Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I)

wherein the groups R¹ to R⁵, A₁ and A₂ have the meanings given in the claims and in the description, particularly the preparation of 7,8-dihydro-5H-pteridin-6-one derivatives and intermediates ...
]]> RE43115 http://www.patentstorm.us/patents/8110683/description.html

The invention is directed to piperidinyl compounds that selectively bind integrin receptors and methods for treating an integrin mediated ...
]]> 8110683 http://www.patentstorm.us/patents/8110682/description.html

Disclosed are compounds of the formula I

or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof,

wherein

• • A is a bond, —C(O)—, or —C(R^3′)(R^4′)—;
  • X is —N(R¹)— or —C(R⁶)(R⁷)—;
  • Y is —S(O)₂—, —C(═O)—, —PO(OR⁹) or ...
    ]]> 8110682 http://www.patentstorm.us/patents/8110681/description.html
  • Patent Number:  8110681
  • Publication Date:  2012-02-07
  • Inventors:  McCall, John M.; Johnson, Graham; Heemskerk, Jill; Fairfax, David; Barnes, Keith D.; Johnson, Matthew Robert

  Compounds of Formula (I) or (II) useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or ...
  ]]> 8110681 http://www.patentstorm.us/patents/8106197/description.html

• Patent Number:  8106197
• Publication Date:  2012-01-31
• Inventors:  Botrous, Iriny; Cui, Jingrong Jean; Bhumralkar, Dilip; Lin, Jason (Qishen); Nelson, Christopher G.; Jia, Lei; Hanau, Cathleen Elizabeth; Kolodziej, Stephen A.; Funk, Lee A.; Harris, G. Davis; Johnson, Joanne; Pairish, Mason Alan; Shen, Hong; Tran-Dube, Michelle; Zhang, Fang-Jie; Zhang, Jennifer; Kung, Pei-Pei; Chu, Ji Yu; Li, Xiaoyuan (Sharon); Meng, Jerry Jialun; Nambu, Mitchell David; Walter, Allison

Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided. Preferred compounds of formula 1 have activity as protein kinase inhibitors, including as inhibitors of ...
]]> 8106197 http://www.patentstorm.us/patents/8106196/description.html

The present invention relates to compounds of the formula (I) or pharmaceutically acceptable salts or hydrates thereof. The present invention further relates to processes for the preparation of the compounds of formula (I) and optical isomers and to use of the compounds of formula (I), isomers, pharmaceutically acceptable salts or hydrates thereof as medicaments, in particular as medicaments for the treatment and prevention of Hepatitis ...
]]> 8106196 http://www.patentstorm.us/patents/8106195/description.html

There are disclosed urethane acrylates of Formula 1:

where R^1a, R^1b and R^1c each independently represent C_2-15hydrocarbylene, preferably linear C_3-12alkylene (such as, C_4-8alkylene; e.g. hexylene); a isophorone unit and/or a tolyl unit. R^2a, R^2b and R^2c each independently represent: a divalent moiety ...
]]> 8106195 http://www.patentstorm.us/patents/8106194/description.html

An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, ...
]]> 8106194 http://www.patentstorm.us/patents/8106193/description.html

There is described novel organo-platinum luminophores comprising a complex of formula (I). The luminophores have application as the emissive component in organic light emitting ...
]]> 8106193 http://www.patentstorm.us/patents/8106192/description.html

The invention relates to a method for producing 5-chloro-N-({5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide starting from 5-chlorothiophene-2-carbonyl chloride, (2S)-3-amino-propane-1,2-diol and ...
]]> 8106192 http://www.patentstorm.us/patents/8106191/description.html

New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula

M-L-Q

where M is a synthetic ligand for an FKBP ...
]]> 8106191 http://www.patentstorm.us/patents/8106190/description.html

To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation.

