JP2002524463A5 - - Google Patents
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- JP2002524463A5 JP2002524463A5 JP2000568853A JP2000568853A JP2002524463A5 JP 2002524463 A5 JP2002524463 A5 JP 2002524463A5 JP 2000568853 A JP2000568853 A JP 2000568853A JP 2000568853 A JP2000568853 A JP 2000568853A JP 2002524463 A5 JP2002524463 A5 JP 2002524463A5
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- alkyl
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- 150000001875 compounds Chemical class 0.000 description 185
- -1 perhaloalkyl Chemical group 0.000 description 99
- 125000003118 aryl group Chemical group 0.000 description 97
- 125000000217 alkyl group Chemical group 0.000 description 91
- 125000004093 cyano group Chemical group *C#N 0.000 description 61
- 125000001072 heteroaryl group Chemical group 0.000 description 61
- 125000005843 halogen group Chemical group 0.000 description 54
- 125000003710 aryl alkyl group Chemical group 0.000 description 46
- 125000004429 atom Chemical group 0.000 description 46
- 125000003107 substituted aryl group Chemical group 0.000 description 44
- 239000003814 drug Substances 0.000 description 42
- 229940124597 therapeutic agent Drugs 0.000 description 42
- 125000004432 carbon atom Chemical group C* 0.000 description 41
- 239000000651 prodrug Substances 0.000 description 35
- 229940002612 prodrug Drugs 0.000 description 35
- 150000003839 salts Chemical class 0.000 description 35
- 125000005842 heteroatom Chemical group 0.000 description 34
- 125000002723 alicyclic group Chemical group 0.000 description 31
- 229910052698 phosphorus Inorganic materials 0.000 description 27
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 25
- 125000001543 furan-2,5-diyl group Chemical group O1C(=CC=C1*)* 0.000 description 21
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 19
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical group [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 19
- 239000011574 phosphorus Substances 0.000 description 19
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 18
- 239000004480 active ingredient Substances 0.000 description 17
- 125000003545 alkoxy group Chemical group 0.000 description 17
- 125000006366 methylene oxy carbonyl group Chemical group [H]C([H])([*:1])OC([*:2])=O 0.000 description 17
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 16
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 description 16
- 125000001424 substituent group Chemical group 0.000 description 16
- 229910052736 halogen Inorganic materials 0.000 description 15
- 150000002367 halogens Chemical class 0.000 description 15
- 125000003342 alkenyl group Chemical group 0.000 description 14
- 125000000304 alkynyl group Chemical group 0.000 description 14
- 229910052799 carbon Inorganic materials 0.000 description 14
- 101710099475 3'-phosphoadenosine 5'-phosphate phosphatase Proteins 0.000 description 13
- 101710196411 Fructose-1,6-bisphosphatase Proteins 0.000 description 13
- 101710186733 Fructose-1,6-bisphosphatase, chloroplastic Proteins 0.000 description 13
- 101710109119 Fructose-1,6-bisphosphatase, cytosolic Proteins 0.000 description 13
- 101710198902 Fructose-1,6-bisphosphate aldolase/phosphatase Proteins 0.000 description 13
- 125000004423 acyloxy group Chemical group 0.000 description 13
- 125000005200 aryloxy carbonyloxy group Chemical group 0.000 description 13
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 description 13
- 239000003112 inhibitor Substances 0.000 description 13
- 206010012601 diabetes mellitus Diseases 0.000 description 10
- 229910052739 hydrogen Inorganic materials 0.000 description 10
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 description 8
- 125000004514 1,2,4-thiadiazolyl group Chemical group 0.000 description 8
- 239000003795 chemical substances by application Substances 0.000 description 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 8
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 8
- 229910052760 oxygen Inorganic materials 0.000 description 8
- 125000004437 phosphorous atom Chemical group 0.000 description 8
- 229910052717 sulfur Inorganic materials 0.000 description 8
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 7
- 201000010099 disease Diseases 0.000 description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 7
- 125000006275 3-bromophenyl group Chemical group [H]C1=C([H])C(Br)=C([H])C(*)=C1[H] 0.000 description 6
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 description 6
- 125000006165 cyclic alkyl group Chemical group 0.000 description 6
- 125000005647 linker group Chemical group 0.000 description 6
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 description 5
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 5
- 125000004502 1,2,3-oxadiazolyl group Chemical group 0.000 description 4
- 125000004504 1,2,4-oxadiazolyl group Chemical group 0.000 description 4
- 125000004530 1,2,4-triazinyl group Chemical group N1=NC(=NC=C1)* 0.000 description 4
- 125000004506 1,2,5-oxadiazolyl group Chemical group 0.000 description 4
- 125000001781 1,3,4-oxadiazolyl group Chemical group 0.000 description 4
- 125000004520 1,3,4-thiadiazolyl group Chemical group 0.000 description 4
- 125000003363 1,3,5-triazinyl group Chemical group N1=C(N=CN=C1)* 0.000 description 4
