ES2684821T3 - Derivados de aminoácidos multicíclicos y métodos de su uso - Google Patents

Derivados de aminoácidos multicíclicos y métodos de su uso Download PDF

Info

Publication number
ES2684821T3
ES2684821T3 ES11005146.3T ES11005146T ES2684821T3 ES 2684821 T3 ES2684821 T3 ES 2684821T3 ES 11005146 T ES11005146 T ES 11005146T ES 2684821 T3 ES2684821 T3 ES 2684821T3
Authority
ES
Spain
Prior art keywords
alkyl
aryl
optionally substituted
heterocycle
hydrogen
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
ES11005146.3T
Other languages
English (en)
Spanish (es)
Inventor
Arokiasamy Devasagayaraj
Haihong Jin
Qingyun Liu
Brent Marinelli
Lakshama Samala
Zhi-Cai Shi
Ashok Tunoori
Ying WANG
Wenxue Wu
Chengmin Zhang
Haiming Zhang
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.)
Lexicon Pharmaceuticals Inc
Original Assignee
Lexicon Pharmaceuticals 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 Lexicon Pharmaceuticals Inc filed Critical Lexicon Pharmaceuticals Inc
Application granted granted Critical
Publication of ES2684821T3 publication Critical patent/ES2684821T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/34One oxygen atom
    • C07D239/36One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D251/00Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
    • C07D251/18Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41921,2,3-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/34Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C229/36Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/40Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/42Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by saturated carbon chains
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/40Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/44Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by unsaturated carbon chains
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/42Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/34One oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/20Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/061,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D251/00Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D251/00Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/22Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to two ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D251/00Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/40Nitrogen atoms
    • C07D251/48Two nitrogen atoms
    • C07D251/52Two nitrogen atoms with an oxygen or sulfur atom attached to the third ring carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/06Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08Systems containing only non-condensed rings with a five-membered ring the ring being saturated
ES11005146.3T 2005-12-29 2006-12-12 Derivados de aminoácidos multicíclicos y métodos de su uso Active ES2684821T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US75495505P 2005-12-29 2005-12-29
US754955P 2005-12-29

Publications (1)

Publication Number Publication Date
ES2684821T3 true ES2684821T3 (es) 2018-10-04

Family

ID=38327831

Family Applications (2)

Application Number Title Priority Date Filing Date
ES06849951T Active ES2395392T3 (es) 2005-12-29 2006-12-12 Derivados aminoácidos multicíclicos y métodos de su uso
ES11005146.3T Active ES2684821T3 (es) 2005-12-29 2006-12-12 Derivados de aminoácidos multicíclicos y métodos de su uso

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES06849951T Active ES2395392T3 (es) 2005-12-29 2006-12-12 Derivados aminoácidos multicíclicos y métodos de su uso

Country Status (21)

