1618-36-6Relevant academic research and scientific papers
Tetrahydropyrrolopyrazoles derivatives Preparation method and application thereof in medicine
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Paragraph 0342-0348, (2021/09/29)
The invention relates to tetrahydropyrrolopyrazol derivatives, a preparation method and an application thereof in medicine. , The present disclosure relates to a tetrahydropyrrolopyrazol derivative represented by the general formula (I), a preparation method thereof, and a use of the derivative-containing pharmaceutical composition and as a therapeutic agent, in particular as AKT1 T1 T1 T1 AKT pan T1 inhibitors and use thereof in the preparation of a medicament for the treatment and/or prevention of tumors.
4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-3,6-DIHYDROPYRIDINE-1-(2H)-CARBOXAMIDE DERIVATIVES AS LIMK AND/OR ROCK KINASES INHIBITORS FOR USE IN THE TREATMENT OF CANCER
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, (2021/12/07)
The present invention concerns a compound of formula (I), in particular as LIMK and/or ROCK kinases inhibitors. The present invention also concerns these new inhibitors for use for the treatment of a condition selected in the group consisting of: cancers, virion infections, ocular hypertension and glaucoma formation, Neurofibromatosis type 1 and 2, psoriatic lesions, inflammatory diseases and hyperalgesia, central sensitization and chronic pain, reproduction erectile dysfunction, and neuronal diseases. The present description discloses the syntheses and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 32 to 127; examples 1 to 96; families 1 to 8; compounds; biological studies; tables). An exemplary compound is e.g. 4-(5-m ethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-phenyl-3,6-dihydropyridine-1-(2H)-carboxamide (example 1; compound 5).
ASK1 INHIBITING PYRROLOPYRIMIDINE AND PYRROLOPYRIDINE DERIVATIVES
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Paragraph 0154, (2019/02/02)
The present invention relates to pyrrolopyrimidine compounds according to Formula (I) and their use in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases. In a particular aspect, the present compounds are ASK inhibitors, particularly ASK1 inhibitors. The present invention also provides methods for the production of a compound of the invention, pharmaceutical compositions comprising a compound of the invention, the use of the compounds in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases. (Formula (I))
4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
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Page/Page column 39; 40, (2015/12/08)
Provided is 4'-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.
Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists
Hu, Yun-Jin,St.-Onge, Miguel,Laliberté, Sébastien,Vallée, Frédéric,Jin, Shujuan,Bedard, Leanne,Labrecque, Jean,Albert, Jeffrey S.
supporting information, p. 3199 - 3203 (2015/02/19)
A series of TRPA1 antagonists is described having a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine or a 1-aryloxyisoquinoline scaffold. These compounds have high ligand efficiency and favorable physical properties and may thus serve as scaffolds for further optimization.
ASK1 INHIBITING PYRROLOPYRIMIDINE DERIVATIVES
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Page/Page column 24, (2012/06/30)
This invention relates to pyrrolopyrimidine derivatives of formula (I): where R1, X, p, R4, R2and R3are as defined herein, and their use as pharmaceuticals.
SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY
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Page/Page column 115-116, (2008/12/06)
The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I); or salts, solvates, tautomers or N-oxides thereof, wherein E is a five membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from O, N and S provided that no more than 1 heteroatom may be other than N; q and r are each is 0 or 1; provided that q+r is 1 or 2; T is N or a group CR5; J1-J2 is N=C(R6), (R7)C=N, (R8)N- C(O), (R8)2C-C(O), N=N or (R7)C=C(R6); Q3 is a bond or a saturated C1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR2R3, CN or OH; m and n are each 0 or 1, provided that m+n is 1 or 2, and provided also that m or n are each 0 when the adjacent ring member of ring E is S or O; R1a and R1b are the same or different and each is hydrogen or a substituent R10; or R1a and R1b together with the carbon atoms or heteroatoms to which they are attached form a 5 or 6-membered aryl or heteroaryl ring, wherein the aryl or heteroaryl rings are optionally substituted by one or more substituents R10; and R2, R3, R4, R5, R7, R6, R8, and R10 are as defined in the claims.
SUBSTITUTED PIPERIDINES CONTAINING A HETEROARYLAMIDE OR HETEROARYLPHENYL MOIETY
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Page/Page column 107-108, (2008/12/06)
The invention provides compounds of the formula (I) having PKA and PKB kinase inhibiting compounds of the formula (I): GP 1 J T 2 J N 4 R N H (I) or salts, solvates, tautomers or N-oxides thereof, wherein (1) GP is a group GP1: HET 2a a Q G (HNCO)f 7 (R )x N * (GP1) (2) GP is a group GP2: 10 (R )r O 2a a QG (CH2)w N V H N * (GP2) wherein HET is a monocyclic or bicyclic heterocyclic group containing up to 4 heteroatom ring members; the ring V is a monocyclic or bicyclic heteroaryl group of 5 to 10 ring members; and J1, J2, R4, R7, R10, Q2a, Ga, x, w and f are as defined in the claims
Heterocyclic ring-fused pyrimidine derivatives
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, (2016/01/12)
The present invention relates to heterocyclic ring-fused pyrimidine derivatives of formula (I) or stereoisomers, pharmaceutically acceptable salts or prodrugs thereof, wherein Z and Y are as defined in the specification. Compounds of formula (I) are useful in the treatment of hyperproliferative diseases, such as cancers and acnes, in mammals:
