Search Patents
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Publication number: 20030055061Abstract: Substituted pyrido[1,2-a]pyrazines of general formula I; wherein Ar and Ar1 represent various carbocyclic and heterocyclic aromatic rings; A represents O, S, SO, SO2, CHOH, C═O, or —(CR3R4); and n is 0-2, as well as precursors thereto, are ligands for dopamine receptor subtypes and serotonin (5HT) within the body and are therefore useful in the treatment of disorders of the dopamine and serotonin systems: 1Type: ApplicationFiled: August 7, 2002Publication date: March 20, 2003Applicant: Pfizer Inc.Inventors: Kishor A. Desai, Anton F. Fliri, Mark A. Sanner
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Patent number: 8697673Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: March 29, 2012Date of Patent: April 15, 2014Assignee: Pfizer Inc.Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Benjamin Adam Fish, Michael Eric Green, Patrick Bradley Mullins, Cory Michael Stiff, Tuan Phong Tran, Thayalan Navaratnam
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Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
Patent number: 8916564Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: September 19, 2013Date of Patent: December 23, 2014Assignee: Pfizer Inc.Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Michael Eric Green, Nandini Chaturbhai Patel, Cory Michael Stiff, Tuan Phong Tran, Gregory Wayne Kauffman, Antonia Friederike Stepan, Patrick Robert Verhoest -
Patent number: 5789408Abstract: Compounds of formula (I) are active antiviral compounds useful in the treatment of viral infections in mammals. The compounds of the invention are readily prepared by reaction of a suitable 2-thiothiazole derivative with an appropriate Het-(CH.sub.2).sub.n -halide.Type: GrantFiled: January 11, 1996Date of Patent: August 4, 1998Assignee: Pfizer Inc.Inventors: Edward Fox Kleinman, Hiroko Masamune, Vinod Dipak Parikh
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Publication number: 20140135338Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: July 12, 2012Publication date: May 15, 2014Applicant: PFIZER INC.Inventors: Mary Didiuk, Kevin J. Filipski, Angel Guzman-Perez, Esther C. Lee, Jeffrey A. Pfefferkorn, Benjamin Stevens, Meihua Tu
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Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
Patent number: 9751877Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: October 7, 2015Date of Patent: September 5, 2017Assignee: PFIZER INC.Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Michael Eric Green, Nandini Chaturbhai Patel, Cory Michael Stiff, Tuan Phong Tran, Gregory Wayne Kauffman, Antonia Friederike Stepan, Patrick Robert Verhoest -
Patent number: 6608064Abstract: The present invention is directed to the use of certain pyrido[1,2-a]-pyrazine derivatives, also described as bis-azabicyclic compounds and defined by the formula (I) herein, in the treatment of Parkinson's disease, attention deficit hyperactivity disorder and microadenomas in mammals, and to related compositions.Type: GrantFiled: May 3, 2001Date of Patent: August 19, 2003Assignee: Pfizer IncInventors: Stafford McLean, Stevin H. Zorn, Elisa R. Jackson
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Patent number: 6465491Abstract: The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.Type: GrantFiled: April 4, 2001Date of Patent: October 15, 2002Assignee: Pfizer Inc.Inventors: John A. Lowe, III, Peter J. Whittle
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Patent number: 7432263Abstract: Compounds which are amino-phthalazinone derivatives according to formula 1 and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or compostions are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, autoimmune diseases and neurodegenerative disorders.Type: GrantFiled: July 30, 2002Date of Patent: October 7, 2008Assignee: Pfizer Italia, S.r.l.Inventor: Maurizio Pulici
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Patent number: 6858613Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which ?7 is known to be involved.Type: GrantFiled: February 14, 2003Date of Patent: February 22, 2005Assignee: Pfizer Inc.Inventors: Bruce N. Rogers, David W. Piotrowski, Daniel Patrick Walker, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Vincent E. Groppi, Jr.