Country Link
US (3) US7723345B2 (US08063057-20111122-C00028.png)
EP (2) EP1984344B1 (US08063057-20111122-C00028.png)
JP (1) JP5483883B2 (US08063057-20111122-C00028.png)
KR (1) KR101360621B1 (US08063057-20111122-C00028.png)
CN (2) CN103265495B (US08063057-20111122-C00028.png)
AU (1) AU2006337137B2 (US08063057-20111122-C00028.png)
BR (1) BRPI0620756B1 (US08063057-20111122-C00028.png)
CA (1) CA2635531C (US08063057-20111122-C00028.png)
DK (1) DK1984344T3 (US08063057-20111122-C00028.png)
EA (1) EA019879B1 (US08063057-20111122-C00028.png)
EC (1) ECSP088590A (US08063057-20111122-C00028.png)
ES (2) ES2395392T3 (US08063057-20111122-C00028.png)
HK (1) HK1124841A1 (US08063057-20111122-C00028.png)
IL (1) IL191998A (US08063057-20111122-C00028.png)
NO (1) NO344848B1 (US08063057-20111122-C00028.png)
NZ (1) NZ568946A (US08063057-20111122-C00028.png)
PL (1) PL1984344T3 (US08063057-20111122-C00028.png)
PT (1) PT1984344E (US08063057-20111122-C00028.png)
UA (1) UA96936C2 (US08063057-20111122-C00028.png)
WO (1) WO2007089335A2 (US08063057-20111122-C00028.png)
ZA (1) ZA200805192B (US08063057-20111122-C00028.png)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1599468T3 (da) 2003-01-14 2008-02-04 Arena Pharm Inc 1,2,3-trisubstituerede aryl- og heteroarylderivater som modulatorer af metabolisme og forebyggelse og behandling af forstyrrelser forbundet dermed såsom diabetes og hyperglykæmi
AR045047A1 (es) 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
EP2287166A3 (en) 2003-07-14 2011-06-22 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
MY148521A (en) 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
CA2595855C (en) 2005-01-25 2017-07-04 Synta Pharmaceuticals Corp. Pyrazine compounds for inflammation and immune-related uses
US7897763B2 (en) * 2005-12-29 2011-03-01 Lexicon Pharmaceuticals, Inc. Process for the preparation of substituted phenylalanines
US7855291B2 (en) * 2005-12-29 2010-12-21 Lexicon Pharmaceuticals, Inc. Process for the preparation of substituted phenylalanines
BRPI0620756B1 (pt) * 2005-12-29 2021-06-01 Tersera Therapeutics Llc Derivados de aminoácido multicíclicos, formulação farmacêutica compreendendo os mesmos e seus usos para inibir a atividade de triptofano hidroxilase 1 (tph1)
DK2848610T3 (da) * 2006-11-15 2017-11-06 Ym Biosciences Australia Pty Hæmmere af kinaseaktivitet
UA99270C2 (en) 2006-12-12 2012-08-10 Лексикон Фармасьютикалз, Инк. 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use
GB0705400D0 (en) * 2007-03-21 2007-05-02 Univ Aberdeen Therapeutic compounds andm their use
CN101784269A (zh) * 2007-06-26 2010-07-21 莱西肯医药有限公司 治疗由5-羟色胺介导的疾病和病症的方法
MX2009013982A (es) * 2007-06-26 2010-04-09 Lexicon Pharmaceuticals Inc Composiciones que comprenden inhibidores de triptofano hidroxilasa.
CA2693400A1 (en) 2007-07-11 2009-01-15 Lexicon Pharmaceuticals, Inc. Methods and compositions for treating pulmonary hypertension and related diseases and disorders
AU2008279426A1 (en) * 2007-07-26 2009-01-29 Lexicon Pharmaceuticals, Inc. Methods of affecting gastrointestinal transit and gastric emptying, and compounds useful therein
MX2010001938A (es) * 2007-08-24 2010-03-11 Lexicon Pharmaceuticals Inc Metodos para preparar compuestos basados en 4-fenil-6-(2,2,2-trifl uoro-1-feniletoxi)pirimidina.
US20100260772A1 (en) * 2007-09-28 2010-10-14 The Trustees Of Columbia University In The City Of New York Methods for treating or preventing diseases associated with low bone mass
TWI439457B (zh) * 2007-09-28 2014-06-01 Lexicon Pharmaceuticals Inc (s)-2-胺基-3-(4-(2-胺基-6-((r)-1-(4-氯-2-(3-甲基-1h-吡唑-1-基)苯基)-2,2,2-三氟乙氧)-嘧啶-4-基)苯基)丙酸乙酯之固體形式與其使用方法
TW200932729A (en) * 2007-10-08 2009-08-01 Lexicon Pharmaceuticals Inc Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-2,2,2-trifluoro-1-(3'-methoxybiphenyl-4-yl)ethoxy)pyrimidin-4-yl)phenyl)propanoic acid and methods of their use
US8273744B2 (en) 2008-02-04 2012-09-25 Mercury Therapeutics, Inc. AMPK modulators
US8759364B2 (en) 2008-03-31 2014-06-24 The Trustees Of Columbia University In The City Of New York Methods of treating bone mass diseases
WO2010011864A2 (en) * 2008-07-23 2010-01-28 The Scripps Research Institute Alpha-helix mimetic with functionalized pyridazine
