HUP0402503A2 - Pirrolidinonszármazékok és a vegyületeket tartalmazó gyógyászati készítmények - Google Patents

Pirrolidinonszármazékok és a vegyületeket tartalmazó gyógyászati készítmények

Info

Publication number
HUP0402503A2
HUP0402503A2 HU0402503A HUP0402503A HUP0402503A2 HU P0402503 A2 HUP0402503 A2 HU P0402503A2 HU 0402503 A HU0402503 A HU 0402503A HU P0402503 A HUP0402503 A HU P0402503A HU P0402503 A2 HUP0402503 A2 HU P0402503A2
Authority
HU
Hungary
Prior art keywords
group
atom
hydroxyl
alkynyl
cycloalkyl
Prior art date
Application number
HU0402503A
Other languages
English (en)
Inventor
Dong Zou
Olivier Dasse
Janelle Evans
Paul Higgins
Jeremy Kintigh
Laurent Knerr
Rama Kondru
Eric Schwartz
Hai-Xiao Zhai
Original Assignee
Ucb, S.A.
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
Application filed by Ucb, S.A. filed Critical Ucb, S.A.
Publication of HUP0402503A2 publication Critical patent/HUP0402503A2/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • AIDS & HIV (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Otolaryngology (AREA)
  • Diabetes (AREA)

Abstract

A találmány tárgyát gyógyászati készítmény képezi, amely hatóanyagként(I) általános képletű vegyületet - a képletben Y jelentése oxigénatomvagy kénatom; G és G' jelentése a közöttük lévő kötéssel együtt HC-CHvagy C=C; V jelentése arilcsoport, heterociklusos csoport vagycikloalkilcsoport; Z jelentése halogénatom, alkilcsoport,alkenilcsoport, alkinilcsoport, hidroxilcsoport, aminocsoport,alkoxicsoport, ariloxicsoport, nitrocsoport vagy cianocsoport; R1jelentése hidrogénatom, halogénatom, alkilcsoport, cikloalkilcsoport,alkenilcsoport, cikloalkenilcsoport, alkiniIcsoport, arilcsoport vagyheterociklusos csoport; R2 jelentése hidrogénatom vagyhidroxilcsoport; R3 jelentése -C(O)R3a, -C(O)OR3a, -C(O)N(R3a)(R3b), -S(O)2R3a, -S(O)R3a vagy -SR3a, ahol R3a és R3b jelentése egymástólfüggetlenül az R1 jelentésére megadott; R4 jelentése hidroxilcsoport,szulfanilcsoport vagy aminocsoport; t értéke 0, 1, 2, 3, 4 vagy 5 vagyannak gyógyászatilag elfogadható sóját vagy metabolikusan hasíthatószármazékát tartalmazza. A fenti hatóanyagok egy része új vegyület.Ezek a vegyületek és készítmények CCR2, MCP-1 vagy az ezek közöttikölcsönhatás által mediált állapotok kezelésére vagy megelőzésérealkalmazhatók. Ó
HU0402503A 2001-10-03 2002-09-26 Pirrolidinonszármazékok és a vegyületeket tartalmazó gyógyászati készítmények HUP0402503A2 (hu)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US97014001A 2001-10-03 2001-10-03
US40080702P 2002-08-01 2002-08-01
PCT/EP2002/010810 WO2003030897A1 (en) 2001-10-03 2002-09-26 Pyrrolidinone derivatives

Publications (1)

Publication Number Publication Date
HUP0402503A2 true HUP0402503A2 (hu) 2005-03-29

Family

ID=27017198

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0402503A HUP0402503A2 (hu) 2001-10-03 2002-09-26 Pirrolidinonszármazékok és a vegyületeket tartalmazó gyógyászati készítmények

Country Status (19)

