cas 199328-31-9, 2-OXOINDOLINE-5-SULPHONYL CHLORIDE 97

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Synthesis and biological evaluation of novel fluorinated anticancer agents incorporating the indolin-2-one moiety
A series of novel fluorinated anticancer agents containing the indolin-2-one moiety were designed, synthesized and evaluated for their anticancer activities in vitro. Among them, compounds 6, 7, 9, 12 and 13 showed potent activities against the tested human cancer cell lines. Notably, compound 6 showed significant activities against A549, Bel7402, HepG2, HCT116 and HeLa cancer cell lines, which were comparable to those of sunitinib. Further study on its mechanisms demonstrated that compound 6 can be used as a potential anticancer agent for inhibiting proliferation and inducing apoptosis of HepG2 cells, along with inhibiting angiogenesis of HUVECs.
Wang, Shuai-Yu,Wang, Li-Jun,Jiang, Bo,Wu, Ning,Li, Xiang-Qian,Luo, Jiao,Wang, Bao-Cheng,Zhang, Ren-Shuai,Xu, Qi,Shi, Da-Yong
p. 91795 - 91801
(2015)
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Design, synthesis and biological evaluation of novel bromophenol derivatives incorporating indolin-2-one moiety as potential anticancer agents
A series of bromophenol derivatives containing indolin-2-one moiety were designed and evaluated that for their anticancer activities against A549, Bel7402, HepG2, HeLa and HCT116 cancer cell lines using MTT assay in vitro. Among them, seven compounds (4g-4i, 5h, 6d, 7a, 7b) showed potent activity against the tested five human cancer cell lines. Wound-healing assay demonstrated that compound 4g can be used as a potent compound for inactivating invasion and metastasis by inhibiting the migration of cancer cells. The structure-activity relationships (SARs) of bromophenol derivatives had been discussed, which were useful for exploring and developing bromophenol derivatives as novel anticancer drugs.
Wang, Li-Jun,Wang, Shuai-Yu,Jiang, Bo,Wu, Ning,Li, Xiang-Qian,Wang, Bao-Cheng,Luo, Jiao,Yang, Meng,Jin, Shui-Hua,Shi, Da-Yong
p. 806 - 823
(2015)
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Design and synthesis of 2-oxindole based multi-targeted inhibitors of PDK1/Akt signaling pathway for the treatment of glioblastoma multiforme
Aggressive behavior and diffuse infiltrative growth are the main features of Glioblastoma multiforme (GBM), together with the high degree of resistance and recurrence. Evidence indicate that GBM-derived stem cells (GSCs), endowed with unlimited proliferative potential, play a critical role in tumor development and maintenance. Among the many signaling pathways involved in maintaining GSC stemness, tumorigenic potential, and anti-apoptotic properties, the PDK1/Akt pathway is a challenging target to develop new potential agents able to affect GBM resistance to chemotherapy. In an effort to find new PDK1/Akt inhibitors, we rationally designed and synthesized a small family of 2-oxindole derivatives. Among them, compound 3 inhibited PDK1 kinase and downstream effectors such as CHK1, GS3Kα and GS3Kβ, which contribute to GCS survival. Compound 3 appeared to be a good tool for studying the role of the PDK1/Akt pathway in GCS self-renewal and tumorigenicity, and might represent the starting point for the development of more potent and focused multi-target therapies for GBM.
Sestito, Simona,Nesi, Giulia,Daniele, Simona,Martelli, Alma,Digiacomo, Maria,Borghini, Alice,Pietra, Daniele,Calderone, Vincenzo,Lapucci, Annalina,Falasca, Marco,Parrella, Paola,Notarangelo, Angelantonio,Breschi, Maria C.,Macchia, Marco,Martini, Claudia,Rapposelli, Simona
p. 274 - 288
(2015)
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DESIGN, SYNTHESIS OF NOVEL RNA-DEPENDENT RNA POLYMERASE OXYINDOLE INHIBITORS
The present invention relates to new compounds represented by formulas I, II and III, including any conformational isomer form, salts and solvates, for the inhibition of RNA polymerase RNA-dependent on DENV. The present invention also relates to a method
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Page/Page column 62