GB0817207D0 (en) 2008-09-19 2008-10-29 Pimco 2664 Ltd therapeutic apsac compounds and their use
GB0817208D0 (en) * 2008-09-19 2008-10-29 Pimco 2664 Ltd Therapeutic apsap compounds and their use
CN102186476A (zh) * 2008-10-03 2011-09-14 莱西肯医药有限公司 色氨酸羟化酶抑制剂及其用法
CN102203069A (zh) * 2008-10-24 2011-09-28 莱西肯医药有限公司 被取代的苯基丙氨酸的制备方法
WO2010062829A1 (en) * 2008-11-28 2010-06-03 Lexicon Pharmaceuticals, Inc. Tryptophan hydroxylase inhibitors for treating osteoporosis
WO2010065333A1 (en) * 2008-12-01 2010-06-10 Lexicon Pharmaceuticals, Inc. 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds for the treatment of osteoporosis
US8815883B2 (en) 2009-11-02 2014-08-26 The Trustees Of Columbia Unviersity In The City Of New York Compounds and methods for inhibiting serotonin synthesis
WO2011056916A1 (en) * 2009-11-05 2011-05-12 Lexicon Pharmaceuticals, Inc. Tryptophan hydroxylase inhibitors for the treatment of cancer
EP2501684A2 (en) 2009-11-19 2012-09-26 Lexicon Pharmaceuticals, Inc. Process for the preparation of substituted phenylalanines
CN102711757A (zh) * 2009-11-23 2012-10-03 莱西肯医药有限公司 用于治疗肠易激综合征的方法和分析法
US20120077831A1 (en) * 2009-11-23 2012-03-29 Philip Manton Brown Methods and assays for the treatment of irritable bowel syndrome
CN102753168A (zh) 2010-02-10 2012-10-24 莱西肯医药有限公司 用于治疗转移性骨病的色氨酸羟化酶抑制剂
TWI513694B (zh) 2010-05-11 2015-12-21 Amgen Inc 抑制間變性淋巴瘤激酶的嘧啶化合物
JP2013530180A (ja) 2010-06-16 2013-07-25 パーデュー、ファーマ、リミテッド、パートナーシップ アリール置換インドールおよびその使用
SG188548A1 (en) 2010-09-22 2013-04-30 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
TW201245183A (en) * 2010-11-05 2012-11-16 Lexicon Pharmaceuticals Inc Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid
GB201203793D0 (en) * 2012-03-05 2012-04-18 Ge Healthcare Ltd Imaging neural activity
US20130303763A1 (en) 2012-03-30 2013-11-14 Michael D. Gershon Methods and compositions for the treatment of necrotizing enterocolitis
WO2014195847A2 (en) 2013-06-03 2014-12-11 Actelion Pharmaceuticals Ltd Novel use of stable isotope labeled l-tryptophan
GB201311361D0 (en) 2013-06-26 2013-08-14 Pimco 2664 Ltd Compounds and their therapeutic use
UA119247C2 (uk) 2013-09-06 2019-05-27 РОЙВЕНТ САЙЕНСИЗ ҐмбГ Спіроциклічні сполуки як інгібітори триптофангідроксилази
TW201609721A (zh) * 2013-11-19 2016-03-16 艾克泰聯製藥有限公司 三環咪唑化合物
AR098436A1 (es) * 2013-11-19 2016-05-26 Actelion Pharmaceuticals Ltd Compuestos tricíclicos de piperidina
WO2015089137A1 (en) * 2013-12-11 2015-06-18 Karos Pharmaceuticals, Inc. Acylguanidines as tryptophan hydroxylase inhibitors
EP3135667A4 (en) 2014-04-24 2017-11-01 Mitsubishi Tanabe Pharma Corporation Novel 2-amino-pyridine and 2-amino-pyrimidine derivatives and medicinal use thereof
US10308648B2 (en) 2014-10-16 2019-06-04 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
EP3262028B1 (en) 2014-12-17 2021-10-27 Pimco 2664 Limited N-(4-hydroxy-4-methyl-cyclohexyl)-4-phenyl-benzenesulfonamide and n-(-4hydroxy-4-methyl-cyclohexyl)-4-(2-pyridyl)-benzenesulfonamide compounds and their therapeutic use
WO2016109501A1 (en) * 2014-12-30 2016-07-07 Karos Pharmaceuticals, Inc. Amide compounds as tryptophan hydroxylase inhibitors
EP3242666A1 (en) 2015-01-06 2017-11-15 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
US9611201B2 (en) 2015-03-05 2017-04-04 Karos Pharmaceuticals, Inc. Processes for preparing (R)-1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanol and 1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanone
JP2016204314A (ja) * 2015-04-23 2016-12-08 国立研究開発法人理化学研究所 化合物及び4−ボロノフェニルアラニン誘導体の製造方法
CA2980100A1 (en) * 2015-05-04 2016-11-10 Actelion Pharmaceuticals Ltd Tricyclic piperidine compounds
JP6838744B2 (ja) 2015-06-22 2021-03-03 アリーナ ファーマシューティカルズ, インコーポレイテッド S1P1レセプター関連障害における使用のための(R)−2−(7−(4−シクロペンチル−3−(トリフルオロメチル)ベンジルオキシ)−1,2,3,4−テトラヒドロシクロペンタ[b]インドール−3−イル)酢酸(化合物1)の結晶性L−アルギニン塩
KR20190116416A (ko) 2017-02-16 2019-10-14 아레나 파마슈티칼스, 인크. 원발 담즙성 담관염을 치료하기 위한 화합물 및 방법
US11407763B2 (en) 2017-08-24 2022-08-09 Gwangju Institute Of Science And Technolgy Tryptophan hydroxylase inhibitor and pharmaceutical composition including same