- 208000002705 Glucose Intolerance Diseases 0.000 description 4
- 206010022489 Insulin Resistance Diseases 0.000 description 4
- 125000002252 acyl group Chemical group 0.000 description 4
- 125000005041 acyloxyalkyl group Chemical group 0.000 description 4
- 125000005205 alkoxycarbonyloxyalkyl group Chemical group 0.000 description 4
- 125000002883 imidazolyl group Chemical group 0.000 description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 4
- 125000001786 isothiazolyl group Chemical group 0.000 description 4
- 125000000842 isoxazolyl group Chemical group 0.000 description 4
- 229910052757 nitrogen Inorganic materials 0.000 description 4
- 125000002971 oxazolyl group Chemical group 0.000 description 4
- 201000009104 prediabetes syndrome Diseases 0.000 description 4
- 230000000069 prophylactic effect Effects 0.000 description 4
- 125000003373 pyrazinyl group Chemical group 0.000 description 4
- 125000003226 pyrazolyl group Chemical group 0.000 description 4
- 125000002098 pyridazinyl group Chemical group 0.000 description 4
- 125000004076 pyridyl group Chemical group 0.000 description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 description 4
- 125000000168 pyrrolyl group Chemical group 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 125000000335 thiazolyl group Chemical group 0.000 description 4
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 description 3
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 description 3
- 201000001320 Atherosclerosis Diseases 0.000 description 3
- 208000035150 Hypercholesterolemia Diseases 0.000 description 3
- 208000031226 Hyperlipidaemia Diseases 0.000 description 3
- 125000005741 alkyl alkenyl group Chemical group 0.000 description 3
- 125000005160 aryl oxy alkyl group Chemical group 0.000 description 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 description 2
- 125000006729 (C2-C5) alkenyl group Chemical group 0.000 description 2
- 125000006730 (C2-C5) alkynyl group Chemical group 0.000 description 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical group NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 description 2
- FKLJPTJMIBLJAV-UHFFFAOYSA-N Compound IV Chemical compound O1N=C(C)C=C1CCCCCCCOC1=CC=C(C=2OCCN=2)C=C1 FKLJPTJMIBLJAV-UHFFFAOYSA-N 0.000 description 2
- 102000012195 Fructose-1,6-bisphosphatases Human genes 0.000 description 2
- 108010017464 Fructose-Bisphosphatase Proteins 0.000 description 2
- 208000008589 Obesity Diseases 0.000 description 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 2
- 239000004202 carbamide Substances 0.000 description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 230000004110 gluconeogenesis Effects 0.000 description 2
- 230000009229 glucose formation Effects 0.000 description 2
- 208000007345 glycogen storage disease Diseases 0.000 description 2
- 125000001188 haloalkyl group Chemical group 0.000 description 2
- 125000001475 halogen functional group Chemical group 0.000 description 2
- 230000002440 hepatic effect Effects 0.000 description 2
- 125000005343 heterocyclic alkyl group Chemical group 0.000 description 2
- 125000000623 heterocyclic group Chemical group 0.000 description 2
- 201000001421 hyperglycemia Diseases 0.000 description 2
- 208000037906 ischaemic injury Diseases 0.000 description 2
- 235000020824 obesity Nutrition 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 229910052711 selenium Inorganic materials 0.000 description 2
- 125000005017 substituted alkenyl group Chemical group 0.000 description 2
- 125000000547 substituted alkyl group Chemical group 0.000 description 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N urea group Chemical group NC(=O)N XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 2
- 206010060378 Hyperinsulinaemia Diseases 0.000 description 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 description 1
- NLFBCYMMUAKCPC-KQQUZDAGSA-N ethyl (e)-3-[3-amino-2-cyano-1-[(e)-3-ethoxy-3-oxoprop-1-enyl]sulfanyl-3-oxoprop-1-enyl]sulfanylprop-2-enoate Chemical compound CCOC(=O)\C=C\SC(=C(C#N)C(N)=O)S\C=C\C(=O)OCC NLFBCYMMUAKCPC-KQQUZDAGSA-N 0.000 description 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 description 1
- 201000008980 hyperinsulinism Diseases 0.000 description 1
- 230000000302 ischemic effect Effects 0.000 description 1
- 208000037891 myocardial injury Diseases 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- ZMZDMBWJUHKJPS-UHFFFAOYSA-N thiocyanic acid Chemical compound SC#N ZMZDMBWJUHKJPS-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13550498P | 1998-09-09 | 1998-09-09 | |
| US60/135,504 | 1998-09-09 | ||
| US11107798P | 1998-12-07 | 1998-12-07 | |
| US60/111,077 | 1998-12-07 | ||
| PCT/US1999/020346 WO2000014095A1 (en) | 1998-09-09 | 1999-09-03 | Novel heteroaromatic inhibitors of fructose 1,6-bisphosphatase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2002524463A JP2002524463A (ja) | 2002-08-06 |
| JP2002524463A5 true JP2002524463A5 (https=) | 2006-10-19 |
Family
ID=26808618
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000568853A Pending JP2002524463A (ja) | 1998-09-09 | 1999-09-03 | フルクトース−1,6−ビスホスファターゼの新規な芳香族インヒビター |
Country Status (21)
| Country | Link |
|---|---|
| US (4) | US6489476B1 (https=) |
