Lausanne, Switzerland
Lausanne, Switzerland

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A method of treating triple-negative breast cancer in a mammal comprising the step of: administering to a patient a pharmaceutical acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1) wherein R^(1 )is alkyl having a carbon number of 1-4, R^(2 )is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R^(3 )is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; NR^(5)(CH_(2))_(m)R^(6 )wherein R^(5 )is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R^(6 )is phenyl or pyridyl optionally substituted by a halogen atom; or NR^(7)CO(CH_(2))_(n)R^(8 )wherein R^(7 )is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R^(8 )is phenyl or pyridyl optionally substituted by a halogen atom, and R^(4 )is (CH_(2))_(n)CONHR^(9 )wherein a is an integer of 1-4, and R^(9 )is alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or (CH_(2))_(b)COOR^(10 )wherein b is an integer of 1-4, and R^(10 )is alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof, in combination with one or more chemotherapy drugs selected from the group consisting of m-TOR inhibitors and mitotic inhibitors.


A method of treating acute myeloid leukemia, acute lymphoblastic leukemia, high risk myelodysplastic syndrome, and/or HR-MDS/AML in a mammal by administering a solid dispersion comprising an amorphous thienotriazolodiazepine compound of the Formula (1) wherein R1 is alkyl having a carbon number of 1-4, R2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; NR5-(CH2)m R6 wherein R5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R6 is phenyl or pyridyl optionally substituted by a halogen atom.


A method of treating non-small cell lung cancer in a mammal by administering to a patient a pharmaceutically acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1) wherein R^(1 )is alkyl having a carbon number of 1-4, R^(2 )is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R^(3 )is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; NR^(5)(CH_(2))_(m)R^(6 )wherein R^(5 )is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R^(6 )is phenyl or pyridyl optionally substituted by a halogen atom; or NR^(7)CO(CH_(2))_(n)R^(8 )wherein R^(7 )is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R^(8 )is phenyl or pyridyl optionally substituted by a halogen atom, and R^(4 )is (CH_(2))_(a)CONHR^(9 )wherein a is an integer of 1-4, and R^(9 )is alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or (CH_(2))_(b)COOR_(10 )wherein b is an integer of 1-4, and R^(10 )is alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof.


A method of treating B-cell malignant cancers or T-cell malignant cancers in a mammal by administering to a patient a pharmaceutically acceptable amount of a composition comprising (S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo-[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide. The B-cell malignant cancers include diffuse large B-cell lymphoma and splenic marginal zone lymphoma. The T-cell malignant cancers include anaplastic large T-cell lymphoma.


A solid dispersion comprising an amorphous thienotriazolodiazepine compound of the Formula (1) wherein X is a halogen, R^(1 )is C_(1)-C_(4 )alkyl, R^(2 )is C_(1)-C_(4 )alkyl, a is an integer of 1-4, R^(3 )is C_(1)-C_(4 )alkyl, C_(1)-C_(4 )hydroxyalkyl, C_(1)-C_(4 )alkoxy, phenyl optionally having substituent(s), or heteroaryl optionally having substituent(s), a pharmaceutically acceptable salt thereof or a hydrate thereof; and a pharmaceutically acceptable polymer. In one embodiment, the pharmaceutically acceptable polymer is HPMCAS. The solid dispersion may be made by spray drying.


Disclosed herein are compositions comprising a galectin-1-targeting compound in a therapeutically effective composition for treating cancer. In an aspect, a galectin-1-targeting compound is OTX-008. Also disclosed herein are methods of making and using such compositions.


A method of treating lymphoblastic leukemia, acute myeloid leukemia, BCR-ABL positive acute lymphoblastic leukemia or CD34 positive acute myeloid leukemia comprising the step of administering to a patient a pharmaceutically acceptable amount of a composition comprising a thienotriazolodiazepine compound according to Formula (1) as a solid dispersion wherein X is a halogen, R^(1 )is C_(1)-C_(4 )alkyl, R^(2 )is C_(1)-C_(4 )alkyl, a is an integer of 1-4, R^(3 )is C_(1)-C_(4 )alkyl, C_(1)-C_(4 )hydroxyalkyl, C_(1)-C_(4 )alkoxy, phenyl optionally having substituent(s), or heteroaryl optionally having substituent(s), a pharmaceutically acceptable salt thereof or a hydrate thereof; and a pharmaceutically acceptable polymer. In one embodiment, the pharmaceutically acceptable polymer is HPMCAS.


A method of treating diffuse large B-cell lymphoma comprising administering to a patient a pharmaceutically acceptable amount of a composition comprising a thienotriazolodiazepine compound, said thienotriazolodiazepine compound being represented by Formula (I), wherein R_(1 )is alkyl having a carbon number of 1-4, R_(2 )is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R_(3 )is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; NR_(5)(CH_(2))_(m)R_(6 )wherein R_(5 )is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R_(6 )is phenyl or pyridyl optionally substituted by a halogen atom; or NR_(7)CO(CH_(2))_(n)R_(8 )wherein R_(7 )is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R_(8 )is phenyl or pyridyl optionally substituted by a halogen atom, and R_(4 )is (CH_(2))_(a)CONHR_(9 )wherein a is an integer of 1-4, and R_(9 )is alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or (CH_(2))_(b)COOR_(10 )wherein b is an integer of 1-4, and R_(10 )is alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof, wherein the patient has activated B-cell diffuse large B-cell lymphoma.


News Article | April 2, 2015
Site: www.fiercebiotech.com

Index Ventures now has 650 million more euros to invest. The venture group, which has two big teams active on both sides of the Atlantic in life sciences as well as tech, filed documents with the SEC noting that its new Index Ventures Growth III--domiciled in Jersey--is fully sold. There was no immediate response to a query from FierceBiotech about its plans for the new money. But Index has been a key go-to VC in the European biotech scene in recent years. And like a lot of VCs, Index is finding that an acquisitive crowd of Big Pharma players has provided some nice exits in a booming market, setting the stage for a whole new generation of funds like this. In just the last few months Index has seen its first exit (for X01) out of its special, asset-centric biotech portfolio set up with J&J and GlaxoSmithKline, the sale of GlycoVaxyn, a spinout from ETH Zurich that was snapped up by GlaxoSmithKline for its work on bioconjugate vaccines, and Merck's buyout of OncoEthix. Even with a weak euro Index still has $706 million to invest, making it one of the bigger new funds to debut in a go-go investment scene. Flagship Ventures rolled out its new early-stage fund with $537 million just days ago, as it was partnering up with Arch Venture to operate a special $150 million venture effort aimed at encouraging the growth of a biotech hub in New York City. Two months ago Lux Capital, which includes biotech in its lineup, raised $350 million. New Enterprise Associates is working on its latest $2.5 billion-plus behemoth, while a whole string of new funds has appeared over the past 18 months promising to bankroll a new wave of biotechs for several years to come. Related Articles: Levicept emerges from Pfizer's R&D ashes with $20M and a new pain drug Egalet scores up to $20M for next-gen pain drug as FDA aims to block abuse Swiss biotech OncoEthix snags $19M round to back leukemia drug study

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