Spiro Ring System Patents (Class 514/409)
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Publication number: 20020128256Abstract: The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof which are specific, potent and safe inhibitors of the Ca2+-activated potassium channel (Gardos channel) of erythrocytes. The compounds can be used as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation.Type: ApplicationFiled: June 13, 2001Publication date: September 12, 2002Inventors: Carlo Brugnara, Jose Halperin, Rudolf Fluckiger, Emile M. Bellott, Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
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Patent number: 6441019Abstract: This invention provides compounds of the formula: wherein A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with an C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, CORA, or NRBCORA; or R1 and R2 are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof.Type: GrantFiled: July 17, 2001Date of Patent: August 27, 2002Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Arthur A. Santilli, Andrew Q. Viet, Puwen Zhang, Andrew Fensome, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Publication number: 20020103217Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1Type: ApplicationFiled: January 8, 2002Publication date: August 1, 2002Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
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Publication number: 20020091115Abstract: The invention is directed to aza-bridged-bicyclic compounds having Formula (I): 1Type: ApplicationFiled: June 26, 2001Publication date: July 11, 2002Inventors: Alexey B. Dyatkin, Bruce E. Maryanoff, William J. Hoekstra, Wei He, William A. Kinney
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Publication number: 20020086874Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: 1Type: ApplicationFiled: December 14, 2001Publication date: July 4, 2002Applicant: American Home Products CorporationInventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20020077338Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optically other antiviral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: ApplicationFiled: June 21, 2001Publication date: June 20, 2002Inventors: Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
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Publication number: 20020068735Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure 1Type: ApplicationFiled: January 9, 2002Publication date: June 6, 2002Applicant: American Home Products CorporationInventors: Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6395743Abstract: Compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and 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 are described. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. The culture Actinoplanes sp. MA7220 (ATCC 202188) is also disclosed, as well as processes for making compounds of the present invention employing the culture.Type: GrantFiled: October 12, 2000Date of Patent: May 28, 2002Assignee: Merck & Co., Inc.Inventors: Brian Heimbuch, Sheo Singh, Deborah L. Zink, Magda Gagliardi, Olga Genilloud, Ana Teran
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Patent number: 6391907Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.Type: GrantFiled: April 19, 2000Date of Patent: May 21, 2002Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6384069Abstract: 2-Pyrrolidinone derivatives substituted in position 4 are provided according to the invention for use as therapeutic active ingredient. It has been found, surprisingly, that these compounds are able markedly to reduce the extracellular glutamate level, and the compounds are therefore suitable for the prophylaxis and treatment of a large number of disorders, in particular, stroke.Type: GrantFiled: July 12, 2000Date of Patent: May 7, 2002Assignee: Klinikum der Albert-Ludwigs-UniversitaetInventors: Thomas J. Feuerstein, Rainer Knoerle
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Patent number: 6380200Abstract: This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug and selective serotonin reuptake inhibitor (SSRI), a prodrug thereof or a pharmaceutically acceptable salt of said SSRI or said prodrug. This invention further relates to methods of using those pharmaceutical compositions for the treatment of diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, myocardial infarction, cataracts and diabetic cardiomyopathy.Type: GrantFiled: December 1, 2000Date of Patent: April 30, 2002Assignee: Pfizer, Inc.Inventor: Banavara L. Mylari
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Publication number: 20020049232Abstract: A method of preventing the development of or treating dyskinesias in patients being treated for Parkinson's Disease requires the administration of a pharmacologically effective amount of a substituted phenylazacycloalkane and a dopamine agonist to the patient.Type: ApplicationFiled: October 12, 2001Publication date: April 25, 2002Inventor: Kjell A. Svensson