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Publication number: 20150087585Abstract: Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H-imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.Type: ApplicationFiled: March 26, 2013Publication date: March 26, 2015Applicant: PFIZER INC.Inventors: Kay Ahn, Markus Boehm, Shawn Cabral, Philip A. Carpino, Kentaro Futatsugi, David Hepworth, Daniel W. Kung, Suvi Orr, Jian Wang
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Patent number: 4861779Abstract: Antibacterial compounds have the formula ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p-aminophenyl; or A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five to seven membered ring which is optionally substituted; and R.sup.2 is a bridged-diazabicycloalkyl group.Type: GrantFiled: August 19, 1986Date of Patent: August 29, 1989Assignee: Pfizer Inc.Inventors: Martin R. Jefson, Paul R. Mc Guirk
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Publication number: 20140179667Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.Type: ApplicationFiled: December 18, 2013Publication date: June 26, 2014Applicant: PFIZER INC.Inventors: Martin Paul EDWARDS, Robert Arnold KUMPF, Pei-Pei KUNG, Indrawan James MCAPLINE, Sacha NINKOVIC, Eugene Yuanjin RUI, Scott Channing SUTTON, John Howard TATLOCK, Martin James WYTHES, Luke Raymond Zehnder
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Patent number: 5852016Abstract: Compounds of formula (I), wherein A represents N or CH; R.sup.1 and R.sup.2 independently represent C.sup.1-4 alkyl, halo or CF.sub.3 ; R.sup.3 represents C.sub.1-4 alkyl (optionally substituted), C.sub.3-7 cycloalkyl, CF.sub.3 or aryl; R.sup.4 represents H, C.sub.3-7 cycloalkyl or C.sub.1-6 alkyl (optionally substituted); and their pharmaceutically acceptable derivatives; are useful in the treatment of, inter alia, neurodogenerative disorders.Type: GrantFiled: March 21, 1997Date of Patent: December 22, 1998Assignee: Pfizer Inc.Inventors: Michael Jonathan Fray, Charles Eric Mowbray, Alan Stobie
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Patent number: 6200978Abstract: Compounds of the formula (I)—shown below—are described. The compounds are useful in the manufacture of a pharmaceutical composition for preventing or treating inflammatory diseases such as arthritis, psoriasis, asthma, or inflammatory bowel disease, disorders of respiratory function, gastrointestinal disorders such as functional bowel disease, functional GI disorders such as irritable bowel syndrome, functional diarrhoea, functional distension, functional pain, non-ulcerogenic dyspepsia or others associated with disorders of motility or secretion, urogenital tract disorders such as incontinence, as analgesics for treating pain including non-somatic pain, or as immunosuppressants to prevent rejection in organ transplant and skin graft.Type: GrantFiled: March 3, 1999Date of Patent: March 13, 2001Assignee: Pfizer Inc.Inventors: Graham Nigel Maw, Donald Stuart Middleton
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Patent number: 6630472Abstract: Compounds that inhibit the peptidyl-prolyl isomerase (rotamase) enzyme activity of the FK-506 binding protein (FKBP) and compositions comprising these compounds are described. The FKBP-inhibiting compounds have a bicyclic [3.3.1], [4.3.1] or polycyclic azaamide nucleus. Pharmaceutical compositions containing such compounds help stimulate the outgrowth of neurites in nerve cells and augmenting nerve regeneration. Methods of treating nerve cells with such compositions are useful to promote repair of neuronal damage caused by disease and physical trauma.Type: GrantFiled: July 16, 1999Date of Patent: October 7, 2003Assignee: Pfizer IncInventors: Susumu Katoh, Hiroshi Kawakami, Hiroki Tada, Maria Angelica Linton, Vincent Kalish, John Howard Tatlock, Jesus Ernesto Villafranca
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Patent number: 7345038Abstract: An aminomethylpyridyloxymethyl/benzisoxazole substituted azabicyclic compound of formula I, pharmaceutical composition comprising same, and a method of treating one or more CNS or other disorders, including concurrent treatment of disorders such as schizophrenia and depression, wherein formula I is or a pharmaceutically acceptable salt or thereof, wherein Z is wherein Y is methylene; X is oxygen; n is 0; R1 and R2 are each hydrogen or halogen; and R3 and R4 together with the nitrogen atom to which they are attached form i) a saturated non-aromatic 3 to 7 membered monocyclic ring, said ring i) being unsubstituted or substituted or substituted with one or more (C1–C4)alkyl, (C1–C4)alkoxy(C1–C4)alkyl, or hydroxy groups.Type: GrantFiled: March 12, 2004Date of Patent: March 18, 2008Assignee: Pfizer, IncInventors: Gene Michael Bright, Michael A. Brodney, Bishop Wlodecki
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Patent number: 7101869Abstract: Novel compounds according to the formula and pharmaceutically acceptable salts, solvates, or hydrates thereof; wherein each occurrence of A is independently selected from CH or N; X is selected from the group consisting of —CH2—, —O—, —NH—, (C1-C6)alkylamino-, (C1-C6)alkylaminocarbonylamino-, (C1-C6)alkylcarbonylamino-, (C1-C6)alkylsulfonylamino-, phenylsulfonylamino-, carbonyl, —NH—C(O)—, —N(C1-C6)alkyl-C(O)—, —S(O)y— where y is 0, 1 or 2, and; n in —(CH2)n— is 1, 2 or 3; and R1, R2, and R3 are as described herein; pharmaceutical compositions that including these compounds, and methods for the treatment of autoimmune disease, inflammation, allergy, transplant rejection, and other circumstances where administration of an immunosuppressive agent is of therapeutic benefit.Type: GrantFiled: November 22, 2002Date of Patent: September 5, 2006Assignee: Pfizer Inc.Inventors: Todd A. Blumenkopf, Eileen Elliott Mueller, Eric Jan Roskamp
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Publication number: 20120108588Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Applicant: Pfizer, Inc.Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
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Patent number: 5304557Abstract: A compound of the formula ##STR1## wherein A.sup.1 and A.sup.2 are independently N or CH;B is a covalent bond or C.dbd. O;R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2 is hydrogen, fluorine, chlorine, bromine, trifluoromethyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, or C.sub.1 -C.sub.4 alkylthio;R.sup.3 is ##STR2## wherein R.sup.4 is phenyl optionally substituted;X is oxygen or sulphur;Y is hydrogen; or Y forms an indole group with the carbon on the ortho position of the phenyl in R.sup.4 ; or a pharmaceutically acceptable base salt thereof when R is hydrogen;with the proviso that when B is a covalent bond, A.sup.1 and A.sup.2 are each CH, and use for the inhibition of aldose reductase activity.Type: GrantFiled: April 30, 1992Date of Patent: April 19, 1994Assignee: Pfizer Inc.Inventor: Banavara L. Mylari