Did You Know...
...that in 1800 ether was first used by partyers as a fun diversion? Sniffing the gas led to hilarious and raucous laughter as people watched each other become more and more intoxicated and silly. Several doctors independently realized the value ether would have to anesthetize surgery patients. Of those who claimed rights to the "discovery," none had a happy ending. One had a seizure and died defending his rights. Another spent his life in an asylum because he had been denied acclaim. A third became addicted to chloroform and, in a New York City jail, he soaked a cloth in the drug, severed an artery and bled to death.
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| Number | Title | Issue Date |
| 7932386 | Preparation of 2-amino-thiazole-5-carboxylic-acid derivatives A method for preparing a compound of the structure I, ... | 04/26/2011 |
| 7855290 | Pyridine derivatives and pyrimidine derivatives (3) A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhi... | 12/21/2010 |
| 7820817 | Modulators of muscarinic receptors The present invention relates to substituted piperazine compounds that are useful modulators of muscarinic receptors. The present invention also provides compositions comprising such compounds, and methods for treating muscarinic receptor mediated diseases. ... | 10/26/2010 |
| 7732601 | Crystalline polymorphs of methanesulfonic acid addition salts of Imatinib This invention relates to the methanesulfonic acid addition salts of Imatinib and to the synthesis thereof. In particular, this invention relates to the synthesis of crystalline α-form of Imatinib methanesulfonate. Furthermore, the invention is directed to a novel ... | 06/08/2010 |
| 7728135 | Synthesis of CCR5 receptor antagonists The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available ... | 06/01/2010 |
| 7589199 | Substituted piperazines Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated... | 09/15/2009 |
| 7550591 | Imatinib production process Provided is a process for producing imatinib and salts thereof, e.g., imatinib mesylate. The process includes reacting 4-(4-methyl-piperazin-1-ylmethyl)-benzoic acid with N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidine-amine in the presence of a carboxylic aci... | 06/23/2009 |
| 7544799 | Crystal modification of a N-phenyl-2-pyrimidineamine derivative, processes for its manufacture and its use The invention relates to a new crystalline form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of formula 1, which may be used for example for tumour therapy. | 06/09/2009 |
| 7534884 | Preparation of pharmaceutical salts In one embodiment, the present invention discloses a process to directly prepare an unequal ratio of rotamers of an acid salt from a basic compound, by creative choice of a solvent medium. The process is particularly useful in preparing specific rotamers of pharmace... | 05/19/2009 |
| 7491821 | Inhibitors of P2X Compounds of formula 1 are modulators of P2X3 useful for the treatment of pain and genitourinary, gastrointestinal, and respiratory disorders: wherein R1 is —C(═S)CH3, pyridyl, pyrimid... | 02/17/2009 |
| 7442698 | Substituted heterocyclic compounds and methods of use The present invention relates to pyrimidine or pyridine carbamate compounds having the general Formula I: and pharmaceutically acceptable salts or derivatives thereof. Also included are methods of treatment of various disea... | 10/28/2008 |
| 7442699 | Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are... | 10/28/2008 |
| 7439371 | Indol kinase inhibitors The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. ... | 10/21/2008 |
| 7435734 | N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are def... | 10/14/2008 |
| 7435814 | 2,4-Pyrimidinediamine compounds and their uses The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a... | 10/14/2008 |
| 7432260 | Pyrimidine compounds The present invention relates to substituted pyrimidines of formula I, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/o... | 10/07/2008 |
| 7423058 | Inhibitors of hepatitis C virus NS3 protease The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of us... | 09/09/2008 |
| 7423039 | (4-phenylpiperazin-1-yl)acylpiperidine derivatives, preparation thereof and application of same in therapeutics The invention relates to substituted (4-phenylpiperazin-1-yl)acylpiperidine derivatives of formula (I) in the form of a base or an addition salt with an acid, and also in the form of a hydrate or solvate, and their preparat... | 09/09/2008 |
| 7420057 | Stable polymorph of flibanserin The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments. ... | 09/02/2008 |
| 7405217 | N-aroyl piperazine derivatives as orexin receptor antagonists This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals. ... | 07/29/2008 |
| 7396830 | Piperazine amidines as antiviral agents This disclosure provides compounds of Formula I as described herein having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with indole and a... | 07/08/2008 |
| 7393845 | Heteroaryl derivates, their preparation and use A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disord... | 07/01/2008 |
| 7390815 | Pyrazole compounds useful as protein kinase inhibitors This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2′, R... | 06/24/2008 |
| 7381719 | Diaryl ethers as opioid receptor antagonist A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3′, E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer o... | 06/03/2008 |
| 7368447 | Capped pyrazinoylguanidine sodium channel blockers The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers. ... | 05/06/2008 |
| 7365074 | Pyridazine, pyrimidine and pyrazine ethyne compounds In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one... | 04/29/2008 |
| 7365069 | Pyrimidone derivatives The present invention relates to novel pyrimidones of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutical... | 04/29/2008 |
| 7365073 | 3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by VLA-4 Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, a... | 04/29/2008 |
| 7361657 | Respiratory syncytial virus replication inhibitors This invention concerns the use of compounds of formula (I) wherein −a1=a2−a3=a4—is a radical of formula —CH═CH—CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—C... | 04/22/2008 |
| 7354924 | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral acti... | 04/08/2008 |
| 7351822 | Serine protease inhibitors Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovasc... | 04/01/2008 |
| 7351828 | Benzimidazoles that are useful in treating sexual dysfunction The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction. ... | 04/01/2008 |
| 7351700 | Aminomethylpyrimidines as allosteric enhancers of the GABA receptors The present invention relates to compounds of formula wherein X is —S— or —NH—; R3/R4 together with the N-atom to which they are attached for... | 04/01/2008 |
| 7342041 | 3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of us... | 03/11/2008 |
| 7335659 | Substituted 10-aryl-11-benzo[]fluorenes and 7-aryl-5, 6-dihydro-benzo[]anthracenes for selective effects on estrogen receptors This invention provides a compound, or its possible salt, having the formula, wherein: Re and ′Re are OH, optionally independently etherified or esterified; Z is —CH2CH2— or... | 02/26/2008 |
| 7329749 | Piperazinylcarbonylquinolines and -isoquinolines Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkins... | 02/12/2008 |
| 7329661 | N-phenyl-3-pyrimidine-amine derivatives The invention relates to N-phenyl-2-pyrimidine-amine derivatives of formula I wherein the substituents are defined as indicated in the description, to processes for the preparation thereof, to medicaments compris... | 02/12/2008 |
| 7326706 | Pyrazine modulators of cannabinoid receptors The present application describes compounds according to Formula I, wherein A, G1, G2 and R1 are described herein. Additionally, the present application describes pharmaceutical compositions comprising at least one compound according... | 02/05/2008 |
| 7326793 | Process for the preparation of diketopyrrolopyrroles The present invention relates to a process for the preparation of diketopyrrolopyrroles of the formula (I), wherein A1, A2, A3 and A4 are as defined in the description of the present invention, to new diketopyrrolopyrroles of the general formula I obtainable by the ... | 02/05/2008 |
| 7323464 | Pyridine and pyrimidine derivatives Compounds of formula (1) are described in which Ra and Rb is each independently a hydrogen atom or a group Rc, or Ra and Rb together form an oxo (═O) or thio (═S) group; X is a N atom or an optionally substi... | 01/29/2008 |