Family Cites Families (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH471146A (de) 1966-03-16 1969-04-15 Geigy Ag J R Verfahren zur Herstellung von neuen Morpholinderivaten
US4866181A (en) * 1986-08-29 1989-09-12 Aldrich-Boranes, Inc. Process for producing optically active alcohols
US4916074A (en) * 1986-10-30 1990-04-10 Chisso Corporation Process for producing optically active compounds
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
EP0504541B1 (en) * 1991-03-21 1998-07-22 Solutia Europe N.V./S.A. Improved catalytic process for selective alkylation of aromatic hydrocarbons
DE4131924A1 (de) * 1991-09-25 1993-07-08 Hoechst Ag Substituierte 4-alkoxypyrimidine, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel
AU660852B2 (en) 1992-11-25 1995-07-06 Elan Pharma International Limited Method of grinding pharmaceutical substances
US5849736A (en) 1993-11-24 1998-12-15 The Dupont Merck Pharmaceutical Company Isoxazoline and isoxazole fibrinogen receptor antagonists
HUT74690A (en) 1993-11-24 1997-01-28 Du Pont Merck Pharma Novel isoxazoline and isoxazole fibrinogen receptor antagonists process for producing them and pharmaceutical compositions containing them
TW384224B (en) 1994-05-25 2000-03-11 Nano Sys Llc Method of preparing submicron particles of a therapeutic or diagnostic agent
US5718388A (en) 1994-05-25 1998-02-17 Eastman Kodak Continuous method of grinding pharmaceutical substances
US5662883A (en) 1995-01-10 1997-09-02 Nanosystems L.L.C. Microprecipitation of micro-nanoparticulate pharmaceutical agents
US5665331A (en) 1995-01-10 1997-09-09 Nanosystems L.L.C. Co-microprecipitation of nanoparticulate pharmaceutical agents with crystal growth modifiers
US5534270A (en) 1995-02-09 1996-07-09 Nanosystems Llc Method of preparing stable drug nanoparticles
US5543133A (en) 1995-02-14 1996-08-06 Nanosystems L.L.C. Process of preparing x-ray contrast compositions containing nanoparticles
US5510118A (en) 1995-02-14 1996-04-23 Nanosystems Llc Process for preparing therapeutic compositions containing nanoparticles
US5718919A (en) 1995-02-24 1998-02-17 Nanosystems L.L.C. Nanoparticles containing the R(-)enantiomer of ibuprofen
GB9518553D0 (en) 1995-09-11 1995-11-08 Fujisawa Pharmaceutical Co New urea derivatives processes for the preparation thereof and pharmaceutical composition comprising the same
US5834025A (en) 1995-09-29 1998-11-10 Nanosystems L.L.C. Reduction of intravenously administered nanoparticulate-formulation-induced adverse physiological reactions
EP0796855B1 (de) 1996-03-20 2002-02-06 Hoechst Aktiengesellschaft Inhibitoren der Knochenresorption und Vitronectinrezeptor-Antagonisten
US5958957A (en) * 1996-04-19 1999-09-28 Novo Nordisk A/S Modulators of molecules with phosphotyrosine recognition units
US7378506B2 (en) 1997-07-21 2008-05-27 Ohio University Synthetic genes for plant gums and other hydroxyproline-rich glycoproteins
US6610502B1 (en) 1997-08-20 2003-08-26 Kyowa Medex Co., Ltd. Compound 2-amino-3-[2-(α-mannopyranosyl)indol-3-yl]propionic acid, process for preparing the same, and method for inspecting function of living body with the novel compound
US6455550B1 (en) 1997-08-22 2002-09-24 Hoffmann-La Roche Inc. N-alkanoylphenylalanine derivatives
