Oxy In Acid Moiety Patents (Class 560/53)
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Patent number: 4147877Abstract: The present invention provides .omega.-aryl-6-hydroxy-PGE.sub.1 compounds which are useful pharmacological agents. These analogs are useful as prostacyclin-like drugs.Type: GrantFiled: June 23, 1978Date of Patent: April 3, 1979Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4145555Abstract: The present invention relates to prostaglandin analogues of the general formula: ##STR1## ?wherein X represents cis or trans-vinylene or ethylene, Z represents ##STR2## R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents a hydrogen atom or a methyl group, R.sup.3 represents a straight- or branched-chain alkylene group containing from 1 to 7 carbon atoms and R.sup.4 represents a cycloalkyl group containing from 5 to 7 carbon atoms, a grouping of the formula: ##STR3## (wherein R.sup.5 and R.sup.6, which may be the same or different, each represent a hydrogen atom or halogen atom, a trifluoromethyl group or a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms), or a grouping of the formula: ##STR4## (wherein R.sup.5 and R.sup.6 are as hereinbefore defined), or R.sup.3 and R.sup.Type: GrantFiled: March 7, 1977Date of Patent: March 20, 1979Assignee: Ono Pharmaceutical CompanyInventors: Masaki Hayashi, Seiji Kori, Yoshinobu Arai, Takanori Okada, Yoshitaka Konishi
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Patent number: 4142052Abstract: Prostaglandin analogs with the following cyclopentane ring structure: ##STR1## are disclosed along with intermediates useful in their preparation and processes for their preparation. These analogs are useful for some of the same pharmacological purposes as the prostaglandins, particularly and especially as blood platelet aggregation inhibitors.Type: GrantFiled: June 23, 1977Date of Patent: February 27, 1979Assignee: The Upjohn CompanyInventor: David C. Peterson
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Patent number: 4140861Abstract: Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as a pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.Type: GrantFiled: May 18, 1978Date of Patent: February 20, 1979Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., John B. Bicking
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Patent number: 4139545Abstract: Novel compounds of the formulae ##STR1## wherein R represents lower alkyl or lower alkoxy, A represents --CH.sub.2 --, --CO-- or ##STR2## n represents an integer of 1 to 8, X represents hydrogen or hydroxyl which may be protected and Y represents hydroxyl which may be protected, and their esters show an excellent action on the lysosomal membranes of cells, and exhibit excellent pharmacological activities such as physiologic host defense control activity, especially immuno-potentiating activity.Type: GrantFiled: April 30, 1975Date of Patent: February 13, 1979Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroshi Morimoto, Isuke Imada, Masazumi Watanabe, Mitsuru Kawada
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Patent number: 4139712Abstract: This invention comprises certain analogs of the prostaglandins in which the double bond between C-13 and C-14 is replaced by a triple bond. Also provided in this invention, are novel chemical processes and novel chemical intermediates useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.Type: GrantFiled: April 28, 1978Date of Patent: February 13, 1979Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4138573Abstract: 11-Deoxy prostaglandin type compounds, i.e. prostaglandin type compounds in which the 11-hydroxy group is replaced by hydrogen, are disclosed, with processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, and labor induction at term.Type: GrantFiled: April 17, 1978Date of Patent: February 6, 1979Assignee: The Upjohn CompanyInventors: Gordon L. Bundy, Norman A. Nelson
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Patent number: 4138574Abstract: The disclosure includes novel compounds which differ from the known prostaglandins PGF.sub.2.alpha., PGF.sub.2.beta., PGE.sub.2, PGA.sub.2, and PGB.sub.2 in that the carbon-carbon double bond in the carboxyl-terminated chain of the novel compounds is in the 4,5-position rather than in the 5,6-position, and in that there is a phenoxy or substituted phenoxy group in the other chain of the novel compounds. These novel compounds are useful for a variety of pharmacological purposes, including abortion, labor induction, and reduction of gastric secretion.Type: GrantFiled: April 28, 1978Date of Patent: February 6, 1979Assignee: The Upjohn CompanyInventor: Barney J. Magerlein
