ES2547124T3 - Inhibidores de autotaxina - Google Patents

Inhibidores de autotaxina Download PDF

Info

Publication number
ES2547124T3
ES2547124T3 ES10707839T ES10707839T ES2547124T3 ES 2547124 T3 ES2547124 T3 ES 2547124T3 ES 10707839 T ES10707839 T ES 10707839T ES 10707839 T ES10707839 T ES 10707839T ES 2547124 T3 ES2547124 T3 ES 2547124T3
Authority
ES
Spain
Prior art keywords
group
independently selected
aryl
alkyl
substituents
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES10707839T
Other languages
English (en)
Inventor
Melanie Schultz
Kai Schiemann
Wolfgang Staehle
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Patent GmbH
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
Application granted granted Critical
Publication of ES2547124T3 publication Critical patent/ES2547124T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • C07D401/02—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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Compuesto según la fórmula (I)**Fórmula** donde: W1, W2 juntos forman independientemente "-N>=N-, -C(O)-O--; Y1 se selecciona independientemente a partir del grupo compuesto por "-C(O)-, -C(S)-, -N(R10)-C(O)-, -C(O)-N(R11)-, -C(R12)(R13)- y enlace sencillo-; Y2 se selecciona independientemente a partir del grupo compuesto por "-C(R14)(R15)-, -O-, -N(R16)-, -C(O)-NH- y enlace sencillo-; Z1 se selecciona independientemente a partir del grupo compuesto por "O, S y N(R17)"; L se selecciona independientemente a partir del grupo compuesto por:**Fórmula** B se selecciona independientemente a partir del grupo compuesto por "arilo", en donde el "arilo" pueden estar sustituidos independientemente con uno o más sustituyentes idénticos o diferentes seleccionados a partir del grupo compuesto por: (i) "hidrógeno, alquilo, alquilo (C9-C30), cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halógeno, -F, -Cl, -Br, -I, -CN, -CF3, -N3, -NH2, -NHX1, -NX2X3, -NO2, -OH, -OCF3, -SCF3, -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-X14, -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, 10 -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 y -C(O)-C(S)-NX111X112-; 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, 15 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 y X112 se seleccionan independientemente entre sí a partir del grupo compuesto por: "alquilo, alquilo (C9-C30), cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo" y donde alternativamente 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, juntos también pueden formar un "heterociclilo"; donde, opcionalmente, los sustituyentes anteriores del grupo de sustituyentes (i) pueden estar sustituidos a su vez independientemente entre sí con uno o más sustituyentes V idénticos o diferentes R1, R2, R3, R4, R10, R11, R12, R13, R14, R15, R16 y R17 se seleccionan independientemente entre sí a partir del grupo compuesto por: "V";
ES10707839T 2009-04-02 2010-03-09 Inhibidores de autotaxina Active ES2547124T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09004866 2009-04-02
EP09004866 2009-04-02
PCT/EP2010/001457 WO2010112124A1 (en) 2009-04-02 2010-03-09 Autotaxin inhibitors

Publications (1)

Publication Number Publication Date
ES2547124T3 true ES2547124T3 (es) 2015-10-01

Family

ID=42235629

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10707839T Active ES2547124T3 (es) 2009-04-02 2010-03-09 Inhibidores de autotaxina

Country Status (14)

