AU2005236055B2 - Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators - Google Patents

Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators Download PDF

Info

Publication number
AU2005236055B2
AU2005236055B2 AU2005236055A AU2005236055A AU2005236055B2 AU 2005236055 B2 AU2005236055 B2 AU 2005236055B2 AU 2005236055 A AU2005236055 A AU 2005236055A AU 2005236055 A AU2005236055 A AU 2005236055A AU 2005236055 B2 AU2005236055 B2 AU 2005236055B2
Authority
AU
Australia
Prior art keywords
phenyl
compound
thiazol
amino
thiophen
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.)
Ceased
Application number
AU2005236055A
Other languages
English (en)
Other versions
AU2005236055A1 (en
Inventor
Robert C. Andrews
Murty N. Arimilli
John Dankwardt
Bapu R. Gaddam
Adnan M. M. Mjalli
Ghassan Qabaja
Govindan Subramanian
Ye E. Tian
Samuel Victory
Jeff Zhu
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.)
vTv Therapeutics LLC
Original Assignee
Trans Tech Pharma 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 Trans Tech Pharma Inc filed Critical Trans Tech Pharma Inc
Publication of AU2005236055A1 publication Critical patent/AU2005236055A1/en
Assigned to TRANSTECH PHARMA, INC. reassignment TRANSTECH PHARMA, INC. Request for Assignment Assignors: TRANSTECH PHARMA INC.
Application granted granted Critical
Publication of AU2005236055B2 publication Critical patent/AU2005236055B2/en
Assigned to TRANSTECH PHARMA, LLC reassignment TRANSTECH PHARMA, LLC Request for Assignment Assignors: TRANSTECH PHARMA, INC.
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/50—Nitrogen atoms bound to hetero atoms
    • C07D277/52—Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/26—Radicals substituted by sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/50—Nitrogen atoms bound to hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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 in position 2
    • C07D277/82—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2005236055A 2004-04-20 2005-04-20 Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators Ceased AU2005236055B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US56388204P 2004-04-20 2004-04-20
US60/563,882 2004-04-20
PCT/US2005/013386 WO2005103022A1 (en) 2004-04-20 2005-04-20 Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators

Publications (2)

Publication Number Publication Date
AU2005236055A1 AU2005236055A1 (en) 2005-11-03
AU2005236055B2 true AU2005236055B2 (en) 2011-10-06

Family

ID=34971867

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2005236055A Ceased AU2005236055B2 (en) 2004-04-20 2005-04-20 Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators

Country Status (12)

Country Link
US (1) US7820704B2 (enExample)
EP (1) EP1753735A1 (enExample)
JP (1) JP4879165B2 (enExample)
CN (1) CN1946703A (enExample)
AU (1) AU2005236055B2 (enExample)
BR (1) BRPI0510095A (enExample)
CA (1) CA2562075C (enExample)
IL (1) IL178597A0 (enExample)
MX (1) MXPA06012130A (enExample)
NZ (1) NZ550114A (enExample)
WO (1) WO2005103022A1 (enExample)
ZA (1) ZA200608225B (enExample)