(2022/01/05)

N-(2-ethylamine) benzenesulfonamide cordycepin derivative as well as preparation method and application thereof
The invention discloses an N-(2-ethylamine) benzenesulfonamide cordycepin derivative as well as a preparation method and an application thereof in inhibiting tumor cell proliferation, and the N-(2-ethylamine) benzenesulfonamide cordycepin derivative is pr
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Paragraph 0039; 0040

(2020/01/25)

Discovery of hybrids of indolin-2-one and nitroimidazole as potent inhibitors against drug-resistant bacteria
With antibiotics resistance developing rapidly, new antibacterial agents are needed to be discovered. We readily synthesized 11 indolin-2-one compounds and found a hybrid of indolin-2-one and nitroimidazole 3-((1-methyl-5-nitro-1H-imidazol-2-yl)methylene)
Zhou, Yuanzheng,Ju, Yuan,Yang, Yang,Sang, Zitai,Wang, Zhenling,He, Gu,Yang, Tao,Luo, Youfu
p. 887 - 897
(2018/07/13)

Discovery of novel bromophenol hybrids as potential anticancer agents through the ros-mediated apoptotic pathway: Design, synthesis and biological evaluation
A series of bromophenol hybrids with N-containing heterocyclic moieties were designed, and their anticancer activities against a panel of five human cancer cell lines (A549, Bel7402, HepG2, HCT116 and Caco2) using MTT assay in vitro were explored. Among t
Wang, Li-Jun,Guo, Chuan-Long,Li, Xiang-Qian,Wang, Shuai-Yu,Jiang, Bo,Zhao, Yue,Luo, Jiao,Xu, Kuo,Liu, Hua,Guo, Shu-Ju,Wu, Ning,Shi, Da-Yong
(2017/12/08)

With tyrosine kinase inhibitory activity of 2 - indolone derivatives and its preparation method and application
The invention discloses a 2-indolone derivative with tyrosine kinase inhibition activity, geometric isomers and medicinal salts thereof, and a preparation method and an application of the above compounds. Tyrosine kinase inhibition activity evaluation confirms that the derivative is a compound with good tyrosine kinase activity, so the derivative has potential antitumor activity, and can be used to prepare tumor disease prevention and treatment medicines (antitumor medicines) as an active component. The derivative provides research and enforcement foundation for tumor treatment, and has a wide application prospect.
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Paragraph 0081; 0082

(2017/07/01)

Phenyl Benzenesulfonylhydrazides Exhibit Selective Indoleamine 2,3-Dioxygenase Inhibition with Potent in Vivo Pharmacodynamic Activity and Antitumor Efficacy
Tryptophan metabolism has been recognized as an important mechanism in immune tolerance. Indoleamine 2,3-dioxygenase plays a key role in local tryptophan metabolism via the kynurenine pathway and has emerged as a therapeutic target for cancer immunotherapy. Our prior study identified phenyl benzenesulfonyl hydrazide 2 as a potent in vitro (though not in vivo) inhibitor of indoleamine 2,3-dioxygenase. Further lead optimization to improve in vitro potencies and pharmacokinetic profiles resulted in N′-(4-bromophenyl)-2-oxo-2,3-dihydro-1H-indole-5-sulfonyl hydrazide 40, which demonstrated 59% oral bioavailability and 73% of tumor growth delay without apparent body weight loss in the murine CT26 syngeneic model, after oral administration of 400 mg/kg. Accordingly, 40, is proposed as a potential drug lead worthy of advanced preclinical evaluation.
Lin, Shu-Yu,Yeh, Teng-Kuang,Kuo, Ching-Chuan,Song, Jen-Shin,Cheng, Ming-Fu,Liao, Fang-Yu,Chao, Min-Wu,Huang, Han-Li,Chen, Yi-Lin,Yang, Chun-Yu,Wu, Mine-Hsine,Hsieh, Chia-Ling,Hsiao, Wenchi,Peng, Yi-Hui,Wu, Jian-Sung,Lin, Li-Mei,Sun, Manwu,Chao, Yu-Sheng,Shih, Chuan,Wu, Su-Ying,Pan, Shiow-Lin,Hung, Ming-Shiu,Ueng, Shau-Hua
p. 419 - 430
(2016/01/28)

