AR039891A1 - Compuestos tiofen-amidinas, sus composiciones farmaceuticas y su uso para la preparacion de medicamentos para tratar enfermedades y trastornos mediados por c1s - Google Patents

Compuestos tiofen-amidinas, sus composiciones farmaceuticas y su uso para la preparacion de medicamentos para tratar enfermedades y trastornos mediados por c1s

Info

Publication number
AR039891A1
AR039891A1 ARP030101873A ARP030101873A AR039891A1 AR 039891 A1 AR039891 A1 AR 039891A1 AR P030101873 A ARP030101873 A AR P030101873A AR P030101873 A ARP030101873 A AR P030101873A AR 039891 A1 AR039891 A1 AR 039891A1
Authority
AR
Argentina
Prior art keywords
alkyl
phenyl
hydrogen
alkenyl
alkoxy
Prior art date
Application number
ARP030101873A
Other languages
English (en)
Original Assignee
Dimensional Pharm 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
Application filed by Dimensional Pharm Inc filed Critical Dimensional Pharm Inc
Publication of AR039891A1 publication Critical patent/AR039891A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/30Hetero atoms other than halogen
    • C07D333/34Sulfur atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/22Radicals substituted by doubly bound hetero atoms, or by two hetero atoms other than halogen singly bound to the same carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • C07F7/081Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
    • C07F9/655345Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Surgery (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)

Abstract

Un compuesto tiofen-amidina de fórmula (1): o un solvato, hidrato o sal farmacéuticamente aceptable del mismo; en donde: Z es -S(O)- o -S(O2)-; R1 es alquilo C1-4, halo, amino, alquiltio C1-6, alqueniltio C2-6, alcoxi C1-6, trifluormetilo, metilsulfonilo, o benciltio; Ar es fenilo, naftilo, piridilo, imidazolilo, tiazolilo, furanilo, tienilo, benzotiazolilo, pirazolilo, pirimidinilo, bencimidazolilo, benzofuranilo, indolilo, benzotiofenilo o benzo[c]cromenilo, cualquiera de los cuales está opcionalmente sustituido; R2, R3 y R4 son independientemente hidrógeno, alquilo C1-4, arilo C6-10, hidroxialquilo C1-4, aminoalquilo C1-4, mono alquilamino(C1-4)alquilo(C2-6), di(C1-4)alquilamino(C2-6)alquilo, carboxi(C1-4)alquilo, ciano, amino, nitro, C1-4 alcoxi, o hidroxi o BCO2Rw, donde Rw es hidrógeno, hidroxi, C1-4 alcoxi, ciano, C1-4alcoxicarbonilo, C1-4 alquilo, C3-8 cicloalquilo, fenilo, bencilo, representado por las fórmulas (2) o (3): donde Rd y Re son independientemente hidrógeno, C1-6 alquilo, C2-6 alquenilo o fenilo, Rf es hidrógeno, C1-6 alquilo, C2-6 alquenilo, o fenilo, Rg es hidrógeno, C1-6 alquilo, C2-6 alquenilo o fenilo, y Rh es C6-10 ar(C1-4)alquilo o C1-6 alquilo; y R7 es hidrógeno, cloro, fluoro o amino. Composiciones farmacéuticas que los comprenden, el uso de dichos compuestos para la preparación de un medicamento para tratar los síntomas de un desorden agudo o crónico mediado por la ruta clásica de la cascada del complemento.
ARP030101873A 2002-05-28 2003-05-28 Compuestos tiofen-amidinas, sus composiciones farmaceuticas y su uso para la preparacion de medicamentos para tratar enfermedades y trastornos mediados por c1s AR039891A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US38313002P 2002-05-28 2002-05-28

Publications (1)

Publication Number Publication Date
AR039891A1 true AR039891A1 (es) 2005-03-09

Family

ID=29584510

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030101873A AR039891A1 (es) 2002-05-28 2003-05-28 Compuestos tiofen-amidinas, sus composiciones farmaceuticas y su uso para la preparacion de medicamentos para tratar enfermedades y trastornos mediados por c1s

