HUP0203954A2 - Inhibitors of factor xa - Google Patents

Inhibitors of factor xa

Info

Publication number
HUP0203954A2
HUP0203954A2 HU0203954A HUP0203954A HUP0203954A2 HU P0203954 A2 HUP0203954 A2 HU P0203954A2 HU 0203954 A HU0203954 A HU 0203954A HU P0203954 A HUP0203954 A HU P0203954A HU P0203954 A2 HUP0203954 A2 HU P0203954A2
Authority
HU
Hungary
Prior art keywords
alkyl
group
optionally substituted
cycloalkyl
alkynyl
Prior art date
Application number
HU0203954A
Other languages
Hungarian (hu)
Inventor
Wenrong Huang
Zhaozhong Jon Jia
James Kanter
Robert M. Scarborough
Yonghong Song
Bing-Yan Zhu
Original Assignee
Millennium 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 Millennium Pharmaceuticals, Inc. filed Critical Millennium Pharmaceuticals, Inc.
Publication of HUP0203954A2 publication Critical patent/HUP0203954A2/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides 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
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides 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
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
    • C07C317/38—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atom of at least one amino group being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfones
    • C07C317/40—Y being a hydrogen or a carbon atom
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    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
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    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
    • C—CHEMISTRY; METALLURGY
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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    • 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
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    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • 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
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    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • C07D487/04—Ortho-condensed systems

Abstract

A találmány (I) általános képletű A-Q-D-E-G-J-X (I) vegyületekre vonatkozik, a képletben A jelentése alkil-,cikloalkil-, -N(R2R3), -C(=NR2)-R3, -C(=NR2)N(R2,R3), -N(R3)-C(=NR2)N(R2,R3) vagy -N(R2) C(=NR3)-R2 általános képletű csoport;adott esetben helyetesített fenil-, naftil- vagy heterociklusoscsoport; R2 és R3 jelentése hidrogénatom, adott esetben helyettesítetthidroxil-, amino-, alkil-, alkenil-, alkinil-, cikloalkil-, cikloalkilalcsoport; vagy R2 és R3 együtt adott esetben helyettesítettcikloalkil- vagy heterociklusos csoportot alkot; Q jelentésevegyértékkötés, adott esetben helyettesített alkilén-, alkenilén-,alkinilén- vagy -C(=O)-, -C(=NH)-, -C(=NMe)-, -N(R4)-, -N(R4)-CH2-, -C(=O)-N(R4)-, -N(R4)-C(=O)-, -S(=O)2-,-O-, -S(=O)2-N(R4)-vagy -N(R4)-S(=O)2- általános képletű csoport; R4 jelentése hidrogénatom, -CF3,adott esetben helyettesített alkil-, aIkenil-, alkinil-, cikloalkil-,fenil- vagy naftilcsoport; D jelentése közvetlen vegyértékkötés, adott esetben helyettesítettfenil-, naftil- vagy heterociklusos csoport; E jelentése közvetlenvegyértékkötés, -(CH2)q-C(=O)-, -(CH2)q N(R5)-C(=O)-(CH2)X-, -(CH2)q-C(=O)-N(R5)-(CH2)X-, -(CH2)q N(R5)-(CH2)X-, -(CH2)q-N(R5)CO-NR6(CH2)X-vagy -SO2-csoport; q és x értéke 0, 1 vagy 2; R5 és R6 