| EP (1) | EP1112275B9 (https=) |
| JP (1) | JP2002524463A (https=) |
| KR (2) | KR100818845B1 (https=) |
| CN (1) | CN1215076C (https=) |
| AT (1) | ATE246197T1 (https=) |
| AU (1) | AU761267C (https=) |
| BR (1) | BR9913532A (https=) |
| CA (1) | CA2343027A1 (https=) |
| CZ (1) | CZ297264B6 (https=) |
| DE (1) | DE69910045T2 (https=) |
| DK (1) | DK1112275T3 (https=) |
| ES (1) | ES2204170T3 (https=) |
| HK (1) | HK1042496B (https=) |
| HU (1) | HUP0103143A3 (https=) |
| NO (1) | NO20011174L (https=) |
| NZ (1) | NZ510308A (https=) |
| PL (1) | PL205184B1 (https=) |
| PT (1) | PT1112275E (https=) |
| SK (1) | SK286080B6 (https=) |
| WO (1) | WO2000014095A1 (https=) |
Families Citing this family (152)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6284748B1 (en) | 1997-03-07 | 2001-09-04 | Metabasis Therapeutics, Inc. | Purine inhibitors of fructose 1,6-bisphosphatase |
| US6312662B1 (en) | 1998-03-06 | 2001-11-06 | Metabasis Therapeutics, Inc. | Prodrugs phosphorus-containing compounds |
| KR100818845B1 (ko) * | 1998-09-09 | 2008-04-01 | 메타베이시스 테라퓨틱스, 인크. | 신규한 프럭토스 1,6-비스포스파타제의 헤테로방향족 억제제 |
| US6756360B1 (en) * | 1998-12-24 | 2004-06-29 | Metabasis Therapeutics, Inc. | Combination of FBPase inhibitors and insulin sensitizers for the treatment of diabetes |
| MXPA01008937A (es) * | 1999-03-05 | 2004-04-05 | Metabasis Therapeutics Inc | Nuevos profarmacos que contienen fosforo. |
| US7205404B1 (en) | 1999-03-05 | 2007-04-17 | Metabasis Therapeutics, Inc. | Phosphorus-containing prodrugs |
| GB9923078D0 (en) * | 1999-09-29 | 1999-12-01 | Phytopharm Plc | Sapogenin derivatives and their use |
| AU784370B2 (en) * | 1999-12-22 | 2006-03-23 | Metabasis Therapeutics, Inc. | Novel bisamidate phosphonate prodrugs |
| EP1743655B1 (en) | 2000-01-21 | 2014-06-25 | Novartis AG | Combinations comprising dipeptidylpeptidase-iv inhibitors and antidiabetic agents |
| JP2003525944A (ja) * | 2000-03-08 | 2003-09-02 | メタバシス・セラピューティクス・インコーポレイテッド | 新規アリールフルクトース−1,6−ビスホスファターゼ阻害剤 |
| US7563774B2 (en) | 2000-06-29 | 2009-07-21 | Metabasis Therapeutics, Inc. | Combination of FBPase inhibitors and antidiabetic agents useful for the treatment of diabetes |
| EP1372660A2 (en) * | 2000-07-06 | 2004-01-02 | Metabasis Therapeutics, Inc. | A combination of fbpase inhibitors and antidiabetic agents useful for the treatment of diabetes |
| US20070129334A1 (en) * | 2001-10-30 | 2007-06-07 | Conforma Therapeutics Corporation | Orally Active Purine-Based Inhibitors of Heat Shock Protein 90 |
| WO2003095665A2 (en) * | 2002-05-13 | 2003-11-20 | Metabasis Therapeutics, Inc. | Pmea and pmpa cyclic producing synthesis |
| EP2223927B1 (en) * | 2002-05-13 | 2014-10-15 | Metabasis Therapeutics, Inc. | Salts of a phosphonic acid based prodrug of PMEA |
| AU2003252676A1 (en) * | 2002-07-23 | 2004-02-09 | Sankyo Company, Limited | Preventive for the onset of diabetes |
| BR0315795A (pt) * | 2002-10-31 | 2005-09-13 | Metabasis Therapeutics Inc | Pró-medicamentos de monofosfato de citarabina |
| US20040254228A1 (en) * | 2002-12-20 | 2004-12-16 | Lin Zhao | Treatment of chronic heart failure |
| US20040122067A1 (en) * | 2002-12-20 | 2004-06-24 | Lin Zhao | Treatment of chronic heart failure |
| SI1611112T1 (sl) * | 2003-02-11 | 2012-12-31 | Vernalis (R&D) Limited | Izoksazolne spojine kot inhibitorji vroäśinskih ĺ ok proteinov |
| CN1882327A (zh) | 2003-11-19 | 2006-12-20 | 症变治疗公司 | 含磷的新的拟甲状腺素药 |
| US7129049B2 (en) * | 2003-12-22 | 2006-10-31 | Regents Of The University Of Minnesota | Method of detecting equine glycogen storage disease IV |
| JP4638355B2 (ja) * | 2003-12-26 | 2011-02-23 | 協和発酵キリン株式会社 | チアゾール誘導体 |
| US7179827B2 (en) * | 2004-03-31 | 2007-02-20 | Lexicon Genetics Incorporated | Thiazoles and methods of their use |
| JP2007261945A (ja) * | 2004-04-07 | 2007-10-11 | Taisho Pharmaceut Co Ltd | チアゾール誘導体 |
| CA2565966A1 (en) * | 2004-06-08 | 2005-12-29 | Metabasis Therapeutics, Inc. | Lewis acid mediated synthesis of cyclic esters |
| JP2008510018A (ja) * | 2004-08-18 | 2008-04-03 | メタバシス・セラピューティクス・インコーポレイテッド | フルクトース−1,6−ビスホスファターゼの新規チアゾール阻害物質 |
| BRPI0519006A2 (pt) * | 2004-12-13 | 2008-12-23 | Daiichi Sankyo Co Ltd | uso de um inibidor de fbpase, kit de uma composiÇço farmacÊutica, uso de uma preparaÇço de biguanida e um inibidor de fbpase, agente terapÊutico para diabetes melito, e, combinaÇço de agentes terapÊuticos |
| EP1825854A1 (en) * | 2004-12-15 | 2007-08-29 | Daiichi Sankyo Company, Limited | MEDICINAL COMPOSITION CONTAINING FBPase INHIBITOR |
| WO2008134474A2 (en) | 2007-04-27 | 2008-11-06 | The Board Of Trustees Of The University Of Illinois | Compositions and methods including cell death inducers and procaspase activation |
| EP1894930A4 (en) * | 2005-06-23 | 2010-06-23 | Kyowa Hakko Kirin Co Ltd | THIAZOLE DERIVATIVE |
| FR2889190A1 (fr) * | 2005-08-01 | 2007-02-02 | Merck Sante Soc Par Actions Si | Nouveaux derives d'imidazoles carboxamides comme inhibiteurs de fructose -1,6-biphosphatase et compositions pharmaceutiques les contenant |
| EP1752450A1 (en) | 2005-08-01 | 2007-02-14 | Merck Sante | Imidazole derivatives as fructose-1,6-bisphosphatase inhibitors and pharmaceutical compositions containing them |
| PT1931350E (pt) | 2005-09-14 | 2014-02-12 | Takeda Pharmaceutical | Administração de inibidores de dipeptidil peptidase |
