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NMR-APPARATUS COMPRISING AN ADJUSTING ELEMENT FOR MATCHING PURPOSES OR FOR ADJUSTING THE RESONATOR TUNING (Fri, 02 Jun 1989)

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PROCESS FOR PREPARING 5-SUBSTITUTED-3-FURALDEHYDES (Wed, 29 May 1991)
This process for preparing 5-substituted-3-furaldehydes of the formula:. in which E is an electrophilic group, comprises reacting 3-furaldehyde with: (1) lithium morpholide, followed by (2) secondary-butyl lithium, followed by (3) an electrophile. Also included are compounds prepared by the above process.
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N-SUBSTITUTED DERIVATIVES OF 3R, 4R-ETHYL-[(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-2-PYRROLIDINONE (Fri, 27 Mar 1992)
The invention relates to racemic and optically active compounds of the following formula and pharmaceutical compositions thereof; wherein R is a substituted or unsubstituted hydrocarbon group.
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Substituted aryl or heteroarylamides having retinoid-like biological activity (Fri, 29 Oct 1999)
These compounds have the formula (1) wherein X is CH or N; R1 is independently H or alkyl of 1 to 6 carbons; m is 0-5; p is 0-2; r is 0-2; L is -(C=Z)-NH- or -NH-(C=Z)- where Z is O or S; Y is an optionally substituted phenyl, naphthyl, pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, imidazolyl or pyrrazolyl; W is independently F, Br, Cl, I, alkyl, fluoro-alkyl, NO2, N3, OH, OCH2OCH3, O-alkyl, tetrazolyl, CN, SO2-alkyl, SO2-fluoroalkyl, SO-alkyl, CO-alkyl, COOR8 or optionally substituted phenyl; A is (CH2)q where q is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds or alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9R10, -CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, -COR7, CR7(OR12)2, or CR7OR13O and where the remaining substituents are defined in the claims; provided that when r is 0 or when Y is phenyl and (W)r is OH then p is not 0 and at least one W in the ring having the X group is not alkyl, OH or Oalkyl...
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Unsubstituted and substituted 4-benzyl-1,3-dihydro-imidazole-2-thiones acting as specific or selective alpha2 adrenergic agonists and methods for using the same (Sat, 27 Nov 2010)
Patent 553566 Disclosed is the use of benzyl substituted 1,3-dihydro-imidazole-2-thione compounds of formula (I), where n is 1 or 2 and R1 is F, Cl, Br or I, for the manufacture of a medicament for the treatment of pain. The pain could be chronic pain, visceral pain, neuropathic pain or corneal pain. Also disclosed are compounds 1-5 as shown and a pharmaceutical composition of compounds 1-5.
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4-(phenylmethyl and substituted phenylmethyl)-imidazole-2-thiones acting as specific alpha2 adrenergic agonists (Sat, 27 Nov 2010)
Patent 553341 Disclosed are 4-(phenylmethyl and substituted phenylmethyl)-imidazole-2-thiones compounds of formula (I) where the variables are disclosed in the specification. Also disclosed is the pharmaceutical composition and use of the compounds for the manufacture of a medicament to treat chronic pain, visceral pain, neuropathic pain, corneal pain, glaucoma, elevated intraocular pressure, ischemic neuropathies, neurodegenerative diseases, diarrhea, nasal congestion, muscle spasticity, diuresis, withdrawal syndromes, neurodegenerative diseases, optic neuropathy, spinal ischemia, stroke, memory and cognition deficits, attention deficit disorder, psychoses, manic disorders, anxiety, depression, hypertension, congestive heart failure, cardiac ischemia, arthritis, spondylitis, gouty arthritis, osteoarthritis, juvenile arthritis, autoimmune diseases, lupus erythematosus, chronic gastrointestinal inflammations, Crohn���s disease, gastritis, irritable bowel syndrome (IBS), functional dyspepsia and ulcerative colitis...
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6- OR 7- (2-IMINO-2-IMIDAZOLIDINE)-1,4-BENZOXAZINES AS ALPHA ADRENERGIC AGENTS (Fri, 25 Feb 1994)
These compounds, which are useful as alpha-adrenergic agents, are of the formula: where each R1 is H or C1-6 alkyl; each R2 is H or C1-6 alkyl or the two R2 groups may jointly represent a carbonyl oxygen; R3 is H, C1-6 alkyl, O, OH or OR7 where R7 is C1-6 alkyl or R3 is COH or COR8 where R8 is C1-6 alkyl; R4 and R5 independently are H, Br, Cl, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl with the proviso that when the R2 groups are a carbonyl oxygen or H then R4 and R5 cannot be H; and R6 is H, Br, Cl, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, and the R5 and the (2-imidazoline-2-yl) amino substituents are connected mutually exclusively to the 6 and 7 positions of the 1,4 benzoxazine nucleus.
