HUP0303624A2 - NEP inhibitor hatású N-fenpropil-ciklopentil-csoporttal szubsztituált glutáramid származékok és ezeket tartalmazó gyógyászati készítmények és eljárás a vegyületek előállítására - Google Patents

NEP inhibitor hatású N-fenpropil-ciklopentil-csoporttal szubsztituált glutáramid származékok és ezeket tartalmazó gyógyászati készítmények és eljárás a vegyületek előállítására

Info

Publication number
HUP0303624A2
HUP0303624A2 HU0303624A HUP0303624A HUP0303624A2 HU P0303624 A2 HUP0303624 A2 HU P0303624A2 HU 0303624 A HU0303624 A HU 0303624A HU P0303624 A HUP0303624 A HU P0303624A HU P0303624 A2 HUP0303624 A2 HU P0303624A2
Authority
HU
Hungary
Prior art keywords
group
heterocyclyl
carbocyclyl
alkyl
groups
Prior art date
Application number
HU0303624A
Other languages
English (en)
Inventor
Stephen Challenger
Andrew Simon Cook
Adam Thomas Gillmore
Donald Stuart Middleton
David Cameron Pryde
Alan Stobie
Original Assignee
Pfizer Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0107750A external-priority patent/GB0107750D0/en
Priority claimed from GB0113112A external-priority patent/GB0113112D0/en
Priority claimed from GB0120152A external-priority patent/GB0120152D0/en
Application filed by Pfizer Inc. filed Critical Pfizer Inc.
Publication of HUP0303624A2 publication Critical patent/HUP0303624A2/hu
Publication of HUP0303624A3 publication Critical patent/HUP0303624A3/hu

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/82Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D319/00Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/101,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/141,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/161,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18Ethylenedioxybenzenes, not substituted on the hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0034Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0034Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • A61K9/0036Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/12Aerosols; Foams
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/39Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
    • C07C323/40Y being a hydrogen or a carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40Acylated substituent nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/81Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/74Benzo[b]pyrans, hydrogenated in the carbocyclic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/62Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to atoms of the carbocyclic ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/06Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00Systems containing two condensed rings
    • C07C2602/02Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane

