Ureido, Guanido, Or Hydrazine Patents (Class 562/439)
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Patent number: 6191171Abstract: para-Aminomethylaryl carboxamides of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.Type: GrantFiled: November 13, 1998Date of Patent: February 20, 2001Assignee: Merck & Co., Inc.Inventors: Stephen E. DeLaszlo, William K. Hagmann
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Patent number: 6156704Abstract: The invention relates to the compounds of Formula XA ##STR1## wherein X and Y represent independently hydrogen, fluorine or chlorine, Z.sub.1 is fluorine or chlorine and M is hydrogen or a salt forming moiety and Z.sub.2 ' is chlorine or fluorine; and the corresponding herbicidal composition and methods of use. The compounds of the invention are useful as auxin transport inhibitors (i.e. useful as herbicides) and useful as potentiators or enhancers of herbicides.Type: GrantFiled: June 7, 1995Date of Patent: December 5, 2000Assignee: Novartix AGInventors: Richard J. Anderson, Ian S. Cloudsdale, Robert J. Lamoreaux, Kristine J. Schaefer, Jost Harr
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Patent number: 6130315Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.Type: GrantFiled: August 24, 1998Date of Patent: October 10, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: H. Michael Kolb, Joseph P. Burkhart, Michael J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
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Patent number: 6127414Abstract: There is provided pharmaceutically useful compounds of formula I, ##STR1## wherein Ar.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have meanings given in the description, which are useful as antagonists of neuropeptide Y and in particular in the treatment of cardiovascular diseases, for example vasoconstriction.Type: GrantFiled: October 26, 1998Date of Patent: October 3, 2000Assignee: Astra AktiebolagInventors: Nils-.ANG.ke Bergman, Thomas D'Ambra, Garry M Pilling
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Patent number: 6063807Abstract: Cyclo-oxygenase inhibitor and amidine derivative salts, preparation methods therefor, pharmaceutical compositions containing said salts and the use thereof particularly as NO synthase and cyclo-oxygenase inhibitors, are disclosed.Type: GrantFiled: January 6, 1998Date of Patent: May 16, 2000Assignee: Societe de Conseils de Recherches d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Etienne Chabrier de Lassauniere, Colette Broquet
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Patent number: 6028223Abstract: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein A is ##STR2## pharmaceutical compositions thereof and methods of using such compounds and compositions as .alpha..sub.v .beta..sub.3 antagonists.Type: GrantFiled: August 27, 1996Date of Patent: February 22, 2000Assignee: G. D. Searle & Co.Inventors: Peter Gerrard Ruminski, Michael Clare, Paul Waddell Collins, Bipinchandra Nanubhai Desai, Richard John Lindmark, Joseph Gerace Rico, Thomas Edward Rogers, Mark Andrew Russell
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Patent number: 5994577Abstract: The present invention provides novel compounds of the formula I and II for the treatment of non-insulin dependent diabetes mellitius (NIDDM) and a new use of known compounds for this purpose.Type: GrantFiled: June 7, 1995Date of Patent: November 30, 1999Inventors: Scott D. Larsen, Valerie A. Vaillancourt, Paul D. May, Steven P. Tanis, John A. Tucker, Martin D. Meglasson, Heinrich J. Schostarez
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Patent number: 5968980Abstract: The present invention relates to compounds represented by the formula [I] and salts thereof, wherein R.sup.1 and R.sup.5 each represents carboxyl, phosphonic or a derivative thereof; R.sup.2 represents hydrogen, lower alkyl, (substituted) phenyl lower alkyl, lower alkoxy or (substituted) phenyl lower alkoxy; R.sup.3 represents lower alkyl or (substituted) phenyl lower alkyl; and R.sup.4 represents a group represented by the formula [XI], [XII] or [XIII]. The compounds of the present invention have endopeptidase 24.11 inhibitory activity and are useful for treating cardiovascular diseases such as heart failure and hypertension, renal diseases such as renal failure, gastroenteric disorders such as diarrhea and hyperchlorhydria, endocrine and metabolic diseases such as obesity, and autoimmune diseases such as rheumatic disease, and for mitigating myosalgia, migraine, etc.Type: GrantFiled: June 3, 1997Date of Patent: October 19, 1999Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Yoichi Kawashima, Ken-ichi Fujimura, Hiroshi Suhara, Noriyoshi Yamamoto, Hiromi Matsumoto, Nobuaki Miyawaki, Yuko Fujita