US6229011B1 (en) * 1997-08-22 2001-05-08 Hoffman-La Roche Inc. N-aroylphenylalanine derivative VCAM-1 inhibitors
MY153569A (en) * 1998-01-20 2015-02-27 Mitsubishi Tanabe Pharma Corp Inhibitors of ?4 mediated cell adhesion
US6114326A (en) * 1998-03-27 2000-09-05 Pharmacia & Upjohn Company Use of cabergoline in the treatment of restless legs syndrome
US6423727B1 (en) * 1998-04-23 2002-07-23 Novartis Ag Certain thiol inhibitors of endothelin-converting enzyme
WO2000019994A1 (en) 1998-10-02 2000-04-13 Board Of Trustees Of The University Of Illinois Estrogen receptor ligands
JP2000204085A (ja) 1998-11-13 2000-07-25 Nippon Bayer Agrochem Co Ltd イソチアゾ―ルカルボン酸誘導体および病害防除剤
US6677360B2 (en) 1998-12-16 2004-01-13 Bayer Aktiengesellschaft Biphenyl and biphenyl-analogous compounds as integrin antagonists
EE200100317A (et) 1998-12-16 2002-08-15 Bayer Aktiengesellschaft Uued bifenüül- ja bifenüülanaloogsed ühendid kui integriini antagonistid
WO2001054486A1 (en) 2000-01-26 2001-08-02 Kansas State University Research Foundation Preparation and use of polymers crosslinked with tyrosine-containing peptides
RU2245874C2 (ru) 1999-02-18 2005-02-10 Ф.Хоффман-Ля Рош Аг Производные тиоамида и фармацевтическая композиция
CA2368049A1 (en) 1999-04-13 2000-10-19 Basf Aktiengesellschaft Integrin receptor ligands
US7045532B2 (en) * 1999-04-30 2006-05-16 Millennium Pharmaceuticals, Inc. ACE-2 modulating compounds and methods of use thereof
JP4156807B2 (ja) 1999-06-01 2008-09-24 エラン ファーマ インターナショナル,リミティド 小型ミル及びその方法
EP1065208A1 (en) * 1999-07-02 2001-01-03 Aventis Pharma Deutschland GmbH Substituted purine derivatives as inhibitors of cell adhesion
JP3795305B2 (ja) 1999-07-19 2006-07-12 田辺製薬株式会社 医薬組成物
AU6903200A (en) 1999-08-16 2001-03-13 Merck & Co., Inc. Heterocycle amides as cell adhesion inhibitors
EP1214292B1 (en) * 1999-09-24 2007-06-13 Genentech, Inc. Tyrosine derivatives
JP2003511355A (ja) * 1999-10-06 2003-03-25 ビーエーエスエフ アクチェンゲゼルシャフト 併用療法のためのエンドセリンシグナル伝達経路のインヒビターおよびαvβ3受容体アンタゴニスト
DE10028575A1 (de) 2000-06-14 2002-03-14 Basf Ag Integrinliganden
JP2003512423A (ja) * 1999-10-27 2003-04-02 スノル・モレキュラー・コーポレーション 組織因子アンタゴニスト及びその使用方法
DE60033684T2 (de) 1999-11-18 2007-12-06 Ajinomoto Co., Inc. Phenylalaninderivate
US6388084B1 (en) * 1999-12-06 2002-05-14 Hoffmann-La Roche Inc. 4-pyridinyl-n-acyl-l-phenylalanines
CA2396087A1 (en) * 1999-12-28 2001-07-19 Louis Stanley Chupak Non-peptidyl inhibitors of vla-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases
FR2804427B1 (fr) * 2000-01-27 2002-09-06 Rhodia Chimie Sa Procede de preparation de cetones alpha-halogenees
WO2002000651A2 (en) 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Factor xa inhibitors
DK1296705T3 (da) * 2000-06-28 2012-09-17 Prana Biotechnology Ltd Beta-amyloid-oligomerer til anvendelse til behandling, lindring eller forebyggelse af Alzheimers sygdom
US6448281B1 (en) * 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
US7015216B2 (en) * 2000-07-21 2006-03-21 Elan Pharmaceuticals, Inc. Heteroaryl-β-alanine derivatives as alpha 4 integrin inhibitors
AU2001278986A1 (en) * 2000-07-21 2002-02-05 Elan Pharmaceuticals, Inc. 3-amino-2-(4-aminocarbonyloxy)phenyl-propionic acid derivatives as alpha-4- integrin inhibitors