jelentésehidrogénatom, alkil-, alkiloxi-, alkenil-, alkinil-, cikloalkil-,cikloalkilalkil-, -alkil-C(=O)-OH, arilalkil-, heteroarilalkil- vagy -alkil-C(=O)-O-alkil csoport; G jelenése adott esetben helyettesítettfenilcsoport vagy heterociklusos gyűrű; J jelentése közvetlenvegyértékkötés, -S(=O)2-, -C(=O)-, -N(R7)-S(=O)2-, -C(=O)-N(R7)-S(=O)2-, -C(=C)-N(R7)-(CH2)y-, -S(=O)2-N(R7)-(CH2)y- vagy -N(R7)-C(=O)-(CH2)y- általános képletű csoport; y értéke 0, 1 vagy 2; R7jelentése hidrogénatom, alkil-, alkenil-, alkinil-, cikloalkil-,cikloalkilalkil-, -alkil-C(=O)-OH, -alkil-OH, -alkil-O-alkil, adottesetben helyettesített (karbociklusos aril)alkilcsoport vagyheterociklusos gyűrűrendszer; X jelentése adott esetben helyettesítettfenil-, naftil- vagy heterociklusos csoport. A vegyületek a Xa faktorszelektív és hatékony gátlói. ÓThe invention relates to compounds of general formula (I) A-Q-D-E-G-J-X (I), where A is alkyl-, cycloalkyl-, -N(R2R3), -C(=NR2)-R3, -C(=NR2)N(R2,R3 ), a group of the general formula -N(R3)-C(=NR2)N(R2,R3) or -N(R2)C(=NR3)-R2; an optionally substituted phenyl, naphthyl or heterocyclic group; R2 and R3 are a hydrogen atom, optionally a substituted hydroxyl, amino, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylal group; or R2 and R3 together form an optionally substituted cycloalkyl or heterocyclic group; Q is a valence bond, optionally substituted alkylene-, alkenylene-, alkynylene- or -C(=O)-, -C(=NH)-, -C(=NMe)-, -N(R4)-, -N(R4 )-CH2-, -C(=O)-N(R4)-, -N(R4)-C(=O)-, -S(=O)2-,-O-, -S(=O) a group of general formula 2-N(R4)-or -N(R4)-S(=O)2-; R 4 is a hydrogen atom, -CF 3 , an optionally substituted alkyl, α-kenyl, alkynyl, cycloalkyl, phenyl or naphthyl group; D is a direct valence bond, an optionally substituted phenyl, naphthyl or heterocyclic group; E is a direct valence bond, -(CH2)q-C(=O)-, -(CH2)q N(R5)-C(=O)-(CH2)X-, -(CH2)q-C(=O)-N(R5 )-(CH2)X-, -(CH2)q N(R5)-(CH2)X-, -(CH2)q-N(R5)CO-NR6(CH2)X-or -SO2- group; q and x are 0, 1 or 2; R5 and R6 are hydrogen, alkyl, alkyloxy, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, -alkyl-C(=O)-OH, arylalkyl-, heteroarylalkyl- or -alkyl-C(=O)-O -alkyl group; G is an optionally substituted phenyl group or a heterocyclic ring; J is a direct valence bond, -S(=O)2-, -C(=O)-, -N(R7)-S(=O)2-, -C(=O)-N(R7)-S(= O)2-, -C(=C)-N(R7)-(CH2)y-, -S(=O)2-N(R7)-(CH2)y- or -N(R7)-C( a group of formula =O)-(CH2)y-; y is 0, 1, or 2; R7 means hydrogen atom, alkyl-, alkenyl-, alkynyl-, cycloalkyl-, cycloalkylalkyl-, -alkyl-C(=O)-OH, -alkyl-OH, -alkyl-O-alkyl, optionally substituted (carbocyclic aryl)alkyl group or heterocyclic ring system ; X is an optionally substituted phenyl, naphthyl or heterocyclic group. The compounds are selective and potent inhibitors of factor Xa. HE

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Families Citing this family (132)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU759711B2 (en) 1998-12-23 2003-04-17 Bristol-Myers Squibb Holdings Ireland Unlimited Company Nitrogen containing heterobicycles as factor XA inhibitors
AU776053B2 (en) 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
TWI290136B (en) 2000-04-05 2007-11-21 Daiichi Seiyaku Co Ethylenediamine derivatives
EP1307444B1 (en) 2000-07-27 2007-10-03 Eli Lilly And Company Substituted heterocyclic amides
