[go: up one dir, main page]

AR076005A1 - Derivados de piperidina y piperazina inhibidores de autotaxinas, composiciones farmaceuticas que los comprenden, proceso para prepararlos y uso de los mismos en el tratamiento del cancer y otras patologias asociadas. - Google Patents

Derivados de piperidina y piperazina inhibidores de autotaxinas, composiciones farmaceuticas que los comprenden, proceso para prepararlos y uso de los mismos en el tratamiento del cancer y otras patologias asociadas.

Info

Publication number
AR076005A1
AR076005A1 ARP100101047A ARP100101047A AR076005A1 AR 076005 A1 AR076005 A1 AR 076005A1 AR P100101047 A ARP100101047 A AR P100101047A AR P100101047 A ARP100101047 A AR P100101047A AR 076005 A1 AR076005 A1 AR 076005A1
Authority
AR
Argentina
Prior art keywords
group
independently
heterocyclyl
alkyl
independently selected
Prior art date
Application number
ARP100101047A
Other languages
English (en)
Inventor
Kai Schiemann
Melanie Schultz
Wolfgang Staehle
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR076005A1 publication Critical patent/AR076005A1/es

Links

Classifications

    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C07D249/18—Benzotriazoles
    • 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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)

Abstract

Reivindicacion 1: Compuesto de acuerdo con la formula (1) en donde W1, W2 forman juntos, de modo independiente, -N=N-, -C(O)-O-, -C(O)-S-, -C(O)-N(R5)-, -C(S)-N(R5a)-, -C(O)-C(R6)(R7)-, -N=C[N(R8)(R9)]-; Y1 está seleccionado, de modo independiente, del grupo que consiste en -C(O)-, -C(S)-, -S(O)2-, -N(R10)-C(O)-, -C(O)-N(R11)-, -OC(O)-, enlace simple; Y2 está seleccionado, de modo independiente, del grupo que consiste en C(R12)(R13)-, -O-, -N(R14)-, -C(O)-, -C(O)-NH-, enlace simple; Y3 está seleccionado, de modo independiente, del grupo que consiste en -O-, -C(O)-, enlace simple; Z1 está seleccionado, de modo independiente, del grupo que consiste en O, S, N(R15); L está seleccionado, de modo independiente, del grupo que consiste en las formulas (2); B está seleccionado, de modo independiente, del grupo que consiste en cicloalquilo, heterociclilo, arilo, heteroarilo, en donde cicloalquilo, heterociclilo, arilo, heteroarilo pueden estar sustituidos, de modo independiente con uno o varios sustituyentes iguales o diferentes seleccionados del grupo que consiste en: (i) hidrogeno, alquilo, alquilo C9-30, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halogeno, -F, -CI, -Br, -I, -CN, -CF3, -SF3, -N3, -NH2, -NHX1, -NX2X3, -NO2, -OH, =O, -OCF3, -SCF3, -OCHF2, -SCHF2, -SH, -O-SO3H, -OP(O)(OH)2, -CHO, -COOH, -C(O)NH2, -SO3H, -P(O)(OH)2, -C(O)-X4, -C(O)O-X5, -C(O)NH-X6, -C(O)NX7X8, -O-X9, -O(-X10-O)a-H (a = 1, 2, 3, 4, 5), -O(-X11-O)b-X12 (b = 1, 2, 3, 4, 5), -OC(O)-X13, -OC(O)-O-X1 