- PLANT GROWTH REGULATOR
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PROBLEM TO BE SOLVED: To provide a plant growth regulator. SOLUTION: The plant growth regulator comprises a compound represented by formula 1, or a salt or ester thereof as an active ingredient. (R1 is H, a halogen atom, a hydroxy group, an alkyl group, or an alkoxy group; R2 is H, a halogen atom, a hydroxy group, an alkyl group, or an alkoxy group; and R3 is a hydroxy group, an alkoxy group, or an amino group.) SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0040
(2018/05/30)
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- INDOLYLMALEIMIDES AS SOFT PAN-PKC INHIBITORS
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The present invention relates to new kinase inhibitors, more specifically soft PKC inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new soft PKC inhibitors compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including autoimmune and inflammatory diseases.
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Page/Page column 51
(2013/03/26)
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- Sulfonamide peri-substituted bicyclics for occlusive artery disease
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Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:
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Page/Page column 57
(2008/06/13)
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- A new modular indole synthesis. Construction of the highly strained CDEF parent tetracycle of nodulisporic acids A and B
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Construction of the highly strained CDEF parent tetracycle, a structural motif found only in the potent ectoparasiticidal agents (+)-nodulisporic acids A and B and related congeners, has been achieved via a new modular indole synthesis, exploiting a sequential Stille cross-coupling/Buchwald-Hartwig union/cyclization tactic. The new indole synthesis holds the promise of rapid assembly of diverse, highly substituted indoles possessing uncommon substitution patterns.
- Smith III, Amos B.,Kuerti, Laszlo,Davulcu, Akin H.
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p. 2167 - 2170
(2007/10/03)
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- Palladium-Catalyzed Synthesis of Indoles by Reductive N-Heteroannulation of 2-Nitrostyrenes
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A palladium-phosphine catalyzed reductive N-heteroannulation of 2-nitrostyrenes, in the presence of carbon monoxide, producing indoles has been developed. Indoles were obtained, in moderate to excellent yield, from substituted 2-nitrostyrenes having either electron-withdrawing (NO2 and CO2-Me) or electron-donating (Br, OH, Me, OMe, and OTf) substituents on the aromatic ring. Best results were obtained using palladium diacetate (6 mol percent) together with triphenylphosphine (24 mol percent) as the catalytic system, under 4 atm of carbon monoxide in acetonitrile at 70 °C. Other palladium(II) and palladium(0) complexes also catalyze the reaction.
- So?derberg, Bjo?rn C.,Shriver, James A.
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p. 5838 - 5845
(2007/10/03)
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- Facile synthesis of 2-benzylindoles
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A wide range of 2-Benzylindoles 2 are conveniently and efficiently prepared by heating N-benzylindoles 1 in polyphosphoric acid. Mechanistic studies suggest an intramolecular rearrangement via the corresponding 3- benzyl intermediates.
- Wiedenau, Paul,Blechert, Siegfried
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p. 2033 - 2039
(2007/10/03)
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- N-benzyl dihydroindole LTD4 antagonists
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This invention relates to pharmaceutical N-benzyl dihydroindole compounds having the general formula: STR1 and their use as LTD4 antagonists.
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- N-SUBSTITUTED IMIDAZOLE AND BENZIMIDAZOLE DERIVATIVES USEFUL AS ANGIOTENSON II ANTAGONISTS
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Compounds are disclosed having the formula STR1 These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
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- Thromboxane A2 synthetase inhibitors with histamine H1-blocking activity: Synthesis and evaluation of a new series of indole derivatives
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A novel series of N-substituted 3-(1H-imidazol-1-ylmethyl)indole carboxylic acid derivatives were prepared and evaluated for thromboxane A2 (TXA2) synthetase-inhibitory and histaminergic H1-blocking activity. Among the compounds synthesized, indole-6-carboxylic acid derivatives showed higher activities than the other positional isomers of carboxylic acid. 1-[3-(4- Benzhydryl-1-piperazinyl)propyl]-3-(1H-imidazol-1-ylmethyl)-1H-indole-6- carboxylic acid (12) had the strongest thromboxane synthetase inhibitory activity (IC50 = 5 x 10-8 M) and H1-blocking activity (IC50 = 8 x 10- 9 M).