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Patent number: 5962722Abstract: An .alpha.-hydrazino acid derivative of general formula (I) is described, wherein R.sub.1, R.sub.2, R.sub.3 are hydrogen or a carbon radical, such that when R.sub.2 and R.sub.3 are different, C* is an asymmetric carbon of L, D or DL configuration, and R.sub.4 and R.sub.5 are a protecting group, characterized in that R.sub.4 is a benzyl ArCH.sub.2 radical of formula (a), wherein Ar is a phenyl radical or phenyl substituted by one or more X groups; X being hydrogen, halogen, a nitro or alkyl radical; and in that R.sub.5 is a Y--O--CO group, where Y is a carbon radical different from R.sub.4.Type: GrantFiled: March 3, 1998Date of Patent: October 5, 1999Assignee: Centre National de la Recherche ScientifiqueInventors: Andre Collet, Joelle Vidal, Jean-Christophe Hannachi, Laure Guy
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Patent number: 5948939Abstract: An .omega.-guanidino-.alpha.-amino-acid (or its functional derivative) or a compound containing it may be prepared by the reaction of the .omega.-amino group of an .alpha.,.omega.-diamino acid (or its functional derivative) or a compound containing it with a formamidinesulfonic acid.Type: GrantFiled: April 20, 1992Date of Patent: September 7, 1999Assignee: Syntex (U.S.A.) Inc.Inventors: Humberto B. Arzeno, David J. Morgans, Jr.
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Patent number: 5936055Abstract: Disclosed is an acid-funtionalized polyurethane adduct and a process for the preparation of such adduct. The adduct having a linear or preferably branched structure comprises a plurality of internal urethane linkages and one or more terminal carboxylic acid groups per molecule. Such acid-funtionalized polyurethane adducts find value in the manufacture of crosslinked aqueous rubber latexes such as might be used in paint compositions.Type: GrantFiled: February 19, 1997Date of Patent: August 10, 1999Assignee: The Dow Chemical CompanyInventors: Michael J. Elwell, Hanno R. van der Wal, Camiel F. Bartelink, Henri J. Grunbauer
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Patent number: 5929120Abstract: Compounds of the following general structureX--Y--Z-Aryl-A--B, ##STR1## which inhibit osteoclast mediated bone resorption.Type: GrantFiled: January 30, 1998Date of Patent: July 27, 1999Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Mark E. Duggan, William F. Hoffman, Nathan C. Ihle
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Patent number: 5922763Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: November 26, 1997Date of Patent: July 13, 1999Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5919824Abstract: Aminophenol derivatives represented by the following formula (1): ##STR1## wherein X is O or S; A is alkylene, R.sup.1 is phenyl, etc., R.sup.2 and R.sup.3 are H or alkyl; R.sup.4 is substituted carbamoylalkyl, etc.; R.sup.5 is substituted amino, etc.; their salts, and optical isomers of the derivatives and salts. Also disclosed are gastrin receptor antagonists, cholecystokinin receptor antagonists, and medicines for digestive diseases. The compounds have strong binding inhibition against gastrin receptor or CCK-A receptor and also they have higher selectivity to either group of CCK-A receptor or gastrin receptor, and therefore, the compounds are useful for preventing and treating gastrointestinal diseases including peptic ulcers as well as central nervous system diseases.Type: GrantFiled: September 12, 1997Date of Patent: July 6, 1999Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Shuichi Yokohama, Keiichi Kawagoe, Yasuyuki Takeda, Yoshihiro Yokomizo, Aki Yokomizo
