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METHOD FOR THE PRODUCTION OF AMINO CROTONYL COMPOUNDS (Wed, 26 Sep 2007)
(12) NACH DEM VERTRAG LBER DIE INTERNATIONALE ZUSAMMEN ARBEIT AW DEM GEBIET DES I'ATENTWESENS (PCT) VEROKKEN TLICHTE INTERNATIONALE ANMELDUNG (19) VVeltorj>anisatk>n fur jii-islijjos Linen lum Internationales Biir (43) Internationales VeroiTenlliehrin>>sdaluni (10) Internationale VorolTi-ntlic!iungsnummer 28. April 2005(28.04.2005) PCT WO 2005/037824 A3 (51) Internationale PalcntklassHik:iti<>n': C071) 41)5/12, 10, 88400 BIBERACH (DE) SIEGER. Peler (DE/DE|: AO IK 31/505. Λ(.||· 35/(X) Klingenacker 7.88441 ΜΓΙΊ LI.BIBERACH (DI >. (74) Gomelnsainer Verlrcler: BOEHRINGER INGEL- (21) Internationales Aklt-nzt-ichen: PCT/l:P2OO4/0l 1378 HEIM INTERNATIONAL GMBH; Binder Strasse 173. 55216 INGELHEIM (DF.i. (22) Internationales Antnoldediilinii: 12. Okiober 2004 (12 10.2004) (81 ) Besliiiuiiungsslaiilen (saweil nit hi antlers an geg ben, ( r jede veifiigbare national)' Schiil:rechlsarr): ΛΕ, AG. AL. ( 5) Eiiimchiiiijjssoniclie: D ulseh AM. AT. All. ΛΖ. BA. BB. BG, BR. BW, BY, BZ. CA. CI I. CN. CO, OR. CM. ("/., E, l)K, DM. DZ, EC. EE. HG. ES. H. GB, GD, GE. GH. GM.11R. I II I, ID, II., IN. IS. JP, Kli. ( 6) VcrnnVnllichun&sspraehe: Deuisch KG, KP. KR, KZ, l.C, I. , l.R. LS. I.T, I.U. I.V. MA. Ml), MG. MK. MN, MW, MX. MZ. NA, NI, NO, NZ, OM. G. (30) Ληι-ati ii .iir Prlorilal: I'll, PI.. IT, RO, RU, SC, SI). SE, SG. SK. SI., SY.TJ, M. 1034') J 139 17. Okloher 2003 (17.10.2003) 1)1· TN, TR. n, TZ, HA. UG. US, UZ. VC, VN, YU. ZA. ZM. 7.W. (71) Ariimldir urfiir AC. AG. ΛΙ, AM. AT. At'. A/.. ΒΛ. ««. Hh. HO. K. BY. (7/. CO. CK. CO. CY. (K4) Bcsliinmungsstaatcn > veit nicht anders a ge^cben. fur C7.. OK. DM. OZ. kC. Ft. hO. F.S. H. Oil. GO. Ok. Oil. jede ve.ijiigbare regionale lnii:rechisarl): ARII'O (BW. OM. UK. III'. II). It.. IN. IS. JR Α'Λ.'. KG. Kl>. K . K/.. IX. Gil, GM. KE, LS. MW. MZ. NA. SD, SI.. SZ. TZ. IJG. I K. IK. I.S. I.I. LI'. I V. MX MP. MO. MK. MN. MW. MX. ZM. ZW). cura-isclics (AM, ΛΖ. BY. KG, KZ, MD. RU. MY.. NA. Nl. NO. NA OM. /'(.'. PH. I'L ΓΤ. KO. KU. SC. T),TM),europai ches(AT, BE, BG.CU.CY.CZ. DE. DK. so. si:, .S' SK. SI., SY. S/. I I. IM, TN. IK. TT. r/.. tix EE. liS. I I. I R.GB.GR. Mil, Hi. IT. LU. MC. Nl.. PL. PI. t'G. V/.. C. VN. YD. /A. 7.M. YAVf- KOKHRINGKR RO. SR. SI, SK. TR). OAPI (BE, BJ. CK CG, CI. CM, GA. INGELHEIM INTERNATIONAL GMBH |I)E/Dli|; GN. GQ. GW. ML. MR, NL. SN, I I). TG). Binder 173. 