Families Citing this family (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200500362A (en) * 2003-04-09 2005-01-01 Japan Tobacco Inc 5-membered heteroaromatic ring compound and pharmaceutical use thereof
US7262318B2 (en) * 2004-03-10 2007-08-28 Pfizer, Inc. Substituted heteroaryl- and phenylsulfamoyl compounds
DK1763517T3 (da) * 2004-06-28 2011-06-06 Hoffmann La Roche Pyrimidinderivater som 11beta-HSD1-inhibitorer
PE20071025A1 (es) * 2006-01-31 2007-10-17 Mitsubishi Tanabe Pharma Corp Compuesto amina trisustituido
DE102006021874B4 (de) 2006-05-11 2008-03-27 Sanofi-Aventis 4,5-Diphenyl-pyrimidinyl-amino substituierte Carbonsäuren, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
MX2008015143A (es) * 2006-06-01 2008-12-10 Hoffmann La Roche Derivados de tiazol.
WO2008011191A1 (en) * 2006-07-21 2008-01-24 Replidyne, Inc. Antibacterial heterocyclic ureas
WO2008022281A1 (en) 2006-08-16 2008-02-21 The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone Small molecule inhibitors of kynurenine-3-monooxygenase
US8071631B2 (en) 2006-08-16 2011-12-06 The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone Small molecule inhibitors of kynurenine-3-monooxygenase
WO2009015193A1 (en) * 2007-07-23 2009-01-29 Replidyne, Inc. Antibacterial sulfone and sulfoxide substituted heterocyclic urea compounds
US8148380B2 (en) 2007-07-23 2012-04-03 Crestone, Inc. Antibacterial amide and sulfonamide substituted heterocyclic urea compounds
CN101889004B (zh) 2007-10-12 2014-09-10 阿斯利康公司 蛋白激酶抑制剂
US7973051B2 (en) * 2007-11-30 2011-07-05 Hoffman-La Roche Inc. Aminothiazoles as FBPase inhibitors for diabetes
DE102008019838A1 (de) * 2008-04-19 2009-12-10 Boehringer Ingelheim International Gmbh Neue Arylsulfonylglycin-Derivate, deren Herstellung und deren Verwendung als Arzneimittel
WO2009132310A1 (en) 2008-04-25 2009-10-29 Wisconsin Alumni Research Foundation Inhibitors of udp-galactopyranose mutase thwart mycobacterial growth
EP2303841A1 (en) 2008-07-14 2011-04-06 Gilead Sciences, Inc. Oxindolyl inhibitor compounds
NZ590320A (en) 2008-07-14 2012-12-21 Gilead Sciences Inc Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases
NZ590283A (en) 2008-07-14 2012-11-30 Gilead Sciences Inc Imidazolylpyrimidine compounds as hdac and / or cdk inhibitors
MX2011001090A (es) 2008-07-28 2011-03-15 Gilead Sciences Inc Compuestos de inhibidor de desacetilasa de histona de cicloalquilideno y heterocicloalquilideno.
JP2012501334A (ja) * 2008-08-29 2012-01-19 トランス テック ファーマ，インコーポレイテッド 置換アミノチアゾール誘導体、医薬組成物、および使用の方法
KR20120031170A (ko) 2009-06-08 2012-03-30 길리애드 사이언시즈, 인코포레이티드 알카노일아미노 벤즈아미드 아닐린 ｈｄａｃ 저해제 화합물
US8283357B2 (en) 2009-06-08 2012-10-09 Gilead Sciences, Inc. Cycloalkylcarbamate benzamide aniline HDAC inhibitor compounds
MX2012006962A (es) 2009-12-17 2012-07-17 Merck Patent Gmbh Inhibidores de la esfingosina quinasa.
WO2011076732A1 (en) * 2009-12-21 2011-06-30 Euroscreen S.A. Compounds, pharmaceutical composition and methods for use in treating gastrointestinal disorders
WO2011076734A1 (en) * 2009-12-21 2011-06-30 Euroscreen S.A. Compounds, pharmaceutical composition and methods for use in treating inflammatory diseases
KR20130016244A (ko) 2010-03-10 2013-02-14 인게니움 파르마코이티칼스 게엠베하 단백질 키나아제의 억제제
NZ705058A (en) 2010-03-12 2016-10-28 Omeros Corp Pde10 inhibitors and related compositions and methods
EP3159331A1 (en) 2010-05-05 2017-04-26 Infinity Pharmaceuticals, Inc. Tetrazolones as inhibitors of fatty acid synthase
WO2012030165A2 (ko) 2010-08-31 2012-03-08 서울대학교산학협력단 P P A R δ 활성물질의 태자재프로그래밍용도