Mitochondrial-Targeting MET Kinase Inhibitor Kills Erlotinib-Resistant Lung Cancer Cells
Lung cancer cells harboring activating EGFR mutations acquire resistance to EGFR tyrosine kinase inhibitors (TKIs) by activating several bypass mechanisms, including MET amplification and overexpression. We show that a significant proportion of activated MET protein in EGFR TKI-resistant HCC827 lung cancer cells resides within the mitochondria. Targeting the total complement of MET in the plasma membrane and mitochondria should render these cells more susceptible to cell death and hence provide a means of circumventing drug resistance. Herein, the mitochondrial targeting triphenylphosphonium (TPP) moiety was introduced to the selective MET kinase inhibitor PHA665752. The resulting TPP analogue rapidly localized to the mitochondria of MET-overexpressing erlotinib-resistant HCC827 cells, partially suppressed the phosphorylation (Y1234/Y1235) of MET in the mitochondrial inner membrane and was as cytotoxic and apoptogenic as the parent compound. These findings provide support for the targeting of mitochondrial MET with a TPP-TKI conjugate as a means of restoring responsiveness to chemotherapy.
Yang, Tianming,Ng, Wai Har,Chen, Huan,Chomchopbun, Kamon,Huynh, The Hung,Go, Mei Lin,Kon, Oi Lian
supporting information
p. 807 - 812
(2016/08/24)

2-indolinone derivatives, preparation and applications thereof
The present invention relates to a class of 2-indolinone derivatives, a combination of the class of the compounds, and applications of the 2-indolinone derivatives in anti-tumor and/or anti-cancer and/or anti-angiogenesis drugs. The present invention furt
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Paragraph 0028; 0038

(2016/10/10)

PLASMINOGEN ACTIVATOR-1 INHIBITORS AND METHODS OF USE THEREOF
The invention relates to plasminogen activator- 1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or disorder associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to prevent or reduce thrombosis and fibrosis, to promote thrombolysis, and to modulate lipid metabolism and treat diseases or disorders associated with elevated PAI-1, cholesterol, or lipid levels.
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Paragraph 00233-00236

(2014/05/24)

Enamino-oxindole HIV protease inhibitors
We have designed and synthesized a series of HIV protease inhibitors (PIs) with enamino-oxindole substituents optimized to interact with the S2′ subsite of the HIV protease binding pocket. Several of these inhibitors have sub-nanomolar Ki and antiviral IC50 in the low nM range against WT HIV and against a panel of multi-drug resistant (MDR) strains.
Eissenstat, Michael,Guerassina, Tanya,Gulnik, Sergei,Afonina, Elena,Silva, Abelardo M.,Ludtke, Douglas,Yokoe, Hiroko,Yu, Betty,Erickson, John
supporting information; experimental part
p. 5078 - 5083
(2012/09/07)

Discovery of a novel noniminosugar acid α glucosidase chaperone series
Pompe disease is an autosomal recessive lysosomal storage disorder (LSD) caused by deficiency of the lysosomal enzyme acid α-glucosidase (GAA). Many disease-causing mutated GAA retain enzymatic activity but are not translocated from endoplasmic reticulum
Xiao, Jingbo,Motabar, Omid,Lea, Wendy A.,Hu, Xin,Zheng, Wei,Southall, Noel,Liu, Ke,Simeonov, Anton,Ferrer, Marc,Marugan, Juan J.,Westbroek, Wendy,Velayati, Arash,Gustafson, Ann Marie,Goldin, Ehud,Sidransky, Ellen,Tamargo, Rafael J.,Ribes, Antonia,Matalonga, Leslie
p. 7546 - 7559,14
(2020/08/24)