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Indole-3-carboxylic acid amide, ester, thioamide and thiol ester compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate (s1p) receptor antagonist biological activity (Sat, 01 Oct 2011)
Patent 570528 The disclosure relates to substituted indole-3-carboxylic acid derivatives represented by the formula shown herein, which may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y are as defined in the specification. These compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis, cardiovascular conditions and diseases, and wound healing.
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4-(condensed cyclicmethyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists (Sat, 27 Nov 2010)
Patent 553290 Disclosed are imidazole-2-thione derivatives as represented by the general formula I, where R1 is independently H, alkyl, CH2OR2, or fluoro substituted alkyl; R2 is independently H, alkyl, C(O)R7, carbocyclic aryl or heterocyclic aryl having 1 to 3 heteroatoms independently selected from N, O and S; R3 is independently selected from the groups consisting of alkyl, alkenyl, alkynyl, CH2OR2, CH2N(R2)2, CH2CN, C(O)R2, C(O)OR6, SO3R6, SO2N(R2)2, CH2SR2, F, Cl, Br, I, fluoro substituted alkyl, CN, N3, NO2, N(R2)2, OR2 or SR2; p is an integer having the values of 0-3; R4 and R5 together with the carbons to which they are attached jointly form a carbocyclic or a heterocyclic ring, the heterocyclic ring having 5 or 6 atoms in the ring and 1 to 3 heteroatoms independently selected from N, O and S; said carbocyclic or heterocyclic ring jointly formed by R4 and R5 being optionally substituted with 1 to 7 R8 groups; R6 is independently H, alkyl, carbocyclic aryl or heterocyclic aryl having 1 to 3 heteroatoms independently selected from N, O and S; R7 is H or alkyl, and R8 is independently selected from the groups consisting of alkyl, alkenyl, alkynyl, CH2OR2, CH2N(R2)2, CH2CN, C(O)R2, C(O)OR6, SO3R6, SO2N(R2)2, CH2SR2, F, Cl, Br, I, fluoro substituted alkyl, CN, N3, NO2, N(R2)2, OR2, SR2 or R8 is O or S double bonded to one carbon of said carbocyclic or heterocyclic ring...
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3-aryl-3-hydroxy-2-amino-propionic acid amides, 3-heteroayryl-3-hydroxy-2-amino-propionic acid amides and related compounds having analgesic and/or immunostimulant activity (Sat, 30 Oct 2010)
Patent 556614 Disclosed are 3-aryl-3-hydroxy-2-amino-propionic acid amides and 3-heteroaryl-3-hydroxy-2-amino-propionic acid amides wherein the substituents are as defined in the specification and their use as analgesic or immuno stimulants.
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Substituted thiazole sulfonamides as antiglaucoma agents (Wed, 22 May 1996)
The present invention provides novel carbonic anhydrase inhibitors represented by the structural formula: ##STR1## wherein
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Pharmaceutical compositions and method for administering 3 and 4-substituted 2(5H)-furanones to a mammal for inhibiting bone loss (Wed, 31 Jul 1996)
3 and 4-substituted 2(5H)-furanone compounds influence the balance between bone production and bone resorption in mammals, including humans. The active compounds are administered to mammals, including humans, in an effective dose which ranges between 0.05 to 100 mg per kilogram, body weight, per day, for the purpose of influencing the balance between bone production and bone resorption, and particularly for treating osteoporosis.
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Oxime substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity (Wed, 04 Mar 1998)
Compounds of the formula ##STR1## have retinoid-like or retinoid antagonist-like biological activity.
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Tetrahydronaphthalene derivatives substituted in the 8 position with alkyhidene groups having retinoid and/or retinoid antagonist-like biological activity (Wed, 10 Jun 1998)
Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
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Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents (Wed, 11 Nov 1998)
The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration, dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2, Y is .dbd.O or represents 2 hydrogen radicals. Certain of the compounds represented by Formula I comprise another aspect of the present invention.
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O- or S- substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity (Wed, 22 Apr 1998)
Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
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O- or S-substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity (Wed, 16 Sep 1998)
Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
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Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and 1,2,3,4-tetrahydroquinoline carboxylic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity (Wed, 06 Jan 1999)
Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.
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Alkyl or aryl substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity (Wed, 01 Jul 1998)
Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
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Oxo-substituted tetrahydronaphthalene derivatives having retinold and/or retinoid antagonist-like biological activity (Wed, 06 May 1998)
Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
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