- Kamiya,Matsui,Shirahase,Nakamura,Wada,Kanda,Shimaji,Kakeya
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p. 1692 - 1695
(2007/10/03)
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- Certain indole derivatives useful as leukotriene antagonists
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A compound of the formula STR1 in which R1 is hydrogen, halo, C1-4 alkyl, C1-4 alkoxy, nitrile, optionally protected carboxy, optionally protected tetrazolyl, trihalomethyl, hydroxy-C1-4 alkyl, aldehydo, --CH2 Z, --CH=CH--Z or --CH2 CH2 Z where Z is optionally protected carboxy or optionally protected tetrazolyl; R2 is halo, nitrile, an optionally protected acid group or --CONR7 R8 where R7 and R8 are each hydrogen or C1-4 alkyl; R3 and R4 are each hydrogen, C1-4 alkyl, optionally substituted phenyl, or C1-4 alkyl substituted by --CONR7 R8 or an optionally protected acid group; R5 is STR2 where W is --CH=CH--, --CH=N--, --N=CH--, --O-- or --S--, R9 is hydrogen, halo, C1-4 alkyl, C1-4 alkoxy or trihalomethyl, and R10 is hydrogen, C1-4 alkyl, C2-6 alkenyl, C3-6 cycloalkyl or C1-4 alkyl-C3-6 cycloalkyl; R6 is hydrogen or C1-4 alkyl; X is --O--(CH2)n CR11 R12, --CR11 R12 --, --CR11 R12.(CH2)n.CR13 R14 -- or --CR11 =CR12 -- where R11, R12, R13 and R14 are each hydrogen or C1-4 alkyl, and n is 0, 1 or 2; and Y is --O--CR15 R16 --, --CR15 =CR16 -- or --CR15 R16.CR17 R18 -- where R15, R16, R17 and R18 are each hydrogen or C 1-4 alkyl; or a salt thereof. The compounds in unprotected form are active as leukotriene antagonists.
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- N-Benzyl-Indoles, processes for their preparation and pharmaceutical compositions containing them
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A compound of the formula in which R1 is hydrogen, halo, C??? alkyl, C??? alkoxy, nitrile, optionally protected carboxy, optionally protected tetrazolyl, trihalomethyl, hydroxy-C??? alkyl, aldehydo,-CH?Z,-CH=CH-Z or-CH?CH?Z where Z is optionally protected carboxy or optionally protected tetrazolyl; R2 is halo, nitrile, an optionally protected acid group or-CONR?R? where R? and R? are each hydrogen or C??? alkyl, R3 and R? are each hydrogen, C??? alkyl, optionally substituted phenyl, or C??? alkyl substituted by-CONR?R? or an optionally protected acid group; R? is where W is-CH=CH-,-CH=N-,-N=CH-,-O-or-S-, R? is hydrogen, halo, C??? alkyl, C? ?? alkoxy or trihalomethyl, and R1? is hydrogen, C? ?? alkyl, C??? alkenyl, C??? cycloalkyl or C??? alkyl-C??? cycloalkyl; R? is hydrogen or C??? alkyl; X is-O-(CH?)nCR11CR12-,-CR11R12-,-CR11R12.(CH?) n.CR13R1?-or-CR11=CR12-where R11, R12, R13 and R1? are each hydrogen or C??? alkyl, and n is 0, 1 or 2; and Y is-O-CR1?R1?-,-CR1?=CR1?-or-CR1? R1?.CR1?R1?-where R1?, R1?, R1? and R1? are each hydrogen or C??? alkyl; or a salt thereof. The compounds in unprotected form are active as leukotriene antagonists.
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- A Regiocontrolled Synthesis of Substituted Indoles by Palladium-Catalyzed Coupling of 2-Bromonitrobenzenes and 2-Bromoacetanilides
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The palladium-catalyzed cross-coupling reaction of 2-bromonitrobenzenes or 2-bromoacetanilides with ethylene has been used to produce a variety of substituted indoles.The mild reaction conditions and selectivity inherent in the coupling reaction have been utilized to produce regiochemically pure 4-, 5-, 6-, and 7-substituted indoles.
- Kasahara, Akira,Izumi, Taeko,Murakami, Satoshi,Miyamoto, Kazuhiro,Hino, Toshimi
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p. 1405 - 1413
(2007/10/02)
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- The Chemistry of Indoles. XXXIII. Substituent Effect in Regioselective Metalation of 3-Indolecarbaldehyde and Syntheses of Indoles Carrying a Carbon Side Chain at the 4-, 5-, 6-, or 7-Position
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The nature of a substituent on the pyrrole ring of 3-indolecarbaldehyde plays a significant role in governing the regioselectivity of metalation.To confirm the structures of the products, various indoles carrying a carbon side chain at the 4-, 5-, 6-, or 7-position were prepared by other methods.Synthesis of 5-substituted 1-hydroxyindoles is also described.Keywords-thallation; mercuration; 4-substituted indole; 5-substituted indole; 6-substituted indole; 7-substituted indole; regioselective metalation; 3-indolecarbaldehyde; thallation-palladation; 1-hydroxyindole
- Somei, Masanori,Saida, Yoshihiro,Komura, Naoko
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p. 4116 - 4125
(2007/10/02)
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- Some Observations on the Formation of 1-Hydroxyindoles in the Leimgruber-Batcho Indole Synthesis
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The factors influencing the formation of 1-hydroxyindoles in the catalytic hydrogenation of β-dimethylamino-2-nitrostyrenes (Leimgruber-Batcho indole synthesis) have been investigated.Significant amounts of 1-hydroxyindoles were obtained only when the β-dimethylamino-2-nitrostyrene was substituted with an electron-withdrawing group at the 5 or 6 position.The proportion of 1-hydroxyindole formed relative to the normal indole product was found to increase as both the amount of catalyst and hydrogen pressure were decreased.
- Clark, Robin D.,Repke, David B.
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p. 121 - 125
(2007/10/02)
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