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Patent number: 4138590Abstract: Derivatives of PGD.sub.2 are prepared. These new compounds not heretofore found in nature display pharmacological activity, for example, inhibition of blood platelet aggregation.Type: GrantFiled: January 13, 1977Date of Patent: February 6, 1979Assignee: American Home Products CorporationInventor: Wenling Kao
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Patent number: 4136192Abstract: Bicyclic compounds useful in the prophylaxis and treatment of allergic diseases, pharmaceutical compositions containing the same, methods of administration of the compositions, intermediates useful in preparing the compounds and conversion of the intermediates to the bicyclic compounds. Examples of compounds are substituted coumarins and indanediones and their pharmaceutically acceptable salts.Type: GrantFiled: March 22, 1977Date of Patent: January 23, 1979Assignee: Beecham Group LimitedInventors: Derek R. Buckle, Harry Smith
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Patent number: 4133959Abstract: Aryloxyalkyl diketones, useful as anti-viral agents, are prepared from an aryloxyalkyl halide and an alkali metal enolate salt of a diketone or keto-ester, or from a haloalkyl-diketone and an alkali metal salt of a phenol.Type: GrantFiled: September 21, 1976Date of Patent: January 9, 1979Assignee: Sterling Drug Inc.Inventors: Joseph C. Collins, Guy D. Diana
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Patent number: 4130718Abstract: This invention comprises certain analogs of the prostaglandins in which the double bond between C-13 and C-14 is replaced by a triple bond. Also provided in this invention, are novel chemical processes and novel chemical intermediates useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.Type: GrantFiled: August 1, 1977Date of Patent: December 19, 1978Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4128725Abstract: This invention comprises certain .omega.-aryl-.omega.-polynor analogs of the prostaglandins in which configuration of the 11-hydroxyl is beta. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.Type: GrantFiled: August 15, 1977Date of Patent: December 5, 1978Assignee: The Upjohn CompanyInventor: Ernest W. Yankee
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Patent number: 4126754Abstract: 11-Deoxy prostaglandin type compounds, i.e. prostaglandin type compounds in which the 11-hydroxy group is replaced by hydrogen, are disclosed, with processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, and labor induction at term.This is a division of application Ser. No. 609,410, filed Sept. 2, 1975.Type: GrantFiled: April 17, 1978Date of Patent: November 21, 1978Assignee: The Upjohn CompanyInventors: Gordon L. Bundy, Norman A. Nelson
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Patent number: 4125731Abstract: Novel indan compounds of the formula ##STR1## wherein A and X are each ethylene or vinylene; B is C.sub.2-4 alkylene; R and R.sub.2 are each hydrogen or C.sub.1-4 alkyl; R.sub.1 is C.sub.1-8 alkyl; <C = Z is <C = O, or ##STR2## and its non-toxic salts, which are useful as antiulcers, gastric secretion inhibitors, and hypotensors.Type: GrantFiled: December 8, 1976Date of Patent: November 14, 1978Assignee: Sumitomo Chemical Company, LimitedInventors: Akihiko Sugie, Hiromi Shimomura, Junki Katsube, Hisao Yamamoto
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Patent number: 4124623Abstract: Prostaglandin analogs with the following cyclopentane ring structure: ##STR1## are disclosed along with intermediates useful in their preparation and processes for their preparation. These analogs are useful for some of the same pharamcological purposes as the prostaglandins, particularly and especially as blood platelet aggregation inhibitors.Type: GrantFiled: June 23, 1977Date of Patent: November 7, 1978Assignee: The Upjohn CompanyInventor: David C. Peterson