Country Status (23)

Country Link
US (2) US7138530B2 (es)
EP (1) EP1549632A4 (es)
JP (1) JP2005538953A (es)
KR (1) KR20050009720A (es)
CN (1) CN100412073C (es)
AR (1) AR039891A1 (es)
AU (1) AU2003251384B2 (es)
BR (1) BR0311419A (es)
CA (1) CA2484822A1 (es)
CO (1) CO5640081A2 (es)
HK (1) HK1081187A1 (es)
HR (1) HRP20041220A2 (es)
IL (1) IL164890A0 (es)
MX (1) MX249034B (es)
MY (1) MY137509A (es)
NO (1) NO20045403L (es)
NZ (1) NZ537346A (es)
PL (1) PL372246A1 (es)
RU (1) RU2359967C2 (es)
TW (1) TW200406395A (es)
UA (1) UA80131C2 (es)
WO (1) WO2003099805A1 (es)
ZA (1) ZA200408711B (es)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4544857B2 (ja) * 2001-06-11 2010-09-15 ヴァイロケム ファーマ インコーポレイテッド Flavivirus感染の治療または予防のための化合物および方法
DE10162114A1 (de) * 2001-12-12 2003-06-26 Schering Ag Neue Amidin-Derivate und deren Verwendung in Arzneimitteln
CA2484822A1 (en) 2002-05-28 2003-12-04 3-Dimensional Pharmaceuticals, Inc. Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
US7402608B2 (en) * 2002-12-10 2008-07-22 Virochem Pharma Inc. Compounds and methods for the treatment or prevention of Flavivirus infections
GB0305575D0 (en) * 2003-03-11 2003-04-16 Glaxo Group Ltd Novel compounds
US7482376B2 (en) * 2003-07-03 2009-01-27 3-Dimensional Pharmaceuticals, Inc. Conjugated complement cascade inhibitors
MXPA06015049A (es) 2004-07-08 2007-02-08 Novo Nordisk As Marcadores prolongadores de polipeptidos que comprenden una porcion tetrazol.
NZ554555A (en) * 2004-10-20 2011-09-30 Univ California Cyclohexyl-urea derivatives as improved inhibitors for the soluble epoxide hydrolase
ME02461B (me) 2005-05-10 2017-02-20 Incyte Holdings Corp Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih
KR20080016597A (ko) * 2005-05-13 2008-02-21 바이로켐 파마 인코포레이티드 플라비바이러스 감염의 예방 또는 치료용 화합물 및 그의예방 또는 치료 방법
ES2540561T3 (es) 2005-12-20 2015-07-10 Incyte Corporation N-hidroxiamidinoheterociclos como moduladores de indolamina 2,3-dioxigenasa
CN102532180B (zh) * 2005-12-30 2016-06-29 安纳考尔医药公司 含硼的小分子
CN101420854B (zh) * 2006-02-16 2013-08-07 安纳考尔医药公司 作为抗炎药的含硼的小分子
US20080146624A1 (en) * 2006-09-19 2008-06-19 Incyte Corporation Amidines as modulators of indoleamine 2,3-dioxygenase
CL2007002650A1 (es) 2006-09-19 2008-02-08 Incyte Corp Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras.
CA2663057C (en) 2006-09-19 2015-12-08 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
KR20090086081A (ko) * 2006-11-15 2009-08-10 바이로켐 파마 인코포레이티드 플라비바이러스 감염의 치료 또는 예방용 티오펜 유사체
US8580735B2 (en) 2007-02-05 2013-11-12 Apellis Pharmaceuticals, Inc. Local complement inhibition for treatment of complement-mediated disorders
JO3396B1 (ar) * 2007-06-20 2019-10-20 Anacor Pharmaceuticals Inc جزيئات صغيرة تحتوي على البورون
RU2474581C2 (ru) * 2007-12-26 2013-02-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Способ получения замещенных гетероциклом производных пиридина
MY171866A (en) 2008-07-08 2019-11-05 Incyte Holdings Corp 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
WO2011090929A1 (en) 2010-01-19 2011-07-28 Theravance, Inc. Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents
AU2012272706B2 (en) 2011-06-22 2017-07-06 Apellis Pharmaceuticals, Inc. Methods of treating chronic disorders with complement inhibitors
US9388126B2 (en) 2012-07-19 2016-07-12 Drexel University Sigma receptor ligands and methods of modulating cellular protein homeostasis using same
MX350575B (es) 2012-09-27 2017-09-11 Bayer Cropscience Ag Procedimiento para la preparación de fenil y piridil pirrolidinas opcionalmente sustituidas.
CA2900029C (en) 2013-02-06 2021-03-02 Bayer Cropscience Aktiengesellschaft Halogen-substituted pyrazol derivatives as pest-control agents
US10221138B2 (en) * 2013-06-27 2019-03-05 Lg Chem, Ltd. Biaryl derivatives as GPR120 agonists
PL3066085T3 (pl) 2013-11-08 2020-11-02 Incyte Holdings Corporation Sposób syntezy inhibitora 2,3-dioksygenazy indoloaminowej
US10538487B2 (en) 2015-02-16 2020-01-21 The University Of Queensland Sulfonylureas and related compounds and use of same
HRP20220195T1 (hr) 2017-07-07 2022-04-15 Inflazome Limited Novi spojevi sulfonamid karboksamida
US11370776B2 (en) 2017-07-07 2022-06-28 Inflazome Limited Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors
WO2019034692A1 (en) 2017-08-15 2019-02-21 Inflazome Limited SULFONYLURATES AND SULFONYLTHIOURES AS INHIBITORS OF NLRP3
US11926600B2 (en) 2017-08-15 2024-03-12 Inflazome Limited Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors
JP2020531453A (ja) 2017-08-15 2020-11-05 インフレイゾーム リミテッド Nlrp3阻害剤としてのスルホニルウレアおよびスルホニルチオウレア
US11518739B2 (en) 2017-08-15 2022-12-06 Inflazome Limited Sulfonamide carboxamide compounds
RU2020110366A (ru) * 2017-08-15 2021-09-16 Инфлазоум Лимитед Новые соединения сульфонамидкарбоксамидов
US11117870B2 (en) 2017-11-01 2021-09-14 Drexel University Compounds, compositions, and methods for treating diseases
EP3707134A1 (en) 2017-11-09 2020-09-16 Inflazome Limited Novel sulfonamide carboxamide compounds
WO2019166619A1 (en) 2018-03-02 2019-09-06 Inflazome Limited Novel compounds
WO2021067526A1 (en) 2019-10-02 2021-04-08 Alexion Pharmaceuticals, Inc. Complement inhibitors for treating drug-induced complement-mediated response
EP4150338A1 (en) 2020-05-15 2023-03-22 Alexion Pharmaceuticals, Inc. Method of using extracellular vesicles to detect complement activation, and uses thereof to assess and/or monitor treatment of a complement-mediated disease
CN115884969A (zh) 2020-09-01 2023-03-31 江苏恒瑞医药股份有限公司 稠合咪唑类衍生物、其制备方法及其在医药上的应用