Abstract

A találmány tárgyát N-fenpropil-ciklopentil-csoporttal szubsztituáltglutáramid-származékok, valamint ezeket tartalmazó gyógyászatikészítmények és egy vagy több további hatóanyagot tartalmazókombinációk képezik; e vegyületek a neutrális endopeptidáz enzim (MEP)inhibitoraiként viselkednek, a találmány tárgyához tartozik az (I)általános képletű vegyületek előállítására szolgáló eljárás is. Az (l)általános képletben a szubsztituensek jelentése igen sokféle, ígypéldául R1 jelentése alkilcsoport, amely egy vagy több szubsztituensthordozhat, ahol a szubsztituensek lehetnek például halogénatom,hidroxil-, alkoxi-, karbociklil-, heterociklil-, -NR2R3, -NR4COR5, -NR4SO2R5, -CONR2R3, -S(O)pR6, -COR7 vagy CO2 csoport; vagy R1jelentése karbociklil- vagy heterociklilcsoport, amely csoportokmindegyike egy vagy több szubsztituenst hordozhat: vagy R1 jelentésehidrogénatom, 1-6 szénatomos alkoxicsoport, -NR2R3 vagy -NR4SO2R5;ahol R2 és R3 jelentése karbociklil- vagy heterociklilcsoport, amelycsoportok mindegyike alkil-, hidroxil- vagy alkoxicsoporttal lehetszubsztituálva; vagy hidrogénatom vagy alkilcsoport; vagy R2 és R3 anitrogénatommal együtt, amelyhez kapcsolódnak pirrolidinil-,piperidino-, morfolino-, piperazinil- vagy N-piperazinil-csoportotképeznek; R4 jelentése hidrogénatom vagy alkilcsoport; R5 jelentésepéldául alkil-, -CF3, karbociklil-, heterociklil-, alkoxicsoport vagy-NR2R3; R6 jelentése alkil-, karbociklil-, heterociklilcsoport vagy -NR2R3; és R7 jelentése alkil-, karbociklil- vagy heterociklilcsoport;p értéke 0, 1, 2 vagy 3; X jelentése -(CH2)n- vagy -CH2)qO- kapcsolócsoport, ahol az Y csoport az oxigénatomhoz kapcsolódik; ahol akapcsoló csoportokban lévő egy vagy több hidrogénatom helyettegymástól függetlenül állhat például alkoxi-, hidroxil-, hidroxil-alkil-, cikloalkil-, heterociklilcsoport; n értéke 3, 4, 5, 6 vagy 7;továbbá q értéke 2, 3, 4, 5 vagy 6; továbbá Y jelentése fenil- vagypiridilcsoport, amely csoportok bármelyike egy vagy több R8 csoporttallehet szubsztituálva, ahol az R8 csoport lehet azonos vagy egymástóleltérő, ahol R8 jelentése például hidroxil-, merkaptocsoport, ciano-,acil-, amino-, karbociklil- vagy heterociklilcsoport - amely csoportokadott esetben szubsztituálva lehetnek; vagy a szomszédos szénatomokonlévő két R8 csoport a kapcsolódó szénatomokkal együtt 5- vagy 6 tagúkondenzált karbociklil- vagy heterociklil gyűrűt képezhetnek. Atalálmány szerinti vegyületek eredményesen alkalmazhatók a nőiszexuális diszfunkció és a férfi erekciós diszfunkció kezelésére. Ó
HU0303624A 2001-03-28 2002-03-18 N-phenpropylcyclopentyl-substituted glutaramide derivatives as nep inhibitors for fsad and process for preparation of the compounds HUP0303624A3 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0107750A GB0107750D0 (en) 2001-03-28 2001-03-28 Novel pharmaceuticals
GB0113112A GB0113112D0 (en) 2001-05-30 2001-05-30 Novel pharmaceuticals
GB0120152A GB0120152D0 (en) 2001-08-17 2001-08-17 Novel pharmaceuticals
PCT/IB2002/000807 WO2002079143A1 (en) 2001-03-28 2002-03-18 N-phenpropylcyclopentyl-substituted glutaramide derivatives as nep inhibitors for fsad

Publications (2)

Publication Number Publication Date
HUP0303624A2 true HUP0303624A2 (hu) 2004-03-01
HUP0303624A3 HUP0303624A3 (en) 2005-06-28

Family

ID=27256128

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0303624A HUP0303624A3 (en) 2001-03-28 2002-03-18 N-phenpropylcyclopentyl-substituted glutaramide derivatives as nep inhibitors for fsad and process for preparation of the compounds

Country Status (34)