4, -OC(O)-NHX15, -O-C(O)-NX16X17, -OP(O)(OX18)(OX19), -OSi(X20)(X21)(X22), -OS(O2)-X23, -NHC(O)-NH2, -NHC(O)-X24, -NX25C(O)-X26, -NH-C(O)-O-X27, -NH-C(O)-NH-X28, -NH-C(O)-NX29X30, -NX31-C(O)-O-X32, -NX33-C(O)-NH-X34, -NX35-C(O)-NX36X37, -NHS(O2)-X38, -NX39S(O2)-X40, -S- X41, -S(O)-X42, -S(O2)-X43, -S(O2)NH-X44, -S(O2)NX45X46, -S(O2)O-X47, -P(O)(OX48)(OX49), -Si(X50)(X51)(X52), -C(NH)-NH2, -C(NX53)-NH2, -C(NH)-NHX54, -C(NH)-NX55X56, -C(NX57)-NHX58, -C(NX59)-NX60X61, -NH-C(O)-NH-O-X62, -NH-C(O)-NX63-O-X64, -NX65-C(O)-NX66-O-X67, -N(-C(O)-NH-O-X68)2, -N(-C(O)-NX69-O-X70)2, -N(-C(O)-NH-O-X71)(-C(O)-NX72-O-X73), -C(S)-X74, -C(S)-O-X75, -C(S)-NH-X76, -C(S)-NX77X78, -C(O)-NH-O-X79, -C(O)-NX80-O-X81, -C(S)-NH-O-X82, -C(S)-NX83-O-X84, -C(O)-NH-NH-X85, -C(O)-NH-NX86X87, -C(O)-NX88-NX89X90, -C(S)-NH-NH-X91, -C(S)-NH-NX92X93, -C(S)-NX94-NX95X96, -C(O)-C(O)-O-X97, -C(O)-C(O)-NH2, -C(O)-C(O)-NHX98, -C(O)-C(O)-NX99X100, -C(S)-C(O)-O-X101, -C(O)-C(S)-O-X102, -C(S)-C(S)-O-X103, -C(S)-C(O)-NH2 , -C(S)-C(O)-NHX104, -C(S)-C(O)-NX105X106, -C(S)-C(S)-NH2, -C(S)-C(S)-NHX107, -C(S)-C(S)-NX108X109, -C(O)-C(S)-NH2, -C(O)-C(S)-NHX110, -C(O)-C(S)-NX111X112; en donde X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12, X13, X14, X15, X16, X17, X18, X19, X20, X21, X22, X23, X24, X25, X26, X27, X28, X29, X30, X31, X32, X33, X34, X35, X36, X37, X38, X39, X40, X41, X42, X43, X44, X45, X46, X47, X48, X49, X50, X51, X52, X53, X54, X55, X56, X57, X58, X59, X60, X61, X62, X63, X64, X65, X66, X67, X68, X69, X70, X71, X72, X73, X74, X75, X76, X77, X78, X79, X80, X81, X82, X83, X84, X85, X86, X87, X88, X89, X90, X91, X92, X93, X94, X95, X96, X97, X98, X99, X100, X101, X102, X103, X104, X105, X106, X107, X108, X109, X110, X111, X112 están seleccionados, de modo independiente entre sí, del grupo que consiste en alquilo, alquilo C9-30, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo y en donde, de modo alternativo X7, X8 y/o X16, X17 y/o X29, X30 y/o X36, X37 y/o X45, X46 y/o X55, X56 y/o X60, X61 y/o X77, X78 y/o X86, X87 y/o X89, X90 y/o X92, X93 y/o X95, X96 y/o X99, X100 y/o X105, X106 y/o X108, X109 y/o X111, X112, respectivamente, también pueden formar juntos heterociclilo, en donde opcionalmente los anteriores sustituyentes del grupo de sustituyentes (i) pueden estar sustituidos, a su vez, de modo independiente entre sí, con uno o varios sustituyentes V iguales o diferentes; R1, R2, R3, R3a, R3b, R4, R4a, R4b, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15 están seleccionados, de modo independiente entre sí, del grupo que consiste en V; de modo alternativo, R3a y R4a, R3b y R4b así como R3 y R4 pueden formar juntos cicloalquilo o heterociclilo; V está seleccionado, de modo independiente, del grupo que consiste en (i) hidrogeno, alquilo, alquilo C9-30, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halogeno, -F, -CI, -Br, -I, -CN, -CF3, -SF3, -N3, -NH2, -NHA1, -NA2A3, -NO2, -OH, =O, -OCF3, -SCF3, -OCHF2, -SCHF2, -SH, -O-SO3H, -OP(O)(OH)2, -CHO, -COOH, -C(O)NH2, -SO3H, -P(O)(OH)2, -C(O)-A4, -C(O)O-A5, -C(O)NH-A6, -C(O)NA7A8, -O-A9, -O-(-A10-O)a-H (a = 1, 2, 3, 4, 5), -O(-A11-O)b-A12 (b = 1, 2, 3, 4, 