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Patent number: 4121038Abstract: This invention comprises certain analogs of the prostaglandins in which the double bond between C-13 and C-14 is replaced by a triple bond. Also provided in this invention, are novel chemical processes and novel chemical intermediates useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.Type: GrantFiled: August 1, 1977Date of Patent: October 17, 1978Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4119648Abstract: The present specification provides novel intermediates and novel processes for the synthesis of various side chain and skeletal analogs of Thromboxane B.sub.2 (11.beta.-homo-11.alpha.-oxa-PGF.sub..alpha.). These analogs are particularly and especially useful as reproductive cycle control agents.Type: GrantFiled: September 6, 1977Date of Patent: October 10, 1978Assignee: The Upjohn CompanyInventor: William P. Schneider
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Patent number: 4119786Abstract: Prostaglandin analogs with the following cyclopentane ring structure: ##STR1## are disclosed along with intermediates useful in their preparation and processes for their preparation. These analogs are useful for some of the same pharmacological purposes as the prostaglandins, particularly and especially as blood platelet aggregation inhibitors.Type: GrantFiled: June 23, 1977Date of Patent: October 10, 1978Assignee: The Upjohn CompanyInventor: David C. Peterson
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Patent number: 4119785Abstract: Prostaglandin analogs with the following cyclopentane ring structure: ##STR1## are disclosed along with intermediates useful in their preparation and processes for their preparation. These analogs are useful for some of the same pharmacological purposes as the prostaglandins, particularly and especially as blood platelet aggregation inhibitors.Type: GrantFiled: June 23, 1977Date of Patent: October 10, 1978Assignee: The Upjohn CompanyInventor: David C. Peterson
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Patent number: 4118577Abstract: This invention is a group of 4,5,6-trinor-3,7-inter-m-phenylene prostaglandin-type compounds and processes for making them. These compounds are useful for a variety of pharmacological purposes, including hypotensive control and inhibition of platelet aggregation.A typical formula for a PGA.sub.Type: GrantFiled: January 31, 1977Date of Patent: October 3, 1978Assignee: The Upjohn CompanyInventor: Norman A. Nelson
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Patent number: 4118591Abstract: Prostaglandin analogs with the following cyclopentane ring structure: ##STR1## are disclosed along with intermediates useful in their preparation and processes for their preparation. These analogs are useful for some of the same pharmacological purposes as the prostaglandins, particularly and especially as blood platelet aggregation inhibitors.Type: GrantFiled: June 23, 1977Date of Patent: October 3, 1978Assignees: The Upjohn Company, The Upjohn CompanyInventor: David C. Peterson
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Patent number: 4117119Abstract: Prostaglandin analogues of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents trans-vinylene or ethylene and Y represents cis-vinylene or ethylene, R represents hydrogen or alkyl of 1 through 12 carbon atoms, R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, or alkyl of 1 through 12 carbon atoms or an aryl group, with the proviso that at least one of the symbols R.sup.1, R.sup.2 and R.sup.3 represents an alkyl or aryl group, are new compounds possessing useful pharmacological properties; they are especially useful for the treatment of gastric ulceration.Type: GrantFiled: May 6, 1977Date of Patent: September 26, 1978Assignee: Ono Pharmaceutical CompanyInventors: Masayasu Kurono, Hisao Nakai, Takashi Muryobayashi