US20120316182A1 (en) 2011-06-10 2012-12-13 Calcimedica, Inc. Compounds that modulate intracellular calcium
US20130143927A1 (en) * 2011-06-10 2013-06-06 Calcimedica, Inc. Compounds that modulate intracellular calcium
WO2013059677A1 (en) 2011-10-19 2013-04-25 Calcimedica, Inc. Compounds that modulate intracellular calcium
WO2013178362A1 (en) * 2012-05-31 2013-12-05 Phenex Pharmaceuticals Ag Carboxamide or sulfonamide substituted thiazoles and related derivatives as modulators for the orphan nuclear receptor ror[gamma]
CA2888889A1 (en) * 2012-10-22 2014-05-01 Egenix, Inc. Compositions and methods for treating or preventing diseases or disorders associated with misregulated eif4e
EP2917194B1 (en) * 2012-11-06 2017-09-27 Eli Lilly and Company Novel benzyl sulfonamide compounds useful as mogat-2 inhibitors
EP2938610A2 (en) * 2012-12-28 2015-11-04 The U.S.A. as represented by the Secretary, Department of Health and Human Services Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof
TWI644899B (zh) 2013-02-04 2018-12-21 健生藥品公司 Ｆｌａｐ調節劑
EP3070085B1 (en) 2013-02-04 2019-01-09 Janssen Pharmaceutica NV Flap modulators
NZ716494A (en) 2014-04-28 2017-07-28 Omeros Corp Processes and intermediates for the preparation of a pde10 inhibitor
NZ716462A (en) 2014-04-28 2017-11-24 Omeros Corp Optically active pde10 inhibitor
US9708344B2 (en) 2014-06-03 2017-07-18 Wisconsin Alumni Research Foundation Inhibitors of UDP-galactopyranose mutase
CN107530313A (zh) 2015-04-24 2018-01-02 奥默罗斯公司 Pde10抑制剂以及相关组合物和方法
HRP20210745T1 (hr) 2015-05-15 2021-06-25 Aurigene Discovery Technologies Limited Supstituirani spojevi tetrahidrokinolinona kao ror gama modulatori
WO2016205304A1 (en) * 2015-06-16 2016-12-22 Signal Pharmaceuticals, Llc Methods of treatment using substituted diaminopyrimidyl compounds
WO2017070089A1 (en) 2015-10-19 2017-04-27 Incyte Corporation Heterocyclic compounds as immunomodulators
CA3003611C (en) 2015-11-04 2022-11-01 Omeros Corporation Solid state forms of a pde10 inhibitor
DK3377488T3 (da) 2015-11-19 2022-10-03 Incyte Corp Heterocykliske forbindelser som immunomodulatorer
MY199705A (en) 2015-12-22 2023-11-20 Incyte Corp Heterocyclic compounds as immunomodulators
US10080757B2 (en) 2016-03-11 2018-09-25 Wisconsin Alumni Research Foundation Inhibitors of UDP-galactopyranose mutase
TW201808950A (zh) 2016-05-06 2018-03-16 英塞特公司 作為免疫調節劑之雜環化合物
CN107382902B (zh) * 2016-05-17 2022-08-12 华东理工大学 噻唑类衍生物及其应用
US20170342060A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
SG11201811414TA (en) 2016-06-20 2019-01-30 Incyte Corp Heterocyclic compounds as immunomodulators
EP3484866B1 (en) 2016-07-14 2022-09-07 Incyte Corporation Heterocyclic compounds as immunomodulators
MA46045A (fr) 2016-08-29 2021-04-28 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
TW201811766A (zh) 2016-08-29 2018-04-01 瑞士商諾華公司 N-(吡啶-2-基)吡啶-磺醯胺衍生物及其用於疾病治療之用途
WO2018119236A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
US20180179202A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018119266A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Benzooxazole derivatives as immunomodulators
KR102641030B1 (ko) 2016-12-22 2024-02-29 인사이트 코포레이션 Pd-l1 내재화 유도제로서의 테트라하이드로 이미다조[4,5-c]피리딘 유도체
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
FI3774791T3 (fi) 2018-03-30 2023-03-21 Incyte Corp Heterosyklisiä yhdisteitä immunomodulaattoreina
BR112020022936A2 (pt) 2018-05-11 2021-02-02 Incyte Corporation derivados de tetra-hidro-imidazo[4,5-c]piridina como imunomoduladores de pd-l1