1 f. INGELHEIM (1)1·). VvrolTi-nllichl: — mil internal 'n lem lien henherit (71) Amiuldcr tniirjiii /) ·.): BOEHRLNGER INGELHEIM — · viir Ahlauf tier fill Andrnmgen tier Ansp Ut he gelirnJrn PHARMA JMBH * CO. MI |l)I Dfc'|; Biitger Slrasse Frist; Yeroffenlli ung irj n-iedfrh lt. Jails Antlentiiiien 173. 55211. INGELHEIM (Dili. cintrefjen (72) Erlliidi'r: und (SK) VorofTcntll liunjjsdaluiii des iii(onia(ioiiakn (75) Krlindt-r/Aiiiiielder (nur (iir US): RALL. Werner li nb ri lils: 21. !U05 11)1 /1 >li(. Beeiboveiisli. 33. 8X441 ΜΓΠ'ΕΙ.ΒΙΒΕΚΛΙ Π ( 1)1 SO ΚΛ. Raiin-r |Ι)Ι·71)Ι·:|: Gesehwisler-Scholl-Sir. /.in krkltinntft tier /.u t ibui hsliihen-Cihlrs nnJ t er anJrrm Al> l i. SS40O BIBERACH 11)1·). KUI.INNA, Christian ktir u>i):eii vtirj auf Jir liikliii gen {"Outdance Nates mi Ca- |I>I7I)E|. Iriedholstr. '). XX44X ΑΊ TENWEILF.R 11)1:1. ties and Abbreviations ") am An/any jeder regulart ii Aus «al>r tier SCH AUBELT, .Iiiergcn |I)E/I)E|: C nsulcntengasse I'C I -Gazette verwiesen. 154) Tillr: METHOD LOR HIE PRODUCTION ΟΓ AMINO CROTONYL COMPOUNDS -→ (54) B /i'khmini;: VERI ΛΙ IREN ZUR IIERS'l EI.I.UNCi VON AMINOCROIONYI.VERBINDUNGEN 00 t-m 1 1 hstra l: I lie inv niion r laic's lo an improved mclhod lor (he produtlion of 4-|(3-e loru-4 lluorophenyl )amim 11 t-(N.N iliuielli laiiiino). I -oxo-2 hulene- 1 -yl |ainino | -7 ((S)-letrahydrofurjne-3-yloxy |uina/.iiline and related amino crolonyl coniixxinds. The invenlioi) al o relates to a .suitable sail i>i 4-|(3-cliloro-4-lluorpheriyl >ainino| 1|4 (N.N dimelhylainiiio)- 1 -oxo-2-liuiene I - »?i o I jaiiiiiui ) 7 i(Si ielnihydri>ruraiie-3-yloxy) quina/.iiline for use as an a live iiigrcclicnl lora inedieanienl. (57) ZuMiiniiH-iifiissuiiK: Die l-rlituliin helrilft ein verbesserles Verla reit ur llctslcllung von 4-[(3 (,'hl r-4-Iluorplie-c nyl ianiiiio|-b-| |4-(N.N-dimelhvlamini') I -oo-2-bulen - 1 - l|amino | -7-((S)-ieiraliydrofuran- -yl xy )-chin:i_ lin un ver andlcr Aminoerolonylverhinduii en und die lleisielluni cines j!eei^neien Sal/es von 4-|( -Chli>r-4-lluiirplicnyliamin»>|-()-ll''-(N.N-dime- Ihylaniinol- 1 o-2-bulen.1 -yl|amin» | - 7-((S) lelraliydroluraii-3-yloxy l-chiita/oliu .ur Verwenduiti; als Ar/neimiliehvirksioll'.
