- NOVEL FUNGICIDAL CARBAMATE COMPOUNDS
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An object of the present invention is to provide a carbamate compound or a salt thereof that controls diseases. The present invention provides a carbamate compound represented by Formula (1), or a salt thereof, wherein R1, R3 and R6 are identical or different and each represents hydrogen, or the like; R2 represents hydrogen, halogen, or C1-6 alkyl; R4 and R5 are identical or different and each represents hydrogen, or the like; R7 represents hydrogen, or the like; R8 represents hydrogen, or C1-6 alkyl; X and Χ1 independently represent oxygen, or sulfur; Y represents oxygen, or sulfur; Z represents oxygen/ or sulfur; l is an integer of 0 to 2; m is an integer of 0 to 3; n is an integer of 0 to 4; and when l, m or n is more than one, the l, m or n may be the same or different.
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Page/Page column 50
(2018/08/20)
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- NEW DIHYDROQUINOLINE PYRAZOLYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R10, R11, R12, R13, R14, R15, R16, R17 and m are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 40
(2016/05/19)
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- NEW DIHYDROQUINOLINE PYRAZOLYL COMPOUNDS
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The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R15, R16, R17 and n are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 47
(2016/05/19)
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- ALDOSTERONE SYNTHASE INHIBITORS
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This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.
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Page/Page column 137; 138
(2012/11/13)
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- EP2/4 AGONISTS
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EP2/4 compounds having improved dual pharmacological activity are described. The uniqueness of using EP2/4 dual agonists resides in their ability to modify both uveoscleral outflow via the ciliary muscle and conventional outflow via trabecular meshwork and Schlemm's canal all in the same treatment paradigm. The compounds can be employed for the treatment of glaucoma and ocular hypertension. Formula (I).
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Page/Page column 64-65
(2010/11/03)
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- METHYL SULFANYL PYRMIDMES USEFUL AS ANTIINFLAMMATORIES, ANALGESICS, AND ANTIEPILEPTICS
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The present invention relates to pyrimidine derivatives of Formula (Ia) and (Ib) (including tautomers, isomers, prodrugs, and pharmaceutically acceptable salts thereof). Said compounds are useful in the treatment of pain (such as neuropathic pain), inflammation, and epilepsy (by acting as anticonvulsants). Methods of medical treatment making use of said compounds, as well as additional compounds of Formula (IIa) and (IIb), are also disclosed.
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Page/Page column 80
(2010/12/18)
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- Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors
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Cyclin-dependent kinase 5 (CDK5) is a serine/threonine kinase that plays a critical role in the early development of the nervous system. Deregulation of CDK5 is believed to contribute to the abnormal phosphorylation of various cellular substrates associated with neurodegenerative disorders such as Alzheimer's disease, amyotrophic lateral sclerosis, and ischemic stroke. Acyclic urea 3 was identified as a potent CDK5 inhibitor and co-crystallographic data of urea 3/CDK2 enzyme were used to design a novel series of 3,4-dihydroquinazolin-2(1H)-ones as CDK5 inhibitors. In this investigation we present our synthetic studies toward this series of compounds and discuss their biological relevance as CDK5 inhibitors.
- Rzasa, Robert M.,Kaller, Matthew R.,Liu, Gang,Magal, Ella,Nguyen, Thomas T.,Osslund, Timothy D.,Powers, David,Santora, Vincent J.,Viswanadhan, Vellarkad N.,Wang, Hui-Ling,Xiong, Xiaoling,Zhong, Wenge,Norman, Mark H.
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p. 6574 - 6595
(2008/03/27)
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- Method for producing 2-halo-6-nitrobenzoic acids
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The present invention relates to a process for the preparation of 2-halo-6-nitrobenzoic acids by oxidation of 2-halo-6-nitro-benzyl alcohols, esters, ethers, or mixtures thereof with nitric acid and to the use of this process as a step in the preparation of 2-halo-6-nitrobenzoic acids from 2-halo-6-nitrotoluenes.