| JP2009537636A (ja) | 2006-05-19 | 2009-10-29 | ザ ボード オブ トラスティーズ オブ ザ ユニヴァーシティー オブ イリノイ | 黒色腫及び他の癌を治療するためのトリフェニルメチルホスホン酸エステルを含めたリン含有化合物 |
| US20100076037A1 (en) | 2006-11-02 | 2010-03-25 | Chiang Lillian W | Methods of Treating Neuropathic Pain with Agonists of PPAR-gamma |
| US20080218127A1 (en) * | 2007-03-07 | 2008-09-11 | O2Micro Inc. | Battery management systems with controllable adapter output |
| US8222870B2 (en) * | 2007-03-07 | 2012-07-17 | O2Micro, Inc | Battery management systems with adjustable charging current |
| US7973515B2 (en) * | 2007-03-07 | 2011-07-05 | O2Micro, Inc | Power management systems with controllable adapter output |
| CN101821276B (zh) * | 2007-08-13 | 2016-08-31 | 症变治疗公司 | 新颖的葡糖激酶活化剂 |
| EP2058308A1 (fr) | 2007-11-12 | 2009-05-13 | Merck Sante | Dérivés de benzimidazoledihydrothiadiazinone comme inhibiteurs de fructose-1,6-biphosphatase et compositions pharmaceutiques les contenant. |
| US8111038B2 (en) * | 2008-06-12 | 2012-02-07 | O2 Micro, Inc | Vehicle electronic systems with battery management functions |
| US8394969B2 (en) * | 2008-09-26 | 2013-03-12 | Merck Sharp & Dohme Corp. | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| EP2348857B1 (en) | 2008-10-22 | 2016-02-24 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| EP2352374B1 (en) | 2008-10-29 | 2014-09-24 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| US8329914B2 (en) * | 2008-10-31 | 2012-12-11 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| JO2870B1 (en) | 2008-11-13 | 2015-03-15 | ميرك شارب اند دوهم كورب | Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes |
| EP2358200A4 (en) | 2008-11-17 | 2012-05-16 | Merck Sharp & Dohme | SUBSTITUTED BICYCLIC AMINES FOR THE TREATMENT OF DIABETES |
| US8778945B2 (en) | 2009-02-09 | 2014-07-15 | The Board Of Trustees Of The University Of Illinois | Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs |
| WO2010093601A1 (en) | 2009-02-10 | 2010-08-19 | Metabasis Therapeutics, Inc. | Novel sulfonic acid-containing thyromimetics, and methods for their use |
| EP2805951B1 (en) | 2009-03-20 | 2018-03-14 | Metabasis Therapeutics, Inc. | Inhibitors of diacylglycerol o-acyltransferase 1 (DGAT-1) and uses thereof |
| CA2768577A1 (en) | 2009-07-23 | 2011-01-27 | Schering Corporation | Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors |
| WO2011011506A1 (en) | 2009-07-23 | 2011-01-27 | Schering Corporation | Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors |
| EP2464228B1 (en) | 2009-08-13 | 2017-12-06 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment |
| BR112012004335A8 (pt) | 2009-09-02 | 2016-06-21 | Merck Sharp & Dohme | Composto, composição farmacêutica, e, uso do composto. |
| WO2011041293A1 (en) | 2009-09-30 | 2011-04-07 | Takeda Pharmaceutical Company Limited | Pyrazolo [1, 5-a] pyrimidine derivatives as apoptosis signal-regulating kinase 1 inhibitors |
| PL2531501T3 (pl) | 2010-02-03 | 2014-05-30 | Takeda Pharmaceuticals Co | Inhibitory kinazy 1 regulującej sygnał apoptotyczny |
| US8853212B2 (en) | 2010-02-22 | 2014-10-07 | Merck Sharp & Dohme Corp | Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes |
| JP2013520502A (ja) | 2010-02-25 | 2013-06-06 | メルク・シャープ・エンド・ドーム・コーポレイション | 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体 |
| US8980929B2 (en) | 2010-05-21 | 2015-03-17 | Merck Sharp & Dohme Corp. | Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes |
| WO2012024183A1 (en) | 2010-08-18 | 2012-02-23 | Merck Sharp & Dohme Corp. | Spiroxazolidinone compounds |
| US8951993B2 (en) * | 2011-02-24 | 2015-02-10 | Jiangsu Hansoh Pharmaceutical Co., Ltd. | Phosphorus containing compounds as protein kinase inhibitors |
| SG192941A1 (en) | 2011-02-25 | 2013-09-30 | Merck Sharp & Dohme | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents |
| US8957062B2 (en) | 2011-04-08 | 2015-02-17 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment |
| AU2012264651A1 (en) | 2011-06-02 | 2013-12-12 | Intervet International B.V. | Imidazole derivatives |
| EP2720544B1 (en) | 2011-06-16 | 2016-12-21 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment |
| EP2760855B1 (en) | 2011-09-30 | 2017-03-15 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds as well as their use in treating type-2 diabetes |
| EP2771000B1 (en) | 2011-10-24 | 2016-05-04 | Merck Sharp & Dohme Corp. | Substituted piperidinyl compounds useful as gpr119 agonists |
| WO2013068328A1 (en) | 2011-11-07 | 2013-05-16 | Intervet International B.V. | Bicyclo [2.2.2] octan-1-ylcarboxylic acid compounds as dgat-1 inhibitors |
| WO2013068439A1 (en) | 2011-11-09 | 2013-05-16 | Intervet International B.V. | 4-amino-5-oxo-7,8-dihydropyrimido[5, 4 -f] [1, 4] oxazepine compounds as dgat1 inhibitors |
| WO2013074581A1 (en) * | 2011-11-15 | 2013-05-23 | Weihua Zhang | Fructose-1,6-biphosphatases as new targets for diagnosing and treating breast cancer brain metastasis |
| WO2013074388A1 (en) | 2011-11-15 | 2013-05-23 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds useful as gpr119 agonists |
| WO2013122920A1 (en) | 2012-02-17 | 2013-08-22 | Merck Sharp & Dohme Corp. | Dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes |
| JP2015519309A (ja) | 2012-04-16 | 2015-07-09 | カネック ファーマ インコーポレイテッド | Ptp−1bインヒビター前駆体としての縮合芳香族ホスホナート誘導体 |