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Patent number: 5914348Abstract: Substance FA-70D which has the following formula (1), or its salt, a method for its production, a pharmaceutical composition comprising the compound as an active ingredient, a method of treating osteoporosis which comprises administering the compound, use of the compound as a drug, and a microorganism capable of producing Substance FA-70D are disclosed. This compound has specific inhibitory activity against cathepsin series proteases and is of value as a therapeutic drug for various diseases, particularly osteoporosis, with which these enzymes are associated.Type: GrantFiled: October 14, 1997Date of Patent: June 22, 1999Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Shizuo Kitano, Toru Sasaki, Kenichiro Yoshida, Toshio Otani, Lei Yu, Yun Wu, Nobuhiko Katsunuma
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Patent number: 5914319Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: June 22, 1999Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5891912Abstract: The present invention related to compounds represented by the following formula (I) and salts thereof, ##STR1## wherein R.sup.1 and R.sup.4 each represents a carboxyl or a carboxyl which is converted into an ester, an amide or hydroxamic acid; R.sup.2 represents a lower alkyl or a phenyl-lower alkyl; R.sup.3 represents a hydrogen atom, a lower alkyl, an amino-lower alkyl, a lower alkylamino-lower alkyl, a hydroxy-lower alkyl, a mercapto-lower alkyl, a carboxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an imidazolyl-lower alkyl, an indolyl-lower alkyl, a (substituted) phenyl group, a (substituted) phenyl-lower alkyl group, a (substituted) naphthyl group, or a (substituted) naphtyl-lower group. The compounds of the present invention have inhibitory effects on endopeptidase 24.Type: GrantFiled: July 15, 1996Date of Patent: April 6, 1999Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Yoichi Kawashima, Ken-ichi Fujimura, Hiroshi Suhara, Nobuaki Miyawaki, Yuko Fujita
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Patent number: 5874472Abstract: Compounds of formula (I) and salts, esters and amides thereof, wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.3-6 cycloalkyl group, a thiol group optionally substituted by a C.sub.1-6 alkyl group, or an amino group optionally substituted by one or two alkyl or alkenyl groups; R.sup.2 is H, C.sub.1-7 straight or branched chain alkyl, C.sub.3-6 cycloalkyl, C.sub.2-7 alkenyl or benzyl; A is a 5 or 6 membered aromatic carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or di C.sub.1-6 alkylamino; r is 0, 1 or 2; their use in medicine and in particular for conditions requiring inhibition of the NO Synthase enzyme, pharmaceutical formulations and processes for the preparation thereof are disclosed.Type: GrantFiled: March 18, 1996Date of Patent: February 23, 1999Assignee: Glaxo Wellcome Inc.Inventors: Barry George Shearer, Karl Witold Franzmann, Harold Francis Hodson
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Patent number: 5866609Abstract: Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.Type: GrantFiled: July 24, 1997Date of Patent: February 2, 1999Assignee: SS Pharmaceutical Co., Ltd.Inventors: Yoshihiko Kanamaru, Hiroyuki Hirota, Akihiro Shibata, Teruo Komoto, Hiroyuki Naito, Koichi Tachibana, Mari Ohtsuka, Fumio Ishii, Susumu Sato
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Patent number: 5852210Abstract: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.Type: GrantFiled: March 27, 1997Date of Patent: December 22, 1998Assignee: G. D. Searle & Co.Inventors: Barbara B. Chen, Helen Y. Chen, Michael Clare, Stephen H. Docter, Ish Kumar Khanna, Francis Jan Koszyk, James W. Malecha, Julie Marion Miyashiro, Thomas D. Penning, Joseph G. Rico, Peter G. Ruminski, Mark A. Russell, Richard Mathias Weier, Xiangdong Xu, Stella S. Yu, Yi Yu
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Patent number: 5847134Abstract: Products prepared by reacting polyisocyanates with alkenyl or alkynyl compounds; then with perfluoroalkyl iodides & dehydroiodinating the product.Type: GrantFiled: January 11, 1996Date of Patent: December 8, 1998Assignee: E. I. du Pont de Nemours and CompanyInventor: Donald Douglas May
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Patent number: 5804595Abstract: The invention provides certain amino acid conjugates of substituted 2-phenyl-N-?1-(phenyl)-2-(1-heterocycloalkyl- or heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid receptors in mammalian tissue.Type: GrantFiled: December 5, 1995Date of Patent: September 8, 1998Assignee: Regents of the University of MinnesotaInventors: Philip S. Portoghese, An-Chih Chang