5), -OC(O)-A13, -OC(O)-O-A14, -OC(O)-NHA15, -O-C(O)-A16A17, -OP(O)(OA18)(OA19), -OSi(A20)(A21)(A22), -OS(O)2-A23, -NHC(O)-NH2, -NHC(O)-A24, -NA25C(O)-A26, -NH-C(O)-O-A27, -NH-C(O)-NH-A28, -NH-C(O)-NA29A30, -NA31-C(O)-O-A32, -NA33-C(O)-NH-A34, -NA35-C(O)-NA36A37, -NHS(O2)-A38, -NA39S(O2)-A40, -S-A41, -S(O)-A42, -S(O2)-A43, -S(O2)NH-A44, -S(O2)NA45A46, -S(O2)O-A47, -P(O)(OA48)(OA49), -Si(A50)(A51)(A52), -C(NH)-NH2, -C(NA53)-NH2, -C(NH)-NHA54, -C(NH)-NA55A56, -C(NA57)-NHA58, -C(NA59)-NA60A61, -NH-C(O)-NH-O-A62, -NH-C(O)-NA63-O-A64, -NA65-C(O)-NA66-O-A67, -N(-C(O)-NH-O-A68)2, -N(-C(O)-NA69-O-A70)2, -N(-C(O)-NH-O-A71)(-C(O)-NA72-O-A73), -C(S)-A74, -C(S)-O-A75, -C(S)-NH-A76, -C(S)-NA77A78, -C(O)-NH-O-A79, -C(O)-NA80-O-A81, -C(S)-NH-O-A82, -C(S)-NA83-O-A84, -C(O)-NH-NH-A85, -C(O)-NH-NA86A87, -C(O)-NA88-NA89A90, -C(S)-NH-NH-A91, -C(S)-NH-NA92A93, -C(S)-NA94-NA95A96, -C(O)-C(O)-O-A97, -C(O)-C(O)-NH2, -C(O)-C(O)-NHA98, -C(O)-C(O)-NA99A100, -C(S)-C(O)-O-A101, -C(O)-C(S)-O-A102, -C(S)-C(S)-O-A103, -C(S)-C(O)-NH2, -C(S)-C(O)-NHA104, -C(S)-C(O)-NA105A106, -C(S)-C(S)-NH2, -C(S)-C(S)-NHA107, -C(S)-C(S)-NA108A109, -C(O)-C(S)-NH2, -C(O)-C(S)-NHA110, -C(O)-C(S)-NA111A112; en donde A1, A2, A3, A4, A5, A6, A7, A8, A9, A10, A11, A12, A13, A14, A15, A16, A17, A18, A19, A20, A21, A22, A23, A24, A25, A26, A27, A28, A29, A30, A31, A32, A33, A34, A35, A36, A37, A38, A39, A40, A41, A42, A43, A44, A45, A46, A47, A48, A49, A50, A51, A52, A53, A54, A55, A56, A57, A58, A59, A60, A61, A62, A63, A64, A65, A66, A67, A68, A69, A70, A71, A72, A73, A74, A75, A76, A77, A78, A79, A80, A81, A82, A83, A84, A85, A86, A87, A88, A89, A90, A91, A92, A93, A94, A95, A96, A97, A98, A99, A100, A101, A102, A103, A104, A105, A106, A107, A108, A109, A110, A111, A112 están seleccionados, de modo independiente entre sí, del grupo que consiste en alquilo, alquilo C9-30, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo y en donde alternativamente A7, A8 y/o A16, A17 y/o A29, A30 y/o A36, A37 y/o A45, A46 y/o A55, A56 y/o A60, A61 y/o A77, A78 y/o A86, A87 y/o A89, A90 y/o A92, A93 y/o A95, A96 y/o A99, A100 y/o A105, A106 y/o A108, A109 y/o A111, A112, respectivamente, también pueden formar juntos heterociclilo; en donde opcionalmente los anteriores sustituyentes del grupo de sustituyentes (i) pueden estar sustituidos, a su vez, de modo independiente entre sí, con uno o varios sustituyentes V iguales o diferentes; m es, de modo independiente, 0, 1, 2, o 3; n es, de modo independiente, 0, 1, 2, o 3; o es, de modo independiente, 0, 1, 2, o 3; y las sales, derivados, profármacos, solvatos y estereoisomeros fisiologicamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP100101047A 2009-04-02 2010-03-31 Derivados de piperidina y piperazina inhibidores de autotaxinas, composiciones farmaceuticas que los comprenden, proceso para prepararlos y uso de los mismos en el tratamiento del cancer y otras patologias asociadas. AR076005A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09004856 2009-04-02