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Patent number: 4117014Abstract: Prostaglandin type compounds of the formula ##STR1## wherein X is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-cis or--C.tbd.C--; Y is CH.sub.2 or O; Q is--CH.sub.2 --CH.sub.2 --or --CH.dbd.CH--; Z is H, OH, CH.sub.3 or CH.sub.2 OH, R is a linear, branched or cyclo alkyl chain of 3 to 7 carbon atoms or certain other moieties, and R" and R'''are H or CH.sub.3. These compounds are prepared by essentially a one-step reaction from a new intermediate of the formula ##STR2## wherein Z, R, R" and Q have the above meaning and P is a removable protective group by condensation with a reactive moiety introducing the entire .alpha.-chain (R'''=CH.sub.3). If desired, the carbonyl function is subsequently reduced to W= --CH(OH)--. The intermediate is useful in making known and new PGEs useful as antihypertensives, gastric acid secretion inhibitors and smooth muscle stimulants.Type: GrantFiled: December 23, 1976Date of Patent: September 26, 1978Assignee: Abbott LaboratoriesInventors: Andre G. Pernet, Hiromasa Nakamoto, Naoyasu Ishizuka
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Patent number: 4116988Abstract: Prostaglandin-type compounds with a phenoxy or substituted-phenoxy substituent at the C-16 position are disclosed, with processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, labor inducement at term, and wound healing.Type: GrantFiled: February 7, 1977Date of Patent: September 26, 1978Assignee: The Upjohn CompanyInventor: Norman A. Nelson
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Patent number: 4113961Abstract: This invention comprises certain analogs of the prostaglandins in which the double bond between C-13 and C-14 is replaced by a triple bond. Also provided in this invention, are novel chemical processes and novel chemical intermediates useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.Type: GrantFiled: August 1, 1977Date of Patent: September 12, 1978Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4113782Abstract: A process for the preparation of formylated phenoxy compounds characterized in that a methylated phenoxy compound such as p-methoxytoluene in oxidized in liquid phase under heating with pressurized gaseous oxygen in the presence of at least one of lower fatty acids and anhydrides thereof and by the aid of at least one of soluble salts of metals selected from the group consisting of cobalt, manganese, chromium and nickel, as catalyst.Type: GrantFiled: February 13, 1976Date of Patent: September 12, 1978Assignee: Agency of Industrial Science and TechnologyInventors: Imamura Juichi, Takehara Masahiko, Kizawa Kazuhiro
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Patent number: 4113963Abstract: This invention comprises certain analogs of the prostaglandins in which the double bond between C-13 and C-14 is replaced by a triple bond. Also provided in this invention, are novel chemical processes and novel chemical intermediates useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.Type: GrantFiled: August 1, 1977Date of Patent: September 12, 1978Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4113962Abstract: This invention comprises certain analogs of the prostaglandins in which the double bond between C-13 and C-14 is replaced by a triple bond. Also provided in this invention, are novel chemical processes and novel chemical intermediates useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.Type: GrantFiled: August 1, 1977Date of Patent: September 12, 1978Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4112225Abstract: A process for producing optically active 16-substituted prostaglandins and new 16-substituted prostaglandins produced thereby which are useful as cardiovascular agents and as agents for inducing labor in pregnant females and for the termination of pregnancy.Type: GrantFiled: December 8, 1976Date of Patent: September 5, 1978Assignee: Hoffman-La Roche Inc.Inventors: George William Holland, Jane Liu Jernow, Perry Rosen
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Patent number: 4111969Abstract: This invention comprises certain analogs of the prostaglandins in which there is a triple bond between C-5 and C-6 or C-4 and C-5. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.Type: GrantFiled: November 4, 1976Date of Patent: September 5, 1978Assignee: The Upjohn CompanyInventor: Chiu-Hong Lin
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Patent number: 4107427Abstract: The present specification provides novel intermediates and novel processes for the synthesis of various side chain and skeletal analogs of Thromboxane B.sub.2 (11.beta.-homo-11a-oxa-PGF.sub.2.alpha.). These analogs are particularly and especially useful as reproductive cycle control agents.Type: GrantFiled: August 20, 1976Date of Patent: August 15, 1978Assignee: The Upjohn CompanyInventor: Robert C. Kelly