ALPHA-GLUCOSIDASE BINDERS AND METHODS OF THEIR USE
Compounds that bind to acid alpha glucosidase are described. Methods of using these compounds for the treatment of diabetes and Pompe disease are also described.
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(2012/05/20)

The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors
Variously substituted indolin-2-ones were synthesized and evaluated for activity against KDR, Flt-1, FGFR-1 and PDGFR. Extension at the 5-position of the oxindole ring with ethyl piperidine (compound 7i) proved to be the most beneficial for attaining both biochemical and cellular potencies. Further optimization of 7i to balance biochemical and cellular potencies with favorable ADME/ PK properties led to the identification of 8h, a compound with a clean CYP profile, acceptable pharmacokinetic and toxicity profiles, and robust efficacy in multiple xenograft tumor models.
Kim, Moon H.,Tsuhako, Amy Lew,Co, Erick W.,Aftab, Dana T.,Bentzien, Frauke,Chen, Jason,Cheng, Wei,Engst, Stefan,Goon, Levina,Klein, Rhett R.,Le, Donna T.,Mac, Morrison,Parks, Jason J.,Qian, Fawn,Rodriquez, Monica,Stout, Thomas J.,Till, Jeffrey H.,Won, Kwang-Ai,Wu, Xiang,Michael Yakes,Yu, Peiwen,Zhang, Wentao,Zhao, Yeping,Lamb, Peter,Nuss, John M.,Xu, Wei
scheme or table
p. 4979 - 4985
(2012/09/07)

COMPOSITIONS AND METHODS FOR TREATMENT OF NEURODEGENERATIVE DISEASE
Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
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(2011/10/13)

PYRROLO-NITROGENOUS HETEROCYCLIC DERIVATIVES, THE PREPARATION AND THE PHARMACEUTICAL USE THEREOF
The invention provides new pyrrolo-nitrogenous heterocyclic derivatives represented by formula (I) or their salts, the preparation thereof, pharmaceutical compositions containing such derivatives and the use of such derivatives as therapeutic agents, espe
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Page/Page column 90-91

(2010/04/23)

2-SULFONYLAMINO-4-HETEROARYL BUTYRAMIDE ANTAGONISTS OF CCR10
This invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein R1, R2, R4. Ar and Het are as defined herein. The invention also relates to methods of using the compound of for
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Page/Page column 123

(2009/11/29)

Pyrroloquinoline Derivatives And Their Use As Protein Kinases Inhibitors
The present invention relates to inhibitors of protein kinases of formula I: which can be used in the treatment of various diseases, notably cancer, inflammation or disorders of the central nervous system. It also relates to pharmaceutical compositions containing the compounds according to the invention and their use in therapy.
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Page/Page column 8

(2009/03/07)

Synthesis and antiproliferative activities of isoindigo and azaisoindigo derivatives
In the course of structure-activity relationship studies, diversely substituted 1-(β- d-acetylatedglucopyranosyl)isoindigo derivatives were prepared from indolines. New 7′-azaisoindigo analogues were also synthesized by coupling a glycosylated isatine and a 7-azaindolin-2-one derivative. Compounds containing a 7′-azaisoindigo framework have never been described before. To get an insight into the substitution pattern required for the best biological potencies, their antiproliferative activities were evaluated toward a human buccal carcinoma cell line (KB) and two human myeloid leukaemia cell lines (K562, HL60).
Bouchikhi, Fadoua,Anizon, Fabrice,Moreau, Pascale
p. 755 - 762
(2008/09/20)

INHIBITION OF SHP2/PTPN11 PROTEIN TYROSINE PHOSPHATASE BY NSC-87877, NSC-117199 AND THEIR ANALOGS
Compounds and associated methods for inhibiting a protein tyrosine phosphatase. By a combination of experimental and virtual screenings of the NCI Diversity Set chemical library, NSC-87877 and NSC-117199 have been identified as Shp2 PTP inhibitors. Signif
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(2010/11/28)