WO2002042270A1 (en) 2000-11-22 2002-05-30 Yamanouchi Pharmaceutical Co., Ltd. Substituted benzene derivatives or salts thereof
US7163938B2 (en) 2000-11-28 2007-01-16 Eli Lilly And Company Substituted carboxamides
US6998408B2 (en) 2001-03-23 2006-02-14 Bristol-Myers Squibb Pharma Company 6-5, 6-6, or 6-7 Heterobicycles as factor Xa inhibitors
WO2002085353A1 (en) * 2001-04-18 2002-10-31 Bristol-Myers Squibb Company 1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-ones as factor xa inhibitors
WO2002085356A1 (en) 2001-04-18 2002-10-31 Bristol-Myers Squibb Company 1, 4, 5, 6-tetrahydropyrazolo-[3, 4-c]-pyrid in-7-ones as factor xa inhibitors
WO2002094197A2 (en) 2001-05-22 2002-11-28 Bristol-Myers Squibb Company Bicyclic inhibitors of factor xa
US7365205B2 (en) 2001-06-20 2008-04-29 Daiichi Sankyo Company, Limited Diamine derivatives
TWI320039B (en) 2001-09-21 2010-02-01 Lactam-containing compounds and derivatives thereof as factor xa inhibitors
BRPI0212726B8 (en) 2001-09-21 2021-05-25 Bristol Myers Squibb Co compounds containing lactams, and derivatives thereof, pharmaceutical composition comprising them and their uses
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
TW200302225A (en) 2001-12-04 2003-08-01 Bristol Myers Squibb Co Substituted amino methyl factor Xa inhibitors
WO2003048081A2 (en) 2001-12-04 2003-06-12 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
EP1456175A1 (en) 2001-12-07 2004-09-15 Eli Lilly And Company Substituted heterocyclic carboxamides with antithrombotic activity
EP1569912B1 (en) 2002-12-03 2015-04-29 Pharmacyclics, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
WO2003099276A1 (en) 2002-05-10 2003-12-04 Bristol-Myers Squibb Company 1,1-disubstituted cycloalkyl derivatives as factor xa inhibitors
AU2003248549B2 (en) 2002-05-24 2010-04-08 Millennium Pharmaceuticals, Inc. CCR9 inhibitors and methods of use thereof
UA79286C2 (en) * 2002-06-29 2007-06-11 Zentaris Gmbh Arylcarbonylpipererazines and heteroarylcarbonylpiperazines and their use in the treatment of benign and malignant tumors
ATE323702T1 (en) 2002-08-06 2006-05-15 Astrazeneca Ab CONDENSED PYRIDINES AND PYRIMIDINES WITH TIE2 (TEK) ACTIVITY
US7227035B2 (en) 2002-11-18 2007-06-05 Chemocentryx Bis-aryl sulfonamides
EP1798223B2 (en) 2002-11-18 2014-07-30 ChemoCentryx, Inc. Aryl sulfonamides
US7420055B2 (en) 2002-11-18 2008-09-02 Chemocentryx, Inc. Aryl sulfonamides
US7741519B2 (en) 2007-04-23 2010-06-22 Chemocentryx, Inc. Bis-aryl sulfonamides
EP1479678A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Pyrazole-derivatives as factor xa inhibitors
ATE444292T1 (en) * 2002-12-23 2009-10-15 Sanofi Aventis Deutschland PYRAZOLE DERIVATIVES AS FACTOR XA INHIBITORS
US7429581B2 (en) 2002-12-23 2008-09-30 Sanofi-Aventis Deutschland Gmbh Pyrazole-derivatives as factor Xa inhibitors
EP1433788A1 (en) * 2002-12-23 2004-06-30 Aventis Pharma Deutschland GmbH Pyrazole-derivatives as factor Xa inhibitors
TWI299664B (en) 2003-01-06 2008-08-11 Osi Pharm Inc (2-carboxamido)(3-amino)thiophene compounds
US7696225B2 (en) 2003-01-06 2010-04-13 Osi Pharmaceuticals, Inc. (2-carboxamido)(3-Amino) thiophene compounds
TW200505447A (en) 2003-02-07 2005-02-16 Daiichi Seiyaku Co Pyrazole derivative
US7122557B2 (en) 2003-03-18 2006-10-17 Bristol-Myers Squibb Company Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors