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Crystalline salts of a potent HCV inhibitor (Thu, 23 Aug 2012)
This invention relates to novel tris(hydroxymethyl)aminomethane, choline and N-methyl-D-glucamine salt forms of the following Compound (1) and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:
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DIGITOXIN ESTERS (Wed, 17 Mar 1976)
1428041 Digitoxin esters BOEHRINGER INGELHEIM GmbH 30 May 1973 [31 May 1972] 25852/73 Heading C2U The invention comprises digitoxin 3111-esters with R2CO 2 H where R2 is C 2 -C 15 alkyl, halo- C 1 -C 4 alkyl, cyano-C 1 -C 4 alkyl, ethoxycarbonyl-C 1 -C 4 alkyl, phenyl-C 1 -C 4 alkyl, phenoxy-C 1 -C 4 alkyl (said phenyl and phenoxy moieties being optionally substituted), C 3 -C 6 cycloalkyl, (C 3 -C 6 cycloalkyl)methyl or (trifluoroacetamido)ethyl; and their preparation from digitoxin by esterification, either direct or via 3111,4111-(alkyl orthoesters). Cardiotonic compositions for oral, rectal and parenteral administration comprise a carrier and a compound of the invention.
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HETEROARYLCARBOXAMIDE DERIVATIVES AS PLASMA KALLIKREIN INHIBITORS (Thu, 04 May 2017)
The present invention relates to compounds of general formula I, wherein D1 to D3, A, R1, R2, Y and n are defined as in claim 1, which have valuable pharmacological properties, in particular are inhibitors of plasma kallikrein. The compounds are suitable for treatment and prevention of diseases which can be influenced by influenced by inhibition of plasma kallikrein, such as diabetic complications, particularly in the treatment of retinal vascular permeability associated with diabetic retinopathy and diabetic macular edema.
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2-ARYL-AMINO-IMIDAZOLINE-2 COMPOUNDS (Wed, 06 Nov 1974)
1373276 2 - Aryl - amino - imidazoline (2) compounds BOEHRINGER INGELHEIM GmbH 21 Jan 1972 [21 Jan 1971] 3031/72 Heading C2C Novel compounds of the Formula I wherein R 1 , R 2 and R 3 which may be the same or different and are hydrogen, fluorine, chlorine, bromine, methyl or ethyl and R 4 is and acid addition salts thereof may be prepared (a) by reaction of a compound II with R 4 CH 2 -Hal, where Hal is chlorine, bromine or iodine or (b) by reaction of a compound IV wherein A is cyano or -C(Y) : NH (in which Y is C 1-4 alkoxy or alkyl thio, amino or mercapto) with ethylene diamine or an acid addition salt thereof and optionally forming a salt of I. Pharmaceutical compositions of the compound I show analgesic activity and lower blood pressure when administered orally, parenterally, rectally or enterally with the usual excipients.
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PREPARATION OF DIHYDROTHIENO [3, 2-D] PYRIMIDINES AND INTERMEDIATES USED THEREIN (Fri, 29 Jul 2011)
Patent 584962 Disclosed herein is a method for preparing 3-oxo-tetrahydrothiophene derivatives of formula 6, comprising the steps of: a) reacting reagents of the formulas HS-CH2-CO2Ra and CHR5=CR4-CO2Ra to obtain an intermediate of formula 7, b) cyclising the intermediate of formula 7 in a solvent and in the presence of TiCl2(OiPr)2, TiCl(OiPr)3, TiCl3(OiPr) (Titanium Chloride Isopropyl compounds) or chiral variants thereof and in the presence of an amine base to obtain the intermediate of formula 6, wherein the substitutents are as defined within the specification and further wherein the intermediate of formula 6 maybe used in a subsequent reaction step without the need for chromographic purification in that step or optionally , all steps thereafter.
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NOVEL IMIDAZOLINES, THE PREPARATION THEREOF AND COMPOSITIONS CONTAINING THE SAME (Wed, 28 Jun 1972)
1279931 Analgesic &c medicines BOEHRINGER INGELHEIM GmbH 18 Nov 1970 [19 Nov 1969] 54835/70 Heading ASB [Also in Division C2] Pharmaceutical compositions having analgesic and blood-pressure decreasing activity comprise, as active ingredient, a 2-(N-phenyl- N-allyl-amino)-imidazoline-(2) of the general formula: wherein each of R 1 , R 2 and R 3 is a hydrogen, fluorine, chlorine or bromine atom or a C 1-3 alkyl, C 1-3 alkoxy, trifluoromethyl or cyano group and each of R 4 and R 5 is a hydrogen or chlorine atom or a methyl group, or a physiologically acceptable acid addition salt thereof, in association with a pharmaceutical carrier or excipient and optionally a further physiologically active ingredient, e.g. a spasmolytic, antihypertonic, sedative or tranquillizer, and may be administered orally, parenterally or enterally as tablets, capsules, suppositories, solutions and powders (optionally containing disintegrants, lubricants and/or sustained release effect substances).