EP1288205B1 (en) 2000-08-18 2011-02-02 Ajinomoto Co., Inc. Novel phenylalanine derivatives
DE10042655A1 (de) 2000-08-31 2002-03-14 Aventis Pharma Gmbh Verfahren zur Herstellung von Inhibitoren der Zell-Adhäsion
MY129000A (en) * 2000-08-31 2007-03-30 Tanabe Seiyaku Co INHIBITORS OF a4 MEDIATED CELL ADHESION
AU2001290303A1 (en) 2000-09-29 2002-04-15 Ajinomoto Co., Inc. Novel phenylalanine derivatives
DE10112768A1 (de) * 2001-03-16 2002-09-19 Merck Patent Gmbh Phenylderivate 3
TWI258469B (en) * 2001-03-19 2006-07-21 Dainippon Pharmaceutical Co Aryl-substituted alicyclic compounds and pharmaceutical composition containing the same
US7081460B2 (en) * 2001-04-09 2006-07-25 Ortho-Mcneil Pharmaceutical, Inc. Quinazoline and quinazoline-like compounds for the treatment of integrin-mediated disorders
DE60225064T2 (de) * 2001-05-29 2009-01-29 Lexicon Pharmaceuticals, Inc., The Woodlands Neue menschliche hydroxylasen und diese codierende polynukleotide
US6976647B2 (en) 2001-06-05 2005-12-20 Elan Pharma International, Limited System and method for milling materials
CA2449490C (en) 2001-06-05 2010-10-05 Elan Pharma International Limited System and method for milling materials
US6951840B2 (en) * 2001-08-31 2005-10-04 Eli Lilly And Company Lipoglycopeptide antibiotics
JP4452899B2 (ja) * 2001-12-13 2010-04-21 味の素株式会社 新規フェニルアラニン誘導体
US20030171368A1 (en) * 2002-02-06 2003-09-11 Werner Seitz Pyrimidinonesulfamoylureas`
AU2003211560A1 (en) 2002-02-20 2003-09-09 Ajinomoto Co., Inc. Novel phenylalanine derivative
CN1646508A (zh) * 2002-04-03 2005-07-27 诺瓦提斯公司 作为ptp酶1b抑制剂的5-取代的1,1-二氧代-1,2,5-噻二唑烷-3-酮衍生物
JPWO2003089410A1 (ja) 2002-04-19 2005-08-25 協和醗酵工業株式会社 フェニルアラニン誘導体
TW200407310A (en) 2002-06-07 2004-05-16 Glaxo Group Ltd Compounds
GB0213122D0 (en) 2002-06-07 2002-07-17 Glaxo Group Ltd Compounds
DE10226921A1 (de) 2002-06-17 2003-12-24 Bayer Ag Antibakterielle Amid-Makrozyklen
DE10234422A1 (de) 2002-07-29 2004-02-12 Bayer Ag Antibakterielle Ester-Makrozyklen
AU2003265398A1 (en) * 2002-08-09 2004-02-25 Transtech Pharma, Inc. Aryl and heteroaryl compounds and methods to modulate coagulation
US20050260126A1 (en) * 2002-08-30 2005-11-24 Yukitsuka Kudo Diagnostic probes and remedies for diseases with accumulation of prion protein, and stains for prion protein
DE60334924D1 (de) 2002-09-11 2010-12-23 Elan Pharma Int Ltd Anoteilchengrösse
AU2003301903A1 (en) 2002-11-06 2004-06-03 Bristol-Myers Squibb Company Isoxazoline derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme
BR0314898A (pt) 2002-11-19 2005-08-02 Galderma Res & Dev Compostos, composição cosmética, uso cosmético de uma composição, uso de um composto e composição farmacêutica
JP2006514043A (ja) * 2002-12-20 2006-04-27 ファルマシア・コーポレーション マイトジェン活性化タンパク質キナーゼ−活性化タンパク質キナーゼ−2を阻害する化合物
ITMI20022738A1 (it) 2002-12-23 2004-06-24 Zambon Spa Derivati ftalazinici inibitori della fosfodiesterasi 4.
ATE412657T1 (de) 2002-12-24 2008-11-15 Astrazeneca Ab Therapeutische quinazolin-derivate
JPWO2004080943A1 (ja) * 2003-03-11 2006-06-08 小野薬品工業株式会社 シンナミルアルコール誘導体化合物およびその化合物を有効成分として含有する薬剤
US20050234066A1 (en) * 2004-04-15 2005-10-20 Agouron Pharmaceuticals, Inc. Alpha substituted carboxylic acids
US20050187266A1 (en) * 2003-04-15 2005-08-25 Pfizer Inc Alpha substituted carboxylic acids