JP2006525355A (en) * 2003-05-01 2006-11-09 アボット・ラボラトリーズ Pyrazole-amides and sulfonamides as sodium channel modulators
US20040220170A1 (en) * 2003-05-01 2004-11-04 Atkinson Robert N. Pyrazole-amides and sulfonamides as sodium channel modulators
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
JP4681548B2 (en) 2003-07-22 2011-05-11 アステックス・セラピューティクス・リミテッド 3,4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinase (CDK) and glycogen synthetase kinase-3 (GSK-3) modulators
SE0302573D0 (en) 2003-09-26 2003-09-26 Astrazeneca Ab Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
US7432281B2 (en) 2003-10-07 2008-10-07 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
JP4928949B2 (en) 2003-12-23 2012-05-09 アステックス、セラピューティックス、リミテッド Pyrazole derivatives as protein kinase modulators
AU2005223483B2 (en) 2004-03-18 2009-04-23 Zoetis Llc N-(1-arylpyrazol-4l)sulfonamides and their use as parasiticides
KR20070083484A (en) 2004-07-14 2007-08-24 피티씨 테라퓨틱스, 인크. Methods for treating hepatitis c
US7772271B2 (en) 2004-07-14 2010-08-10 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7868037B2 (en) 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
EP1781289A1 (en) 2004-07-22 2007-05-09 PTC Therapeutics, Inc. Thienopyridines for treating hepatitis c
KR20070045226A (en) 2004-08-03 2007-05-02 와이어쓰 Indazoles useful in treating cardiovascular diseases
AR051094A1 (en) 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc HETEROCICLIC DERIVATIVES AND THEIR USE AS INHIBITORS OF ESTEAROIL-COA DESATURASA
EP1804799B1 (en) 2004-09-20 2013-08-21 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
BRPI0515483A (en) 2004-09-20 2008-07-22 Xenon Pharmaceuticals Inc heterocyclic derivatives for the treatment of stearoyl coa desaturase mediated diseases
AU2005286846A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as therapeutic agents
AR051202A1 (en) 2004-09-20 2006-12-27 Xenon Pharmaceuticals Inc HETEROCICLIC DERIVATIVES AND THEIR USE AS INHIBITORS OF ESTEAROIL-COA DESATURASA
TW200626572A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
BRPI0515505A (en) 2004-09-20 2008-07-29 Xenon Pharmaceuticals Inc heterocyclic derivatives and their use as stearoyl coat desaturase inhibitors
BRPI0515897A (en) 2004-09-24 2008-08-12 Astrazeneca Ab compound, use thereof, pharmaceutical composition, and method for pain therapy in a warm-blooded animal, and for the preparation of a compound
US7381732B2 (en) * 2004-10-26 2008-06-03 Bristol-Myers Squibb Company Pyrazolobenzamides and derivatives as factor Xa inhibitors
CA2593993C (en) 2004-12-30 2014-07-29 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
JP5184891B2 (en) 2005-01-07 2013-04-17 シンタ ファーマシューティカルズ コーポレーション Compounds used for inflammation and immunity related applications
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
CA2594474C (en) 2005-01-21 2016-03-29 Astex Therapeutics Limited Pharmaceutical compounds
WO2006077428A1 (en) 2005-01-21 2006-07-27 Astex Therapeutics Limited Pharmaceutical compounds
AR054425A1 (en) 2005-01-21 2007-06-27 Astex Therapeutics Ltd PIPERIDIN ADDITION SALTS 4-IL-ACID AMID 4- (2,6-DICLORO-BENZOILAMINO) 1H-PIRAZOL-3-CARBOXILICO.
US7576099B2 (en) 2005-02-28 2009-08-18 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
MX2007011105A (en) 2005-03-10 2007-10-08 Pfizer Substituted n-sulfonylaminophenylethyl-2-phenoxy acetamide compounds.