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Patent number: 4104474Abstract: This invention comprises certain analogs of the prostaglandins in which the double bond between C-13 and C-14 is replaced by a triple bond. Also provided in this invention, are novel chemical processes and novel chemical intermediates useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.Type: GrantFiled: August 1, 1977Date of Patent: August 1, 1978Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4100352Abstract: Disclosed are prostaglandin analogues having the structural formula, ##STR1## in which: T is selected from the group consisting of carboxyl, alkoxycarbonyl or cyano;M is selected from the group consisting of carbonyl, R-hydroxymethylene or S-hydroxymethylene;L is selected from the group consisting of methylene or methine, provided L is methine only if J is methine;J is selected from the group consisting of methylene, ethylene, R-hydroxymethylene, S-hydroxymethylene or methine, provided J is methine only if L is methine;W is selected from the group consisting of ##STR2## T.sub.1 and T.sub.2 are attached to adjacent carbon atoms; T.sub.1 is selected from the group consisting of hydrogen or phenyl, provided T.sub.1 is phenyl only if T.sub.2 is lower alkyl;T.sub.2 is selected from the group consisting of n-pentyl or lower alkyl, provided T.sub.2 is lower alkyl only if T.sub.1 is phenyl;Or T.sub.1 and T.sub.2 are joined together to form an alkylene group of 4 or 6 carbon atoms.Type: GrantFiled: April 20, 1977Date of Patent: July 11, 1978Assignee: Miles Laboratories, Inc.Inventor: Robert Thomas Buckler
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Patent number: 4100185Abstract: Disclosed are prostaglandin analogues having the structural formula, ##STR1## in which: T is selected from the group consisting of carboxyl, alkoxycarbonyl or cyano;M is selected from the group consisting of carbonyl, R-hydroxymethylene or S-hydroxymetylene;L is selected from the group consisting of methylene or methine, provided L is methine only if J is methine;J is selected from the group consisting of methylene, ethylene, R-hydroxymethylene, S-hydroxymethylene or methine, provided J is methine only if L is methine;W is selected from the group consisting of ##STR2## T.sub.1 and T.sub.2 are attached to adjacent carbon atoms; T.sub.1 is selected from the group consisting of hydrogen or phenyl, provided T.sub.1 is phenyl only if T.sub.2 is lower alkyl;T.sub.2 is selected from the group consisting of n-pentyl or lower alkyl, provided T.sub.2 is lower alkyl only if T.sub.1 is phenyl;Or T.sub.1 and T.sub.2 are joined together to form an alkylene group of 4 or 6 carbon atoms.Type: GrantFiled: April 20, 1977Date of Patent: July 11, 1978Assignee: Miles Laboratories, Inc.Inventor: Robert Thomas Buckler
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Patent number: 4100353Abstract: Disclosed are prostaglandin analogues having the structural formula, ##STR1## in which: T is selected from the group consisting of carboxyl, alkoxycarbonyl or cyano;M is selected from the group consisting of carbonyl, R-hydroxymethylene or S-hydroxymethylene;L is selected from the group consisting of methylene or methine, provided L is methine only if J is methine;J is selected from the group consisting of methylene, ethylene, R-hydroxymethylene, S-hydroxymethylene or methine, provided J is methine only if L is methine;W is selected from the group consisting of ##STR2## T.sub.1 and T.sub.2 are attached to adjacent carbon atoms; T.sub.1 is selected from the group consisting of hydrogen or phenyl, provided T.sub.1 is phenyl only if T.sub.2 is lower alkyl;T.sub.2 is selected from the group consisting of n-pentyl or lower alkyl, provided T.sub.2 is lower alkyl only if T.sub.1 is phenyl; orT.sub.1 and T.sub.2 are joined together to form an alkylene group of 4 to 6 carbon atoms.Type: GrantFiled: April 20, 1977Date of Patent: July 11, 1978Assignee: Miles Laboratories, Inc.Inventor: Robert Thomas Buckler