Publications (1)

Publication Number Publication Date
AR076005A1 true AR076005A1 (es) 2011-05-11

Family

ID=42359429

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101047A AR076005A1 (es) 2009-04-02 2010-03-31 Derivados de piperidina y piperazina inhibidores de autotaxinas, composiciones farmaceuticas que los comprenden, proceso para prepararlos y uso de los mismos en el tratamiento del cancer y otras patologias asociadas.

Country Status (16)

Country Link
US (2) US8822476B2 (es)
EP (4) EP2623491A3 (es)
JP (2) JP5591318B2 (es)
KR (1) KR20120027177A (es)
CN (1) CN102369186B (es)
AR (1) AR076005A1 (es)
AU (1) AU2010234087B2 (es)
BR (1) BRPI1012679A2 (es)
CA (1) CA2757368C (es)
EA (1) EA201101400A1 (es)
ES (3) ES2775000T3 (es)
IL (1) IL215260A (es)
MX (1) MX2011010203A (es)
SG (1) SG174928A1 (es)
WO (1) WO2010115491A2 (es)
ZA (1) ZA201107985B (es)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102369186B (zh) * 2009-04-02 2014-07-09 默克专利有限公司 作为自分泌运动因子抑制剂的哌啶和哌嗪衍生物
US8598156B2 (en) 2010-03-25 2013-12-03 Glaxosmithkline Llc Chemical compounds
US8815265B2 (en) 2010-06-30 2014-08-26 Avon Products, Inc. Cosmetic use of N-substituted sulfonyloxybenzylamines and related compounds
CN106727054A (zh) 2010-06-30 2017-05-31 雅芳产品公司 用于刺激magp‑1以改善皮肤外观的组合物和方法
WO2012083178A1 (en) * 2010-12-17 2012-06-21 Neo Oncology Inc. Methods and devices for using isoperillyl alcohol
US20160038600A1 (en) 2012-08-03 2016-02-11 Neonc Technologies Inc. Pharmaceutical compositions comprising poh derivatives
EP2629851A1 (en) * 2010-10-22 2013-08-28 Janssen Pharmaceutica N.V. Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors
AU2012314943B9 (en) 2011-09-26 2017-06-08 Merck Patent Gmbh Benzyl piperidine compounds as lysophosphatidic acid (LPA) receptor antagonist
WO2013070879A1 (en) 2011-11-10 2013-05-16 Bristol-Myers Squibb Company Methods for treating spinal cord injury with lpa receptor antagonists
CN104364239B (zh) 2012-06-13 2017-08-25 霍夫曼-拉罗奇有限公司 二氮杂螺环烷烃和氮杂螺环烷烃
CA2878442A1 (en) 2012-09-25 2014-04-03 F. Hoffmann-La Roche Ag Hexahydropyrrolo[3,4-c]pyrrole derivatives and related compounds as autotaxin (atx) inhibitors and as inhibitors of the lysophosphatidic acid (lpa) production for treating e.g. renal diseases
CN104968656B (zh) 2012-12-19 2017-08-11 诺华股份有限公司 自分泌运动因子抑制剂
US9409895B2 (en) 2012-12-19 2016-08-09 Novartis Ag Autotaxin inhibitors
WO2014133112A1 (ja) * 2013-03-01 2014-09-04 国立大学法人東京大学 オートタキシン阻害活性を有する８－置換イミダゾピリミジノン誘導体
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
EA035256B1 (ru) 2013-07-18 2020-05-21 Новартис Аг Ингибиторы аутотаксинов, содержащие гетероарил-бензил-амидное ядро
WO2015042052A1 (en) 2013-09-17 2015-03-26 Pharmakea, Inc. Heterocyclic vinyl autotaxin inhibitor compounds
JP2016530209A (ja) 2013-09-17 2016-09-29 ファーマケア，インク． ビニルオートタキシン阻害剤化合物
JP2016531874A (ja) 2013-09-26 2016-10-13 ファーマケア，インク． オートタキシン阻害剤化合物
MY182095A (en) 2013-11-22 2021-01-18 Sabre Therapeutics Llc Autotaxin inhibitor compounds
CA2930735A1 (en) 2013-11-22 2015-05-28 Pharmakea, Inc. Tetracyclic autotaxin inhibitors