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Tripeptides having a hydroxyproline ether of a substituted quinoline for the inhibition of NS3 (Hepatitis C) (Thu, 03 Apr 2003)
Disclosed herein are compounds of formula (I), wherein R1 is hydroxy or NHSO2R1A wherein R1A is (C1-8)alkyl, (C3-7)cycloalkyl or {(C1-6)alkyl-(C3-7)cycloalkyl}, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O-(C1-6)alkyl, amido, amino or phenyl, or R1A is C6 or C10 aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O-(C1 6)alkyl, amido, amino or phenyl; R2 is (C4-6)cycloalkyl; R3 is t-btuyl or (C5-6)cycloalkyl and R4 is (C4-6)cycloalkyl; or a pharmaceutically acceptable salt thereof. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of Hepatitis C.
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Heterocyclic tripeptides as hepatitis c inhibitors (Thu, 03 Apr 2003)
Compounds of formula (I):wherein R1 is hydroxyl or sulfonamide derivative; R2 is t−butyl or −CH2−C(CH3)3 or −CH2−cyclopentyl; R3 is t−butyl or cyclohexil and R4 is cyclobutyl, cyclopentyl or cyclohexyl; or a pharmaceutically acceptable salt thereof, are described as useful as inhibitor of the HCV NS3 protease.
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Macrocyclic peptides active against the hepatitis C virus (Thu, 31 Aug 2006)
Patent 534929 Compounds of general formula I or a pharmaceutically acceptable salt thereof, useful as inhibitors of the HCV NS3 protease.
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CRYSTALLINE SALTS OF A POTENT HCV INHIBITOR (Thu, 15 Sep 2011)
This invention relates to novel tris(hydroxymethyl)aminomethane, choline and N-methyl-D-glucamine salt forms of the following Compound (1) and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:
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HEPATITIS C INHIBITING COMPOUNDS (Thu, 25 Nov 2004)
Compounds of formula (I) wherein B, X, R3, R21, R22, R1 and Rc are defined herein. The compounds are useful as inhibitors of HCV NS3 protease.
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ANALOGUES OF PROSCILLARIDIN (Wed, 13 Nov 1974)
1374079 Proscillaridin esters BOEHRINGER INGELHEIM GmbH 22 Dec 1971 [23 Dec 1970] 59726/71 Heading C2U The invention comprises compounds of formula wherein R 1 is the group R 2 is C 1-4 haloalkyl, (cycloalkyl)-C 1-4 alkyl, C 2-4 alkyl, C 3-8 cyeloalkyl, aryl, haloaryl, aralkyl; ar-haloaralkyl, or, when R 3 is other than H or acetyl, R 2 may be methyl; R 3 is H, C 1-3 alkyl, acetyl, heteroaroyl (e.g. thenoyl) or -COR1 2 where R1 2 is as defined for R 2 , the groups R 2 and R1 2 being the same or different. Preparation of compounds I is by selective hydrolysis of compounds of formula (wherein R 4 is C 1-4 alkyl), e.g. using aqueous acid. Preparation of compounds IVa is by reaction of proscillaridin with R 2 -C(OR 4 ) 3 , followed when required by alkylation or acylation of the 41-hydroxy group. Compounds I are said to be cardioactive, and may be made up with carriers into pharmaceutical compositions for oral, rectal and parenteral administration. Reference has been directed by the Comptroller to Specifications 1,286,232 and 1,266,251.