US20060128956A1 (en) * 2003-04-21 2006-06-15 Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky (Purin-6-yl) amino acid and production method thereof
AU2004247013B2 (en) * 2003-05-14 2010-07-08 Neurogenetic Pharmaceuticals, Inc. Compounds and uses thereof in modulating amyloid beta
BRPI0411674A (pt) * 2003-06-20 2006-08-29 Galderma Res & Dev compostos, composição cosmética, uso cosmético de uma composição, uso de um composto, composição farmacêutica, e processo cosmético para o embelezamento da pele
US20050042177A1 (en) 2003-07-23 2005-02-24 Elan Pharma International Ltd. Novel compositions of sildenafil free base
CA2531796A1 (en) 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
WO2005014534A1 (en) 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
JP2008502583A (ja) * 2003-10-01 2008-01-31 バイエル・ヘルスケア・アクチェンゲゼルシャフト 抗細菌性アミド大員環
WO2005035551A2 (en) * 2003-10-08 2005-04-21 Incyte Corporation Inhibitors of proteins that bind phosphorylated molecules
MXPA06004642A (es) * 2003-11-05 2006-06-27 Hoffmann La Roche Derivados de heteroaril como activadores de los receptores activados de proliferadores de peroxisoma (ppar).
DE10358824A1 (de) 2003-12-16 2005-07-21 Bayer Healthcare Ag Antibakterielle Makrozyklen mit substituiertem Biphenyl
RU2390520C2 (ru) * 2003-12-22 2010-05-27 Адзиномото Ко., Инк. Новые производные фенилаланина
US20060148680A1 (en) * 2004-01-14 2006-07-06 Kieliszewski Marcia J Glycoproteins produced in plants and methods of their use
JP2007126358A (ja) 2004-01-20 2007-05-24 Fujiyakuhin Co Ltd フェニルアラニン誘導体
EP2561884B1 (en) 2004-02-05 2017-01-04 The Ohio State University Research Foundation Chimeric VEGF peptides
US20050192279A1 (en) * 2004-02-10 2005-09-01 Kent Barbay Pyridazinones as antagonists of alpha4 integrins
US7517908B2 (en) * 2004-05-21 2009-04-14 Duke University Method for augmenting the effects of serotonin reuptake inhibitors
EP1778214A4 (en) * 2004-07-27 2010-04-14 Glaxosmithkline Llc NEW BIPHENYL COMPOUNDS AND THEIR USE
WO2006021886A1 (en) * 2004-08-26 2006-03-02 Pfizer Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
BRPI0620756B1 (pt) * 2005-12-29 2021-06-01 Tersera Therapeutics Llc Derivados de aminoácido multicíclicos, formulação farmacêutica compreendendo os mesmos e seus usos para inibir a atividade de triptofano hidroxilase 1 (tph1)
US7897763B2 (en) * 2005-12-29 2011-03-01 Lexicon Pharmaceuticals, Inc. Process for the preparation of substituted phenylalanines
UA99270C2 (en) * 2006-12-12 2012-08-10 Лексикон Фармасьютикалз, Инк. 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use
MX2009013982A (es) * 2007-06-26 2010-04-09 Lexicon Pharmaceuticals Inc Composiciones que comprenden inhibidores de triptofano hidroxilasa.
CA2693400A1 (en) * 2007-07-11 2009-01-15 Lexicon Pharmaceuticals, Inc. Methods and compositions for treating pulmonary hypertension and related diseases and disorders
TWI439457B (zh) * 2007-09-28 2014-06-01 Lexicon Pharmaceuticals Inc (s)-2-胺基-3-(4-(2-胺基-6-((r)-1-(4-氯-2-(3-甲基-1h-吡唑-1-基)苯基)-2,2,2-三氟乙氧)-嘧啶-4-基)苯基)丙酸乙酯之固體形式與其使用方法
TW200932729A (en) * 2007-10-08 2009-08-01 Lexicon Pharmaceuticals Inc Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-2,2,2-trifluoro-1-(3'-methoxybiphenyl-4-yl)ethoxy)pyrimidin-4-yl)phenyl)propanoic acid and methods of their use

