- Synthesis and antifungal activity of imidazo[1,2-b]pyridazine derivatives against phytopathogenic fungi
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A series of 3,6-disubstituted imidazo[1,2-b]pyridazine derivatives have been synthesized and characterized with spectroscopic analyses. The antifungal activities of these compounds against nine phytopathogenic fungi were evaluated by the mycelium growth rate method. The in vitro antifungal bioassays indicated that most of compounds displayed excellent and broad-spectrum antifungal activities. Especially, compounds 4a, 4c, 4d, 4l and 4r exhibited 1.9–25.5 fold more potent than the commercially available fungicide hymexazol against Corn Curvalaria Leaf Spot (CL), Alternaria alternate (AA), Pyricularia oryzae (PO) and Alternaria brassicae (AB) strains. Structure-activity relationship analysis showed that the enhanced antifungal activity is significantly affected by the substituents on the benzene ring and pyridazine ring.
- Fan, Judi,Fan, Lingling,Li, Yi,Li, Yong,Liu, Xinyun,Luo, Zhongfu,Tang, Lei,Xue, Wei
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supporting information
(2020/05/18)
-
- Application of 3,6-disubstituted imidazo[1, 2-b] pyridazine derivatives in preparation of fungicides
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The invention belongs to the technical field of farm chemicals, and specifically relates to application of 3,6-disubstituted imidazo[1, 2-b] pyridazine derivatives in preparation of fungicides. The 3,6-disubstituted imidazo[1, 2-b] pyridazine derivatives are prepared and applied in farm chemical preparation. The inhibition activity of the derivatives on nine common plant pathogenic fungi is testedby adopting a hypha growth rate inhibition method; some of the derivatives show excellent fungistat activity, and are expected to be used for preventing and treating plant diseases caused by pathogenic fungi such as wheat scab, rice blast, cotton blight, tobacco brown spot, cabbage black spot, pumpkin blight, apple ring spot, Curvularia lunata(Walk) Boed and potato dry rot.
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Paragraph 0030; 0034-0036; 0079
(2020/06/20)
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- Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor
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3,6-Disubstituted imidazo[1,2-b]pyridazine derivatives were synthesized to identify new inhibitors of various eukaryotic kinases, including mammalian and protozoan kinases. Among the imidazo[1,2-b]pyridazines tested as kinase inhibitors, several derivatives were selective for DYRKs and CLKs, with IC50?50?=?82?nM), CLK4 (IC50?=?44?nM), DYRK1A (IC50?=?50?nM), and PfCLK1 (IC50?=?32?nM). The compounds were also tested against Leishmania amazonensis. Several compounds showed anti-leishmanial activity at rather high (10?μM) concentration, but were not toxic at 1?μM or 10?μM, as judged by viability assays carried out using a neuroblastoma cell line.
- Bendjeddou, Lyamin Z.,Loa?c, Nadège,Villiers, Beno?t,Prina, Eric,Sp?th, Gerald F.,Galons, Hervé,Meijer, Laurent,Oumata, Nassima
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supporting information
p. 696 - 709
(2016/10/13)
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- AMIDO-SUBSTITUTED IMIDAZOPYRIDAZINES USEFUL IN THE TREATMENT OF HYPER-PROLIFERATIVE AND/OR ANGIOGENESIS DISORDERS
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The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): in which A, E, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
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Paragraph 0525; 0526; 0530; 0531; 0532
(2017/02/28)
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- 6-HYDROXYBENZOFURANYL- AND 6-ALKOXYBENZOFURANYL-SUBSTITUTED IMIDAZOPYRIDAZINES
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The present invention relates to 6-hydroxybenzofuranyl- and 6-alkoxybenzofuranyl- substituted imidazopyridazine compounds of general formula (I) in which R1 and R2 are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
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Page/Page column 62
(2016/07/27)
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- AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES
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The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I), in which A, R1, R2, R3, R4, R5 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
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Paragraph 0157-0159
(2015/03/31)
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- AMIDO-SUBSTITUTED IMIDAZOPYRIDAZINES USEFUL IN THE TREATMENT OF HYPER-PROLIFERATIVE AND/OR ANGIOGENESIS DISORDERS
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The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): in which A, E, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper- proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
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Page/Page column 92; 93
(2015/07/23)
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- (R)-2-Phenylpyrrolidine substituted imidazopyridazines: A new class of potent and selective pan-TRK inhibitors
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Deregulated kinase activities of tropomyosin receptor kinase (TRK) family members have been shown to be associated with tumorigenesis and poor prognosis in a variety of cancer types. In particular, several chromosomal rearrangements involving TRKA have be
- Choi, Ha-Soon,Rucker, Paul V.,Wang, Zhicheng,Fan, Yi,Albaugh, Pamela,Chopiuk, Greg,Gessier, Francois,Sun, Fangxian,Adrian, Francisco,Liu, Guoxun,Hood, Tami,Li, Nanxin,Jia, Yong,Che, Jianwei,McCormack, Susan,Li, Allen,Li, Jie,Steffy, Auzon,Culazzo, Annemarie,Tompkins, Celine,Phung, Van,Kreusch, Andreas,Lu, Min,Hu, Bin,Chaudhary, Apurva,Prashad, Mahavir,Tuntland, Tove,Liu, Bo,Harris, Jennifer,Seidel, H. Martin,Loren, Jon,Molteni, Valentina
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supporting information
p. 562 - 567
(2015/05/27)
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- ARYL AMIDE KINASE INHIBITORS
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The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
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Page/Page column 118; 119
(2015/02/02)
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- SUBSTITUTED-IMIDAZO[1,2-B]PYRIDAZINES AS MKNK1 INHIBITORS
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The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): (Ia) (Ib) (Ic) (Id) in which A, Y, R1, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
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Page/Page column 203; 204; 215; 229; 230
(2014/09/03)
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- Nitrogen bicyclic compounds as inhibitors for Scyl1 and Grk5
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The present invention relates to compounds assumed to be capable of modulating the activity of the proteins ScyI1 and Grk5, thereby regulating the expression and/or release of insulin as well as to pharmaceutical compositions containing such compounds and the use thereof especially for the treatment of a metabolic disease such as diabetes, obesity and impaired adipogenesis.