| EP2874622A4 (en) | 2012-07-23 | 2015-12-30 | Merck Sharp & Dohme | TREATMENT OF DIABETES WITH DIPEPTIDYLPEPTIDASE IV INHIBITORS |
| RU2015106909A (ru) | 2012-08-02 | 2016-09-27 | Мерк Шарп И Доум Корп. | Антидиабетические трициклические соединения |
| WO2014031441A1 (en) | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel benzimidazole tetrahydrofuran derivatives |
| EP2888008B1 (en) | 2012-08-22 | 2018-12-26 | Merck Sharp & Dohme Corp. | Novel azabenzimidazole tetrahydrofuran derivatives |
| WO2014031445A1 (en) | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel benzimidazole tetrahydropyran derivatives |
| WO2014031468A1 (en) | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel benzimidazole hexahydrofuro[3,2-b]furan derivatives |
| WO2014031465A1 (en) | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel azabenzimidazole tetrahydropyran derivatives |
| EP2888005B1 (en) | 2012-08-22 | 2019-04-03 | Merck Sharp & Dohme Corp. | Novel azabenzimidazole hexahydrofuro[3,2-b]furan derivatives |
| CN103665043B (zh) | 2012-08-30 | 2017-11-10 | 江苏豪森药业集团有限公司 | 一种替诺福韦前药及其在医药上的应用 |
| EP2931734B1 (en) | 2012-12-17 | 2020-12-02 | Merck Sharp & Dohme Corp. | Novel glucokinase activator compounds, compositions containing such compounds, and methods of treatment |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| EP3068768B1 (en) | 2013-11-15 | 2019-07-31 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| WO2015089809A1 (en) | 2013-12-19 | 2015-06-25 | Merck Sharp & Dohme Corp. | Antidiabetic substituted heteroaryl compounds |
| WO2015112465A1 (en) | 2014-01-24 | 2015-07-30 | Merck Sharp & Dohme Corp. | Isoquinoline derivatives as mgat2 inhibitors |
| AU2015217221A1 (en) | 2014-02-13 | 2016-08-11 | Ligand Pharmaceuticals, Inc. | Prodrug compounds and their uses |
| US9732103B2 (en) | 2014-02-25 | 2017-08-15 | Achillion Pharmaceuticals, Inc. | Carbamate, ester, and ketone compounds for treatment of complement mediated disorders |
| WO2015176267A1 (en) | 2014-05-22 | 2015-11-26 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| CN106687118A (zh) | 2014-07-02 | 2017-05-17 | 配体药物公司 | 前药化合物及其用途 |
| WO2016022742A1 (en) | 2014-08-08 | 2016-02-11 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| US10662171B2 (en) | 2014-08-08 | 2020-05-26 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| WO2016022446A1 (en) | 2014-08-08 | 2016-02-11 | Merck Sharp & Dohme Corp. | [5,6]-fused bicyclic antidiabetic compounds |
| CN107108715A (zh) | 2014-10-24 | 2017-08-29 | 默沙东公司 | 胰高血糖素和glp‑1受体的共激动剂 |
| EP3701969A1 (en) | 2014-10-31 | 2020-09-02 | NGM Biopharmaceuticals, Inc. | Compositions and methods of use for treating metabolic disorders |
| TW201625635A (zh) | 2014-11-21 | 2016-07-16 | 默沙東藥廠 | 作為可溶性鳥苷酸環化酶活化劑之三唑并吡基衍生物 |
| WO2016191334A1 (en) | 2015-05-27 | 2016-12-01 | Merck Sharp & Dohme Corp. | Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators |
| WO2016191335A1 (en) | 2015-05-28 | 2016-12-01 | Merck Sharp & Dohme Corp. | Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators |
| WO2017035401A1 (en) | 2015-08-26 | 2017-03-02 | Achillion Pharmaceuticals, Inc. | Amide compounds for treatment of immune and inflammatory disorders |
| WO2017035409A1 (en) | 2015-08-26 | 2017-03-02 | Achillion Pharmaceuticals, Inc. | Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders |
| US10385097B2 (en) | 2015-08-26 | 2019-08-20 | Achillion Pharmaceuticals, Inc. | Ether compounds for treatment of medical disorders |
| AR106018A1 (es) | 2015-08-26 | 2017-12-06 | Achillion Pharmaceuticals Inc | Compuestos de arilo, heteroarilo y heterocíclicos para el tratamiento de trastornos médicos |
| WO2017035351A1 (en) | 2015-08-26 | 2017-03-02 | Achillion Pharmaceuticals, Inc. | Amino compounds for treatment of medical disorders |
| WO2017035408A1 (en) | 2015-08-26 | 2017-03-02 | Achillion Pharmaceuticals, Inc. | Compounds for treatment of immune and inflammatory disorders |
| WO2017035357A1 (en) * | 2015-08-26 | 2017-03-02 | Achillion Pharmaceuticals, Inc. | Phosphonate compounds for treatment of medical disorders |
| WO2017035361A1 (en) | 2015-08-26 | 2017-03-02 | Achillion Pharmaceuticals, Inc. | Disubstituted compounds for the treatment of medical disorders |
| AR105808A1 (es) | 2015-08-26 | 2017-11-08 | Achillion Pharmaceuticals Inc | Compuestos de amida para el tratamiento de trastornos médicos |
| WO2017035405A1 (en) | 2015-08-26 | 2017-03-02 | Achillion Pharmaceuticals, Inc. | Amino compounds for treatment of immune and inflammatory disorders |
| AR105809A1 (es) | 2015-08-26 | 2017-11-08 | Achillion Pharmaceuticals Inc | Compuestos para el tratamiento de trastornos médicos |
| CN108289899A (zh) * | 2015-09-22 | 2018-07-17 | 维京治疗公司 | 采用葡萄糖生成的抑制剂的联合疗法 |
| WO2017062334A1 (en) | 2015-10-05 | 2017-04-13 | Merck Sharp & Dohme Corp. | Antibody peptide conjugates that have agonist activity at both the glucagon and glucagon-like peptide 1 receptors |
| EP3383868B1 (en) | 2015-11-30 | 2022-10-05 | Merck Sharp & Dohme LLC | Aryl sulfonamides as blt1 antagonists |
| WO2017107052A1 (en) | 2015-12-22 | 2017-06-29 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase stimulators |
| WO2017197555A1 (en) | 2016-05-16 | 2017-11-23 | Merck Sharp & Dohme Corp. | Fused pyrazine derivatives useful as soluble guanylate cyclase stimulators |
