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Solvents for NMR spectroscopy (Wed, 05 May 1976)
Organic solvents containing less than 0.2 atom percent of .sup.13 C and which preferably are at least partially deuterated are produced from .sup.13 C-depleted gaseous carbon compounds and are advantageously employed as solvents for .sup.13 C NMR spectroscopy.
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CRYSTALLINE ROXIFIBAN (Thu, 24 Feb 2000)
The potent platelet glycoprotein lib/Ilia antagonist, roxifiban, is produced in crystalline form. Crystalline roxifiban exists in two polymorphic forms, designated Form 1 and Form 2. These polymorphic forms are characterized by x-ray powder diffraction and solid-state carbon NMR. Pharmaceutical compositions and methods for the treatment or prevention of diseases mediated by platelet aggregation are described.
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Solvents for NMR spectroscopy (Wed, 01 Jun 1977)
Organic solvents containing less than 0.2 atom percent of .sup.13 C and which preferably are at least partially deuterated are produced from .sup.13 C-depleted gaseous carbon compounds and are advantageously employed as solvents for .sup.13 C NMR spectroscopy.
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SILICON CARBONACEOUS FILM FORMING COMPOSITION COMPRISING POLYCARBOSILANE AND METHOD FOR MANUFACTURING SILICON CARBONACEOUS FILM USING THE SAME (Fri, 15 Feb 2019)
[Problem]To provide a composition comprising polycarbosilane, which has excellent filling property, can form a film at a lower temperature, and makes electrical property of the produced film excellent. [Means for Solution] A silicon carbonaceous film forming composition comprising polycarbosilane and a solvent, wherein the ratio of the integrated intensity at 3.92 to 4.20 ppm to the integrated intensity at3.60 to 5.50 ppm in the H-NMR spectrum of said polycarbosilane is 27 to 50%.
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CRYSTALLINE ROXIFIBAN (Thu, 24 Dec 1998)
The potent platelet glycoprotein IIb/IIIa antagonist, roxifiban, is produced in crystalline form. Crystalline roxifiban exists in two polymorphic forms, designated Form 1 and Form 2. These polymorphic forms are characterized by x-ray powder diffraction and solid-state carbon NMR. Pharmaceutical compositions and methods for the treatment or prevention of diseases mediated by platelet aggregation are described.
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Crystalline roxifiban (Thu, 13 Jul 2000)
The potent platelet glycoprotein IIb/IIIa antagonist, roxifiban, is produced in crystalline form. Crystalline roxifiban exists in two polymorphic forms, designated Form 1 and Form 2. These polymorphic forms are characterized by x-ray powder diffraction and solid-state carbon NMR. Pharmaceutical compositions and methods for the treatment or prevention of diseases mediated by platelet aggregation are described.
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TRANSPARENT NMR SHIFT REAGENTS (Wed, 19 Jun 1974)
Rare earth metal chelates of beta -diketones that are deuterated or deuterated plus halogenated and contain no more than 5 hydrogen atoms in the diketone moiety are described. The novel chelates are useful NMR shift reagents particularly because they not only solubilize the rare earth metal but additionally the beta -diketone ligand is substantially to completely transparent to proton NMR analysis. The chelates are prepared by reacting the rare earth metal nitrate with the beta -diketones by conventional methods.
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FORMATION OF TETRA-SUBSTITUTED ENAMIDES AND STEREOSELECTIVE REDUCTION THEREOF (Fri, 17 Feb 2006)
The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I). (see formula V) (see formula III) (see formula IV) (see formula II) (see formula I)
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Cholecystokinin antagonists (Wed, 24 Jul 1985)
The compound having Formula I and several minor related compounds are produced by the aerobic fermentation of Aspergillus alliaceus Thom and Church, ATCC No. 20655 or ATCC No. 20656. ##STR1## The compound of Formula I and the several minor related compounds are antagonists of cholecystokinin (CCK). CCK antagonists are useful in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems of animals, especially humans.
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Crystal forms of a HCV protease inhibitor (Fri, 21 Feb 2014)
The present invention relates to different forms of a HCV inhibitory compound.
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Sterol inhibitors of testosterone 5-alpha-reductase. (Thu, 10 May 1990)
The compounds of Formula I are produced by the aerobic fermentation of a fungus of the genus GLIOCLADIUM, ATCC No. 20826. The compounds of Formula I are inhibitors of testosterone 5 alpha -reductase and are useful in the treatment and prevention of acne, seborrhea, female hirsutism and benign prostatic hypertrophy.
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Compounds and methods for leukotriene biosynthesis inhibition (Fri, 03 Apr 2009)
This invention provides novel salt and crystalline forms thereof of (−)4-(4-fluorophenyl)-7-[({5-[1-hydroxy-1-(trifluoromethyl)propyl]-1,3,4-oxadiazol-2-yl}amino)-methyl]-2H-chromen-2-one. The compounds are 5-LO inhibitors and are useful for treatment of conditions such as asthma, allergic rhinitis, COPD, and atherosclerosis.
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OXYTOCIN AND VASOPRESSIN ANTAGONISTS (Thu, 25 Feb 1988)
Cyclic peptides having the formula: are produced by the controlled aerobic fermentation of Streptomyces silvensis, ATCC No. 53525 or ATCC No. 53526. These compounds are antagonists of oxytocin and are useful in the treatment of preterm labor and vasopressin and are thus useful in the treatment and prevention of disease states wherein vasopressin may be involved, for example congestive heart failure, hypertension, edema and hyponatremia.