PE20160845A1 (es) * 2013-11-26 2016-09-10 Hoffmann La Roche Nuevo octahidro-ciclobuta[1,2-c;3,4-c']dipirrol-2-ilo
EA032357B1 (ru) 2014-03-26 2019-05-31 Ф. Хоффманн-Ля Рош Аг Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
HUE046820T2 (hu) 2014-03-26 2020-03-30 Hoffmann La Roche Biciklusos vegyületek autotaxin (ATX) és lizofoszfatidsav (LPA) termelésgátlókként
AP2016009496A0 (en) 2014-04-04 2016-10-31 X-Rx Inc Substituted spirocydic inhibitors of autotaxin
WO2015162558A1 (en) 2014-04-24 2015-10-29 Novartis Ag Autotaxin inhibitors
US9051320B1 (en) 2014-08-18 2015-06-09 Pharmakea, Inc. Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor
GB201501870D0 (en) 2015-02-04 2015-03-18 Cancer Rec Tech Ltd Autotaxin inhibitors
GB201502020D0 (en) 2015-02-06 2015-03-25 Cancer Rec Tech Ltd Autotaxin inhibitory compounds
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
US9879016B2 (en) 2015-04-17 2018-01-30 Abbvie Inc. Indazolones as modulators of TNF signaling
WO2016168641A1 (en) 2015-04-17 2016-10-20 Abbvie Inc. Tricyclic modulators of tnf signaling
US20160304496A1 (en) 2015-04-17 2016-10-20 Abbvie Inc. Indazolones as modulators of tnf signaling
ES2915267T3 (es) 2015-05-27 2022-06-21 Sabre Therapeutics Llc Inhibidores de autotaxina y usos de los mismos
CA2988306A1 (en) 2015-06-05 2016-12-08 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
MX377277B (es) 2015-09-04 2025-03-07 Hoffmann La Roche Derivados de fenoximetilo.
BR112018006034A2 (pt) 2015-09-24 2018-10-09 Hoffmann La Roche compostos bicíclicos como inibidores de atx
MA42923A (fr) 2015-09-24 2021-04-28 Hoffmann La Roche Composés bicycliques comme inhibiteurs mixtes de atx/ca
RU2725138C2 (ru) 2015-09-24 2020-06-30 Ф. Хоффманн-Ля Рош Аг Новые бициклические соединения в качестве двойных ингибиторов аутотаксина (atx)/карбоангидразы (ca)
WO2017050732A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
WO2018106643A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Heterocyclic azoles for the treatment of demyelinating diseases
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles for the treatment of demyelinating diseases
KR20190129924A (ko) 2017-03-16 2019-11-20 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물
CN110382484B (zh) 2017-03-16 2022-12-06 豪夫迈·罗氏有限公司 新的作为atx抑制剂的二环化合物
KR101798840B1 (ko) 2017-05-17 2017-11-17 주식회사 레고켐 바이오사이언스 신규 오토탁신 저해 화합물 및 이를 함유하는 약제학적 조성물
US10961242B2 (en) 2017-05-17 2021-03-30 Legochem Biosciences, Inc. Compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same
MX2020004557A (es) 2017-11-02 2020-10-05 Calico Life Sciences Llc Moduladores de la vía de estrés integrada.
CA3091142C (en) 2018-02-26 2023-04-11 Gilead Sciences, Inc. Substituted pyrrolizine compounds and uses thereof
WO2022042613A1 (zh) * 2020-08-27 2022-03-03 上海和誉生物医药科技有限公司 一种1h-吡唑-4-酰胺衍生物，其制备方法和应用
CN117396471A (zh) * 2021-10-01 2024-01-12 株式会社次代生物科学 新的哌啶衍生物和包含其的用于抑制自分泌运动因子的药物组合物
KR102502940B1 (ko) * 2021-11-30 2023-02-24 주식회사 넥스트젠바이오사이언스 오토탁신 저해제로서의 신규 화합물 및 이의 용도