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Page/Page column 4-5
(2008/06/13)
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- 2-oxo-1,3,4-trihydroquinazolinyl derivatives and methods of use
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Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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- AMINE DERIVATIVES
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A compound of the formula: ???whereinX and X' are the same or different, and each represents a hydrogen atom, a fluorine atom, a chlorine atom or an amino optionally having substituents, and at least one of X and X' represents a fluorine atom, a chlorine atom or an amino optionally having substituents;R1 and R2 represent a hydrogen atom or C1-6 alkyl optionally having substituents, or R1 and R2, together with the adjacent nitrogen atom, form a nitrogen-containing heterocyclic ring optionally having substituents;Y and Q are the same or different, and each represents a bond or a spacer having a main chain of 1 to 6 atoms;... represents a single bond or a double bond;T1 and T2 are the same or different, and each represents C(R9) (R9 represents a hydrogen atom, a hydroxy or C1-6 alkyl) or N, when each of the adjacent ... is a single bond, and C when the adjacent ... is a double bond; andAr represents an aromatic group optionally having substituents, a C3-9 cycloalkyl group optionally having substituents, a 3 to 9-membered saturated heterocyclic group optionally having substituents, a hydrogen atom or a halogen atom; provided that 6-chloro-3-(R,S)-(N,N-dimethylamino)methyl-1-[3-(indol-3-yl)-2-[(R)-(4-phenylpiperazin-1-yl)carbonylamino]propanoyl]-1,2,3,4-tetrahydroquinoline; 6-chloro-3-(R,S)-(N,N-dimethylamino)methyl-1-[3-(indol-3-yl)-2-[(R)-4-(2-oxo-2,3-dihydro-1H-benzimidazol-1-yl)piperidinocarbonylamino]propanoyl]-1,2,3,4-tetrahydroquinoline and 1-benzoyl-N-[(R)-2-[6-chloro-3-[(N,N-dimethylamino)methyl]-1,2,3,4-tetrahydroquinolin-1-yl]-1-[3-(indol-3-yl)propanoyl]-4-piperidinecarboxamide are excluded; a salt thereof or a prodrug thereof has an excellent somatostatin receptor binding inhibition action and is useful for preventing and/or treating diseases associated with somatostatin.
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- Synthesis and diuretic activity of 4,5-dihydro-6H-imidazo[4,5,1- ij]quinoline-6-one 6-oxime-O-sulfonic acid derivatives
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Using our previously reported 7-chloro-2,3-dihydro-1-(2-methylbenzoyl)- 4(1H)-quinolinone 4-oxime-O-sulfonic acid potassium salt la (M17055) as a lead, a series of tricyclic (2a-o, 3, 4, 5) and tetracyclic (6) quinolinone oxime O-sulfonic acid derivatives were synthesized by ring annulation of the 1-(2-methylbenzoyl) moiety to the quinolinone skeleton. They were compared with furosemide and compound 1a for diuretic activity in dogs; some tricyclic 4,5-dihydro-6H-imidazo[4,5,1-ij]quinoline-6-one 6-oxime-O-sulfonic acid derivatives showed diuretic activity comparable (2c,e) or superior (2m) to the lead compound 1a. These results are discussed on the basis of a comparison of the conformational and electronic characteristics of the relevant compounds with the aid of computer graphics.
- Nishijima, Kazumi,Shinkawa, Tomoaki,Ito, Manabu,Nishida, Hidemitsu,Yamamoto, Ichirou,Onuki, Yoshiaki,Inaba, Hitoshi,Miyano, Soutarou
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p. 763 - 774
(2007/10/03)
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- Polyaza Heterocycles. Part 2. Nucleophilic Substitution of Halogens in Halogenoquinoxalinocinnolines
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10-Chloroquinoxalinocinnoline readily undergoes methoxydechlorination when treated with sodium methoxide.The 1-, 2-, 3-, 4- and 9-chloro isomers are unreactive towards this reagent, but the 9,10-dichloro derivative undergoes substitution of both chlorines (the 10-position being much the more reactive).The 9- and 10-bromo analogues are both unreactive towards sodium methoxide, but the 9- and 10-fluoro analogues are both highly reactive, to the extent that it has not been possible even to isolate the 10-fluoro compound.Routes to 9- and 10-piperidinoquinoxalinocinnolines are described.
- Ahmad, Arshad,Dunbar, Linda J.,Green, Iain G.,Harvey, Ian W.,Shepherd, Thomas,et al.
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p. 2751 - 2758
(2007/10/02)
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- Compounds interacting with tubulin: Part I: Synthesis of ortho-ortho' substituted phenylpyrroles with free or restricted rotation.
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The synthesis of ortho-ortho' substituted phenylpyrroles that are susceptible to isomerization of the biaryl type (atropisomerism) was performed using a Michael addition of isocyanoacetates with nitrostyrenes.Atropisomerism in phenylpyrroles 14 and 15 was studied by means of 1H NMR spectroscopy using chiral lanthanide shift reagents (LSR*).In the case of chiral phenylpyrrole 21, an evaluation of the interconversion parameters between diastereomers (k, ΔGT*) was attempted. - - - tubulin / phenylpyrrole / atropisomers / chiral shift reagents
- Alazard, JP.,Boye, O.,Gillet, B.,Guenard, D.,Beloeil, JC.,Thal, C.
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p. 779 - 787
(2007/10/02)
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- Mass Spectrometric Fragmentation Reactions. XXXI-The Fragmentation Behaviour of o-Halobenzoic Acids Substituted in the 5-Position: A Novel Ortho Effect
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A fragmentation sequence typical for o-halobenzoic acids carrying a heteroatom substituent in the 5-position is described.
- Breuer, M.,Budzikiewicz, H.
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p. 229 - 234
(2007/10/02)
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