3- (AMINOMETHYLIDEN) 2-INDOLINONE DERIVATIVES AND THEIR USE AS CELL PROLIFERATION INHIBITORS
The present invention encompasses compounds of general formula (1) wherein R1, R2, R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
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Page/Page column 10

(2008/06/13)

HETEROCYCLIC DERIVATIVES FOR MODULATION OF CALCIUM CHANNELS
Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
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Page/Page column 190

(2008/06/13)

Sulfonylated pyrrole-2-indolinone derivatives as kinase inhibitors
The present invention relates to compounds having the following chemical structure (Formula I): where the substituents R1-R10 are defined herein. The compounds of this invention are useful in treating disorders related to abnormal kinase activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
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Page/Page column 30

(2008/06/13)

Resistance-repellent retroviral protease inhibitors
Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
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(2010/02/14)

FORMULATIONS FOR PHARMACEUTICAL AGENTS IONIZABLE AS FREE ACIDS OR FREE BASES
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Page/Page column 170; 220

(2008/06/13)

BROADSPECTRUM SUBSTITUTED OXINDOLE SULFONAMIDE HIV PROTEASE INHIBITORS
The present invention concerns the compounds having the formula (I) N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C 1-6/s
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Page 25

(2008/06/13)

Hexahydro-cyclohepta-pyrrole oxindole as potent kinase inhibitors
The present invention is directed to a class indolinone compounds, hexahydro-cyclohepta-pyrrole oxindoles, which are useful as protein kinase inhibitors.
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(2010/02/08)

NOVEL SUBSTITUTED BENZIMIDAZOLE DERIVATIVES
The invention provides a compound of Formula I (I) wherein n is 1 or 2; R1 is selected from hydrogen, halogen, CN, COOR6, CONR6R7 or CH2OR6; R2 is selected from hydrogen, halogen
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Page 18

(2010/02/09)

5-sulfonamido-substituted indolinone compounds as protein kinase inhibitors
The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
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Page/Page column 28

(2010/02/08)

Sulfonamide substituted indolinones as inhibitors of DNA dependent protein kinase (DNA-PK)
The present invention relates generally to the field of radiosensitizing agents which are capable of enhancing radiotherapy by inhibiting DNA-PK (DNA-protein kinase). In particular, it relates to sulfonamide substituted indolinones which inhibit DNA-PK.
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Page 24

(2010/02/10)

Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase
A novel series of substituted 3-[3-(aminopropyl)-4,5,6,7-tetrahydro-1H- indol-2-ylmethylene]-1,3-dihydro-indole-2-ones was discovered as potent inhibitors of the non-receptor tyrosine kinase Src and Yes. A structure-activity relationship was developed in order to optimize their potency and selectivity. Syntheses of these compounds are also described herein.
Guan, Huiping,Laird, A. Douglas,Blake, Robert A.,Tang, Cho,Liang, Chris
p. 187 - 190
(2007/10/03)

Prodrugs of a 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
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(2008/06/13)

3-(PIPERAZINYLBENZYLIDENYL)-2-INDOLINONE COMPOUNDS AND DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS
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(2008/06/13)

Combination therapy for the treatment of cancer
The present invention relates to methods for treatment or prevention of neoplasia disorders using protein tyrosine kinase inhibitors in combination with cyclooxygenase inhibitors, in particular cyclooxygenase-2 selective inhibitors.
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(2008/06/13)

Potent small molecule inhibitors of spleen tyrosine kinase (Syk)
A series of oxindoles demonstrating inhibition of the phosphorylation of biotinylated substrates of Syk and IgE/FcεRI triggered basophil cell degranulation has been identified. A study of the SAR around sulfonamide 31 (IC50=5 nM, EC50=1400 nM) is discussed. The modest cellular activity representative of the sulfonamide series was overcome when the Polar Surface Area was lowered to 2, leading to the identification of amide 32 (IC50=145 nM, EC50=100 nM).
Lai, Justine Y. Q.,Cox, Paul J.,Patel, Rajesh,Sadiq, Shazia,Aldous, David J.,Thurairatnam, Sukanthini,Smith, Keith,Wheeler, Darren,Jagpal, Savita,Parveen, Sofia,Fenton, Gary,Harrison, Trevor K. P.,McCarthy, Clive,Bamborough, Paul
p. 3111 - 3114
(2007/10/03)