Country Link
US (3) US20050004180A1 (hu)
EP (1) EP1434577A1 (hu)
JP (1) JP2005523238A (hu)
KR (1) KR20040048936A (hu)
CN (1) CN1564685A (hu)
AR (1) AR036672A1 (hu)
BG (1) BG108660A (hu)
BR (1) BR0212968A (hu)
CA (1) CA2463198A1 (hu)
CO (1) CO5390075A1 (hu)
CZ (1) CZ2004442A3 (hu)
HU (1) HUP0402503A2 (hu)
IL (1) IL160642A0 (hu)
MX (1) MXPA04002982A (hu)
NO (1) NO20041767L (hu)
NZ (1) NZ532018A (hu)
PL (1) PL370355A1 (hu)
RU (1) RU2004109818A (hu)
WO (1) WO2003030897A1 (hu)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101513402B (zh) 2001-08-10 2012-03-21 盐野义制药株式会社 抗病毒药
US7109186B2 (en) 2002-07-09 2006-09-19 Bristol-Myers Squibb Company HIV integrase inhibitors
NZ539297A (en) * 2002-09-13 2008-04-30 Biogen Idec Inc Method of purifying polypeptides by simulated moving bed chromatography
MXPA06013764A (es) * 2004-05-26 2007-02-08 Janssen Pharmaceutica Nv Mercaptoimidazoles como antagonistas del receptor ccr2.
US20070244138A1 (en) * 2004-05-26 2007-10-18 Janssen Pharmaceutica N.V. Mercaptoimidazoles as Ccr2 Receptor Antagonists
JP2008509201A (ja) * 2004-08-11 2008-03-27 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｃｃｒ２受容体アンタゴニストとしてのメルカプトイミダゾール
JP2008512463A (ja) * 2004-09-08 2008-04-24 ボーイズ タウン ナショナル リサーチ ホスピタル マトリックスメタロプロテイナーゼ−１２に関連する糸球体基底膜疾患の治療
US20090012148A1 (en) * 2005-11-01 2009-01-08 Maxfield Frederick R Reducing cellular cholesterol levels and/or treating or preventing phospholipidosis
US20080076120A1 (en) * 2006-09-14 2008-03-27 Millennium Pharmaceuticals, Inc. Methods for the identification, evaluation and treatment of patients having CC-Chemokine receptor 2 (CCR-2) mediated disorders
US20100069380A1 (en) * 2006-09-22 2010-03-18 Soongyu Choi Heterocyclic inhibitors of bacterial peptidyl trna hydrolase and uses thereof
WO2008055945A1 (en) * 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
PE20081785A1 (es) 2007-02-19 2009-01-12 Novartis Ag Derivados de ciclohexil-amida del acido aril carboxilico
WO2008103367A2 (en) * 2007-02-20 2008-08-28 Sergey Kozmin Method for assembling high-purity chemical libraries, proapoptotic compounds discovered by same
KR20100016076A (ko) 2007-03-30 2010-02-12 시오노기 앤드 컴파니, 리미티드 신규 피롤리논 유도체 및 그것을 함유하는 의약 조성물
FR2929851B1 (fr) * 2008-04-09 2012-11-30 Centre Nat Rech Scient Molecules inhibant une voie metabolique impliquant la proteine tyrosine kinase syk et procede d'identification de ces molecules
JP5637562B2 (ja) * 2008-09-25 2014-12-10 塩野義製薬株式会社 新規ピロリノン誘導体およびそれを含有する医薬組成物
AU2010270153A1 (en) * 2009-07-10 2012-02-02 Vivalis Substituted pyrrolidinone as inhibitors of hepatitis C NS5B polymerase, the pharmaceutical composition thereof and their therapeutic use
WO2011004017A1 (en) * 2009-07-10 2011-01-13 Vivalis 1-(6 members azo-heterocyclic)-pyrrolin-2-one compounds as inhibitors of hepatitis c ns5b polymerase, the pharmaceutical composition thereof and their therapeutic use