| WO2017201683A1 (en) | 2016-05-25 | 2017-11-30 | Merck Sharp & Dohme Corp. | Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists |
| US10414775B2 (en) | 2016-08-15 | 2019-09-17 | Merck Sharp & Dohme Corp. | Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease |
| WO2018034918A1 (en) | 2016-08-15 | 2018-02-22 | Merck Sharp & Dohme Corp. | Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease |
| US11008313B2 (en) | 2016-09-20 | 2021-05-18 | Merck Sharp & Dohme Corp. | Substituted 1-methyl-1,2,3,4-tetrahydroisoquinoline molecules as PCSK9 allosteric binders |
| AU2017360939B2 (en) | 2016-11-18 | 2022-03-03 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2 |
| EP3541376B1 (en) | 2016-11-18 | 2023-04-19 | Merck Sharp & Dohme LLC | Indole derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| WO2018107415A1 (en) | 2016-12-15 | 2018-06-21 | Merck Sharp & Dohme Corp. | Hydroxy isoxazole compounds useful as gpr120 agonists |
| CN110603252A (zh) | 2017-03-01 | 2019-12-20 | 艾其林医药公司 | 用于治疗医学障碍的芳基、杂芳基和杂环药物化合物 |
| EP3589287B1 (en) | 2017-03-01 | 2022-09-14 | Achillion Pharmaceuticals, Inc. | Macrocyclic compounds for treatment of medical disorders |
| WO2018160891A1 (en) | 2017-03-01 | 2018-09-07 | Achillion Pharmaceutical, Inc. | Pharmaceutical compounds for treatment of medical disorders |
| US11040947B2 (en) | 2017-03-22 | 2021-06-22 | The Research Foundation For The State University Of New York | Substituted quinazolines as matrix metalloproteinase-9 hemopexin domain inhibitors |
| EP3661493A4 (en) | 2017-08-02 | 2021-04-14 | Achillion Pharmaceuticals, Inc. | THERAPY PLANS FOR TREATMENT OF PAROXYSMALER NIGHTLY HEMOGLOBINURIA |
| CA3087932A1 (en) | 2018-01-09 | 2019-07-18 | Ligand Pharmaceuticals, Inc. | Acetal compounds and therapeutic uses thereof |
| IL279363B2 (en) | 2018-06-21 | 2025-12-01 | Merck Sharp & Dohme | Pcsk9 antagonist compounds |
| WO2020051538A1 (en) | 2018-09-06 | 2020-03-12 | Achillion Pharmaceuticals, Inc. | Morphic forms of complement factor d inhibitors |
| JP7443375B2 (ja) | 2018-09-06 | 2024-03-05 | アキリオン ファーマシューティカルズ, インコーポレーテッド | 医学的障害の治療のための大環状化合物 |
| KR20210093855A (ko) | 2018-09-25 | 2021-07-28 | 아칠리온 파르마세우티칼스 인코포레이티드 | 보체 인자 d 억제제의 형태체 형태 |
| WO2020131974A1 (en) | 2018-12-17 | 2020-06-25 | Achillion Pharmaceuticals, Inc. | Targeted dosing for the treatment of complement mediated disorders |
| BR112021018456A2 (pt) | 2019-03-22 | 2021-11-23 | Achillion Pharmaceuticals Inc | Compostos farmacêuticos para o tratamento de distúrbios mediados por complemento |
| KR102691198B1 (ko) | 2019-03-28 | 2024-08-05 | 백동민 | 로봇청소기 및 그 제어방법 |
| WO2020205688A1 (en) | 2019-04-04 | 2020-10-08 | Merck Sharp & Dohme Corp. | Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes |
| EP4021919A1 (en) | 2019-08-30 | 2022-07-06 | Merck Sharp & Dohme Corp. | Pcsk9 antagonist compounds |
| EP3842061A1 (en) | 2019-12-23 | 2021-06-30 | Merck Sharp & Dohme Corp. | Stapled triazole co-agonists of the glucagon and glp-1 receptors |
| EP3842449A1 (en) | 2019-12-23 | 2021-06-30 | Merck Sharp & Dohme Corp. | Stapled olefin co-agonists of the glucagon and glp-1 receptors |
| EP3842060A1 (en) | 2019-12-23 | 2021-06-30 | Merck Sharp & Dohme Corp. | Stapled lactam co-agonists of the glucagon and glp-1 receptors |
| WO2021236405A1 (en) | 2020-05-18 | 2021-11-25 | Merck Sharp & Dohme Corp. | Novel diacylglyceride o-acyltransferase 2 inhibitors |
| AR123701A1 (es) | 2020-10-08 | 2023-01-04 | Merck Sharp & Dohme | Preparación de derivados de oxindol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2 |
| TW202229243A (zh) | 2020-10-08 | 2022-08-01 | 美商默沙東藥廠 | 作為新穎二醯基甘油酯o-醯基轉移酶2抑制劑之苯并咪唑酮衍生物的製備 |
| IL310851A (en) | 2021-08-19 | 2024-04-01 | Merck Sharp & Dohme Llc | Compounds for the treatment of diseases associated with PCSK9 activity |
| KR20250025685A (ko) | 2022-06-15 | 2025-02-24 | 머크 샤프 앤드 돔 엘엘씨 | 인터류킨-1 베타를 포획하기 위한 시클릭 펩티드 |
| KR20250107282A (ko) | 2022-12-02 | 2025-07-11 | 머크 샤프 앤드 돔 엘엘씨 | 신규 디아실글리세리드 o-아실트랜스퍼라제 2 억제제로서의 융합된 아졸 유도체의 제조 |
| CN117486955B (zh) * | 2023-10-17 | 2026-04-17 | 上海交通大学 | 一种非经典c-糖苷及其立体专一性合成方法和应用 |
| TW202540146A (zh) | 2023-11-14 | 2025-10-16 | 美商默沙東有限責任公司 | 用於捕捉介白素-1 β之環狀肽 |
| US20260116923A1 (en) | 2023-12-15 | 2026-04-30 | Merck Sharp & Dohme Llc | Cyclic peptide il-1beta trap for the treatment of atherosclerosis and inflammatory disorders |
| WO2026019977A1 (en) | 2024-07-19 | 2026-01-22 | Merck Sharp & Dohme Llc | Pyrrolopyridazine vegfr inhibitors |
Family Cites Families (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR34480E (https=) | 1929-01-17 | 1929-06-19 | ||
| US3551422A (en) | 1968-03-27 | 1970-12-29 | Stevens & Co Inc J P | N-(oxymethyl) derivatives of phosphonopolyamino-s-triazines |
| US3822296A (en) | 1969-01-23 | 1974-07-02 | Merck & Co Inc | 1-trifluoromethyl-1,2-epoxyethyl-1-phosphonic acid and its salts |
| US3657282A (en) | 1969-01-23 | 1972-04-18 | Merck & Co Inc | Carboxyepoxyethyl-1-phosphonic acid and derivatives |
| GB1343022A (en) | 1970-04-19 | 1974-01-10 | British Oxygen Co Ltd | Phosphorus-containing guanamines |
| US4000305A (en) | 1972-09-27 | 1976-12-28 | Imperial Chemical Industries Limited | 15-, 16- AND 17-Indolyl or indolinyl nor prostanoic acid derivatives |