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19608653A1 (de) 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido[5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
JP4166296B2 (ja) 1997-04-25 2008-10-15 塩野義製薬株式会社 ドーパミン受容体拮抗作用を有する化合物
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
WO2000061186A1 (en) 1999-04-08 2000-10-19 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
AR033517A1 (es) * 2000-04-08 2003-12-26 Astrazeneca Ab Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
GB0107907D0 (en) 2001-03-29 2001-05-23 Smithkline Beecham Plc Novel compounds
US20030139431A1 (en) 2001-09-24 2003-07-24 Kawakami Joel K. Guanidines which are agonist/antagonist ligands for neuropeptide FF (NPFF) receptors
US7019017B2 (en) 2002-05-14 2006-03-28 Baylor College Of Medicine Small molecule inhibitors of HER2 expression
EP1511738A4 (en) 2002-05-17 2007-05-09 Scios Inc TREATMENT OF FIBROPROLIFERATIVE DISEASES USING TGF BETA INHIBITORS
DE10228103A1 (de) 2002-06-24 2004-01-15 Bayer Cropscience Ag Fungizide Wirkstoffkombinationen
EP1554272B1 (en) * 2002-08-09 2006-10-25 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
AU2003288994A1 (en) * 2002-12-10 2004-06-30 Ono Pharmaceutical Co., Ltd. Nitrogen-containing heterocyclic compounds and medicinal use thereof
AU2003293555A1 (en) 2002-12-17 2004-07-29 Schering Corporation 17 beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
AR042956A1 (es) * 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
RU2366655C2 (ru) * 2003-03-14 2009-09-10 Оно Фармасьютикал Ко., Лтд. Азотсодержащие гетероциклические производные и лекарственные средства, содержащие их в качестве активного ингредиента
JP2007505951A (ja) * 2003-06-13 2007-03-15 シエーリング アクチエンゲゼルシャフト Ｃｃｒ−５アンタゴニストとしてのキノリルアミド誘導体類
US7563748B2 (en) 2003-06-23 2009-07-21 Cognis Ip Management Gmbh Alcohol alkoxylate carriers for pesticide active ingredients
JO2525B1 (en) 2004-04-08 2010-03-17 شركة جانسين فارماسوتيكا ان. في Derived 4-alkyl-and-4-canoelperidine derivatives and their use as anti-neroquin
EP1769092A4 (en) 2004-06-29 2008-08-06 Europ Nickel Plc IMPROVED LIXIVIATION OF BASE METALS
US20070032475A1 (en) * 2005-04-15 2007-02-08 Ye Xiaocong M Novel compounds useful for bradykinin B1 receptor antagonism
DE602006020138D1 (de) 2005-06-29 2011-03-31 Compumedics Ltd Sensoranordnung mit leitfähiger brücke
DE102005050892A1 (de) * 2005-10-21 2007-04-26 Boehringer Ingelheim Pharma Gmbh & Co. Kg Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
JP2009528280A (ja) * 2006-02-16 2009-08-06 シェーリング コーポレイション Ｅｒｋインヒビターとしてのピロリジン誘導体
MX2008012161A (es) 2006-03-21 2008-10-03 Schering Corp Compuestos heterociclicos de piridina sustituida con actividad antagonista de cxcr3.
WO2007115805A2 (en) 2006-04-05 2007-10-18 European Molecular Biology Laboratory (Embl) Aurora kinase inhibitors
TW200801513A (en) 2006-06-29 2008-01-01 Fermiscan Australia Pty Ltd Improved process
EP2041117B1 (en) * 2006-07-14 2012-08-22 Merck Sharp & Dohme Corp. Heterocyclic substituted piperazine compounds with cxcr3 antagonist activity
EP2099454A4 (en) 2006-11-17 2010-11-10 Abbott Lab AMINOPYRROLIDINES AS CHEMOKINE RECEPTOR ANTAGONISTS
EP2220073B1 (en) * 2007-11-15 2014-09-03 MSD Italia S.r.l. Pyridazinone derivatives as parp inhibitors
MX2011002001A (es) * 2008-08-26 2011-05-25 Merisant Company Composiciones endulzantes que comprenden rebaudiosida a, eritritol, un carbohidrato de disacarido o fructosa y una cantidad mejorada del sabor de celulosa, y metodos para su fabricacion.
TW201038572A (en) 2009-03-25 2010-11-01 Gruenenthal Gmbh Substituted spiro-amide compounds
AU2010230646B2 (en) * 2009-04-02 2015-11-26 Merck Patent Gmbh Heterocyclic compounds as autotaxin inhibitors
CN102369186B (zh) * 2009-04-02 2014-07-09 默克专利有限公司 作为自分泌运动因子抑制剂的哌啶和哌嗪衍生物