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Publication number: 20020037863Abstract: An anthelmintic composition comprising:Type: ApplicationFiled: April 6, 2001Publication date: March 28, 2002Inventor: Timothy G. Geary
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Publication number: 20020035099Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds that are antagonists of the progesterone receptor having the general structure: 1Type: ApplicationFiled: October 15, 2001Publication date: March 21, 2002Applicant: American Home Products CorporationInventors: Gary S. Grubb, John W. Ullrich, Andrew Fensome, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6358887Abstract: The present invention relates to new compounds of the formula (I) in which X, Y and Z have the meanings given in the description and Het represents one of the groups in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation, and to their use as pesticides and herbicides.Type: GrantFiled: August 5, 1997Date of Patent: March 19, 2002Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Norbert Lui, Michael Ruther, Arno Widdig, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Peter Dahmen, Norbert Mencke, Andreas Turberg
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Patent number: 6355648Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structures: wherein: R1 and R2 are H, alkyl, substituted alkyl; OH; O(alkyl); O(substituted alkyl); OAc; aryl; substituted aryl; heteroaryl; substituted heteroaryl; alkylaryl; alkylheteroaryl; 1-propynyl; or 3-propynyl; or R1 and R2 are joined to form an alkyl, alkenyl or heterocyclic ring; or R1 and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, alkynyl, substituted alkynyl, or CORA; RA is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NH2, NO2, C1 to C6 alkyl, or substituted C1 to C6 alkyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; R5 is optionally substituted and selected from a benzene riType: GrantFiled: April 19, 2000Date of Patent: March 12, 2002Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
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Patent number: 6352995Abstract: The present invention discloses compounds of formula (I), or a pharmaceutically acceptable salt thereof; wherein n is 1 or 2 or 3, A is —O—, —S—, —CH—, —O—CH2—, or —CH2—O—; B is —O—, —S—, —CH2—, —0—CH2—, or —CH2—O—; and C is N, or —CR1—; D is N, or —CR2—; E is N, or —CR3—; and F is N, or —CR4—; wherein R1, R2, R3 and R4 each independently are selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6 membered heteroaryl group. The compounds of the invention are useful for the treatment of disorders or diseases responsive to the activity of nicotinic ACh receptor modulators.Type: GrantFiled: October 14, 1999Date of Patent: March 5, 2002Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon Feldbaek Nielsen, Elsebet Nielsen
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Publication number: 20020006963Abstract: This invention encompasses methods for the treatment and prevention of disorders that include, but are not limited to, eating disorders; weight gain; obesity; irritable bowel syndrome; obsessive-compulsive disorders; platelet adhesion; apnea; affective disorders such as attention deficit disorders, depression, and anxiety; male and female sexual function disorders; restless leg syndrome; osteoarthritis; substance abuse including nicotine and cocaine addiction; narcolepsy; pain such as neuropathic pain, diabetic neuropathy, and chronic pain; migraines; cerebral function disorders; chronic disorders such as premenstrual syndrome; and incontinence.Type: ApplicationFiled: January 29, 2001Publication date: January 17, 2002Inventors: James W. Young, Thomas P. Jerussi
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Publication number: 20020004519Abstract: A method and product for treating and preventing diarrhea and scours is provided. The method involves treating a subject who has diarrhea, or scours, or is at risk of getting diarrhea or scours with an aromatic compound of the invention. The products of the invention are a veterinary preparation of the aromatic compound of the invention and an anti-scours agent, and a pharmaceutical preparation of the aromatic compound of the invention and an anti-diarrheal agent.Type: ApplicationFiled: September 23, 1998Publication date: January 10, 2002Inventors: WAYNE I. LENCER, CARLO BRUGNARA, SETH ALPER
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Patent number: 6337327Abstract: The invention relates to pharmaceutical compositions comprising an aldose reductase inhibitor and an ACE inhibitor, and their use in the treatment of diabetic complications such as diabetic neuropathy, diabetic retinopathy and diabetic nephropathy.Type: GrantFiled: January 7, 2000Date of Patent: January 8, 2002Assignee: Zeneca LimitedInventors: David Patrick Tuffin, Frank Carey, Mary Anne Cotter, Norman Eugene Cameron