Also Published As

Publication number Publication date
WO2007089335A3 (en) 2007-10-11
NZ568946A (en) 2010-07-30
CN103265495A (zh) 2013-08-28
EP2386547B1 (en) 2018-06-20
WO2007089335A2 (en) 2007-08-09
ECSP088590A (es) 2008-11-27
US20100280054A1 (en) 2010-11-04
IL191998A0 (en) 2009-02-11
KR101360621B1 (ko) 2014-02-07
US7723345B2 (en) 2010-05-25
JP2009522265A (ja) 2009-06-11
UA96936C2 (uk) 2011-12-26
HK1124841A1 (en) 2009-07-24
US20120157484A1 (en) 2012-06-21
JP5483883B2 (ja) 2014-05-07
US8063057B2 (en) 2011-11-22
ES2395392T3 (es) 2013-02-12
CA2635531A1 (en) 2007-08-09
DK1984344T3 (da) 2013-01-14
KR20080081159A (ko) 2008-09-08
EP1984344B1 (en) 2012-09-26
EP1984344A2 (en) 2008-10-29
NO344848B1 (no) 2020-05-25
AU2006337137A1 (en) 2007-08-09
BRPI0620756A2 (pt) 2011-11-22
CN103265495B (zh) 2016-11-16
PL1984344T3 (pl) 2013-03-29
CN101351451A (zh) 2009-01-21
ZA200805192B (en) 2009-11-25
EP2386547A1 (en) 2011-11-16
BRPI0620756B1 (pt) 2021-06-01
EA019879B1 (ru) 2014-07-30
US8629156B2 (en) 2014-01-14
US20070191370A1 (en) 2007-08-16
IL191998A (en) 2015-01-29
CN101351451B (zh) 2013-02-20
NO20083324L (no) 2008-08-13
PT1984344E (pt) 2012-12-21
AU2006337137B2 (en) 2012-06-14
EA200870127A1 (ru) 2009-02-27
CA2635531C (en) 2014-06-17

Similar Documents

Publication Publication Date Title
ES2684821T3 (es) Derivados de aminoácidos multicíclicos y métodos de su uso
ES2625083T3 (es) Compuestos basados en 4-fenil-6-(2,2,2-trifluoro-1-feniletoxi)-pirimidina y métodos para su uso
AU2008275179B2 (en) Methods and compositions for treating pulmonary hypertension and related diseases and disorders
US20090005381A1 (en) Methods of treating serotonin-mediated diseases and disorders
AU2008268409B2 (en) Compositions comprising tryptophan hydroxylase inhibitors
KR20100055436A (ko) 위장관 통과 및 위 배출에 영향을 주는 방법, 및 그에 유용한 화합물
CA2779681A1 (en) Tryptophan hydroxylase inhibitors for the treatment of cancer
MX2008008483A (en) Multicyclic amino acid derivatives and methods of their use