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Oxytocin and vasopressin antagonists. (Thu, 17 Aug 1989)
Cyclic peptides are produced by the controlled aerobic fermentation of Streptomyces silvensis, ATCC No. 53525 or ATCC No. 53526. These compounds are antagonists of oxytocin and are useful in the treatment of preterm labor and vasopressin and are thus useful in the treatment and prevention of disease states wherein vasopressin may be involved, for example congestive heart failure, hypertension, edema and hyponatremia.
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PHARMACEUTICALLY ACTIVE HETEROCYCLIC COMPOUNDS CONTAINING AT LEAST FOUR RING-NITROGEN ATOMS, THEIR PREPARATION AND FERMENTATION BROTHS OF ASPERGILLUS ALLIACEUS ATCC 20655 AND 20656 (Thu, 23 Aug 1984)

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PROCESS FOR SYNTHESIZING A CETP INHIBITOR (Thu, 18 Feb 2016)
An efficient process is disclosed for producing a compound that is an inhibitor of CETP. The last step of the process is the coupling of an oxazolidinone derivative with a biphenyl moiety to provide a compound of formula I. In a specific embodiment of this synthesis, a crystalline product is produced which is characterized as a non-solvated crystalline polymorph.
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Sterol inhibitors of testosterone 5.alpha.-reductase (Wed, 22 Mar 1989)
The compounds of Formula I are produced by the aerobic fermentation of a fungus of the genus GLIOCLADIUM, ATCC No. 20826. ##STR1## The compounds of Formula I are inhibitors of testosterone 5.alpha.-reductase and are useful in the treatment and prevention of acne, seborrhea, female hirsutism and benign prostatic hypertrophy.
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Fermentation analogs of virginiamycin M1 (Wed, 10 Aug 1988)
Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III, and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527, while the analog of Formula II is produced by chemical synthesis.
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CHROMENONE DERIVATIVES AND THEIR USE FOR LEUKOTRIENE BIOSYNTHESIS INHIBITION (Fri, 03 Apr 2009)
This invention provides novel salt and crystalline forms thereof of (-) 4-(4- fluorophenyl)-7-[({5-[1-hydroxy-1-(tri- fluoromethyl)propyl]-1,3,4-oxadiazol-2-yl}-amino)-methyl]-2H-chromen-2-one. The compounds are 5-LO inhibitors and are useful for treatment of conditions such as asthma, allergic rhinitis, COPD, and atherosclerosis.
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Chromenone derivatives and their use for leukotriene biosynthesis inhibition (Fri, 02 Apr 2010)
This invention provides novel salt and crystalline forms thereof of (-) 4-(4-fluorophenyl)-7-[({5-[1-hydroxy-1-(trifluoromethyl)propyl]-1,3,4-oxadiazol-2-yl}-amino)-methyl]-2H-chromen-2-one. The compounds are 5-LO inhibitors and are useful for treatment of conditions such as asthma, allergic rhinitis, COPD, and atherosclerosis.
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CHOLESTEROL LOWERING AGENTS AND ANTIFUNGAL AGENTS (Thu, 24 Sep 1992)
This invention relates to compounds of formula (I) which are useful as antifungal agents and cholesterol-lowering agents.
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Process for producing N-amino-1-hydroxy-alkylidene-1,1-bisphosphonic acids (Wed, 24 Apr 1996)
A process for continuously producing alkylpyrophosphonate, alkylpyrophosphate and multimers thereof and for producing 4-amino-1-hydroxyalkylidene-1,1-bisphosphonic acids or salts thereof.
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POLYMORPHIC FORM OF MONTELUKAST SODIUM (Fri, 29 Oct 2004)
The invention provides novel polymorphic form of montelukast sodium, as well as methods of using and pharmaceutical compositions containing saud novel form. Also provided are montelukast sodium: acetonitrile solvates, which are intermediates in the formation of crystalline montelukast sodium.
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Process for synthesizing a CETP inhibitor (Fri, 11 Jan 2008)
An efficient process is disclosed for producing a compound that is an inhibitor of CETP. The last step of the process is the coupling of an oxazolidinone derivative with a biphenyl moiety to provide a compound of formula (I). In a specific embodiment of this synthesis, a crystalline product is produced which is characterized as a non-solvated crystalline polymorph.
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DIFFICIDIN AND DERIVATIVE ANTIBACTERIALS (Thu, 20 Dec 1984)

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Dopamine .beta.-hydroxylase inhibitors (Wed, 12 Dec 1984)
Two fermentation isolates, C.sub.7 H.sub.9 NO.sub.4 and C.sub.6 H.sub.7 NO.sub.3, presumably trihydroxy, methyl-pyridine derivatives, are inhibitors of dopamine .beta.-hydroxylase. These natural product compounds are produced by fermentation of Streptoverticillium hiroshimense and each may prove useful as antihypertensive agents.
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Antihypercholesterolemics. (Thu, 10 Oct 1991)
This invention relates to compounds of structural formula (I): which are useful for treating hypercholesterolemia and inhibiting fungal growth.
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PROCESS FOR SYNTHESIZING A CETP INHIBITOR (Fri, 12 Jan 2007)
An efficient process is disclosed for producing a compound that is an inhibitor of CETP. The last step of the process is the coupling of an oxazolidinone derivative with a biphenyl moiety to provide a compound of formula (I). In a specific embodiment of this synthesis, a crystalline product is produced which is characterized as a non-solvated crystalline polymorph.
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Polymorphs of an androgen receptor modulator (Fri, 08 Jun 2007)
Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
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Antifungal substances (Thu, 20 Jul 1989)
A series of macrolides is isolated from the fermentation broth of a microorganism identified as MA-5000 which morphological analysis reveals to be a strain of Streptomyces hygroscopicus. The compounds have antifungal activity and are thought to have the structure:- wherein R3 is a phosphate group and either R<2> is NH3 and R1 is H or R<2> is OH and R1 is
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