The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an ...
]]> 8106190 http://www.patentstorm.us/patents/8101755/description.html

An organometallic complex is provided by which favorable red-color light emission can be obtained. Further, an organometallic complex having a peak of light emission at about 620 nm is provided because the wavelength of light which is perceived as excellent red-color light is about 620 nm. Furthermore, an organometallic complex is provided by which red-color light emission with high luminous efficiency (cd/A) can be obtained. An organometallic complex represented by the following general ...
]]> 8101755 http://www.patentstorm.us/patents/8101754/description.html

The invention relates to compounds of the formula I:

wherein

• n is 1 or 2,
• Ar is a C-bound 1,2,4-triazol radical which carries a radical R¹ on the remaining carbon atom and a radical R^1a on one of the nitrogen atoms;
• R¹ is hydrogen, C₁-C₆ alkyl, C₃-C₆ cycloalkyl, C₁-C₄ alkoxymethyl, fluorinated ...
  ]]> 8101754 http://www.patentstorm.us/patents/8101753/description.html
• Patent Number:  8101753
• Publication Date:  2012-01-24
• Inventor:  Mizuno, Hajime

4-amino-6-alkynyloxypyrimidine compounds shown by the formula (V)

• which has a controlling activity against pests can be produced by the method which comprises
• the first step which produces a 4-fluoro-6-alkynyloxypyrimidine compound shown by the formula (I)

• by making a 4,6-difluoropyrimidine compound shown by the formula (II) react with an alcohol compound shown by the formula ...
  ]]> 8101753 http://www.patentstorm.us/patents/8101752/description.html
• Patent Number:  8101752
• Publication Date:  2012-01-24
• Inventors:  Schils, Didier Philippe Robert; Stappers, Alfred Elisabeth

This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot ...
]]> 8101752 http://www.patentstorm.us/patents/8101751/description.html

Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to ...
]]> 8101751 http://www.patentstorm.us/patents/8101750/description.html

The present invention relates to a new process for the manufacture of the compound 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile as a free base and pharmaceutically acceptable salts thereof, particularly the 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile citrate, and to new intermediates prepared in said process suitable for large scale manufacturing of said ...
]]> 8101750 http://www.patentstorm.us/patents/8101749/description.html

The invention relates to a method for producing onium salts with tetrafluoroborate anion by reacting an onium halide with an oxonium tetrafluoroborate, sulfonium tetrafluoroborate, or triphenylcarbonium ...
]]> 8101749 http://www.patentstorm.us/patents/8097724/description.html

A process for the preparation of a compound of formula (I) such as 2(R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]-7(8H)-pyrazinyl]-1-(2,4,5-trifluorophenyl)-2-butanamine, or a salt thereof, in the anhydrous or hydrated form, either as a mixture of enantiomers, or as a single (R) or (S) enantiomer,

comprising the conversion of a compound of formula (II), or a salt thereof, either as a single (R) or (S) enantiomer or as a mixture ...
]]> 8097724 http://www.patentstorm.us/patents/8097723/description.html

Process for the preparation of abacavir, or its salts or its solvates comprising the step of reacting a compound (IV) where R₁ is a (C₁-C₄)-alkyl radical with anhydrous hydrochloric acid/(C₁-C₆)-alcohol, and then with tri(C₁-C₄)-alkyl orthoformate, in the absence of water. The preparation process may include further steps of reacting the compound obtained with cyclopropylamine and subsequently hydrolysis to yield ...
]]> 8097723 http://www.patentstorm.us/patents/8097722/description.html

Inhibitors of the enzyme prenylated methylated protein methyl esterase (PMPMEase), the last step in the prenylation process for many eukaryotic proteins, having the general structure R₁-X-A-B(R₂)-Y or R₁-X-A(R₂)-B-Y, where R₁ is preferably a polyisoprenyl group, X is a linking group, Y is a group that promotes affinity interactions to the active site of PMPMEase and imparts hydrolysis resistance to the inhibitor, A and B are bridge ...
]]> 8097722