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Patent number: 5773644Abstract: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.Type: GrantFiled: March 27, 1997Date of Patent: June 30, 1998Assignee: G. D. Searle & Co.Inventors: Barbara B. Chen, Helen Y. Chen, Michael Clare, Shashidhar N. Rao, Mark A. Russell
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Patent number: 5773646Abstract: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.Type: GrantFiled: March 27, 1997Date of Patent: June 30, 1998Assignee: G. D. Searle & Co.Inventors: Nizal Chandrakumar, Barbara B. Chen, Helen Y. Chen, Michael Clare, Alan F. Gasiecki, Richard A. Haack, James W. Malecha, Peter G. Ruminski, Mark A. Russell
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Patent number: 5767088Abstract: The small compounds of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK.sub.3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.Type: GrantFiled: September 4, 1996Date of Patent: June 16, 1998Assignee: Warner-Lambert CompanyInventors: David Christopher Horwell, William Howson, Martyn Clive Pritchard, Jennifer Raphy
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Patent number: 5763635Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: June 21, 1996Date of Patent: June 9, 1998Assignee: ALLERGANInventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Tien T. Duong, Yuan Lin, Roshantha A. Chandraratna
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Patent number: 5760057Abstract: The invention concerns acid derivatives of formula IR.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --G(I)and pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.Type: GrantFiled: December 16, 1996Date of Patent: June 2, 1998Assignee: Zeneca LimitedInventors: Andrew George Brewster, Peter William Rodney Caulkett, Alan Wellington Faull, Robert James Pearce, Richard Eden Shute
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Patent number: 5747535Abstract: The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: ##STR1## in which R.sup.1 represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsubstituted aryl or N-containing heterocyclic group,X represents a group of formula ##STR2## R.sup.2 and R.sup.3 independently of one another represent hydrogen; cycloalkyl substituted or unsubstituted with carboxyl or alkoxycarbonyl; arylalkyloxy; hydroxy; or lower alkyl substituted or unsubstituted with carboxyl, alkoxycarbonyl or hydroxy, orR.sup.2 and R.sup.3 together with nitrogen atom to which they are attached can form a piperidine group substituted with carboxyl or alkoxycarbonyl,R.sup.4 represents hydrogen, lower alkyl or lower alkoxy,R.sup.Type: GrantFiled: January 16, 1996Date of Patent: May 5, 1998Assignee: LG Chemical Ltd.Inventors: Yeong Soo Oh, Sang Soo Kim, Sang Yeul Hwang, Mi Kyung Yun, Seong Ryul Hwang, Seong Won Hong, Yong Hee Lee, Yi Na Jeong, Koo Lee, You Seung Shin
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Patent number: 5736559Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: August 1, 1996Date of Patent: April 7, 1998Assignee: Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5728868Abstract: A compound which comprises a prodrug of a protein tyrosine kinase inhibitor (PTKi) linked to a protecting group which is capable of being cleaved from the compound to release the PTKi, said PTKi prodrugs including tyrphostins, of formula (I), ##STR1## where X represents C, N or a group N.fwdarw.O, n is 1 to 3; each group R.sup.1, which may be the same or different is H, OH, mercapto, carboxy, formyl, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxyC.sub.1-4 alkyl, carboxyC.sub.2-4 alkenyl, C.sub.1-4 alkylsulphoxy, halo, nitro, amino, C.sub.1-4 alkylamino, or C.sub.1-4 dialkylamino, or when n is 2 or 3 two R.sup.1 groups may together form a methylenedioxy or ethylenedioxy group; R.sup.2 is H, OH, C.sub.1-4 alkyl or together with position 2 of the ring to which the group(s) R.sup.1 is (are) attached forms a 5 or 6 membered aliphatic or heterocyclic ring, optionally containing a ketone group; and R.sup.3 is cyano, carboxy, carbamoyl, thiocarbamoyl, C(O)HNCH.sub.2 CN, C(NH.sub.Type: GrantFiled: July 1, 1996Date of Patent: March 17, 1998Assignee: Cancer Research Campaign Technology LimitedInventors: Caroline Joy Springer, Richard Marais
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Patent number: 5726159Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: March 10, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