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Patent number: 4098815Abstract: The present invention relates to novel not naturally occurring analogues of prostanoic acids of the formula ##STR1## as well as a process for their preparation. The compounds of the invention have valuable pharmacological properties similar to those of the natural prostaglandins and therefore can be used as medicaments.Type: GrantFiled: December 17, 1976Date of Patent: July 4, 1978Assignee: Hoechst AktiengesellschaftInventors: Milos Babej, Wilhelm Bartmann, Gerhard Beck, Ulrich Lerch
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Patent number: 4099013Abstract: This invention is a group of 4,5,6-trinor-3,7-inter-m-phenylene prostaglandin-type compounds and processes for making them. These compounds are useful for a variety of pharmacological purposes, including hypotensive control and inhibition of platelet aggregation.A typical formula for a PGE.sub.Type: GrantFiled: January 31, 1977Date of Patent: July 4, 1978Assignee: The Upjohn CompanyInventor: Norman A. Nelson
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Patent number: 4099015Abstract: This invention comprises certain analogs of the prostaglandins in which the double bond between C-13 and C-14 is replaced by a triple bond. Also provided in this invention, are novel chemical processes and novel chemical intermediates useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.Type: GrantFiled: August 1, 1977Date of Patent: July 4, 1978Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4099014Abstract: Prostaglandin analogs with the following cyclopentane ring structure: ##STR1## are disclosed along with intermediates useful in their preparation and processes for their preparation. These analogs are useful for some of the same pharmacological purposes as the prostaglandins, particularly and especially as blood platelet aggregation inhibitors.Type: GrantFiled: June 23, 1977Date of Patent: July 4, 1978Assignee: The Upjohn CompanyInventor: David C. Peterson
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Patent number: 4097496Abstract: The present invention relates to novel not naturally occurring 10,11-dihydro-derivatives of prostaglandins of the A-series as well as a process for their preparation. The compounds of the invention have an antiprostaglandin effect and may be used as medicaments for the inhibition or suppression of pharmacological properties of the prostaglandins.Type: GrantFiled: June 23, 1976Date of Patent: June 27, 1978Assignee: Hoechst AktiengesellschaftInventors: Milos Babej, Wilhelm Bartmann, Gerhard Beck, Ulrich Lerch
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Patent number: 4097516Abstract: Disclosed are prostaglandin analogues having the structural formula, ##STR1## in which: T is selected from the group consisting of carboxyl, alkoxycarbonyl or cyano;M is selected from the group consisting of carbonyl, R-hydroxymethylene or S-hydroxymethylene;L is selected from the group consisting of methylene or methine, provided L is methine only if J is methine;J is selected from the group consisting of methylene, ethylene, R-hydroxymethylene, S-hydroxymethylene or methine, provided J is methine only if L is methine;W is selected from the group consisting of --CH.sub.2 --CH-- or trans --CH.dbd.C--;T.sub.1 and T.sub.2 are attached to adjacent carbon atoms;T.sub.1 is selected from the group consisting of hydrogen or phenyl, provided T.sub.1 is phenyl only if T.sub.2 is lower alkyl;T.sub.2 is selected from the group consisting of n-pentyl or lower alkyl, provided T.sub.2 is lower alkyl only if T.sub.1 is phenyl;Or T.sub.1 and T.sub.2 are joined together to form an alkylene group of 4 or 6 carbon atoms.Type: GrantFiled: April 20, 1977Date of Patent: June 27, 1978Assignee: Miles Laboratories, Inc.Inventor: Robert Thomas Buckler
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Patent number: 4097519Abstract: 2,2-Difluoro prostaglandin E, F.sub..alpha., F.sub..beta., A and B analogs are disclosed with intermediates and with processes for making them. These compounds differ from the prostaglandins in that they have two fluoro atoms at the C-2 position in place of the two hydrogen atoms at C-2 in the prostaglandins. These compounds are useful for a variety of pharmacological purposes, including antiulcer, inhibition of platelet aggregation, increase in nasal patency, labor induction at term, and wound healing.Type: GrantFiled: September 17, 1976Date of Patent: June 27, 1978Assignee: The Upjohn CompanyInventor: Udo F. Axen