- -
-
Paragraph 0119
(2015/01/18)
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- AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES
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The present invention relates to amino-substituted imidazopyridazine compounds of general formula(I): in which A, R1, R3 and n are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
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Page/Page column 74
(2013/03/26)
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- SUBSTITUTED IMIDAZOPYRIDAZINES
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The present invention relates to substituted imidazopyridazine compounds of general formula(I): in which A, Q, R1, R3,R4 and n are as defined in the claims, to methods of preparing said compounds,to intermediate compounds useful for preparing said compoun
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Page/Page column 73; 78; 87
(2013/04/10)
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- AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES
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The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I), in which A, R1, R2, R3, R4, R5 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper- proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients
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Page/Page column 56
(2013/10/21)
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- AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES
-
The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I); in which A, R1, R2, R3, R4, R5 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparin
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Page/Page column 60-61
(2013/10/22)
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- AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES
-
The present invention relates to amino-substituted imidazopyndazine compounds of general formula (I) : in which A, R1, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
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Page/Page column 55-56
(2013/07/05)
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- IMIDAZO [1,2-B] PYRIDAZINE AND IMIDAZO [4,5-B] PYRIDINE DERIVATIVES AS JAK INHIBITORS
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New imidazo[1,2-b]pyridazine and imidazo[4,5-b]pyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
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Page/Page column 46-47
(2012/06/15)
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- Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
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New imidazo[1,2-b]pyridazine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
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Page/Page column 18
(2012/06/18)
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- COMPOUNDS AND COMPOSITIONS AS TRK INHIBITORS
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The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.
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Page/Page column 36
(2012/03/27)
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- HETEROCYCLYL AMINOIMIDAZOPYRIDAZINES
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The present invention relates to heterocyclyl aminoimidazopyridazine compounds of general formula (I) : in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper- proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
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Page/Page column 76
(2013/02/28)
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- MODULATORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE
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The present invention relates to modulators of IRAK kinase and provides compositions comprising such modulators, as well as methods therewith for treating conditions or diseases mediated by or associated with IRAK kinase.
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Page/Page column 17
(2011/02/18)
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- HETEROCYCLIC HYDRAZONE COMPOUNDS AND THEIR USES TO TREAT CANCER AND INFLAMMATION
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The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
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Page/Page column 54
(2011/02/24)
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- HETEROCYCLIC OXIME COMPOUNDS
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The invention relates to compounds of formula (I) and salts thereof wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
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Page/Page column 57-58
(2011/04/13)
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- Oxo-substituted imidazo[1,2b]pyridazines, their preparation and use as pharmaceuticals
-
The invention relates to novel inhibitors of kinases of the general formula (I): in which Q and R1 are defined in the claims, method for preparing such inhibitors, intermediates for preparing such inhibitors and uses of such inhibitors.
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Page/Page column 6
(2009/04/24)
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- COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS
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The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Ros, KDR, FMS, c-FMS, FLT3, c-Kit, JAK2, JAK3, Aurora, PDGFR, Lck, TrkA, TrkB, TrkC, IGF-1R, ALK4, ALK5 and ALK or combinations thereof.
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Page/Page column 143
(2009/12/23)
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- 6-AMINOIMIDAZO[1,2-b]PYRIDAZINE ANALOGS AS RHO KINASE INHIBITORS FOR THE TREATMENT OF RHO KINASE-MEDIATED DISEASES AND CONDITIONS
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Methods for using 6-aminoimidazo[1,2-b]pyridazine analogs are disclosed herein to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of 6-aminoimidazo[1,2-b]pyridazine analogs, are disclosed herein.
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Page/Page column 22
(2008/12/06)
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- IMIDAZO[1,2-B]PYRIDAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS
-
The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II), or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.
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Page/Page column 49; 60
(2008/12/05)
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- HETEROCYCLIC COMPOUNDS AS ANTIINFLAMMATORY AGENTS
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A compound of Formula Ia or Ib in free or salt or solvate form, where R1, R2, R3, R4, R5 R20, R24, R25, X, Y and Z have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. These compounds are also useful for treating diseases mediated by the Pi3k receptor, the JAK-2 receptor and the TRK receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
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Page/Page column 50
(2008/12/05)
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- Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7
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A high-throughput screening campaign identified a number of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. Further synthetic chemistry efforts enabled the preparation of a number of analogues with promising in vitro potencies. Although these compounds show likely broad spectrum inhibitory activity, they represent a useful starting point for further chemical optimisation.
- Bouloc, Nathalie,Large, Jonathan M.,Smiljanic, Ela,Whalley, David,Ansell, Keith H.,Edlin, Christopher D.,Bryans, Justin S.
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scheme or table
p. 5294 - 5298
(2009/05/08)
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- SUBSTITUTED IMIDAZOPYRIDAZINES AND PYRROLOPYRIMIDINES AS LIPID KINASE INHIBITORS
-
The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.
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Page/Page column 84
(2009/01/20)
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