- THERAPEUTIC INHIBITORY COMPOUNDS
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Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds which are complement factor D inhibitors. Such compounds are useful for treating complement related disorders including, but are not limited to, autoimmune, inflammatory, and neurodegenerative diseases.
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Paragraph 00276
(2017/07/04)
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- Heterocyclic core analogs of a direct thrombin inhibitor
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Thrombin is a serine protease that plays a key role in blood clotting. Pyrrolidine 1 is a potent thrombin inhibitor discovered at Merck several years ago. Seven analogs (2-8) of 1 in which the pyrrolidine core was replaced with various heterocycles were p
- Blizzard, Timothy A.,Singh, Sanjay,Patil, Basanagoud,Chidurala, Naresh,Komanduri, Venukrishnan,Debnath, Samarpita,Belyakov, Sergei,Crespo, Alejandro,Struck, Alice,Kurtz, Marc,Wiltsie, Judyann,Shen, Xun,Sonatore, Lisa,Arocho, Marta,Lewis, Dale,Ogletree, Martin,Biftu, Tesfaye
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p. 1111 - 1115
(2014/03/21)
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- THROMBIN INHIBITORS
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Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein Q is CH2, NR4, O, S, S(O) or S(O2
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Page/Page column 29; 30
(2013/10/21)
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- SATURATED BICYCLIC HETEROCYCLIC DERIVATIVES AS SMO ANTAGONISTS
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The present invention relates to compounds of formula I: and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smoantagonists. Thus the compounds of this invention are useful for the treatment of diseases associated with abnormal hedgehog pathway activation, including cancer, for example basal cell carcinoma, medulloblastoma, prostate, pancreatic, breast, colon, bone and small cell lung cancers, and cancers of the upper GI tract.
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Page/Page column 41
(2010/04/06)
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- Disubstituted pyrimidines as Lck inhibitors
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We have developed a family of 4-benzimidazolyl-N-piperazinethyl-pyrimidin-2-amines that are subnanomolar inhibitors of Lck. A subset of these Lck inhibitors, with heterocyclic substituents at the benzimidazole C5, are also low-nanomolar inhibitors of cell
- Hunt, Julianne A.,Beresis, Richard T.,Goulet, Joung L.,Holmes, Mark A.,Hong, Xinfang J.,Kovacs, Ernest,Mills, Sander G.,Ruzek, Rowena D.,Wong, Frederick,Hermes, Jeffrey D.,Park, Young-Whan,Salowe, Scott P.,Sonatore, Lisa M.,Wu, Lin,Woods, Andrea,Zaller, Dennis M.,Sinclair, Peter J.
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supporting information; scheme or table
p. 5440 - 5443
(2010/04/26)
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- QUINOLINE DERIVATIVES AS ANTIBACTERIALS
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The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt and/or N-oxide thereof: corresponding novel medicaments, pharmaceutical compositions and/or methods of
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- HYDROXAMIC ACID DERIVATIVES
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Novel hydroxamic acid derivatives, e.g., of formula (I), wherein R1, R2, R3 and R4 are as defined, are found to be useful as pharmaceuticals, e.g., for the suppression of TNF release and the treatment of autoimm
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Page/Page column 31
(2008/06/13)
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- HIV protease inhibitors useful for the treatment of AIDS
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Compounds of formula STR1 where R1 and R2 are independently hydrogen or optionally-substituted C1-4 alkyl or aryl, or R1 and R2 are joined together to form a monocyclic or bicyclic ring system, are HIV protease inhibitors. These compounds are useful in the treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of treating infection by HIV are also described.
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- L-735,524: The design of a potent and orally bioavailable HIV protease inhibitor
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A series of HIV protease inhibitors possessing a hydroxylaminepentanamide transition state isostere have been developed. Incorporation of a basic amine into the backbone of the L-685,434 (2) series provided antiviral potency combined with a highly improved pharmacokinetic profile in animal models. Guided by molecular modeling and an X-ray crystal structure of the inhibited enzyme complex, we were able to design L-735,524. This compound is potent and competitively inhibits HIV-1 PR and HIV-2 PR with K(i) values of 0.52 and 3.3 nM, respectively. It also stops the spread of the HIV-1(IIIb)-infected MT4 lymphoid cells at concentrations of 25-50 nM. To date, numerous HIV-PR inhibitors have been reported, but few have been studied in humans because they lack acceptable oral bioavailability. L-735,524 is orally bioavailable in three animals models, using clinically acceptable formulations, and is currently in phase II human clinical trials.
- Dorsey,Levin,McDaniel,Vacca,Guare,Darke,Zugay,Emini,Schleif,Quintero,Lin,Chen -,Holloway,Fitzgerald,Axel,Ostovic,Anderson,Huff
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p. 3443 - 3451
(2007/10/02)
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