Methods of modulating protein tyrosine kinase function with substituted indolinone compounds
The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein kinases using indolinone compounds and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.
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(2008/06/13)

Pyrrole substituted 2-indolinone protein kinase inhibitors
The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
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(2008/06/13)

3-heteroarylidene-2-indolinone protein kinase inhibitors
The present invention relates to novel 3-heteroarylidene-2-indolinone compounds and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
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(2008/06/13)

Pyrrole substituted 2-indolinone protein kinase inhibitors
The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
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(2008/06/13)

3-(cycloalkanoheteroarylidenyl)-2-indolinone protein tyrosine kinase inhibitors
The present invention relates to novel 3-(cycloalkano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.
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Page column 21-22

(2010/02/05)

Oxindole derivatives
The invention relates to compounds of formula (I), wherein: R2represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino, nitro, C2-4alkanoyl, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylthio, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, {overscore (N)}—C1-4alkylcarbamoyl, {overscore (N)},{overscore (N)}-di(C1-4alkyl)carbamoyl, aminosulphonyl, {overscore (N)}—C1-4alkylaminosulphonyl, {overscore (N)},{overscore (N)}-di(C1-4alkyl)aminosulphonyl, C1-4alkylsulphonylamino, or a group R4X1wherein X1represents a direct bond, C2-4alkanoyl, —CONR5R6—, —SO2NR7R8— or —SO2R9— (wherein R5and R7, each independently represents hydrogen or C1-2alkyl and R6, R8and R9each independently represents C1-4alkyl and wherein R4is linked to R6, R8or R9) and R4represents an optionally substituted group selected from phenyl and a 5 or 6-membered heterocyclic group; n is an integer from 0 to 4, R1represents hydrogen, C1-4alkyl, C1-4alkoxymethyl, di(C1-4alkoxy)methyl or C1-4alkanoyl; m is an integer from 0 to 4; and R3represents hydroxy, halogeno, nitro, trifluoromethyl, C1-3alkyl, cyano, amino or R10X2(wherein X2represents a direct bond, —CH2—, or a single or double heteroatom linker group including —S—, —SO— and —NR15— (wherein R15represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl), and R10is an alkenyl or alkynyl chain optionally substituted by for example hydroxy, amino, nitro, alkyl, cycloalkyl, alkoxyalkyl, or an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring, which alkyl, alkenyl or alkynyl chain may have a heteroatom linker group, or R10is an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF and FGF, properties of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
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(2008/06/13)

2-indolinone derivatives as modulators of protein kinase activity
The present invention relates to novel imidazoly 2-indolinones and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
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(2008/06/13)

3-(cycloalkanoheteroarylidenyl)-2- indolinone protein tyrosine kinase inhibitors
The present invention relates to novel 3-(cycloalkanoheteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.
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(2008/06/13)

3-(CYCLOHEXANOHETEROARYLIDENYL)-2-INDOLINONE PROTEIN TYROSINE KINASE INHIBITORS
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(2008/06/13)

New α-substituted succinate-based hydroxamic acids as TNFα convertase inhibitors
Tumor necrosis factor α convertase (TACE), the enzyme responsible for the processing of proTNFα to TNFα, has been reported to be a metalloproteinase closely related to matrix metalloproteinases (MMPs). Current inhibitors of TACE such as succinate-based hy
Barlaam, Bernard,Bird, T. Geoffrey,Lambert-Van Der Brempt, Christine,Campbell, Douglas,Foster, Steve J.,Maciewicz, Rose
p. 4890 - 4908
(2007/10/03)