| GB1428137A (en) | 1972-09-27 | 1976-03-17 | Ici Ltd | Prostanoic acid derivatives |
| US4092323A (en) | 1975-09-16 | 1978-05-30 | Imperial Chemical Industries Limited | Hydrazine derivatives of pyridyl-ketones |
| GB1516347A (en) | 1975-09-16 | 1978-07-05 | Ici Ltd | Process for the preparation of alkylphosphonate esters |
| DE2855659A1 (de) | 1978-12-22 | 1980-07-03 | Bayer Ag | Benzimidazolyl-2-alkan-phosphonsaeuren |
| ATE16799T1 (de) | 1980-01-10 | 1985-12-15 | Nyegaard & Co As | Pyrimidin-2-sulfide und ihre s-oxide zur verwendung in der medizin, die verbindungen enthaltende pharmazeutische zusammensetzungen, verfahren zu ihrer herstellung und die verbindungen an sich, sofern sie neu sind. |
| FR2531088B1 (fr) | 1982-07-29 | 1987-08-28 | Sanofi Sa | Produits anti-inflammatoires derives de l'acide methylenediphosphonique et leur procede de preparation |
| IL77243A (en) | 1984-12-21 | 1996-11-14 | Procter & Gamble | Pharmaceutical compositions containing geminal diphosphonic acid compounds and certain such novel compounds |
| US4902679A (en) | 1985-12-13 | 1990-02-20 | Norwich Eaton Pharmaceuticals, Inc. | Methods of treating diseases with certain geminal diphosphonates |
| US4968788A (en) | 1986-04-04 | 1990-11-06 | Board Of Regents, The University Of Texas System | Biologically reversible phosphate and phosphonate protective gruops |
| DE3770982D1 (de) | 1986-04-24 | 1991-08-01 | Fujisawa Pharmaceutical Co | Diphosphonsaeure-verbindungen, verfahren zu deren herstellung und sie enthaltende arzneimittel. |
| JPS636089A (ja) | 1986-06-27 | 1988-01-12 | Nippon Shokubai Kagaku Kogyo Co Ltd | 石炭−水スラリ−用分散剤 |
| US5091552A (en) | 1986-06-30 | 1992-02-25 | Board Of Regents, The University Of Texas System | Novel antitumor aldophosphamide analogs |
| DE3776880D1 (de) | 1986-11-21 | 1992-04-02 | Ciba Geigy Ag | Neue substituierte alkandiphosphonsaeuren. |
| JPS63250290A (ja) | 1987-04-06 | 1988-10-18 | Matsushita Electric Ind Co Ltd | 電子スチルカメラ |
| US4912175A (en) | 1988-08-01 | 1990-03-27 | E. I. Du Pont De Nemours And Company | Process for in creasing polyamide molecular weight with P containing catalyst |
| US4968790A (en) | 1988-08-12 | 1990-11-06 | American Cyanamid Company | Antidiabetic phosphates |
| US4943629A (en) * | 1988-08-12 | 1990-07-24 | American Cyanamid Company | Antidiabetic alpha-substituted phosphonates |
| US5658889A (en) | 1989-01-24 | 1997-08-19 | Gensia Pharmaceuticals, Inc. | Method and compounds for aica riboside delivery and for lowering blood glucose |
| DE69014562T2 (de) * | 1989-01-24 | 1995-06-22 | Gensia Pharma | Verfahren und verbindungen zur verabreichung von aica ribosiden und zur erniedrigung des blutglucose gehaltes. |
| MX21452A (es) | 1989-07-07 | 1994-01-31 | Ciba Geigy Ag | Preparaciones farmaceuticas que se administran en forma topica. |
| DE4029444A1 (de) | 1989-09-19 | 1991-03-28 | Ciba Geigy Ag | Phosphonyl-enamine als pflanzenwuchsregulatoren |
| EP0438375B1 (de) | 1990-01-18 | 1995-12-27 | Ciba-Geigy Ag | Phoshponsäure- und Thionophosphonsäure-Derivate |
| US5116919A (en) | 1990-12-05 | 1992-05-26 | E. I. Du Pont De Nemours And Company | Process for increasing the relative viscosity of polyamides with reduced thermal degradation |
| FI89366C (fi) | 1990-12-20 | 1993-09-27 | Leiras Oy | Foerfarande foer framstaellning av nya farmakologiskt anvaendbara metylenbisfosfonsyraderivat |
| US5194616A (en) | 1991-01-24 | 1993-03-16 | E. I. Du Pont De Nemours And Company | Preparation of 2-(pyridyl)ethyl bis-(trialkyl silyl)phosphonate derivatives |
| WO1992019629A1 (en) | 1991-04-27 | 1992-11-12 | Japat Ltd. | Triazole compounds |
| EP0528760A1 (en) | 1991-08-09 | 1993-02-24 | Japat Ltd | Novel triazoles |
| US5142000A (en) | 1991-08-28 | 1992-08-25 | E. I. Du Pont De Nemours And Company | Process for increasing polyamide molecular weight with organophosphonic acid or ester catalysts in the presence of alumina-containing titanium dioxide |
| US5302586A (en) | 1991-12-19 | 1994-04-12 | G. D. Searle & Co. | Phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compounds for treatment of neurotoxic injury |
| MX9300141A (es) | 1992-01-13 | 1994-07-29 | Smithkline Beecham Corp | Compuestos de imidazol novedosos, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen. |
| GB9202779D0 (en) | 1992-02-10 | 1992-03-25 | Ici Plc | Novel compounds |
| CH683996A5 (fr) | 1992-03-05 | 1994-06-30 | Symphar Sa | Dérivés aminophosphonates substitués, leur procédé de préparation et compositions pharmaceutiques les contenant. |
| US5731299A (en) | 1992-05-29 | 1998-03-24 | The Procter & Gamble Company | Phosphonosulfonate compounds, pharmaceutical compositions, and methods for treating abnormal calcium and phosphate metabolism |
| JP2787407B2 (ja) | 1992-06-19 | 1998-08-20 | 株式会社大塚製薬工場 | ホスホン酸ジエステル誘導体 |
| US5728704A (en) | 1992-09-28 | 1998-03-17 | Pfizer Inc. | Substituted pyridmidines for control of diabetic complications |
| GB2271113A (en) | 1992-10-02 | 1994-04-06 | Japat Ltd | Triazolyl alkyl phosphates or phosphonates |
| DE4303648A1 (de) | 1993-02-09 | 1994-08-11 | Basf Ag | Verwendung von Aminovinylphosphonsäureestern als Lichtschutzmittel und Stabilisatoren für organisches Material |