Also Published As

Publication number Publication date
EA201101400A1 (ru) 2012-07-30
US8822476B2 (en) 2014-09-02
ES2880623T3 (es) 2021-11-25
JP5965947B2 (ja) 2016-08-10
CN102369186B (zh) 2014-07-09
US20140343075A1 (en) 2014-11-20
SG174928A1 (en) 2011-11-28
WO2010115491A3 (en) 2011-02-03
AU2010234087B2 (en) 2016-05-12
EP2623101B1 (en) 2021-04-21
ES2775000T3 (es) 2020-07-23
EP2414330A2 (en) 2012-02-08
US20120059016A1 (en) 2012-03-08
IL215260A (en) 2015-02-26
CN102369186A (zh) 2012-03-07
EP2623101A1 (en) 2013-08-07
JP2012522732A (ja) 2012-09-27
BRPI1012679A2 (pt) 2016-04-05
US9452997B2 (en) 2016-09-27
EP2623491A2 (en) 2013-08-07
ZA201107985B (en) 2012-07-25
EP2626072A1 (en) 2013-08-14
IL215260A0 (en) 2011-12-29
CA2757368A1 (en) 2010-10-14
EP2626072B1 (en) 2019-12-04
MX2011010203A (es) 2011-10-14
EP2414330B1 (en) 2013-05-01
CA2757368C (en) 2019-03-12
JP5591318B2 (ja) 2014-09-17
WO2010115491A2 (en) 2010-10-14
KR20120027177A (ko) 2012-03-21
ES2422718T3 (es) 2013-09-13
JP2014208700A (ja) 2014-11-06
AU2010234087A1 (en) 2011-11-17
EP2623491A3 (en) 2014-07-30

Similar Documents

Publication Publication Date Title
AR076005A1 (es) Derivados de piperidina y piperazina inhibidores de autotaxinas, composiciones farmaceuticas que los comprenden, proceso para prepararlos y uso de los mismos en el tratamiento del cancer y otras patologias asociadas.
AR076007A1 (es) Compuestos heterociclicos inhibidores de autotaxinas utiles para el tratamiento del cancer, composiciones farmaceuticas que los comprenden y proceso para prepararlos.
ES2407852T3 (es) Pirido[4,3-d]pirimidinas 2,5-diamino sustituidas como inhibidores de autotaxina frente al cáncer
Smelick et al. Prevalence of acid-reducing agents (ARA) in cancer populations and ARA drug–drug interaction potential for molecular targeted agents in clinical development
EP1877055A2 (en) 4-aminoquinoline compounds for treating virus-related conditions
JP2009535340A (ja) ジメチルフェニル化合物の結晶性形態
NO20050068L (no) Nye karboksamid-forbindelser med en mch-antagonist-virkning, medikamenter inneholdende disse forbindelsene, og fremgangsmater for fremstilling derav
RU2014146993A (ru) Производное хиназолиндиона
CA2958520A1 (en) Quinolium conjugates of cyclosporin
AU2024203755A1 (en) Methods and compositions for treating pruritus, xerosis, and associated disease using CCR3-inhibitors
Luo et al. Calcitonin gene-related peptide (CGRP) receptor antagonists: Pyridine as a replacement for a core amide group
Matsui-Sakata et al. Pharmacokinetic-pharmacodynamic analysis of antipsychotics-induced extrapyramidal symptoms based on receptor occupancy theory incorporating endogenous dopamine release
RU2012131223A (ru) Производные аминоалкилпиримидина в качестве антагонистов h4 рецептора гистамина
CN102791273A (zh) 小分子嘧啶衍生物及其使用方法
하균김 et al. Current trends in treatment of allergic rhinitis
WO2023141278A2 (en) Composite particle formulations and applications thereof
Lee Diagnosis and treatment of allergic rhinitis
AR126412A1 (es) Composiciones, métodos y sistemas para la administración de fármacos en aerosol
US20240316205A1 (en) Composition containing cationic hydroxyethyl cellulose
EP4308077A1 (en) Long acting injectable formulation comprising risperidone and biodegradable polymers
Pérez Calibrating a household survey by using the CALMAR program.
Zhang et al. Suppression of Cytokine Release by Fluticasone Furoate vs
Radulescu et al. The solubility of oxicams, antifungal azoles and selected psychotropic drugs in simulated gastro-intestinal fluids and the consequences on their biopharmaceutical classification
Kaul et al. Pharmacokinetic (PK) interaction between efavirenz (EFV) and diltiazem (DTZ) or itraconazole (ITR) after multiple-dose administration in adult healthy subjects
González Vázquez et al. Predissociation in methyl iodide. An efficient test for MRCI/CASSCF methodology including nonadiabatic couplings

Legal Events

Date Code Title Description
FB Suspension of granting procedure