EP2540296A1 (en) 2005-06-03 2013-01-02 Xenon Pharmaceuticals Inc. Arminothiazole derivatives as human stearoyl-coa desaturase inhibitors
US8343953B2 (en) 2005-06-22 2013-01-01 Astex Therapeutics Limited Pharmaceutical compounds
JP5345842B2 (en) 2005-06-23 2013-11-20 アステックス・セラピューティクス・リミテッド Pharmaceutical combinations containing pyrazole derivatives as protein kinase modulators
US7781460B2 (en) 2005-09-05 2010-08-24 Ranbaxy Laboratories Limited Substituted indazoles as inhibitors of phosphodiesterase type-IV
US7915286B2 (en) 2005-09-16 2011-03-29 Ranbaxy Laboratories Limited Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors
GB0521244D0 (en) 2005-10-19 2005-11-30 Astrazeneca Ab Benzamide compounds
US8399442B2 (en) 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
TW200745049A (en) 2006-03-23 2007-12-16 Astrazeneca Ab New crystalline forms
TW200808769A (en) 2006-04-18 2008-02-16 Astrazeneca Ab Therapeutic compounds
JP5564249B2 (en) 2006-06-23 2014-07-30 アレシア・バイオセラピューティクス・インコーポレーテッド Polynucleotide and polypeptide sequences involved in cancer
US8435970B2 (en) 2006-06-29 2013-05-07 Astex Therapeutics Limited Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea
WO2008059335A1 (en) 2006-11-13 2008-05-22 Pfizer Products Inc. Diaryl, dipyridinyl and aryl-pyridinyl derivatives and uses thereof
US20080207659A1 (en) 2007-02-15 2008-08-28 Asit Kumar Chakraborti Inhibitors of phosphodiesterase type 4
GB0704932D0 (en) 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
EA020531B1 (en) * 2007-04-13 2014-11-28 Милленниум Фармасьютикалз, Инк. COMBINATION ANTICOAGULANT THERAPY WITH A COMPOUND THAT ACTS AS A FACTOR Xa INHIBITOR
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
WO2010060186A1 (en) 2008-11-03 2010-06-03 Alethia Biotherapeutics Inc. Antibodies that specifically block the biological activity of a tumor antigen
ES2740424T3 (en) 2009-03-13 2020-02-05 Agios Pharmaceuticals Inc Methods and compositions for disorders related to cell proliferation
JP5756457B2 (en) 2009-04-06 2015-07-29 アジオス ファーマシューティカルズ， インコーポレイテッド Pyruvate kinase M2 modulators, therapeutic compositions and related methods of use
EP2438059A1 (en) 2009-06-05 2012-04-11 Link Medicine Corporation Aminopyrrolidinone derivatives and uses thereof
PT2448582T (en) 2009-06-29 2017-07-10 Agios Pharmaceuticals Inc Quinoline-8-sulfonamide derivatives having an anticancer activity
EP3561077B1 (en) 2009-10-21 2022-12-21 Les Laboratoires Servier Methods for cell-proliferation-related disorders
EP3257854A1 (en) 2009-11-05 2017-12-20 University of Notre Dame du Lac Imidazo[1,2-a]pyridine compounds, synthesis thereof, and methods of using same
CN102918034B (en) 2010-03-30 2015-06-03 维颂公司 Multisubstituted aromatic compounds as inhibitors of thrombin
CN101870636B (en) * 2010-04-01 2013-01-23 大唐(杭州)医药化工有限公司 Preparation method of 2-bromo-6-fluoronaphthalene
ES2564952T3 (en) 2010-12-17 2016-03-30 Agios Pharmaceuticals, Inc. New derivatives of N- (4- (azetidine-1-carbonyl) phenyl) - (hetero-) arylsulfonamide as modulators of pyruvate kinase M2 (PKM2)
EP2655350B1 (en) 2010-12-21 2016-03-09 Agios Pharmaceuticals, Inc. Bicyclic pkm2 activators
TWI549947B (en) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 Therapeutic compounds and compositions
BR112013025198A2 (en) 2011-03-31 2018-12-04 Alethia Biotherapeutics Inc. kidney-associated antigen 1 antibodies and antigen-binding fragments thereof
ES2746558T3 (en) 2011-05-03 2020-03-06 Agios Pharmaceuticals Inc Pyruvate kinase R activators for therapy use
MX367387B (en) 2011-05-03 2019-08-19 Agios Pharmaceuticals Inc Pyruvate kinase activators for use in therapy.