Country Link
US (2) US8329907B2 (es)
EP (1) EP2414346B1 (es)
JP (1) JP5779172B2 (es)
KR (1) KR20120004483A (es)
CN (1) CN102369195B (es)
AR (1) AR076007A1 (es)
AU (1) AU2010230585B2 (es)
CA (1) CA2757415C (es)
EA (1) EA201101396A1 (es)
ES (1) ES2547124T3 (es)
IL (1) IL215259A (es)
MX (1) MX2011010218A (es)
SG (1) SG174518A1 (es)
WO (1) WO2010112124A1 (es)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2794153C (en) 2010-03-25 2018-01-02 Glaxosmithkline Llc Substituted indoline derivatives as perk inhibitors
CN102358742B (zh) * 2011-08-24 2014-04-09 天津药物研究院 具有抗肿瘤活性的噻唑类化合物
JP6258928B2 (ja) 2012-06-13 2018-01-10 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規ジアザスピロシクロアルカンおよびアザスピロシクロアルカン
CN102702135B (zh) * 2012-06-15 2014-05-28 中国农业大学 一种含苯并噻唑结构的苯甲酰基硫脲类化合物及其制备方法和应用
AU2013322838B2 (en) * 2012-09-25 2018-02-01 F. Hoffmann-La Roche Ag New bicyclic derivatives
US9409895B2 (en) 2012-12-19 2016-08-09 Novartis Ag Autotaxin inhibitors
CA2895448A1 (en) 2012-12-19 2014-06-26 Novartis Ag Autotaxin inhibitors
US20160002247A1 (en) * 2013-03-01 2016-01-07 The University Of Tokyo 8-substituted imidazopyrimidinone derivative having autotaxin inhibitory activity
AR095079A1 (es) * 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
EP3269716B1 (en) 2013-03-14 2020-09-16 Galapagos N.V. Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders
WO2015042053A1 (en) * 2013-09-17 2015-03-26 Pharmakea, Inc. Vinyl autotaxin inhibitor compounds
WO2015042052A1 (en) * 2013-09-17 2015-03-26 Pharmakea, Inc. Heterocyclic vinyl autotaxin inhibitor compounds
WO2015048301A1 (en) * 2013-09-26 2015-04-02 Pharmakea, Inc. Autotaxin inhibitor compounds
MX2016006623A (es) 2013-11-22 2017-03-10 Pharmakea Inc Compuestos de inhibidor de autotaxina.
US9926318B2 (en) 2013-11-22 2018-03-27 Pharmakea, Inc. Tetracyclic autotaxin inhibitors
UA118201C2 (uk) * 2013-11-26 2018-12-10 Ф. Хоффманн-Ля Рош Аг НОВИЙ ОКТАГІДРОЦИКЛОБУТА[1,2-c;3,4-c']ДИПІРОЛ-2-ІЛ
EA037928B1 (ru) * 2014-03-26 2021-06-08 Ф. Хоффманн-Ля Рош Аг Бициклические соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
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)
CN107106559A (zh) 2014-04-04 2017-08-29 X-Rx股份有限公司 自分泌运动因子的取代的螺环抑制剂
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
EA036337B1 (ru) 2015-05-27 2020-10-28 Сабре Терапьютикс Ллс Ингибиторы аутотаксина и их применения
EP3302465A1 (en) 2015-06-05 2018-04-11 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
MX2020004504A (es) 2015-09-04 2021-11-10 Hoffmann La Roche Derivados de fenoximetilo.
MA42918A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
PE20180552A1 (es) 2015-09-24 2018-04-02 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca
EP3353181B1 (en) 2015-09-24 2021-08-11 F. Hoffmann-La Roche AG Bicyclic compounds as dual atx/ca inhibitors
MA42919A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
EP3182211A1 (fr) * 2015-12-17 2017-06-21 Nivarox-FAR S.A. Pièce composite avec moyens élastiques sous contrainte
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles 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
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
EP3596060B1 (en) 2017-03-16 2023-09-20 F. Hoffmann-La Roche AG New bicyclic compounds as atx inhibitors
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
CN111788204B (zh) 2018-02-26 2023-05-05 吉利德科学公司 作为hbv复制抑制剂的取代吡咯嗪化合物
MX2021015996A (es) 2019-07-11 2022-06-08 Escape Bio Inc Indazoles y azaindazoles como inhibidores de cinasa de repetición rica en leucina 2 (lrrk2).
CN112778274B (zh) * 2019-11-05 2022-02-15 四川海思科制药有限公司 一种含氮杂环衍生物及其制备
CN111454278B (zh) * 2020-05-15 2021-03-19 四川大学 Pak1抑制剂及其合成和在制备抗肿瘤药物中的应用
CN117980300A (zh) * 2021-09-21 2024-05-03 明斯特大学 自分泌运动因子抑制剂
KR102502940B1 (ko) * 2021-11-30 2023-02-24 주식회사 넥스트젠바이오사이언스 오토탁신 저해제로서의 신규 화합물 및 이의 용도

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL135176A0 (en) * 1997-11-10 2001-05-20 Bristol Myers Squibb Co Benzothiazole derivatives and pharmaceutical compositions containing the same
DE19834751A1 (de) 1998-08-01 2000-02-03 Boehringer Ingelheim Pharma Disubstituierte bicyclische Heterocyclen, ihre Herstellung und ihre Verwendung als Arzneimittel
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
AU4972900A (en) 1999-04-08 2000-11-14 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
US20030139431A1 (en) 2001-09-24 2003-07-24 Kawakami Joel K. Guanidines which are agonist/antagonist ligands for neuropeptide FF (NPFF) receptors
EP1511738A4 (en) 2002-05-17 2007-05-09 Scios Inc TREATMENT OF FIBROPROLIFERATIVE DISEASES USING TGF BETA INHIBITORS
EP1628970A2 (en) 2003-04-30 2006-03-01 The Institutes of Pharmaceutical Discovery, LLC Heterocycle substituted carboxylic acids as inhibitors of protein tyrosine phosphatase-1b
AU2004253967B2 (en) 2003-07-03 2010-02-18 Cytovia, Inc. 4-arylamino-quinazolines as activators of caspases and inducers of apoptosis
US7749999B2 (en) 2003-09-11 2010-07-06 Itherx Pharmaceuticals, Inc. Alpha-ketoamides and derivatives thereof
WO2005092899A1 (en) * 2004-03-26 2005-10-06 Methylgene Inc. Inhibitors of histone deacetylase
EP1828152B1 (en) 2004-12-08 2008-08-20 Bristol-Myers Squibb Company Heterocyclic compounds as inhibitors of factor viia
EP1838690A2 (en) 2004-12-21 2007-10-03 Devgen N.V. Compounds with kv4 ion channel activity
CA2592900A1 (en) 2005-01-03 2006-07-13 Myriad Genetics Inc. Nitrogen containing bicyclic compounds and therapeutical use thereof
RS51385B (en) 2005-01-07 2011-02-28 Pfizer Products Inc. HETEROAROMATIC COMPOUNDS OF HINOLINE AND THEIR USE AS PDE10 INHIBITORS
NZ561029A (en) 2005-03-14 2011-03-31 High Point Pharmaceuticals Llc Benzazole dervatives, compositions, and method of use as beta-secretase inhibitors
MX2007012449A (es) 2005-04-06 2007-12-05 Irm Llc Compuestos y composiciones que contienen diaril-amina, y su uso como moduladores de los receptores nucleares de hormonas esteroideas.
WO2006124874A2 (en) * 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
CN101277939A (zh) 2005-09-09 2008-10-01 布里斯托尔-迈尔斯斯奎布公司 无环ikur抑制剂
ATE541844T1 (de) 2005-12-21 2012-02-15 Abbott Lab Antivirale verbindungen
WO2007110868A2 (en) 2006-03-28 2007-10-04 Atir Holding S.A. Heterocyclic compounds and uses thereof in the treatment of sexual disorders
WO2008014286A1 (en) 2006-07-24 2008-01-31 University Of Virginia Patent Foundation Vinyl phosphonate lysophosphatidic acid receptor antagonists
GB0619176D0 (en) 2006-09-29 2006-11-08 Lectus Therapeutics Ltd Ion channel modulators & uses thereof
EP2099454A4 (en) 2006-11-17 2010-11-10 Abbott Lab AMINOPYRROLIDINES AS CHEMOKINE RECEPTOR ANTAGONISTS
ES2531256T3 (es) 2007-01-25 2015-03-12 Du Pont Amidas fungicidas
WO2008124393A1 (en) * 2007-04-04 2008-10-16 Irm Llc Benzothiazole derivatives and their use as protein kinase inhibitors