| JPH06298779A (ja) | 1993-04-15 | 1994-10-25 | Hoechst Japan Ltd | ヘテロ環イミノビスメチレンビスホスホン酸誘導体 |
| ATE199906T1 (de) | 1993-06-29 | 2001-04-15 | Mitsubishi Chem Corp | Phosphonat-nukleotid ester-derivate |
| IT1266570B1 (it) | 1993-07-30 | 1997-01-09 | Zambon Spa | Derivati della propanammide n-eteroaril sostituiti utili nel trattamento delle malattie cardiovascolari |
| EP0719273B1 (en) | 1993-09-17 | 2010-11-03 | Gilead Sciences, Inc. | Nucleotide analogs |
| US5728650A (en) | 1993-10-07 | 1998-03-17 | Zeneca Limited | Herbicidal aza bisphosphonic acids and compositions containing the same |
| GB9324143D0 (en) | 1993-11-24 | 1994-01-12 | Schering Agrochemicals Ltd | Triazole phosphonate pesticides |
| DE19501843A1 (de) | 1994-12-16 | 1996-06-20 | Bayer Ag | Substituierte Sulfonylharnstoffe |
| DE69624143T2 (de) | 1995-12-27 | 2003-06-12 | Otsuka Pharmaceutical Factory, Inc. | Phosphonsaurediester-derivate |
| AR008789A1 (es) | 1996-07-31 | 2000-02-23 | Bayer Corp | Piridinas y bifenilos substituidos |
| US6011049A (en) | 1997-02-19 | 2000-01-04 | Warner-Lambert Company | Combinations for diabetes |
| DE69819311T2 (de) | 1997-03-07 | 2004-07-29 | Metabasis Therapeutics Inc., San Diego | Neue benzimidazol inhibitoren der fructose-1,6-bisphosphatase |
| US6054587A (en) | 1997-03-07 | 2000-04-25 | Metabasis Therapeutics, Inc. | Indole and azaindole inhibitors of fructose-1,6-bisphosphatase |
| US6284748B1 (en) | 1997-03-07 | 2001-09-04 | Metabasis Therapeutics, Inc. | Purine inhibitors of fructose 1,6-bisphosphatase |
| US6312662B1 (en) | 1998-03-06 | 2001-11-06 | Metabasis Therapeutics, Inc. | Prodrugs phosphorus-containing compounds |
| CA2322487C (en) | 1998-03-06 | 2010-07-20 | Metabasis Therapeutics, Inc. | Novel prodrugs for phosphorus-containing compounds |
| WO1999047549A1 (en) | 1998-03-16 | 1999-09-23 | Ontogen Corporation | PIPERAZINES AS INHIBITORS OF FRUCTOSE-1,6-BISPHOSPHATASE (FBPase) |
| KR100818845B1 (ko) | 1998-09-09 | 2008-04-01 | 메타베이시스 테라퓨틱스, 인크. | 신규한 프럭토스 1,6-비스포스파타제의 헤테로방향족 억제제 |
| PL352756A1 (en) | 1998-12-24 | 2003-09-08 | Metabasis Therapeutics, Inc. | A combination of fbpase inhibitors and insulin sensitizers for the treatment of diabetes |
| US6756360B1 (en) | 1998-12-24 | 2004-06-29 | Metabasis Therapeutics, Inc. | Combination of FBPase inhibitors and insulin sensitizers for the treatment of diabetes |
| US6284672B1 (en) | 1999-03-02 | 2001-09-04 | Advanced Micro Devices, Inc. | Method of forming a super-shallow amorphous layer in silicon |
| AU784370B2 (en) | 1999-12-22 | 2006-03-23 | Metabasis Therapeutics, Inc. | Novel bisamidate phosphonate prodrugs |
| EP1743655B1 (en) | 2000-01-21 | 2014-06-25 | Novartis AG | Combinations comprising dipeptidylpeptidase-iv inhibitors and antidiabetic agents |
| JP2003525944A (ja) | 2000-03-08 | 2003-09-02 | メタバシス・セラピューティクス・インコーポレイテッド | 新規アリールフルクトース−1,6−ビスホスファターゼ阻害剤 |
| US7563774B2 (en) | 2000-06-29 | 2009-07-21 | Metabasis Therapeutics, Inc. | Combination of FBPase inhibitors and antidiabetic agents useful for the treatment of diabetes |
| EP1372660A2 (en) | 2000-07-06 | 2004-01-02 | Metabasis Therapeutics, Inc. | A combination of fbpase inhibitors and antidiabetic agents useful for the treatment of diabetes |
| JP2008510018A (ja) | 2004-08-18 | 2008-04-03 | メタバシス・セラピューティクス・インコーポレイテッド | フルクトース−1,6−ビスホスファターゼの新規チアゾール阻害物質 |
-
1999
- 1999-09-03 KR KR1020017003079A patent/KR100818845B1/ko not_active Expired - Lifetime
- 1999-09-03 AU AU10905/00A patent/AU761267C/en not_active Ceased
- 1999-09-03 NZ NZ510308A patent/NZ510308A/xx not_active IP Right Cessation
- 1999-09-03 PT PT99954595T patent/PT1112275E/pt unknown
- 1999-09-03 HU HU0103143A patent/HUP0103143A3/hu unknown
- 1999-09-03 SK SK316-2001A patent/SK286080B6/sk not_active IP Right Cessation
- 1999-09-03 CZ CZ20010840A patent/CZ297264B6/cs not_active IP Right Cessation
- 1999-09-03 ES ES99954595T patent/ES2204170T3/es not_active Expired - Lifetime
- 1999-09-03 DE DE69910045T patent/DE69910045T2/de not_active Expired - Lifetime
- 1999-09-03 BR BR9913532-9A patent/BR9913532A/pt not_active Application Discontinuation
- 1999-09-03 CA CA002343027A patent/CA2343027A1/en not_active Abandoned
- 1999-09-03 AT AT99954595T patent/ATE246197T1/de active
- 1999-09-03 EP EP99954595A patent/EP1112275B9/en not_active Expired - Lifetime
- 1999-09-03 JP JP2000568853A patent/JP2002524463A/ja active Pending
- 1999-09-03 US US09/389,698 patent/US6489476B1/en not_active Expired - Lifetime
- 1999-09-03 CN CNB998130362A patent/CN1215076C/zh not_active Expired - Fee Related
- 1999-09-03 DK DK99954595T patent/DK1112275T3/da active
- 1999-09-03 PL PL346520A patent/PL205184B1/pl not_active IP Right Cessation
- 1999-09-03 HK HK02104187.3A patent/HK1042496B/zh not_active IP Right Cessation
- 1999-09-03 WO PCT/US1999/020346 patent/WO2000014095A1/en not_active Ceased
- 1999-09-03 KR KR1020077006087A patent/KR20070053264A/ko not_active Ceased
-
2001
- 2001-03-07 NO NO20011174A patent/NO20011174L/no not_active Application Discontinuation
-
2003
- 2003-08-06 US US10/636,474 patent/US7312219B2/en not_active Expired - Fee Related
-
2007
- 2007-04-30 US US11/742,023 patent/US20070232571A1/en not_active Abandoned
- 2007-08-20 US US11/842,035 patent/US20080015195A1/en not_active Abandoned
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