EP3846793B1 (en) * 2018-09-07 2024-01-24 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
CN109730999B (zh) * 2018-12-28 2021-12-24 中山大学 噻唑苯甲酰胺衍生在制备抗骨质疏松、抗骨关节炎药物中的应用
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11753406B2 (en) 2019-08-09 2023-09-12 Incyte Corporation Salts of a PD-1/PD-L1 inhibitor
BR112022002698A2 (pt) 2019-08-14 2022-07-19 Incyte Corp Compostos de imidazolil pirimidinilamina como inibidores de cdk2
MX2022003578A (es) 2019-09-30 2022-05-30 Incyte Corp Compuestos de pirido[3,2-d]pirimidina como inmunomoduladores.
MX2022004390A (es) 2019-10-11 2022-08-08 Incyte Corp Aminas biciclicas como inhibidores de la cinasa dependiente de ciclina 2 (cdk2).
BR112022009031A2 (pt) 2019-11-11 2022-10-11 Incyte Corp Sais e formas cristalinas de um inibidor de pd-1/pd-l1
US11753403B2 (en) 2020-03-03 2023-09-12 PIC Therapeutics, Inc. EIF4E inhibitors and uses thereof
CA3180670A1 (en) 2020-04-24 2021-10-28 Bayer Aktiengesellschaft Substituted aminothiazoles as dgkzeta inhibitors for immune activation
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式
MX2023005362A (es) 2020-11-06 2023-06-22 Incyte Corp Proceso para hacer un inhibidor de proteina de muerte programada 1 (pd-1)/ligando de muerte programada 1 (pd-l1) y sales y formas cristalinas del mismo.
CN112209886A (zh) * 2020-11-09 2021-01-12 沈阳药科大学 2-(3-氰基-4-烷氧基)苯基嘧啶衍生物及其制备方法和用途
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
CA3229560A1 (en) 2021-08-25 2023-03-02 Christopher L. Vandeusen Eif4e inhibitors and uses thereof
JP2024532276A (ja) 2021-08-25 2024-09-05 ピク セラピューティクス， インコーポレイテッド ｅＩＦ４Ｅ阻害剤及びその使用
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2607369B2 (ja) 1987-02-20 1997-05-07 興和株式会社 新規な複素環化合物
US5502025A (en) 1987-08-13 1996-03-26 Monsanto Company Safening herbicidal pyrazolylsulfonylureas
YU48319B (sh) 1988-08-01 1998-05-15 Monsanto Company Bezbednosni herbicidni derivati benzoeve kiseline
US5201933A (en) 1988-08-01 1993-04-13 Monsanto Company Safening herbicidal benzoic acid derivatives
FR2656610B1 (fr) 1989-12-29 1992-05-07 Sanofi Sa Derives d'amino-2 phenyl-4 thiazole, leur procede de preparation et leur application therapeutique.
JPH0532662A (ja) 1990-11-09 1993-02-09 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
DK0934937T3 (da) 1990-11-30 2002-04-02 Otsuka Pharma Co Ltd Azolderivater som superoxidradikalinhibitor
DE4124942A1 (de) 1991-07-27 1993-01-28 Thomae Gmbh Dr K 5-gliedrige heterocyclen, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
EP0627423A4 (en) 1992-01-22 1995-02-15 Nissan Chemical Ind Ltd SUBSTITUTED PYRAZOLE DERIVATIVES AND BACTERICIDES FOR AGRICULTURE AND GARDENING.
WO1993017681A1 (en) 1992-03-02 1993-09-16 Abbott Laboratories Angiotensin ii receptor antagonists
US6310034B1 (en) 1993-05-21 2001-10-30 Ut-Battelle, Llc Agouti polypeptide compositions
JPH07149745A (ja) 1993-11-30 1995-06-13 Hisamitsu Pharmaceut Co Inc 新規な２−アミノチアゾール誘導体
US5627131A (en) 1995-01-09 1997-05-06 Zeneca Limited Herbicidal compositions of 4-benzoylisoxazole and antidotes therefor
US5766877A (en) 1996-05-10 1998-06-16 Amgen Inc. Genes encoding art, an agouti-related transcript
WO1997047299A1 (en) 1996-06-12 1997-12-18 3-Dimensional Pharmaceuticals, Inc. Amidino and guanidino heterocyclic protease inhibitors
FR2754258B1 (fr) 1996-10-08 1998-12-31 Sanofi Sa Derives d'aminothiazole, leur procede de preparation et les compositions pharmaceutiques les contenant
US6011048A (en) 1997-01-28 2000-01-04 Merck & Co., Inc. Thiazole benzenesulfonamides as β3 agonists for treatment of diabetes and obesity
