- HETEROARYL SUBSTITUTED SPIROPIPERIDINYL DERIVATIVES AND PHARMACEUTICAL USES THEREOF
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The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 R2, R4 and X1 are defeined herein, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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Page/Page column 154-155
(2022/02/22)
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- Spirocyclic derivatives
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The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease, disorder or condition ameliorated by inhibition of a dopamine transporter); and methods of treating patients with such compounds; wherein R1, R2, R3, R4, R5, R6, R9, R10, Q, X, Y, Z, A, L, B, m, n and p are as defined herein.
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Page/Page column 114; 115
(2016/04/09)
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- N-(HETERO)ARYL-SUBSTITUTED HETEROYCLIC DERIVATIVES USEFUL FOR THE TREATMENT OF DISEASES OR CONDITIONS RELATED TO THE CENTRAL NERVOUS SYSTEM
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The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease, disorder or condition ameliorated by inhibition of a dopamine transporter); and methods of treating patients with such compounds; wherein R1, R2, R3, R4, R9a, R9b, R9c, R9d, R9e, R9f, m, n, A, L and B are as defined herein.
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Page/Page column 51
(2016/04/20)
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- METABOTROPIC GLUTAMATE RECEPTOR NEGATIVE ALLOSTERIC MODULATORS (NAMS) AND USES THEREOF
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Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.
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Paragraph 00398
(2016/01/01)
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- HEPATITIS B VIRAL ASSEMBLY EFFECTORS
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Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.
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Paragraph 00122
(2015/05/05)
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- ANTIVIRAL PYRIMIDINES
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Disclosed herein are novel compounds comprising substituted pyrimidines, pyrazolopyrimtdines, and imidazolopyrimidines, the syntheses thereof, and compositions thereof, including pharmaceutical compositions, comprising the novel pyrimidines, pyrazolopyrimtdines, imidazolpyrimidines and related compounds. Such compounds function to inhibit entry of viruses of the Flaviviridae family, including Hepatitis C virus (HCV), into cells that are susceptible to virus infection. These compounds are useful for the treatment, therapy and/or prophylaxis of viral diseases and infection, including HCV infection.
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Page/Page column 45
(2010/11/03)
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- INSECTICIDAL PYRIMIDINYL ARYL HYRDRAZONES
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Pyrimidinyl aryl hydrazones are effective at controlling insects.
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Page/Page column 6-7
(2009/04/24)
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- Metal-bearing and trifluoromethyl-substituted pyrimidines: Generation and functionalization
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5-Pyrimidyllithium species are fairly stable when the metal is flanked by two electron-withdrawing substituents such as trifluoromethyl and chlorine or bromine. Thus, the corresponding 5-carboxylic acids are produced in high yields from 4,5-dibromo-6-(trifluoromethyl)pyrimidine and 5-bromo-4-chloro-6- (trifluoromethyl)pyrimidine upon halogen/metal permutation accomplished with isopropylmagnesium chloride or butyllithium followed by carboxylation. Satisfactory or excellent yields of 5-carboxylic acids are equally obtained when 4-chloro-, 2,4-dichloro- and 2,4-dibromo-6-(trifluoromethyl)pyrimidine are deprotonated with lithium diisopropylamide before being allowed to react with dry ice. In contrast, consecutive treatment of 2-bromo-4-(trifluoromethyl) pyrimidine and 2-chloro-5-iodo-4-(trifluoromethyl)pyrimidine with butyllithium affords the expected carboxylic acids in only poor yields and not even trace amounts of acid were detected when 4-bromo-6-(trifluoromethyl)pyrimidine served as the substrate. The formation of bipyrimidines, emerging from either one of two competing mechanistic pathways, is a permanently menacing side reaction. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.
- Schlosser, Manfred,Lefebvre, Olivier,Ondi, Levente
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p. 1593 - 1598
(2007/10/03)
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- COMPOUNDS USEFUL AS CHEMOKINE RECEPTOR ANTAGONISTS
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The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.
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Page/Page column 87-88
(2008/06/13)
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- Pyrimidines.9.Chlorination of 6-Trifluoromethyluracil with Phosphorus Oxychloride in the Presence of Trialkylamines
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Ring-chlorination of 6-trifluoromethyluracil in phosphorus oxychloride in the presence of triethyl, tri-n-propyl, and tri-n-butylamines was studied with respect to by-product formation.Comparisons were made with the results obtained by treating the prefor
- Gershon, Herman,Grefig, Anthony T.,Clarke, Donald D
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p. 1243 - 1247
(2007/10/02)
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- Pyrimidines. 7. A Study of the Chlorination of Pyrimidines with Phosphorus Oxychloride in the Presence of N,N-Dimethylaniline
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The chlorination of 6-trifluoromethyluracils by phosphorus oxychloride in the presence of N,N-dimethylaniline was studied and compared with results obtained with 6-methyluracils. 6-Trifluoromethyluracils and its 5-chloro analog afforded moderate yields of the di- and trichloropyrimidines, accompanied by good yields of the 2-N-methylanilino by-products, after a 3-hour reaction time.After 24 hours, the 2-N-methylanilinopyrimidines were the primary or sole products.A small yield of 2,4-bis(N-methylanilino)-6-trifluoromethylpyrimidine was also obtained.The 6-methyluracils afforded high yields of the di- and trichloropyrimidines, after 3 and 24 hours, along with minor amounts of the 2-N-methylanilino by-products.After 48 hours, the proportion of 2,4-dichloro-6-methylpyrimidine decreased, and the 2-N-methylanilino product increased. 2-Chloro-4-methylanilino-6-methylpyrimidine and bis(2-N-methylanilino)-6-methylpyrimidine were also formed in small amounts.The chlorination products from 5-chloro-6-methyluracil remained constant over 188 hours of reaction time. It appears that the Π electron distribution around the ring, as influenced by the substituents, controls the course of the chlorination and by-product formation.Since the amination by a tertiary amine is a type of Hoffmann reaction, the presence of the chlorine in 5 position of the ring adds steric hindrance and thus enhances the regiospecificity of the formation of by-products.
- Gershon, Herman,Grefig, Anthony T.
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p. 1161 - 1167
(2007/10/02)
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