CN102827073A (en) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 Therapeutically active compositions and application methods thereof
CN102827170A (en) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 Active treatment compositions and use method thereof
BR112014016723A2 (en) 2012-01-09 2018-07-24 Alethia Biotherapeutics Inc. method for treating breast cancer
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
CN103483242A (en) * 2012-06-15 2014-01-01 上海朴颐化学科技有限公司 Preparation methods of 4-(2'-pyridyl)benzyl hydrazine and its intermediate
JP2015531395A (en) 2012-10-04 2015-11-02 ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ Pyrrolo [3,2-C] pyridine tropomyosin-related kinase inhibitor
ES2702182T3 (en) 2013-03-15 2019-02-27 Verseon Corp Aromatic compounds multisubstituted as serine protease inhibitors
BR112015023214A8 (en) 2013-03-15 2019-12-24 Verseon Corp compound, pharmaceutical composition, and, use of a pharmaceutical compound or composition
EP3019480B1 (en) 2013-07-11 2020-05-06 Agios Pharmaceuticals, Inc. 2,4- or 4,6-diaminopyrimidine compounds as idh2 mutants inhibitors for the treatment of cancer
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
WO2015003360A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
CA2926950C (en) 2013-10-10 2022-10-11 Eastern Virginia Medical School 4-((2-hydroxy-3-methoxybenzyl)amino) benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase
WO2015138839A1 (en) 2014-03-14 2015-09-17 Agios Pharmaceuticals, Inc. Pharmaceutical compositions of therapeutically active compounds
DK3154947T3 (en) * 2014-06-11 2018-06-18 Bayer Cropscience Ag PROCEDURE FOR PREPARING 3,5-BIS (HALOGENAL COOL) PYRAZOLES BY ACYLATION OF KETIMINES
CN104016944B (en) * 2014-06-16 2016-05-18 山东大学 N-(2-(amine methyl) phenyl) thiazole-4-carboxamide derivative and preparation method thereof and application
AU2015317522A1 (en) 2014-09-17 2017-03-23 Verseon Corporation Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
HRP20221287T1 (en) 2015-02-27 2023-02-03 Verseon International Corporation Substituted pyrazole compounds as serine protease inhibitors
EP4344703A1 (en) 2015-06-11 2024-04-03 Agios Pharmaceuticals, Inc. Methods of using pyruvate kinase activators
WO2016202756A1 (en) 2015-06-18 2016-12-22 Bayer Pharma Aktiengesellschaft Substituted 2-(1h-pyrazol-1-yl)-1h-benzimidazole compounds
CA2998375A1 (en) 2015-09-17 2017-03-23 Marvin J. Miller Benzyl amine-containing heterocyclic compounds and compositions useful against mycobacterial infection
EP3362065B1 (en) 2015-10-15 2024-04-03 Les Laboratoires Servier Combination therapy comprising ivosidenib, cytarabine and daunorubicin or idarubicin for treating acute myelogenous leukemia
EA039829B1 (en) 2015-10-15 2022-03-17 Аджиос Фармасьютикалз, Инк. Combination therapy for treating malignancies
MX2020003671A (en) 2017-10-06 2020-08-03 Forma Therapeutics Inc Inhibiting ubiquitin specific peptidase 30.
UA126458C2 (en) 2018-02-13 2022-10-05 Гіліад Сайєнсіз, Інк. Pd-1/pd-l1 inhibitors
US10899735B2 (en) 2018-04-19 2021-01-26 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
WO2019207463A1 (en) 2018-04-26 2019-10-31 Pfizer Inc. 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
GB201810581D0 (en) 2018-06-28 2018-08-15 Ctxt Pty Ltd Compounds
MX2021000100A (en) 2018-07-13 2021-03-25 Gilead Sciences Inc Pd-1/pd-l1 inhibitors.
HUE062240T2 (en) 2018-10-05 2023-10-28 Forma Therapeutics Inc Fused pyrrolines which act as ubiquitin-specific protease 30 (usp30) inhibitors
WO2020086556A1 (en) 2018-10-24 2020-04-30 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
PE20220808A1 (en) 2019-06-18 2022-05-20 Pfizer BENZISOXAZOLE SULFONAMIDE DERIVATIVES
US11834441B2 (en) 2019-12-06 2023-12-05 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofurans as modulators of sodium channels
EP4347031A1 (en) 2021-06-04 2024-04-10 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides as modulators of sodium channels

Family Cites Families (3)

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PL334250A1 (en) * 1996-12-23 2000-02-14 Du Pont Pharm Co Nitrogen containing hetero-aromatic compounds and inhibitors of xa factor
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