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Patent number: 4096336Abstract: Disclosed are prostaglandin analogues having the structural formula, ##STR1## in which: T is selected from the group consisting of carboxyl, alkoxycarbonyl or cyano;M is selected from the group consisting of carbonyl, R-hydroxymethylene or S-hydroxymethylene;L is selected from the group consisting of methylene or methine, provided L is methine only if J is methine;J is selected from the group consisting of methylene, ethylene, R-hydroxymethylene, S-hydroxymethylene or methine, provided J is methine only if L is methine;W is selected from the group consisting of --CH.sub.2 --CH-- or trans --CH.dbd.C--;T.sub.1 and T.sub.2 are attached to adjacent carbon atoms;T.sub.1 is selected from the group consisting of hydrogen or phenyl, provided T.sub.1 is phenyl only if T.sub.2 is lower alkyl;T.sub.2 is selected from the group consisting of n-pentyl or lower alkyl, provided T.sub.2 is lower alkyl only if T.sub.1 is phenyl;Or T.sub.1 and T.sub.2 are joined together to form an alkylene group of 4 or 6 carbon atoms.Type: GrantFiled: April 20, 1977Date of Patent: June 20, 1978Assignee: Miles Laboratories, Inc.Inventor: Robert Thomas Buckler
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Patent number: 4096337Abstract: The disclosure relates to novel 15-(3-aryl- or 3-aralkyl-cyclobutyl, -cyclopentyl and -cyclohexyl)-.omega.-pentanor prostaglandin analogues, for example 9.alpha.,11.alpha.,15.alpha.-trihydroxy-15-(trans-3-phenylcyclobutyl)-16,1 7,18,19,20-pentanor-5-cis,13-trans-prostadienoic acid, to pharmaceutical or veterinary compositions containing such a compound, and to a method of inducing luteolysis in animals by orally administering such a compound.Type: GrantFiled: June 1, 1976Date of Patent: June 20, 1978Assignee: Imperial Chemical Industries LimitedInventor: Peter Robert Marsham
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Patent number: 4096178Abstract: Prostaglandin-type compounds with a phenoxy or substituted-phenoxy substituent at the C-16 position are disclosed, with processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, labor inducement at term, and wound healing.Type: GrantFiled: February 10, 1977Date of Patent: June 20, 1978Assignee: The Upjohn CompanyInventor: Norman A. Nelson
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Patent number: 4096335Abstract: Prostaglandin-type compounds with a phenoxy or substituted-phenoxy substituent at the C-16 position are disclosed, with processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, labor inducement at term, and wound healing.Type: GrantFiled: February 7, 1977Date of Patent: June 20, 1978Assignee: The Upjohn CompanyInventor: Norman A. Nelson
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Patent number: 4096179Abstract: Prostaglandin-type compounds with a phenoxy or substituted-phenoxy substituent at the C-16 position are disclosed, with processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, labor inducement at term, and wound healing.Type: GrantFiled: February 10, 1977Date of Patent: June 20, 1978Assignee: The Upjohn CompanyInventor: Norman A. Nelson
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Patent number: 4096267Abstract: [1-Oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]aklanoic acid, derivatives thereof, their salts, esters and amides are disclosed. The products display a dual pharmaceutical utility in that they exhibit diuretic, saluretic and uricosuric activity. Also disclosed are processes for the preparation of such [1-oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]alkanoic acids, pharmaceutical compositions comprising therapeutically effective amounts of such compounds and methods of treatment comprising administering such compounds and compositions.Type: GrantFiled: June 10, 1975Date of Patent: June 20, 1978Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
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Patent number: 4091015Abstract: 9-Oxo-15-Substituted prostanoic acids, and intermediates for their preparation are disclosed. The final products have bronchodilatory activity.Type: GrantFiled: May 17, 1974Date of Patent: May 23, 1978Assignee: American Home Products CorporationInventor: Donald P. Strike