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Patent number: 5719152Abstract: A tricyclic quinoxalinedione derivative represented by the formula 1: ##STR1## wherein X represents hydrogen, alkyl, halogen, cyano, trifluoromethyl, or nitro;R.sup.1 represents hydrogen, alkyl, cycloalkyl, or cycloalkylalkyl;G represents --CONR.sup.2 -- or --NR.sup.2 CO--, wherein R.sup.2 represents hydrogen or alkyl;J represents an acidic group or a group which is convertible thereto in vivo;E represents an basic group or a group which is convertible thereto in vivo;Y represents a single bond, alkylene, alkenylene, substituted alkylene, or Y.sup.1 --Q--Y.sup.2, wherein Y.sup.1 represents a single bond or alkylene, Y.sup.2 represents alkylene, and Q represents a heteroatom selected from oxygen or sulfur;Z represents alkylene,or a pharmaceutically acceptable salt thereof, these compounds are selective antagonists of glycine binding site of the NMDA receptor.Type: GrantFiled: March 6, 1996Date of Patent: February 17, 1998Assignee: Sumitomo Pharmaceuticals Co., Ltd.Inventors: Ryu Nagata, Norihiko Tanno, Toru Kodo, Hiroshi Yamaguchi, Nobuyuki Ae
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Patent number: 5716989Abstract: The invention relates to bicyclo?3.3.0!octane compounds of formula I, ##STR1## wherein the variable are defined in this specification, as well as their enantiomers, and their salts with physiologically compatible bases. .alpha.-, .beta.-, or .tau.-Cyclodextrin clathrates of the compounds and the compounds encapsulated with liposomes are also included. The invention is further directed to processes for production of the compounds and their pharmaceutical use.Type: GrantFiled: November 27, 1991Date of Patent: February 10, 1998Assignee: Schering AktiengesellschaftInventors: Ulrich Klar, Hartmut Rehwinkel, Helmut Vorbruggen, Karl Heinz Thierauch, Peter Verhallen
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Patent number: 5710130Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 20, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5710324Abstract: The present invention is directed to a new class of compound which are useful as inhibitors of the biosynthesis of nitric oxide.Type: GrantFiled: October 4, 1994Date of Patent: January 20, 1998Assignee: Merrell Pharmaceuticals Inc.Inventors: Jeffrey P. Whitten, Ian A. McDonald, Laurie E. Lambert, Niall S. Doherty
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Patent number: 5707966Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 13, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5705487Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 6, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5698569Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: December 16, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5681838Abstract: The present invention relates to novel substituted amino compounds of the formula I:R.sup.1 -(A).sub.a -(B).sub.b -(D).sub.c -(CH.sub.2).sub.m -N(R.sup.2)-(CH.sub.2).sub.n -R.sup.3as defined in the present application, and to a process for preparing such compounds. The invention also includes pharmaceutical compositions containing the present compounds, and the preparation of such compositions. The invention also relates to the use of the present compounds as inhibitors of blood-platelet aggregation, formation of metastases by carcinoma cells, and the binding of osteoclasts to bone surfaces, in the treatment of hosts in need thereof.Type: GrantFiled: July 18, 1995Date of Patent: October 28, 1997Assignee: Hoechst AktiengesellschaftInventors: Gerhard Zoller, Bernd Jablonka, Melitta Just, Otmar Klingler, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig
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Patent number: 5661139Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a bis-(2-aryl)hydrazone capable of inhibiting the formation of advanced glycosylation endproducts of target proteins. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.Type: GrantFiled: June 7, 1995Date of Patent: August 26, 1997Assignee: Alteon Inc.Inventors: Michael E. Lankin, David H. Shih, Dilip R. Wagle, San-Bao Hwang