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59139357A (ja) * 1983-01-28 1984-08-10 Torii Yakuhin Kk アミジン誘導体
US4510130A (en) 1983-05-20 1985-04-09 Genetic Diagnostics Corporation Promoting animal and plant growth with leupeptin
US4727064A (en) 1984-04-25 1988-02-23 The United States Of America As Represented By The Department Of Health And Human Services Pharmaceutical preparations containing cyclodextrin derivatives
GB8506792D0 (en) 1985-03-15 1985-04-17 Janssen Pharmaceutica Nv Derivatives of y-cyclodextrin
US4916219A (en) 1985-03-28 1990-04-10 University Of Iowa Research Foundation Oligosaccharide heparin fragments as inhibitors of complement cascade
US4722890A (en) 1985-08-27 1988-02-02 The United States Of America As Represented By The Department Of Health And Human Services Quantitative assay for human terminal complement cascade activation
US5002935A (en) 1987-12-30 1991-03-26 University Of Florida Improvements in redox systems for brain-targeted drug delivery
US5256642A (en) 1988-04-01 1993-10-26 The Johns Hopkins University Compositions of soluble complement receptor 1 (CR1) and a thrombolytic agent, and the methods of use thereof
US5268363A (en) 1989-09-12 1993-12-07 The Beth Israel Hospital Association Method of treatment to inhibit the undesirable activation of the complement cascade with factor J, an inhibitor of complement C1
ZA928276B (en) * 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.
US5466811A (en) 1994-07-18 1995-11-14 Merck & Co., Inc. Dioxolenylmethyl carbamates pro moieties for amine drugs
DE19650196A1 (de) * 1996-12-04 1998-06-10 Bayer Ag Thienylsulfonylamino(thio)carbonylverbindungen
AU6959898A (en) * 1997-04-11 1998-11-11 David J. Grainger Compounds and therapies for the prevention of vascular and non-vascular pathol ogies
GB9721964D0 (en) 1997-10-16 1997-12-17 Pfizer Ltd Isoquinolines
US6291514B1 (en) 1998-02-09 2001-09-18 3-Dimensional Pharmaceuticals, Inc. Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
NZ506507A (en) * 1998-02-09 2003-08-29 Dimensional Pharm Inc Heteroaryl amidine, methylamidine or guanidine derivatives useful as urokinase inhibitors
US6727238B2 (en) * 1998-06-11 2004-04-27 Pfizer Inc. Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
DE19840319A1 (de) 1998-09-04 2000-03-09 Bayer Ag Verfahren zur Herstellung von aromatischen oder heteroaromatischen Sulfonsäurechloriden
FR2783519B1 (fr) * 1998-09-23 2003-01-24 Sod Conseils Rech Applic Nouveaux derives d'amidines, leur preparation, leur application a titre de medicaments et les compositions pharmaceutiques les contenant
JP3450724B2 (ja) * 1998-11-06 2003-09-29 キヤノン株式会社 画像形成装置
JP2003529536A (ja) * 1999-02-09 2003-10-07 3−ディメンショナル ファーマシューティカルズ, インコーポレイテッド C1s介在疾患および状態の処置法、およびそれのための化合物および組成物
BR9917036A (pt) * 1999-02-09 2002-07-30 Dimensional Pharm Inc Amidinas heteroarila, metilamidinas e guanidinas como inibidores de protease
US6838479B2 (en) 2000-09-11 2005-01-04 Genentech, Inc. Amidine inhibitors of serine proteases
DE10112041A1 (de) * 2001-03-14 2002-09-26 Aventis Pharma Gmbh p-Thienylbenzyl-Amide als Agonisten von Angiotensin-(1-7)-Rezeptoren, Verfahren zu ihrer Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
CA2484822A1 (en) 2002-05-28 2003-12-04 3-Dimensional Pharmaceuticals, Inc. Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
TWI299664B (en) * 2003-01-06 2008-08-11 Osi Pharm Inc (2-carboxamido)(3-amino)thiophene compounds

