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Analysis

1 / 10
1.WO/2020/2534152-METHYL-1,8-NAPHTHYRIDINE COMPOUND, AND PREPARATION METHOD AND APPLICATION THEREFOR
WO - 24.12.2020
Int.Class C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
 Appl.No PCT/CN2020/089428 Applicant WUYI UNIVERSITY Inventor CHEN, Xiuwen
The present invention relates to the technical field of synthesis, and particularly relates to a 2-methyl-1,8-naphthyridine compound, and a preparation method and an application therefor. The 2-methyl-1,8-naphthyridine compound of the present invention has the structure shown in formula I, wherein R1 is selected from the group composed of phenyl, substituted phenyl, thiazolyl, pyrazinyl, furyl, benzothienyl, and 1,3-benzodioxy, and R2 is hydrogen or alkyl; or R1 and R2 are connected to form a ring structure; the substituted phenyl is nitrophenyl, halophenyl, methoxyphenyl, or trifluoromethylphenyl; and the alkyl is C1-6 alkyl. The 2-methyl-1,8-naphthyridine compound of the present invention has a novel structure, and has high biological activity and certain potential for application in anti-tumour drugs; there is no need to add metal catalyst during preparation, and the conditions are mild and environmentally friendly, efficiency is high, and operation is simple and safe.
2.WO/2020/256636A NOVEL CRYSTALLINE FORM OF OLAPARIB AND A PROCESS FOR PREPARING THE SAME
WO - 24.12.2020
Int.Class C07D 237/32
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
237Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
26condensed with carbocyclic rings or ring systems
30Phthalazines
32with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
 Appl.No PCT/SG2020/050332 Applicant SCINOPHARM TAIWAN, LTD. Inventor LIN, Wen-Wei
In certain aspects, the invention provides a novel crystalline form of olaparib (4-[(3-[(4-cyclopropylcarbonyl)piperazin-4-yl]carbonyl)-4-fluorophenyl]methyl(2H)phthalazin-1-one). In related aspects, the invention provides a processe for preparing the novel crystalline form of olaparib. The process includes forming a solution comprising crude olaparib and an organic solvent; adding the solution to an anti-solvent to form a slurry comprising a precipitate; isolating the precipitate; and drying the precipitate to obtain a crystalline form III of olaparib.
3.WO/2020/254299COMBINATION OF A MCL-1 INHIBITOR AND A STANDARD OF CARE TREATMENT FOR BREAST CANCER, USES AND PHARMACEUTICAL COMPOSITIONS THEREOF
WO - 24.12.2020
Int.Class A61K 31/357
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
357having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
 Appl.No PCT/EP2020/066575 Applicant LES LABORATOIRES SERVIER Inventor BANQUET, Sébastien
A combination comprising a Mcl-1 inhibitor and a second anticancer agent, wherein the second anticancer agent is selected from eribulin and fulvestrant, and compositions and uses thereof.
4.WO/2020/254617ANTI-CTLA4 COMPOUNDS WITH LOCALIZED PK PROPERTIES
WO - 24.12.2020
Int.Class A61K 47/69
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
69the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
 Appl.No PCT/EP2020/067165 Applicant ASCENDIS PHARMA ONCOLOGY DIVISION A/S Inventor ROSEN, David B
The present invention relates to a water-insoluble controlled-release anti-CTLA4 compound for use in the treatment of a cell-proliferation disorder, wherein said water-insoluble controlled-release anti-CTLA4 compound releases one or more anti-CTLA4 drugs, and wherein intra-tissue administration of a therapeutic dose results in a maximum systemic concentration of anti-CTLA4 drug within 48 hours after said intra-tissue administration that is at least 2-fold lower compared to the maximum systemic concentration of the corresponding anti-CTLA4 drug within 48 hours after systemic administration of a dose of said anti-CTLA4 drug that provides essentially the same anti-tumor activity; and related aspects.
5.WO/2020/254607ANTI-CTLA4 COMPOUNDS WITH LOCALIZED PD PROPERTIES
WO - 24.12.2020
Int.Class A61K 47/69
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
69the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
 Appl.No PCT/EP2020/067153 Applicant ASCENDIS PHARMA ONCOLOGY DIVISION A/S Inventor ROSEN, David B
The present invention relates to a water-insoluble controlled-release anti-CTLA4 compound for use in the treatment of a cell-proliferation disorder, wherein the compound is administered by intra-tissue administration and wherein such intra-tissue administration induces local anti-CTLA4-induced T cell activation; and related aspects.
6.WO/2020/253722ANTI-CD40 ANTIBODIES AND USES THEREOF
WO - 24.12.2020
Int.Class C07K 16/28
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
16Immunoglobulins, e.g. monoclonal or polyclonal antibodies
18against material from animals or humans
28against receptors, cell surface antigens or cell surface determinants
 Appl.No PCT/CN2020/096574 Applicant EUCURE (BEIJING) BIOPHARMA CO., LTD Inventor YANG, Yi
Provided are anti-CD40 (TNF Receptor Superfamily Member 5) antibodies, antigen -binding fragments, and the uses thereof.
7.WO/2020/257253CHROMENOPYRIDINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS
WO - 24.12.2020
Int.Class C07D 493/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
493Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
 Appl.No PCT/US2020/038091 Applicant HIBERCELL, INC. Inventor KESICKI, Edward A.
The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula (I) where A1, A2, G, R1, R2, R3, R4, and W are described herein.
8.WO/2020/257165MACROCYCLES FOR USE IN TREATING DISEASE
WO - 24.12.2020
Int.Class A61K 31/5383
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5383ortho- or peri-condensed with heterocyclic ring systems
 Appl.No PCT/US2020/037886 Applicant TURNING POINT THERAPEUTICS, INC. Inventor CUI, Jingrong Jean
The present disclosure relates to certain chiral diaryl macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat cancer, pain, neurological diseases, autoimmune diseases, and inflammation.
9.WO/2020/257184METHODS FOR MODULATING SPLICING
WO - 24.12.2020
Int.Class A61K 31/501
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
50Pyridazines; Hydrogenated pyridazines
501not condensed and containing further heterocyclic rings
 Appl.No PCT/US2020/037910 Applicant SKYHAWK THERAPEUTICS, INC. Inventor LUZZIO, Michael
Described herein are methods of use of small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of treating diseases and conditions associated with gene expression or activity of proteins encoded by genes.
10.WO/2020/254547NEW EGFR INHIBITORS
WO - 24.12.2020
Int.Class A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
 Appl.No PCT/EP2020/067057 Applicant F. HOFFMANN-LA ROCHE AG Inventor DOLENTE, Cosimo
The invention provides novel a compound having the general formula (I), (I) as described herein, compositions including the compound and methods of using the compound.
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