AU3964499A (en) 1998-03-30 1999-10-18 Gryphon Sciences Agouti-related protein analogs and methods of use
US6689873B1 (en) 1998-04-29 2004-02-10 Merck & Co., Inc. Nucleic acid encoding rat agouti related protein
EP1077960A1 (en) 1998-05-12 2001-02-28 American Home Products Corporation (2-acylaminothiazole-4-yl)acetic acid derivatives
CN1308618A (zh) 1998-05-12 2001-08-15 美国家用产品公司 用于治疗胰岛素抗性和高血糖的噁唑芳基－羧酸
US6699896B1 (en) 1998-05-12 2004-03-02 Wyeth Oxazole-aryl-carboxylic acids useful in the treatment of insulin resistance and hyperglycemia
GB9818666D0 (en) 1998-08-27 1998-10-21 Rhone Poulenc Agriculture New herbicidal method
US6303749B1 (en) 1999-01-29 2001-10-16 Amgen Inc. Agouti and agouti-related peptide analogs
CN1348370A (zh) 1999-04-15 2002-05-08 布里斯托尔-迈尔斯斯奎布公司 环状蛋白酪氨酸激酶抑制剂
US20040132788A1 (en) 1999-10-11 2004-07-08 Chabrier De Lassauniere Pierre-Etienne Derivatives of heterocycles with 5 members, their preparation and their use as medicaments
US7291641B2 (en) 1999-10-11 2007-11-06 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Derivatives of heterocycles with 5 members, their preparation and their use as medicaments
EP1125579A3 (en) 2000-01-18 2003-01-02 Pfizer Products Inc. Uses of agrp-melanocortin receptor binding modulating compounds
DE10006453A1 (de) 2000-02-14 2001-08-16 Bayer Ag Piperidylcarbonsäuren als Integrinantagonisten
HRP20030027A2 (en) * 2000-06-28 2004-02-29 Teva Pharma Carvedilol
AU2001268718B2 (en) 2000-06-29 2006-01-05 Abbott Laboratories Aryl phenylheterocyclyl sulfide derivatives and their use as cell adhesion-inhibiting anti-inflammatory and immune-suppressive agents
HUP0202719A3 (en) 2001-08-21 2006-01-30 Pfizer Prod Inc Pharmaceutical compositions for the treatment of female sexual dysfunctions
DE60208815T2 (de) 2001-10-12 2006-07-20 Bayer Pharmaceuticals Corp., West Haven Phenyl substituierte 5-gliedrige stickstoff enthaltende heterocyclen zur behandlung von fettleibigkeit
NZ532883A (en) 2001-11-08 2007-09-28 Ortho Mcneil Pharm Inc Novel 1,2,4-thiadiazole derivatives as melanocortin receptor modulators
EP1452530A4 (en) 2001-12-03 2005-11-30 Japan Tobacco Inc AZOL CONNECTION AND THEIR MEDICAL USE
US20030158199A1 (en) 2002-01-25 2003-08-21 Kylix, B.V. Novel compounds for inhibition of Tie-2
WO2003068738A1 (en) 2002-02-11 2003-08-21 Neurocrine Biosciences, Inc. Pyrrole derivatives as ligands of melanocortin receptors
PL372463A1 (en) * 2002-02-28 2005-07-25 F.Hoffmann-La Roche Ag Thiazole derivatives as npy receptor antagonists
UA79755C2 (en) * 2002-04-16 2007-07-25 Bayer Pharmaceuticals Corp Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation
WO2004004447A2 (en) 2002-07-03 2004-01-15 Merck & Co., Inc. Agouti-related protein deficient cells, non-human transgenic animals and methods of selecting compounds which regulate energy metabolism
BR0313278A (pt) * 2002-08-07 2005-07-05 Hoffmann La Roche Compostos, processo para a preparação de um composto, composição farmacêutica que compreende o mesmo e sua utilização, método para o tratamento e profilaxia de enfermidades e obesidade e utilização dos compostos
TW200500362A (en) 2003-04-09 2005-01-01 Japan Tobacco Inc 5-membered heteroaromatic ring compound and pharmaceutical use thereof
US20050009891A1 (en) 2003-07-09 2005-01-13 Lee Francis Y. Combination of SRC Kinase inhibitors and chemotherapeutic agents for the treatment of proliferative diseases
WO2006038594A1 (ja) 2004-10-04 2006-04-13 Ono Pharmaceutical Co., Ltd. Ｎ型カルシウムチャネル阻害薬