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FURYLMETHYLAMINOIMIDAZOLINES (Wed, 16 Jan 1974)
1344022 2-(N-Phenyl-N-furylmethyl-amino)- imidazolines-(2) BOEHRINGER INGELHEIM GmbH 23 June 1972 29635/72 Heading C2C [Also in Division A5] Novel 2 - (N - phenyl - N - furylmethylamino) - imidazolines - (2) of the general formula wherein each of R 1 , R 2 and R 3 is a hydrogen, fluorine, chlorine or bromine atom or a methyl, ethyl, methoxy, trifluoromethyl or cyano group and R 4 is a hydrogen atom or a methyl or ethyl group, and acid addition salts thereof are prepared (a) by reaction of a 2-phenylaminoimidazoline-(2) of the general formula with a furyl methyl halide of the general formula wherein Hal is a chlorine, bromine or iodine atom; (b) by reaction of an N-phenyl-N-furymethylamine of the general formula wherein A is a cyano group or a group of the formula -C(Y)=NH, in which Y is an alkoxy or alkylthio group of up to 4 carbon atoms or an amino or mercapto group, with ethylenediamine or an acid addition salt thereof; and (c) by reaction of a salt of the general formula wherein M is a metal or ammonium cation and n represents the charge on said cation, with a furylmethyl halide of the third general formula above (a 1-furylmethyl-2-phenylamino-2-imidazoline is also produced); followed optionally by conversion of a resulting free base into an acid addition salt thereof.
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HEPATITIS C INHIBITOR PEPTIDE ANALOGS (Thu, 25 Nov 2004)
Compounds of formula (I) : wherein B, Y, R3, R24, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease.
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Heterocyclic tripeptides as hepatitis C inhibitors (Fri, 23 Dec 2005)
Patent 534730 A compound of formula (I) wherein R1 is hydroxy or NHSO2R1A wherein R1A is (C1-8)alkyl, (C3-7)cycloalkyl or {(C1-6)alkyl-(C3-7)cycloalkyl}, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O-(C1-6)alkyl, amido, amino or phenyl, or R1A is C6 or C10 aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O-(C1-6)alkyl, amido, amino or phenyl; R2 is t-butyl, -CH2-C(CH3)3, or -CH2-cyclopentyl; R3 is t-butyl or cyclohexyl and R4 is cyclobutyl, cyclopentyl, or cyclohexyl; or a pharmaceutically acceptable salt thereof.
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PREPARATION OF CATALYSTS (Fri, 18 May 2007)
The present invention discloses a novel synthesis method for a catalyst of formula (6), wherein n is an integer from 1 to 3, R1 is a substituent and L is a neutral ligand.
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MESYLATE SALT FORMS OF A POTENT HCV INHIBITOR (Thu, 03 Oct 2013)
This invention relates to novel mesylate salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in methods for the treatment of Hepatitis C Viral (HCV) infection.
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THIOPHOSPHATES AND THIOPHOSPHONATES (Wed, 16 Sep 1970)
1,205,099. Halogen-substituted thiophosphates and thiophosphonates. BOEHRINGER INGELHEIM G.m.b.H. 4 Dec., 1968 [4 Dec., 1967; 27 Feb., 1968], No. 57625/68. Heading C2C. [Also in Division A5] Novel compounds of the general formula where R 1 is C 1-4 alkyl, R 2 is C 1-4 alkyl or alkoxy, or a phenyl group, and R 3 is -S(O) n R 4 (where n is 0 or 1 and R 4 is C 1-8 alkyl, or cyclohexyl) with the proviso that R 3 does not represent a 4-alkylthio group containing from 1 to 3 carbon atoms when the two chlorine atoms are in the 2- and 5-, or 3- and 5-positions, are prepared by reacting a phenol of formula with a compound of formula (R 1 O)(R 2 )P(S)X, where X is chlorine or bromine, preferably in the presence of an acid-binding agent and at elevated temperature. The phenol reactants may be used in the form of their salts. The products have pesticidal properties. 1 - Methylthio - 2,3,6 - trichlorobenzene is prepared by reacting 1,2,3,4-tetrachlorobenzene with methyl mercaptan in the presence of methyl alcohol and NaOH. 1-Methylthio-3,4- dichlorophenol and 1-methylthio-3,6-dichloro phenol are prepared by reacting 1-methylthio- 2,3,6 - trichlorobenzene with methanol and NaOH. 2 - Methylsulphinyl - 3,4 - dichlorophenol is prepared by oxidizing the corresponding 2-methylthio compound with H 2 O 2 in glacial acetic acid.
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MODIFIED CYCLIC DINUCLEOTIDE COMPOUNDS (Thu, 27 Sep 2018)
Compounds of formula (I) wherein Base1 and Base2 are defined as in claim 1 are modulators of STING.
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