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Patent number: 6329416Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds that are antagonists of the progesterone receptor having the general structure: wherein: R1, and R2 are chosen independently from each other from H, OH; OAc; alkylaryl; alkylheteroaryl; 1-propynyl; 3-propynyl; and optionally substituted alkyl, O(alkyl); aryl; or heteroaryl groups; or R1 and R2 are joined to FORM a ring comprising —CH2(CH2)nCH2— where n=0-5; —CH2CH2CMe2CH2CH2—; —O(CH2)mCH2— where m=1-4; O(CH2)pO— where p=1-4; —CH2CH2OCH2CH2—; —CH2CH2N(H or alkyl)CH2CH2—; or R1, and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, CORA; or optionally substituted alkenyl or alkynyl groups; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoType: GrantFiled: April 19, 2000Date of Patent: December 11, 2001Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Gary S. Grubb, John W. Ullrich, Andrew Fensome, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6316638Abstract: Novel substituted amino acids of formula are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: August 16, 2000Date of Patent: November 13, 2001Assignee: Warner-Lambert CompanyInventors: Justin Stephen Bryans, David Christopher Horwell, Jean-Marie Receveur
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Patent number: 6300361Abstract: The invention relates to the use of certain acid donors as stabilizers in pharmaceutical compositions, and to the stabilized pharmaceutical compositions resulting there-from.Type: GrantFiled: June 6, 1995Date of Patent: October 9, 2001Assignee: Novartis AGInventors: Richard V. Vivilecchia, Bruce A. Ross
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Patent number: 6300362Abstract: The invention relates to the use of certain acid donors as stabilizers in pharmaceutical compositions, and to the stabilized pharmaceutical compositions resulting therefrom.Type: GrantFiled: June 6, 1995Date of Patent: October 9, 2001Assignee: Novartis AG (formerly Sandoz Ltd.)Inventors: Richard V. Vivilecchia, Bruce A. Ross
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Patent number: 6288102Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups and G, V, W, X, Y and Z are each as defined in the description, to processes and intermediates for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: June 4, 1999Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Hermann Hagemann, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Alan Graff, Wolfram Andersch
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Publication number: 20010014676Abstract: A pharmaceutical composition containing a non-specific (NS) suppressor cell inducing compound and a non NS suppressor cell cell inducing immunosuppressive compound and a pharmaceutically acceptable carrier or diluent, and method of inducing an immunosuppressive effect in a mammal, including a human, in need thereof which comprises administering an effective dose of a NS suppressor cell inducing compound and a non NS suppressor cell cell inducing immunosuppressive compound to such mammal.Type: ApplicationFiled: January 29, 2001Publication date: August 16, 2001Inventor: Alison Mary Badger
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Patent number: 6271264Abstract: The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises administering a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polymer composition to a mammal, such as a human, whereby bile acids are sequestered. The polymers of the invention comprise spirobicyclic ammonium moieties and optionally, further comprise a hydrophobic substituent, a quaternary ammonium-containing substituent or a combination thereof.Type: GrantFiled: December 1, 1998Date of Patent: August 7, 2001Assignee: GelTex Pharmaceuticals, Inc.Inventors: Pradeep K. Dhal, Steven C. Polomoscanik
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Patent number: 6262060Abstract: The invention relates to azacycloalkane derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to methods for the treatment of hyperglycaemia, diabetes, obesity or inflammation utilizing them.Type: GrantFiled: November 27, 2000Date of Patent: July 17, 2001Assignee: Sanofi-SynthelaboInventors: Manuel Bedoya-Zurita, Juan Antonio Diaz Martin, Marc Daumas
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Patent number: 6218417Abstract: Compounds having platelet anti-aggregating activity and antihypertension activity having reduced branchial side effects.Type: GrantFiled: November 8, 1999Date of Patent: April 17, 2001Assignee: Nicox, S.A.Inventor: Piero Del Soldato
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Patent number: 6207697Abstract: The present application describes inhibitors of factor Xa of formula I: or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3 may be N or C and J, Ja, and Jb combine to form a substituted carbocycle or heterocycle.Type: GrantFiled: September 8, 1998Date of Patent: March 27, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Qi Han, Celia Dominguez, Eugene C. Amparo, Jeongsook M. Park, Mimi L. Quan, Karen A. Rossi
