- TREATMENT OF RESPIRATORY DISEASES WITH AMINO ACID COMPOUNDS
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The invention relates to methods of therapy using compounds of formula (I) and formula (II): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (II) and pharmaceutical compositions thereof are integrin inhibitors that are useful in therapy for a condition, for example, caused by or associated with an infectious agent, shock, pancreatitis, or trauma. The condition can include one or more of pulmonary fibrosis associated with rheumatoid arthritis or progressive familial intrahepatic cholestasis (PFIC).
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Paragraph 0268
(2021/11/13)
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- DOSAGE FORMS AND REGIMENS FOR AMINO ACID COMPOUNDS
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The invention relates to dosage forms for daily administration of compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are ανβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP),
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Paragraph 00364
(2020/10/21)
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- AMINO ACID COMPOUNDS AND METHODS OF USE
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The invention relates to compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
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Paragraph 0660; 0661
(2019/09/20)
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- 1-HETEROARYL-INDOLINE-4-CARBOXAMIDES AS MODULATORS OF GPR52 USEFUL FOR THE TREATMENT OR PREVENTION OF DISORDERS RELATED THERETO
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The present invention relates to compounds of Formula (la) and pharmaceutical compositions thereof that modulate the activity of GPR52. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a GPR52-mediated disorder (e.g., Huntington's disease, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder (ADHD), or Tourette's syndrome); an extrapyramidal or movement disorder; a motor disorder; a hyperkinetic movement disorder; a psychotic disorder; catatonia; a mood disorder; a depressive disorder; an anxiety disorder; obsessive-compulsive disorder (OCD); an autism spectrum disorder; a prolactin-related disorder (e.g., hyperprolactinemia); a neurocognitive disorder; a trauma- or stressor-related disorder (e.g., posttraumatic stress disorder (PTSD)); a disruptive, impulse-control, or conduct disorder; a sleep-wake disorder; a substance-related disorder; an addictive disorder; a behavioral disorder; hypofrontality; an abnormality in the tuberoinfundibular, mesolimbic, mesocortical, or nigrostriatal pathway; decreased activity in the striatum; cortical dysfunction; neurocognitive dysfunction; and conditions related thereto.
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Page/Page column 91
(2016/11/17)
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- PROCESSES FOR THE PREPARATION OF (R)-2-ACETAMIDO-N-BENZYL-3-METHOXYPROPIONAMIDE AND INTERMEDIATES THEREOF
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This invention relates to processes for the preparation of (R)-2- acetamido-/V-benzyl-3-methoxypropionamide (I) and intermediates thereof. Formula (I).
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Page/Page column 17
(2013/03/28)
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- PROCESS FOR THE PREPARATION OF LACOSAMIDE
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The present invention relates to an improved process for the preparation of Lacosamide of Formula (I), comprising: O-methylating a compound of Formula (V) or a compound of Formula (XX) or a compound of Formula XXII; in the presence of a methylating agent and a base to produce Lacosamide of Formula (I).
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Paragraph 0121
(2013/05/22)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF LACOSAMIDE
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The present invention relates to an improved process for the preparation of Lacosamide of Formula (I), comprising: O-methylating a compound of Formula (V) or a compound of Formula (XX) or a compound of Formula XXII; in the presence of a methylating agent and a base to produce Lacosamide of Formula (I).
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Page/Page column 28
(2011/12/04)
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- SUBSTITUTED PYRAZOLE AND TRIAZOLE COMPOUNDS AS KSP INHIBITORS
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Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof
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Page/Page column 59
(2008/12/05)
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- Synthesis and pharmacological evaluation of novel γ-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors
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We have previously demonstrated that the prototypical GABAB receptor agonist baclofen inhibits transient lower esophageal sphincter relaxations (TLESRs), the most important mechanism for gastroesophageal reflux. Thus, GABAB agonists could be exploited for the treatment of gastroesophageal reflux disease. However, baclofen, which is used as an antispastic agent, and other previously known GABAB agonists can produce CNS side effects such as sedation, dizziness, nausea, and vomiting at higher doses. We now report the discovery of atypical GABAB agonists devoid of classical GABAB agonist related CNS side effects at therapeutic doses and the optimization of this type of compound for inhibition of TLESRs, which has resulted in a candidate drug (R)-7 (AZD3355) that is presently being evaluated in man.
- Alstermark, Christer,Amin, Kosrat,Dinn, Sean R.,Elebring, Thomas,Fjellstr?m, Ola,Fitzpatrick, Kevin,Geiss, William B.,Gottfries, Johan,Guzzo, Peter R.,Harding, James P.,Holmén, Anders,Kothare, Mohit,Lehmann, Anders,Mattsson, Jan P.,Nilsson, Karolina,Sundén, Gunnel,Swanson, Marianne,Von Unge, Sverker,Woo, Alex M.,Wyle, Michael J.,Zheng, Xiaozhang
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supporting information; scheme or table
p. 4315 - 4320
(2009/05/30)
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- Substituted imidazole compounds as KSP inhibitors
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The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses of the compounds. The compounds of the invention have the following general formula:
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Page/Page column 27
(2008/06/13)
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- Aziridinium from N,N-dibenzyl serine methyl ester: Synthesis of enantiomerically pure β-amino and α,β-diamino esters
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Reaction of N,N-dibenzyl-O-methylsulfonyl serine methyl ester with a variety of heteronucleophiles (sodium azide, sodium phthalimide, amines, thiols) and carbanions (sodium malonate) gave, via an aziridinium intermediate, the corresponding β-amino or α,β-
- Couturier, Cedric,Blanchet, Jerome,Schlama, Thierry,Zhu, Jieping
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p. 2183 - 2186
(2007/10/03)
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- A flexible and efficient synthesis of the pyrrolidine α-glycosidase inhibitor 1,4-dideoxy-1,4-imino-D-arabinitol (DAB-1)
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The synthesis of the pyrrolidine α-glycosidase inhibitor 1,4-dideoxy-1,4-imino-D-arabinitol (DAB-1) was discussed. The synthesis used serine-derived α-dibenzylamino aldehyde in a highly diastereoselective glycolate aldol reaction. The glycolate derivative of Evans' oxazolidinone compound was found to be prepared using benzyl-oxyacetyl chloride and 4-benzyloxazolidin-2-one. The analysis showed that the deprotection of the N-benzyl protecting groups was completed within the first 2-3 h of the reaction.
- Hulme, Alison N.,Montgomery, Charles H.,Henderson, David K.
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p. 1837 - 1841
(2007/10/03)
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- Total synthesis of the cyclopeptide alkaloid sanjoinine G1 and its C-11 epimer
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The naturally occurring cyclopeptide alkaloid sanjoinine G1 and its C- 11 epimer were synthesized in 18 steps from D-serine. The key steps in the synthesis were the formation of the alkylaryl ether linkage via an S(N)Ar reaction with 4-fluorobenzonitrile
- East, Stephen P.,Shao, Feng,Williams, Lorenzo,Joullie, Madeleine M.
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p. 13371 - 13390
(2007/10/03)
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