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Patent number: 5658943Abstract: Novel antagonists of endothelin are described, as well as novel intermediates used in their preparation, methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, essential, renovascular, malignant and pulmonary hypertension, cerebral infarction, myocardial ischemia, cerebral ischemia, congestire heart failure and subarachnoid hemorrhage.Type: GrantFiled: January 5, 1995Date of Patent: August 19, 1997Assignee: Warner-Lambert CompanyInventors: Kent Alan Berryman, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Sylvester Klutchko
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Patent number: 5658944Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein Ar is a mono- or bicyclic aromatic group optionally containing one or two heteroatoms independently selected from nitrogen, oxygen and sulphur, said group being optionally substituted by one or more atoms or groups independently selected from halogen, nitro, amino, --NRR.sup.1 where R and R.sup.1 are independently selected from hydrogen, C.sub.1-8 alkyl and C.sub.1-8 alkanoyl, cyano, carboxyalkoxy, alkoxycarbonylalkoxy, C.sub.1-8 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-8 alkoxy (including cycloalkoxy and cycloalkylalkoxy), C.sub.Type: GrantFiled: April 14, 1995Date of Patent: August 19, 1997Assignee: The University of South CarolinaInventors: James Mood Chapman, Jr., Roy Lee Hawke, Karl Witold Franzmann, Kevin Julian O'Connor
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Patent number: 5631293Abstract: Amino acid-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent and a medicament containing themBenzoylguanidines of the formula I ##STR1## in which the radicals R(1) to R(5) have the meanings given in the description, are described. They are prepared by reacting a compound of the formula II ##STR2## in which R(1) to R(5) and L have the meanings given in the description, with guanidine. The compound I is suitable for the preparation of cardiovascular medicaments.Type: GrantFiled: September 8, 1995Date of Patent: May 20, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5624956Abstract: Novel urea derivatives and pharmaceutical compositions thereof are provided which inhibit platelet aggregation.Type: GrantFiled: May 24, 1995Date of Patent: April 29, 1997Assignee: The Monsanto CompanyInventors: Foe S. Tjoeng, Mihaly V. Toth, Dudley E. McMackins, Steven P. Adams
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Patent number: 5620977Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: April 15, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5616789Abstract: Disclosed are certain 3-phenylpyridazines, compositions thereof which are herbicidal and methods of using such compositions for controlling undesired plants. Intermediates useful in preparing the 3-phenylpyridazines are disclosed.Type: GrantFiled: June 6, 1995Date of Patent: April 1, 1997Assignee: Monsanto CompanyInventors: Michael S. South, Terri L. Jakuboski
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Patent number: 5612373Abstract: The invention concerns acid derivatives of formula IR.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --GIand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.Type: GrantFiled: June 27, 1994Date of Patent: March 18, 1997Assignee: Zeneca LimitedInventors: Andrew G. Brewster, Peter W. R. Caulkett, Alan W. Faull, Robert J. Pearce, Richard E. Shute
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Patent number: 5602275Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 25, 1995Date of Patent: February 11, 1997Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
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Patent number: 5602277Abstract: A compound of the Formula (I): ##STR1## or pharmaceutically-suitable salts or prodrug forms thereof, wherein: n is 0-1;m is 0;p is 0-1;R.sup.1 is --CO.sub.2 H;R.sup.2 is selected from the group consisting of H, --OH, and --NH.sub.2 ;R.sup.3 is H;R.sup.4 is --C(O)NHR.sup.8 ;R.sup.5 is --NHC(R.sup.6)NH.sub.2R.sup.6 is selected from the group consisting of .dbd.NH, .dbd.NOH, .dbd.NCN, .dbd.O, and .dbd.S; andR.sup.8 is selected from the group consisting of C.sub.1 -C.sub.4 linear or branched alkyl substituted with 0-3 halogens on each carbon.Type: GrantFiled: March 30, 1995Date of Patent: February 11, 1997Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, David A. Walsh
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Patent number: 5597825Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: May 16, 1994Date of Patent: January 28, 1997Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, G unter Linz, Thomas M uller, Wolfgang Eisert, Johannes Weisenberger