Country Link
EP (1) EP1373192A1 (hu)
JP (1) JP4018545B2 (hu)
KR (1) KR100564466B1 (hu)
CN (1) CN1243723C (hu)
AP (1) AP1689A (hu)
AR (1) AR035795A1 (hu)
BG (1) BG108130A (hu)
BR (1) BR0208455A (hu)
CA (1) CA2437113A1 (hu)
CZ (1) CZ20032534A3 (hu)
DO (1) DOP2002000364A (hu)
EA (1) EA006154B1 (hu)
EE (1) EE200300469A (hu)
GE (1) GEP20063783B (hu)
HK (1) HK1060724A1 (hu)
HR (1) HRP20030751A2 (hu)
HU (1) HUP0303624A3 (hu)
IL (1) IL157009A0 (hu)
IS (1) IS6877A (hu)
MA (1) MA26996A1 (hu)
MX (1) MXPA03006597A (hu)
MY (1) MY134081A (hu)
NO (1) NO20034299L (hu)
NZ (1) NZ527012A (hu)
OA (1) OA12553A (hu)
PA (1) PA8542401A1 (hu)
PE (1) PE20021014A1 (hu)
PL (1) PL365101A1 (hu)
RS (1) RS75303A (hu)
SK (1) SK11822003A3 (hu)
TN (1) TNSN02032A1 (hu)
TW (1) TWI254038B (hu)
UY (1) UY27227A1 (hu)
WO (1) WO2002079143A1 (hu)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040014761A1 (en) * 1997-10-28 2004-01-22 Place Virgil A. Treatment of female sexual dysfunction with phosphodiesterase inhibitors
US7183410B2 (en) 2001-08-02 2007-02-27 Bidachem S.P.A. Stable polymorph of flibanserin
UA78974C2 (en) 2001-10-20 2007-05-10 Boehringer Ingelheim Pharma Use of flibanserin for treating disorders of sexual desire
US10675280B2 (en) 2001-10-20 2020-06-09 Sprout Pharmaceuticals, Inc. Treating sexual desire disorders with flibanserin
EP1441707A1 (en) * 2001-11-09 2004-08-04 Pharmacia AB Anti-muscarinic agent and estrogen-agonist for treating unstable or overactive bladder
GB0130219D0 (en) * 2001-12-18 2002-02-06 Pfizer Ltd Compounds for the treatment of sexual dysfunction
GB0230036D0 (en) * 2002-12-23 2003-01-29 Pfizer Ltd Novel pharmaceuticals
GB0230025D0 (en) * 2002-12-23 2003-01-29 Pfizer Ltd Novel pharmaceuticals
PA8597401A1 (es) * 2003-03-14 2005-05-24 Pfizer Derivados del acido 3-(1-[3-(1,3-benzotiazol-6-il) propilcarbamoil] cicloalquil) propanoico como inhibidores de nep
US7452875B2 (en) 2003-09-26 2008-11-18 Solvay Pharmaceuticals Gmbh Amidomethyl-substituted 1-(carboxyalkyl) cyclopentyl-carbonylamino-benzazepine-N-acetic acid compounds, process and intermediate products for their preparation and pharmaceutical compositions containing them
US7427611B2 (en) 2003-09-26 2008-09-23 Solvay Pharmaceuticals Gmbh Amidomethyl-substituted 1-(carboxyalkyl)-cyclopentyl-carbonylamino-benzazepine-N-acetic acid compounds, process and intermediate products for their preparation and pharmaceutical compositions containing them
US7262184B2 (en) 2003-09-26 2007-08-28 Solvay Pharmaceuticals Gmbh Amidomethyl-substituted 1-(carboxyalkyl) cyclopentyl-carbonylamino-benzazepine-N-acetic acid compounds, process and intermediate products for their preparation and pharmaceutical compositions containing them
US7649002B2 (en) 2004-02-04 2010-01-19 Pfizer Inc (3,5-dimethylpiperidin-1yl)(4-phenylpyrrolidin-3-yl)methanone derivatives as MCR4 agonists
WO2005107810A2 (en) 2004-05-11 2005-11-17 Emotional Brain B.V. Pharmaceutical formulations and uses thereof in the treatment of female sexual dysfunction
US20060025420A1 (en) * 2004-07-30 2006-02-02 Boehringer Ingelheimn International GmbH Pharmaceutical compositions for the treatment of female sexual disorders
WO2006027680A1 (en) * 2004-09-10 2006-03-16 Pfizer Limited 3-(1-carbamoylcyclohexyl) propionic acid derivatives as inhibitors of neutral endopeptidase enzyme
JP2009503020A (ja) 2005-08-03 2009-01-29 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 肥満症の治療におけるフリバンセリンの使用
JP2009513604A (ja) 2005-10-29 2009-04-02 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 月経前障害及び他の女性の性的障害治療用のベンゾイミダゾロン誘導体
EP1790343A1 (en) * 2005-11-11 2007-05-30 Emotional Brain B.V. Pharmaceuticals formulations and uses thereof in the treatment of female sexual dysfunction
DE602007004615D1 (de) 2006-06-30 2010-03-18 Boehringer Ingelheim Pharma Flibanserin zur behandlung von harninkontinenz und assoziierten erkrankungen
KR20090042967A (ko) 2006-08-14 2009-05-04 베링거 인겔하임 인터내셔날 게엠베하 플리반세린 제형 및 이의 제조방법
AU2007287639A1 (en) 2006-08-25 2008-02-28 Boehringer Ingelheim International Gmbh Controlled release system and method for manufacturing the same
EP2099767A1 (en) * 2006-11-01 2009-09-16 Brystol-Myers Squibb Company Modulators of glucocorticoid receptor, ap-1, and/or nf- b activity and use thereof
EP1925307A1 (en) 2006-11-03 2008-05-28 Emotional Brain B.V. Use of 3-alpha-androstanediol in the treatment of sexual dysfunction
PE20091188A1 (es) 2007-09-12 2009-08-31 Boehringer Ingelheim Int Compuesto 1-[2-(4-(3-trifluorometil-fenil)piperazin-1-il)etil]-2,3-dihidro-1h-benzimidazol-2-ona (flibanserina), sus sales de adicion y composiciones farmaceuticas que los contienen
US8993631B2 (en) 2010-11-16 2015-03-31 Novartis Ag Method of treating contrast-induced nephropathy
US8877815B2 (en) * 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
EP3082428A4 (en) 2013-12-09 2017-08-02 Respira Therapeutics, Inc. Pde5 inhibitor powder formulations and methods relating thereto
MA41562B1 (fr) 2015-06-03 2019-05-31 Bristol Myers Squibb Co Agonistes d'apj 4-hydroxy-3-(heteroaryl)pyridine-2-one a utiliser dans le traitement de troubles cardio-vasculaires
MX2019006938A (es) 2016-12-14 2019-09-06 Respira Therapeutics Inc Metodos y composiciones para trataminto de hipertension pulmonar y otros trastornos del pulmon.
CN107746400A (zh) * 2017-12-04 2018-03-02 武汉药明康德新药开发有限公司 苯并二氢吡喃‑6‑磺酰氯的制备方法
IL277071B1 (en) 2018-03-08 2024-03-01 Incyte Corp Aminopyrizine diol compounds as PI3K–y inhibitors
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
CN110483403A (zh) * 2019-09-02 2019-11-22 南通大学 一种5-溴-4-甲氧基-1h-吲唑的合成方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH075530B2 (ja) 1989-11-21 1995-01-25 シェリング・コーポレーション カルボキシアルキルカルボニルアミノ酸エンドペプチダーゼ阻害剤
GB9000725D0 (en) 1990-01-12 1990-03-14 Pfizer Ltd Therapeutic agents
GB9004260D0 (en) 1990-02-26 1990-04-18 Pfizer Ltd Therapeutic agents
US5208236A (en) * 1992-09-23 1993-05-04 Schering Corporation N-(acylaminomethyl)glutaryl amino acids and use
IL139457A0 (en) 1999-11-08 2001-11-25 Pfizer Compounds for the treatment of female sexual dysfunction
US20020052370A1 (en) * 2000-07-06 2002-05-02 Barber Christopher Gordon Cyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase

Also Published As

Publication number Publication date
PA8542401A1 (es) 2002-10-28
PE20021014A1 (es) 2002-11-12
WO2002079143A1 (en) 2002-10-10
PL365101A1 (en) 2004-12-27
CN1243723C (zh) 2006-03-01
CA2437113A1 (en) 2002-10-10
NO20034299L (no) 2003-11-27
CZ20032534A3 (cs) 2004-07-14
KR100564466B1 (ko) 2006-03-29
CN1492852A (zh) 2004-04-28
AP2002002467A0 (en) 2002-06-30
AP1689A (en) 2006-12-07
SK11822003A3 (sk) 2004-09-08
MA26996A1 (fr) 2004-12-20
MY134081A (en) 2007-11-30
TNSN02032A1 (fr) 2005-12-23
HUP0303624A3 (en) 2005-06-28
JP4018545B2 (ja) 2007-12-05
TWI254038B (en) 2006-05-01
NO20034299D0 (no) 2003-09-26
HK1060724A1 (en) 2004-08-20
BG108130A (bg) 2004-07-30
EP1373192A1 (en) 2004-01-02
UY27227A1 (es) 2002-10-31
JP2004531505A (ja) 2004-10-14
GEP20063783B (en) 2006-04-10
EE200300469A (et) 2004-02-16
KR20030092032A (ko) 2003-12-03
EA200300777A1 (ru) 2003-12-25
BR0208455A (pt) 2004-03-02
EA006154B1 (ru) 2005-10-27
OA12553A (en) 2006-06-07
IS6877A (is) 2003-07-17
HRP20030751A2 (en) 2005-08-31
MXPA03006597A (es) 2004-10-15
AR035795A1 (es) 2004-07-14
IL157009A0 (en) 2004-02-08
NZ527012A (en) 2005-03-24
DOP2002000364A (es) 2002-10-15
RS75303A (en) 2006-12-15