Also Published As

Publication number Publication date
US20130023556A1 (en) 2013-01-24
CN102369195A (zh) 2012-03-07
US20120015976A1 (en) 2012-01-19
EA201101396A1 (ru) 2012-09-28
AU2010230585B2 (en) 2016-03-24
CA2757415A1 (en) 2010-10-07
JP2012522734A (ja) 2012-09-27
KR20120004483A (ko) 2012-01-12
CN102369195B (zh) 2014-04-16
WO2010112124A1 (en) 2010-10-07
SG174518A1 (en) 2011-10-28
AR076007A1 (es) 2011-05-11
EP2414346B1 (en) 2015-06-24
MX2011010218A (es) 2011-10-10
IL215259A0 (en) 2011-12-29
US8329907B2 (en) 2012-12-11
CA2757415C (en) 2018-02-06
IL215259A (en) 2016-05-31
AU2010230585A8 (en) 2012-01-19
US8497283B2 (en) 2013-07-30
EP2414346A1 (en) 2012-02-08
AU2010230585A1 (en) 2011-11-17
JP5779172B2 (ja) 2015-09-16

Similar Documents

Publication Publication Date Title
ES2547124T3 (es) Inhibidores de autotaxina
ES2407852T3 (es) Pirido[4,3-d]pirimidinas 2,5-diamino sustituidas como inhibidores de autotaxina frente al cáncer
AR066145A1 (es) Derivados de tetrahidrocarbazol como ligandos de receptores acoplados a la proteina g(gpcr),composiciones farmaceuticas que los contienen y usos para el tratamiento de trastornos neurologicos o neurodegenerativos,de fertilidad,infecciones por vih,y como agentes antineoplasicos.
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.
PE20080914A1 (es) Anticuerpos anti-activina a
WO2008122441A4 (en) Anti-amyloid antibodies and their use in diagnosis and therapy of amyloid diseases
CL2019002195A1 (es) Anticuerpos vista antihumanos y su uso. (divisional solicitud 201802925).
PE20081409A1 (es) Antagonistas del receptor de progesterona
DE602005016162D1 (de) Benzimidazolderivate und ihre Verwendung als AII Rezeptor-Antagonist
JP2009062537A5 (es)
ATE406286T1 (de) Stufe für ein fahrzeug
WO2009054434A1 (ja) Ｎｐｙ ｙ５受容体拮抗作用を有するアミン誘導体およびその用途
Stanić There are exactly 172 connected integral graphs up to 10 vertices.
WO2007096782A3 (en) Compositions for disorders associated wtth metachromatic cell activation
JP2015528463A5 (es)
PE20091782A1 (es) Derivados de sulfonamida sustituida
ATE400472T1 (de) Verfahren zum anklappen eines aussenspiegels eines kraftfahrzeugs
Khalili The Characteristics of a University Professor in Iran's Higher Education Based on the Thoughts of the Supreme Leader; A Data Base Study
Bersteind et al. Pricing and revenue management: present and trends.
Škrbić et al. Faculty information system based on open source technologies.
Febrero A present overview on functional data analysis.
Shinmura Feature Selection of Singh et al. Microarray Data (12)
Ugarte A brief introduction to spatio-temporal modelling.
Aparicio et al. Time-Reversion of VARMA processes by polynomical methods.
Villarroel Probabilistic valuation of certain unit-linked contracts.