Non-Patent Citations (20)

* Cited by examiner, † Cited by third party
Title
BEILSTEIN Accession BRN: 113818 *
BEILSTEIN Accession BRN: 13161 *
BEILSTEIN Accession BRN: 14989 *
BEILSTEIN Accession BRN: 294410 *
BEILSTEIN Accession BRN: 2991 *
BEILSTEIN Accession BRN: 307223 *
BEILSTEIN Accession BRN: 309225 *
BEILSTEIN Accession BRN: 326592 *
BEILSTEIN Accession BRN: 3348 *
BEILSTEIN Accession BRN: 42255 *
BEILSTEIN Accession BRN: 42256 *
BEILSTEIN Accession BRN: 44621 *
BEILSTEIN Accession BRN: 4647 *
BEILSTEIN Accession BRN: 4957 *
BEILSTEIN Accession BRN: 5169 *
BEILSTEIN Accession BRN: 644518 *
BEILSTEIN Accession BRN: 678128 *
BEILSTEIN Accession BRN: 687549 *
BEILSTEIN Accession BRN: 7541410 *
BEILSTIEN Accession BRN: 112451 *

Also Published As

Publication number Publication date
EP1753735A1 (en) 2007-02-21
CA2562075A1 (en) 2005-11-03
ZA200608225B (en) 2008-01-08
CN1946703A (zh) 2007-04-11
WO2005103022A1 (en) 2005-11-03
US20050261294A1 (en) 2005-11-24
CA2562075C (en) 2012-08-14
AU2005236055A1 (en) 2005-11-03
NZ550114A (en) 2011-02-25
MXPA06012130A (es) 2007-01-31
JP4879165B2 (ja) 2012-02-22
US7820704B2 (en) 2010-10-26
IL178597A0 (en) 2007-02-11
BRPI0510095A (pt) 2007-10-16
JP2007533752A (ja) 2007-11-22

Similar Documents

Publication Publication Date Title
AU2005236055B2 (en) Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators
JP5212101B2 (ja) 新規化合物
JP5739527B2 (ja) ＲｈｏキナーゼインヒビターとしてのＮ−環式−３−（環状カルボニルアミノメチル）ベンズアミド誘導体
CN102596923B (zh) 1,2,4-噻唑烷-3-酮衍生物及其在癌症治疗中的用途
AU2007229637A1 (en) Amide derivatives and their application for the treatment of G protein related diseases
WO2010024903A1 (en) BENZO[d]OXAZOLES AND BENZO[d]THIAZOLES AS KINASE INHIBITORS
TW201125865A (en) Oxadiazole derivative having inhibion activity on endothelial lipase
TW200825075A (en) Sulfonylurea derivatives as a selective MMP-13 inhibitor
WO2016044323A1 (en) Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists
JP2003510320A (ja) 薬剤活性のあるスルホニルアミノ酸誘導体
TW200946117A (en) Compounds having NPY Y5 receptor antagonistic activity
WO2019178324A1 (en) Amino-benzoisothiazole and amino-benzoisothiadiazole amide compounds
JP2009520738A (ja) Ｃｃｒ９活性の阻害剤
WO2019136093A1 (en) Inhibitors of low molecular weight protein tyrosine phosphatase (lmptp) and uses thereof
CA3202033A1 (en) Selective inhibitors of rock1 and rock2 protein kinases and uses thereof
CA3205780A1 (en) Tetrahydrothienopyrimidinesulfonamide compounds
AU2006328900A1 (en) Inhibitors of CCR9 activity
US20090247536A1 (en) Bissulfonamide Compounds As Agonists Of GalR1, Compositions, And Methods Of Use
CA2963601C (en) Benzylhydroxyde derivatives, preparation thereof and therapeutic use as inhibitors of the complex 1 of the mitochondrial respiratory chain
AU2020299632A1 (en) Inhibitors of low molecular weight protein tyrosine phosphatase (LMPTP) and uses thereof
CN102076682A (zh) 五元环化合物
HK1102680A (en) Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators

Legal Events

Date Code Title Description
TC Change of applicant's name (sec. 104)

Owner name: TRANSTECH PHARMA, INC.

Free format text: FORMER NAME: TRANSTECH PHARMA INC.

FGA Letters patent sealed or granted (standard patent)
PC Assignment registered

Owner name: TRANSTECH PHARMA, LLC

Free format text: FORMER OWNER WAS: TRANSTECH PHARMA, INC.

MK14 Patent ceased section 143(a) (annual fees not paid) or expired