directed to compounds of the formula wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
Composition, film, lens, solid state imaging element, and compounds
An object of the present invention is to provide a composition capable of forming a film having a high refractive index and excellent exterior characteristics. Another object of the present invention is to provide a film, a lens, and a solid-state imaging element in which the composition is used. Still another object of the present invention is to provide novel compounds. The composition according to an embodiment of the present invention contains a compound represented by General Formula (I), a solvent, and a resin, in which a solubility of the compound represented by General Formula (I) in the solvent is less than 0.5% by mass at 25° C., and a maximum absorption wavelength of the compound represented by General Formula (I) at a wavelength range of 300 to 800 nm is equal to or shorter than 450 nm.
AB-C).sub.n (I)