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1.WO/2020/232807NAPHTHOQUINONE FUSED TRIAZOLE DERIVATIVE, PREPARATION METHOD AND APPLICATION THEREOF
WO 26.11.2020
Int.Class C07D 249/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
249Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
16condensed with carbocyclic rings or ring systems
22Naphthotriazoles
Appl.No PCT/CN2019/095288 Applicant GUANGZHOU UNIVERSITY OF CHINESE MEDICINE (GUANGZHOU ACADEMY OF CHINESE MEDICINE) Inventor LIU, Jiawei
Provided are a naphthoquinone fused triazole derivative, preparation method and application thereof. The naphthoquinone fused triazole derivative has a structure represented by the following formula (I), wherein X is C or N; R 1, R 2, R 3, R 4, R 5, R 6, R 7, R 8 are each independently any one of hydrogen, halogen, hydroxyl, cyano, sulfydryl, amino, nitro, nitroso, alkyl, alkoxy, ester group, carboxyl and sulfonyl. Also provided is the application of the naphthoquinone fused triazole derivative or a pharmaceutically acceptable salt or hydrate thereof in preparation of a medicament for treating a disease with abnormal signal transduction of STAT3.
2.WO/2020/233677PROCESS FOR PREPARING AMIDE-SUBSTITUTED IMIDAZO COMPOUNDS
WO 26.11.2020
Int.Class C07D 235/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
235Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02condensed with carbocyclic rings or ring systems
Appl.No PCT/CN2020/091603 Applicant BEIGENE (BEIJING) CO., LTD. Inventor WANG, Hexiang
Disclosed herein is a process for preparing amide-substituted imidazo compounds. In particular, disclosed herein is the process for preparing certain amide-substituted imidazo compounds that are useful for inhibiting indoleamine 2, 3-dioxygenase and for treating diseases or disorders mediated thereby.
3.WO/2020/235587TANDOSPIRONE DERIVATIVE
WO 26.11.2020
Int.Class C07D 209/76
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
56Ring systems containing three or more rings
58- or -condensed
724,7-Endo-alkylene-iso-indoles
76with oxygen atoms in positions 1 and 3
Appl.No PCT/JP2020/019911 Applicant NATIONAL UNIVERSITY CORPORATION UNIVERSITY OF TOYAMA Inventor KONDO Takashi
A compound represented by formula (1) or a pharmaceutically acceptable salt thereof can be used as an active ingredient of a drug for central nervous system diseases or as a candidate compound for a precursor of said active ingredient. In formula (1), R1, R2, and R3 each independently represent a substance selected from the group consisting of a hydrogen atom, a hydroxy group, and an alkoxy group having 1-6 carbon atoms, and at least one of R1, R2, and R3 is a hydroxy group.
4.20200369682FUSED THIOPHENE DERIVATIVES AND THEIR USES
US 26.11.2020
Int.Class C07D 495/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Appl.No 16967751 Applicant ENYO PHARMA Inventor ERIC MELDRUM

The present invention relates to a new class of fused thiophene derivatives and their uses for treating diseases such as infection, cancer, metabolic diseases, cardiovascular diseases, iron storage disorders and inflammatory disorders.

5.202003696722,4,6,7-TETRAHYDRO-PYRAZOLO[4,3-D]PYRIMIDIN-5-ONE DERIVATIVES AND RELATED COMPOUNDS AS C5A RECEPTOR MODULATORS FOR TREATING VASCULITIS AND INFLAMMATORY DISEASES
US 26.11.2020
Int.Class C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Appl.No 16961600 Applicant Idorsia Pharmaceuticals Ltd. Inventor Sylvie FROIDEVAUX

The present invention relates to derivatives of formula (I)

embedded image

wherein Ring A, X, Y, Z, RA, R1, R2, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as C5a receptor modulators.

6.20200368362IMPROVED PROCESS FOR THE SYNTHESIS OF LINKER-DRUG VC-SECO-DUBA
US 26.11.2020
Int.Class A61K 47/68
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET 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
51the non-active ingredient being a modifying agent
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Appl.No 16766150 Applicant BYONDIS B.V. Inventor Vladimir JANOUSEK

The present invention relates to an improved process for the synthesis of linker-drug vc-seco-DUBA and its intermediates, as well as to the use of said improved process in a process for preparing an antibody-drug conjugate comprising the vc-seco-DUBA linker-drug.

7.20200369622METHOD FOR PREPARING IMIDAZOLINE-2 KETONE COMPOUND
US 26.11.2020
Int.Class C07D 235/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
235Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02condensed with carbocyclic rings or ring systems
Appl.No 16993362 Applicant SOOCHOW UNIVERSITY Inventor Shilei ZHANG

A method of preparing an imidazolin-2-tones compound includes: dissolving a cycloheptatrienone and an aromatic isocyanate in a solvent; and reacting the cycloheptatrienone and the aromatic isocyanate in the solvent without an oxidant and a catalyst to obtain the imidazolin-2-tone compound.

8.20200369612Method for Safely Preparing Pimavanserin and Tartrate Thereof by Using Triphosgene
US 26.11.2020
Int.Class C07D 211/98
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
92with a hetero atom directly attached to the ring nitrogen atom
98Nitrogen atom
Appl.No 16764315 Applicant Livzon New North River Pharmaceutical Co., Ltd. Inventor Biao Wang

The present disclosure discloses a method for safely preparing pimavanserin and tartrate thereof by using triphosgene. The synthesis route includes:

embedded image

Raw materials used in the method of the present disclosure are safe and inexpensive, thereby effectively reducing the production costs. The method of the present disclosure has mild reaction conditions, and avoids using phosgene, which is highly toxic and difficult to handle is avoided. Thus, the method is readily implemented industrially.

9.20200369632FXR (NR1H4) MODULATING COMPOUNDS
US 26.11.2020
Int.Class C07D 261/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
261Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
02not condensed with other rings
06having two or more double bonds between ring members or between ring members and non-ring members
10with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
Appl.No 16989335 Applicant Gilead Sciences, Inc. Inventor Peter A. Blomgren

The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

10.20200369662SOLID STATE FORMS
US 26.11.2020
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 16878824 Applicant AMGEN INC. Inventor Mary CHAVES

The present disclosure provides crystalline and amorphous forms of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin-2(1H)-one, including several anhydrous, hydrate and solvate forms, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.