Also Published As

Publication number Publication date
AU2003251384B2 (en) 2009-01-29
HRP20041220A2 (hr) 2006-04-30
CN100412073C (zh) 2008-08-20
JP2005538953A (ja) 2005-12-22
PL372246A1 (en) 2005-07-11
WO2003099805A1 (en) 2003-12-04
US20040009995A1 (en) 2004-01-15
NO20045403L (no) 2004-12-10
US7138530B2 (en) 2006-11-21
MXPA04011671A (es) 2005-03-07
CN1665800A (zh) 2005-09-07
MX249034B (es) 2007-09-14
US20050234081A1 (en) 2005-10-20
NZ537346A (en) 2006-12-22
MY137509A (en) 2009-02-27
AU2003251384A1 (en) 2003-12-12
US7109354B2 (en) 2006-09-19
CA2484822A1 (en) 2003-12-04
ZA200408711B (en) 2006-10-25
RU2359967C2 (ru) 2009-06-27
KR20050009720A (ko) 2005-01-25
TW200406395A (en) 2004-05-01
EP1549632A1 (en) 2005-07-06
HK1081187A1 (en) 2006-05-12
BR0311419A (pt) 2005-04-05
IL164890A0 (en) 2005-12-18
RU2004138787A (ru) 2005-07-10
EP1549632A4 (en) 2005-11-09
CO5640081A2 (es) 2006-05-31
UA80131C2 (en) 2007-08-27