DK2545047T3 (da) 2010-03-10 2014-07-28 Probiodrug Ag Heterocycliske inhibitorer af glutaminylcyclase (QC, EC 2.3.2.5)
WO2012093174A1 (en) 2011-01-07 2012-07-12 Vivalis 1-(6-membered azo-heterocyclic)-2,5-dihydro-1h-pyrrol-2-one derivatives as anti-hepatitis c virus, the pharmaceutical composition thereof and their therapeutic use
US9493412B2 (en) 2011-09-27 2016-11-15 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
US9249096B2 (en) 2011-09-27 2016-02-02 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
WO2013048982A1 (en) 2011-09-27 2013-04-04 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
WO2014025942A1 (en) * 2012-08-09 2014-02-13 Emory University Nmda receptor modulators and uses related thereto
KR102527797B1 (ko) 2012-12-21 2023-05-03 길리애드 사이언시즈, 인코포레이티드 폴리시클릭-카르바모일피리돈 화합물 및 그의 제약 용도
US9682085B2 (en) * 2013-02-22 2017-06-20 Shifa Biomedical Corporation Anti-proprotein convertase subtilisin kexin type 9 (anti-PCSK9) compounds and methods of using the same in the treatment and/or prevention of cardiovascular diseases
BR112015023294A2 (pt) * 2013-03-15 2017-07-18 Shifa Biomedical Corp método para tratamento ou prevenção de uma doença
WO2014157047A1 (ja) * 2013-03-27 2014-10-02 千葉県 神経変性疾患治療剤
WO2015004610A1 (en) 2013-07-11 2015-01-15 Adamed Sp. Z O.O. 1,5-dihydropyrrol-2-one derivatives as inhibitors of p53-mdm2/mdm4 protein-protein interaction
NO2865735T3 (hu) 2013-07-12 2018-07-21
CA2916993C (en) 2013-07-12 2019-01-15 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
TWI744723B (zh) 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
NO2717902T3 (hu) 2014-06-20 2018-06-23
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
TWI695003B (zh) 2014-12-23 2020-06-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
AU2016244035B2 (en) 2015-04-02 2018-11-01 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
KR102370515B1 (ko) 2016-06-21 2022-03-03 시파 바이오메디칼 코포레이션 항-프로단백질 전환효소 서브틸리신 켁신 유형 9(항-pcsk9) 화합물 및 심혈관 질환의 치료 및/또는 예방에 이를 사용하는 방법
CN114262290B (zh) * 2021-12-20 2024-03-22 华东师范大学 一类4-亚甲基吡咯烷-2-硫酮类化合物及其合成方法和应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS4988864A (hu) * 1972-12-29 1974-08-24
SU1114676A1 (ru) * 1983-03-31 1984-09-23 Пермский государственный фармацевтический институт 1,5-Дифенил-3-окси-4-метилсульфонил-2,5-дигидропиррол-2-он в качестве промежуточного продукта дл синтеза 1,5-дифенил-3-оксиэтиламино-4-метилсульфонил-2,5-дигидропиррол-2-она, обладающего антиагрегатной активностью против тромбоцитов
US5202344A (en) * 1990-12-11 1993-04-13 G. D. Searle & Co. N-substituted lactams useful as cholecystokinin antagonists
US5508300A (en) * 1994-01-14 1996-04-16 Pfizer Inc. Dihydro pyrazolopyrroles, compositions and use
GB9803228D0 (en) * 1998-02-17 1998-04-08 Zeneca Ltd Chemical compounds
AU4143300A (en) * 1999-04-28 2000-11-17 Takeda Chemical Industries Ltd. Cyclic amide compounds, process for the preparation of the same and uses thereof