Similar Documents

Publication Publication Date Title
HUP0303624A2 (hu) NEP inhibitor hatású N-fenpropil-ciklopentil-csoporttal szubsztituált glutáramid származékok és ezeket tartalmazó gyógyászati készítmények és eljárás a vegyületek előállítására
HUP0104867A2 (hu) Gyulladásos betegségek kezelésére használható heterociklusos vegyületek, eljárás előállításukra és ilyen vegyületeket tartalmazó gyógyászati készítmények és alkalmazásuk
HUP9904703A2 (hu) Aminotiofén-karbonsav-amidok, ezeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
HUP0300743A2 (hu) Heteroarilszármazékok és alkalmazásuk gyógyszerként
EA200201179A1 (ru) Производные 2-аминокарбонил-9h-пурина
HRP20040317A2 (en) 1,8-naphthyridine derivatives as antidiabetics
MXPA03010142A (es) Nuevos derivados de arilheteroalquilamina.
MXPA03011510A (es) Derivados de5-halo-triptamina usados como ligandos de receptores de serotonina 5-ht-6 y/o 5-ht-7.
HUP0202049A2 (hu) Egyebek mellett osteoporosis kezelésére alkalmazható indolszármazékok
HUP0300480A2 (hu) 2-Acil-indol-származékok és tumorellenes szerként történő alkalmazásuk
IL108259A0 (en) Piperazine derivates, their preparation and pharmaceutical compositions containing them
HUP0204354A2 (hu) Új heterociklusos vegyületek, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
HUP0002763A2 (hu) N-Triazolil-2-indolkarboxamid-származékok és CCK-A agonistaként történő alkalmazásuk
ZA971892B (en) Compositions and use of benzamides and nicotin-amides as anti-inflammatory agents
HUP0203976A2 (hu) Adenozin a3 receptor antagonisták, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
HUP0301587A2 (hu) Foszfodiészteráz V gátló hatású 5-amino-alkil-pirazolo[4,3-d]pirimidinek, ezeket tartalmazó gyógyszerkészítmények és eljárások az elżállításaikra
HUP0105407A2 (hu) Triazolo[1,5-a]kinolinszármazékok, eljárás előállításukra, ezeket tartalmazó gyógyszerkészítmények, valamint intermedierek
HUP9702393A2 (hu) bisz(2-Halogén-etil)-amino-fenil szubsztituált distamycinszármazékok, tumorellenes és vírusellenes hatóanyagok
HUP0202479A2 (hu) Indolszármazékok
ES2104370T3 (es) Derivados de (arilalquilaminobencil)aminopropionamidas sustituidas, su preparacion y utilizacion.
ATE151423T1 (de) Carbocyclische nucleoside mittel nützlich als selektive inhibitoren von proinflammatorischen cytokinen
DK1430047T3 (da) Substituerede alkylaminopyridazinonderivater, fremgangsmåde til fremstilling deraf og en farmaceutisk sammensætning indeholdende disse
HUP0105420A2 (hu) Bulímia nervosa kezelésére szolgáló antikonvulzív származékok
IL115085A0 (en) Bicyclic carboxamide derivatives their preparation and pharmaceutical compositions containing them
HUP0200023A2 (hu) ((Amino-imino-metil)-amino)-alkán-karboxamidok és gyógyászati alkalmazásuk és eljárás a vegyületek előállítására

Legal Events

Date Code Title Description
FD9A Lapse of provisional protection due to non-payment of fees