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Patent number: 6200932Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which A, B, G, X, Y, Z and n are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: February 1, 1999Date of Patent: March 13, 2001Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Udo Schneider, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Ulrike Wachendorff-Neumann
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Patent number: 6191160Abstract: Compounds of the general structural formula I are selective NPY Y5 receptor antagonists. The compounds and compositions of the present invention are useful in the treatment of obesity and complications associated therewith.Type: GrantFiled: November 8, 1999Date of Patent: February 20, 2001Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ying-Duo Gao, Douglas J. MacNeil, Lihu Yang, Nancy R. Morin, Takehiro Fukami, Akio Kanatani, Takahiro Fukuroda, Yasuyuki Ishii, Masaki Ihara
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Patent number: 6187752Abstract: A method is provided for treating schizophrenia in a mammalian species by administering an ACE inhibitor, such as captopril, alone or with a neuroleptic such as cholecystokinin, fluphenazine or haloperidol.Type: GrantFiled: September 12, 1991Date of Patent: February 13, 2001Assignee: E.R. Squibb & Sons, Inc.Inventors: Abraham Sudilovsky, Joram Feldon, Ina Weiner, A. David Smith, John N. P. Rawlins
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Patent number: 6156783Abstract: Novel azabicyclic derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.Type: GrantFiled: October 30, 1998Date of Patent: December 5, 2000Assignee: SmithKline Beecham p.l.c.Inventor: Laramie Mary Gaster
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Patent number: 6121261Abstract: A tachykinin receptor antagonist is useful for treating or preventing attention deficit disorder, optionally associated with hyperactivity, in a patient.Type: GrantFiled: November 19, 1998Date of Patent: September 19, 2000Assignee: Merck & Co., Inc.Inventors: David L. Glatt, Mark S. Kramer, Nadia Rupniak
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Patent number: 6110872Abstract: The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) in whichHet represents one of the groups ##STR1## wherein A, B, D, G, X, Y and Z have the meaning given in the description, several processes and intermediate products for their preparation and their use as pest control agents and herbicides.Type: GrantFiled: December 22, 1997Date of Patent: August 29, 2000Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Alan Graff, Norbert Mencke, Andreas Turberg, Peter Dahmen
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Patent number: 6107328Abstract: The present application is directed to the use of 5HT.sub.1B or 5HT.sub.1D receptor antagonists in the treatment of vascular diseases, in particular angina, Raynaud's syndrome, peripheral vascular syndrome or portal hypertension.Type: GrantFiled: July 1, 1998Date of Patent: August 22, 2000Assignee: SmithKline Beecham p.l.c.Inventor: Andrew Parsons
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Patent number: 6100265Abstract: A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.Type: GrantFiled: July 15, 1999Date of Patent: August 8, 2000Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
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Patent number: 6060469Abstract: The present invention relates to compounds of formula (I), ##STR1## wherein R.sup.1 represents halogen, hydroxy, C.sub.1-6 alkyl group optionally substituted by one or three fluorine atoms, C.sub.1-6 alkoxy group optionally substituted by one to three fluorine atoms, or C.sub.1-6 alkylthio optionally substituted by one to three fluorine atoms; R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or when R.sup.2 is adjacent to R.sup.1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R.sup.3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; R.sup.4, R.sup.5, R.sup.6, R.sup.9 and R.sup.Type: GrantFiled: May 18, 1998Date of Patent: May 9, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Timothy Harrison, Christopher John Swain, Brian John Williams
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Patent number: 6051596Abstract: A pharmaceutical composition containing a non-specific (NS) suppressor cell inducing compound and cyclosporin A and a pharmaceutically acceptable carrier or diluent, and method of inducing an immunosuppressive effect in a mammal, including a hyman, in need thereof which comprises administering an effective dose of a non-specific suppressor cell inducing compound and cyclosporin A to such mammal.Type: GrantFiled: August 1, 1997Date of Patent: April 18, 2000Assignee: AnorMED, Inc.Inventor: Alison Mary Badger
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Patent number: 6048877Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.Type: GrantFiled: January 20, 1998Date of Patent: April 11, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