Also Published As

Publication number Publication date
IL160642A0 (en) 2004-07-25
AR036672A1 (es) 2004-09-22
US6727275B2 (en) 2004-04-27
BG108660A (en) 2005-03-31
MXPA04002982A (es) 2004-07-15
CO5390075A1 (es) 2004-04-30
BR0212968A (pt) 2004-10-13
JP2005523238A (ja) 2005-08-04
EP1434577A1 (en) 2004-07-07
US20050004180A1 (en) 2005-01-06
NZ532018A (en) 2004-12-24
KR20040048936A (ko) 2004-06-10
RU2004109818A (ru) 2005-05-10
US6936633B2 (en) 2005-08-30
CZ2004442A3 (cs) 2005-03-16
US20030149081A1 (en) 2003-08-07
CN1564685A (zh) 2005-01-12
US20040157914A1 (en) 2004-08-12
PL370355A1 (en) 2005-05-16
WO2003030897A1 (en) 2003-04-17
NO20041767L (no) 2004-04-30
CA2463198A1 (en) 2003-04-17

Similar Documents

Publication Publication Date Title
HUP0402503A2 (hu) Pirrolidinonszármazékok és a vegyületeket tartalmazó gyógyászati készítmények
HUP0400710A2 (hu) Tioéter helyettesítővel helyettesített imidazokinolinszármazékok, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
HUP0004529A2 (hu) VLA-4 által mediált leukocita adhéziót gátló szulfonilezett dipeptid-származékok, ezeket tartalmazó gyógyászati készítmények, valamint alkalmazásuk
EA200200708A1 (ru) Производные бензазола и их применение в качестве модуляторов jnk
AU2418188A (en) Therapeutic heterocyclic compounds
HUP0400321A2 (hu) Fluorpirrolidin-származékok mint dipeptidil-dipeptidáz inhibitorok és ezeket tartalmazó gyógyszerkészítmények
HUP0401740A2 (hu) N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok és ezeket tartalmazó gyógyszerkészítmények
HUP0101999A2 (hu) 4-Hidroxi-kinolin-3-karboxamid- és -hidrazid-származékok, ezeket tartalmazó gyógyászati készítmények, valamint e vegyületek alkalmazása
HUP0401889A2 (hu) 1,8-Naftiridin-származékok mint antidiabetikumok és ezeket tartalmazó gyógyszerkészítmények
DK1487829T3 (da) Thiadizolylpiperazinderivater, der er nyttige til behandling eller forebyggelse af smerte
HUP0300350A2 (hu) Új 3-amino-azetidin-származékok, előállításuk és ezeket tartalmazó gyógyszerkészítmények
HUP0401537A2 (hu) Tiohidantoin-származékok, eljárás előállításukra, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk gyógyszerkészítmények előállítására
HUP0001446A2 (hu) HIV reverz transzkriptáz inhibitor hatású 4,4-diszubsztituált-3,4-dihidro-2(1H)-kinazolinon-származékok, alkalmazásuk és a vegyületeket tartalmazó gyógyszerkészítmények
HUP0001154A2 (hu) 3-Piperidil-4-oxo-kinazolin-származékok és a vegyületeket tartalmazó gyógyászati készítmények
HUP0401009A2 (hu) 5-Hidroxitriptamin-6-ligandumokként alkalmazható 1-aril- vagy 1- alkil-szulfonilbenzazol-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
HUP0203884A2 (hu) Kristályos oximinoalkánsav-származékok és cukorbaj elleni alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
HUP0401018A2 (hu) 2H-1-benzopirán-származékok, eljárás ezek előállítására és ezeket tartalmazó gyógyászati készítmények
MXPA03010867A (es) Nuevos derivados heterociclicos y uso farmaceutico de los mismos.
HUP0103166A2 (hu) Karbamát- és karbamidtartalmú készítmények, és neurotróf alkalmazásuk
HUP0004058A2 (hu) Készítmények és eljárások biológiai membránok permeabilitásának reverzibilis növelésére
DK1209166T3 (da) Hidtil ukendte A-500 359-derivater
KR950702544A (ko) 비페닐메탄 유도체 및 이를 함유하는 약제
HUP0202647A2 (hu) Új arilalkanoilszármazékok, előállításuk és alkalmazásuk, valamint e vegyületeket tartalmazó gyógyászati készítmények
HUP0204579A2 (hu) Pirrolopiridazinszármazékok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
HUP0202438A2 (hu) Dioxo-tiazolidin-származékok és ezeket tartalmazó gyógyszerkészítmények és eljárás előállításukra

Legal Events

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