Similar Documents

Publication Publication Date Title
AR039891A1 (es) Compuestos tiofen-amidinas, sus composiciones farmaceuticas y su uso para la preparacion de medicamentos para tratar enfermedades y trastornos mediados por c1s
JP5406716B2 (ja) インドール化合物
ES2435799T3 (es) Un método de inhibición del virus de la hepatitis C mediante combinación de una 5,6-dihidro-1H-piridin-2-ona y de uno o más compuestos antivirales adicionales
ES2977656T3 (es) Inhibidores de KDM1A para el tratamiento de enfermedades
ES2548228T3 (es) Derivados de bencimidazol e imidazopiridina como moduladores de canal de sodio
ES2884067T3 (es) Derivados de indolina sustituidos como inhibidores de la replicación viral del dengue
ES2945834T3 (es) Pirrolinas fusionadas que actúan como inhibidores de la proteasa 30 específica de ubiquitina (USP30)
BR112021002327A2 (pt) derivados de 6-(4-amino-3-metil-2-oxa-8-azaespiro[4,5]decan-8-il)-3-(2,3-diclorofenil)-2-metilpirimidin-4(3h)-ona e compostos relacionados como inibidores de ptpn11(shp2) para o tratamento do câncer
AR064561A1 (es) Derivados de 2-aza-biciclo[3.1.0]hexano y su uso en la preparacion de un medicamento para el tratamiento de enfermedades relacionadas con disfunciones generales del sistema de la orexina.
NO20045589L (no) Nye forbindelser
UY28132A1 (es) Derivados de pirrolopirimidina
CA2963681A1 (en) Induction of gata2 by hdac1 and hdac2 inhibitors
AR020727A1 (es) Uso de compuestos derivados 3-amino-4-aril-maleimidas para la preparacion de medicamentos para condiciones asociadas a una necesidad de inhibicion de lagsk-3, dichos compuestos, procedimiento para su preparacion y composiciones farmaceuticas que los comprenden
EA200500018A1 (ru) Бензконденсированные гетероариламидные производные тиенопиридинов, применяемые в качестве терапевтических агентов, фармацевтические композиции, включающие их, и способы их применения
NO20092723L (no) Indazolylester og amidderivater for behandling av gluccocorticoid reseptormedierte sykdommer
BR0206955A (pt) Ligantes de receptores de canabinóides
CY1110977T1 (el) Υποκατεστημενα παραγωγα ινδολης για φαρμακευτικη συνθεση για θεραπεια ασθενειων του αναπνευστικου
RU2007120454A (ru) Производные хинуклидина и их применение в качестве антагонистов мускариновых рецепторов м3
NO20064151L (no) Nye forbindelser
ES2920888T3 (es) Derivado de sulfonamida y método de preparación y uso del mismo
CA3018316C (en) Griseofulvin compound
DE60206911D1 (de) Imidazol-2-carbonsäureamid derivate als raf-kinase-inhibitoren
AR056321A1 (es) COMBINACIONES TERAPÉUTICAS PARA EL TRATAMIENTO O LA PREVENCIoN DE TRASTORNOS PSICoTICOS
JP2022003063A (ja) 置換n−アセチル−l−システイン誘導体及び関連化合物
AR040580A1 (es) Derivados de pirazol heterobiciclico como inhibidores de la quinasa

Legal Events

Date Code Title Description
FB Suspension of granting procedure