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Patent number: 6025364Abstract: Invented is a method of treating asthma, in mammals, including humans, which comprises administering to such human an effective amount of a substituted azaspirane.Type: GrantFiled: January 15, 1999Date of Patent: February 15, 2000Assignee: AnorMed, Inc.Inventors: Alison Mary Badger, John Gerald Gleason
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Patent number: 6015912Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: August 26, 1997Date of Patent: January 18, 2000Assignee: The Procter & Gamble CompanyInventors: Zhe Wang, Neil Gregory Almstead, Rimma Sandler Bradley, Michael George Natchus, Biswanath De, Stanislaw Pikul, Yetunde Olabisi Taiwo
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Patent number: 6013652Abstract: Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.Type: GrantFiled: December 4, 1997Date of Patent: January 11, 2000Assignee: Merck & Co., Inc.Inventors: Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Yuan-Ching P. Chiang, Patrick T. Dunn, Hiroo Koyama
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Patent number: 6013644Abstract: The present invention is directed spiro-substituted azacycles of formula I: (wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, k, l and m are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: December 12, 1997Date of Patent: January 11, 2000Assignee: Merck & Co., Inc.Inventors: Sander G. Mills, Malcolm Maccoss, Martin S. Springer
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Patent number: 5994274Abstract: The present invention relates to new compounds of the formula (I) ##STR1## in which X represents alkyl,Y represents halogen or alkyl andZ represents halogen or alkyl,with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl,Het represents one of the groups ##STR2## in which A, B, D and G have the meanings given in the description,a plurality of processes for their preparation and their use as pesticides and herbicides.Type: GrantFiled: December 23, 1997Date of Patent: November 30, 1999Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
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Patent number: 5994350Abstract: The subject of the invention is indolin-2-one derivatives of formula: ##STR1## in which: W represents a --CH.sub.2 -- or --SO.sub.2 -- group;Cy forms, with the carbon to which it is bonded, a non-aromatic, saturated or unsaturated C.sub.3 -C.sub.12 hydrocarbon ring which is optionally condensed or substituted by one or a number of (C.sub.1 -C.sub.7)alkyl groups, it being possible for the said groups to substitute the same carbon atom one or a number of times, or by a C.sub.3 -C.sub.6 spirocycloalkyl;T represents a (C.sub.1 -C.sub.4)alkylene which is optionally interrupted by a (C.sub.3 -C.sub.6)cycloalkylene, the said alkylenes optionally being substituted one or a number of times on the same carbon atom by a (C.sub.1 -C.sub.3)alkyl; or alternatively T represents a direct bond;Z represents in particular an amino group;R.sub.1 and R.sub.2, as well as R.sub.3 and R.sub.4, are either hydrogen or substituents, such as, for example, a halogen, an alkyl, and the like.Type: GrantFiled: April 17, 1998Date of Patent: November 30, 1999Assignee: Sanofi-SynthelaboInventors: Loic Foulon, Georges Garcia, Claudine Serradeil-Le Gal, Gerard Valette
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Patent number: 5981567Abstract: The invention concerns substituted spiroheterocyclic 1H-3-arylpyrrolidine-2,4-dione derivatives of formula (I) in which A and B together with the carbon atom to which they are bound, are an unsubstituted or substituted 5- or 6-membered ring including at least one hetero atom; X is alkyl, halogen or alkoxy; Y is hydrogen, alkyl, halogen, alkoxy or alkyl halide; Z is alkyl, halogen or alkoxy; n is 0, 1, 2 or 3; G is hydrogen (a) or one of the groups (b), (c), (d), (e), (f) or (g), E is a metal-ion equivalent or an ammonium ion; L and M are each oxygen or sulphur and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined in the description. The invention also concerns methods of preparing such compounds as well as intermediates of formula (XVII) and (II) in which A, B, X, Y, Z and n are as defined in claim 1 and R.sup.8 is alkyl. Compounds of formula (I) are suitable for use as pest-control agents.Type: GrantFiled: December 28, 1995Date of Patent: November 9, 1999Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kruger, Hans-Joachim Santel, Markus Dollinger, Christoph Erdelen, Ulrike Wachendorff-Neumann
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Patent number: 5977111Abstract: A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.Type: GrantFiled: June 21, 1996Date of Patent: November 2, 1999Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
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Patent number: 5972951Abstract: Novel piperidine derivatives of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use as medicaments for the treatment of CNS disorders are disclosed.Type: GrantFiled: October 2, 1997Date of Patent: October 26, 1999Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Francis David King, Paul Adrian Wyman