Patent(s) and the Corresponding Patented Drug(s) |
Top |
World Intellectual Property Organization (WIPO) |
Patent ID |
WO2014183555 |
Title |
Cycloalkyl Acid Derivative, Preparation Method Thereof, and Pharmaceutical Application Thereof. |
Abstract |
The present invention relates to a cycloalkyl acid derivative, a preparation method thereof, and a pharmaceutical application thereof, and in particular, the present invention relates to a cycloalkyl. |
Applicant(s) |
Shanghai Hengrui Pharmaceutical Co., Ltd |
Representative Drug(s) |
D03UNB |
Drug Info
|
IC50 = 33.7 nM |
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[1] |
2
|
D02USA
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
WO2012048058 |
Title |
Developing Potent Urate Transporter Inhibitors: Compounds Designed for Their Uricosuric Action. |
Abstract |
A compound represented by the general Formula (I): a pharmaceutically acceptable salt or ester thereof, a solvate thereof, a chelate thereof, a non-covalent complex thereof, a pro-drug thereof, a deuterated radio-labeled analog thereof, and mixtures of any of the foregoing, wherein: A - K are individually selected from carbon or nitrogen; X = -O, -NR1,or -S; R1-11 are individually selected from the group consisting of-H, C1-C6 alkyl, C6-C aryl, substituted C6-C14 aryl, C1-C14-alkoxy, halogen, hydroxyl, carboxy, cyano, C1-C6-alkanoyloxy, C1-C6-alkylthio, C1-C6-alkylsulfonyl, trifluoromethyl, hydroxy, C2-C6-alkoxycarbonyl, C2-C6-alkanoylamino, -O-R12, S-R12,-SO2-Ri2, -NHSO2R12 and -NHCO2R12, wherein R12 is phenyl, naphthyl, or phenyl or naphthly substituted with one to three groups selected from C1-C6-alkyl, C6-C10 aryl,C1-C6-alkoxy and halogen, and C4-C20 hydroxyheteroaryl wherein the heteroatoms are selected from the group consisting of sulfur, nitrogen, and oxygen. |
Applicant(s) |
J-Pharma Co., Ltd |
Representative Drug(s) |
D06RFO |
Drug Info
|
IC50 < 50 nM |
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[1] |
2
|
D07FCV
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
WO2013027801 |
Title |
Fused Heterocyclic Derivative and Pharmaceutical Use Thereof. |
Abstract |
Provided is a compound that is useful as a prophylactic or therapeutic agent for diseases or the like caused by an abnormal serum uric acid level. The present invention relates to a fused heterocyclic derivative represented by formula (I), a prodrug thereof or a salt thereof, said fused heterocyclic derivative exhibiting xanthine oxidase inhibitory activity and useful as a prophylactic or therapeutic agent for diseases caused by an abnormal serum uric acid level. In formula (I), ring U represents a C6-10 aryl group or the like; each R1 independently represents a hydrogen atom, a hydroxyl group, a C1-6 alkyl group or the like; m represents an integer of 1-2; ring Q represents a five-membered heteroaryl group; n represents an integer of 1-3; and each R2 independently represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like. |
Applicant(s) |
Kissei Pharmaceutical Co., Ltd |
Representative Drug(s) |
D0D5YG |
Drug Info
|
N.A. |
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[1] |
2
|
D0ND8U
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
WO2014170793 |
Title |
Sulfonamides for The Treatment of Gout. |
Abstract |
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide URAT-1 inhibitors of formula (I): (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the description. URAT-1 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly gout. |
Applicant(s) |
Pfizer Limited |
Representative Drug(s) |
D02JOK |
Drug Info
|
IC50 = 58 nM |
[1] |
Patent ID |
WO2014170792 |
Title |
Sulfonamide Derivatives As Urat-1 Inhibitors. |
Abstract |
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide URAT-1 inhibitors of formula (I): or pharmaceutically acceptable salt thereofs, wherein R1, R2, R3, R4, R5 and R6 are as defined in the description. URAT-1 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly gout. |
Applicant(s) |
Pfizer Limited |
Representative Drug(s) |
D0HG2S |
Drug Info
|
IC50 = 13 nM |
[1] |
Patent ID |
WO2013057722 |
Title |
New Salt and Medical Use. |
Abstract |
The invention provides 4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2- fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide or a pharmaceutically acceptable salt thereof for the treatment of a disease associated with elevated blood uric acid levels, such as hyperuricemia or gout. In another aspect the invention provides the tosylate salt of 4-[2-(5-amino-1H-pyrazol-4- yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide. |
Applicant(s) |
Pfizer Limited |
Representative Drug(s) |
D06LEZ |
Drug Info
|
IC50 = 3540 nM |
[1] |
Patent ID |
WO2012125533 |
Title |
3-Benzyloxyphenyloxoacetic Acid Compounds for Reducing Uric Acid. |
Abstract |
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I) or its pharmaceutically acceptable salts. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum-induced inflammation. R1 is hydrogen or alkyl having from 1 to 3 carbon atoms. R2 is alkyl having from 1 to 3 carbon atoms, alkoxy having from 1 to 3 carbon atoms, hydroxy, nitro, halo, thio, alkylthio, or cyano. R3 and R4 are each independently hydrogen, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, perfluoromethoxy, halo, hydroxy, nitro, or amino. |
Applicant(s) |
SHARMA, Shalini et al |
Representative Drug(s) |
D0CK1D |
Drug Info
|
IC50 = 1000 nM |
[1] |
Patent ID |
WO2012033720 |
Title |
Benzoic Acid Compounds for Reducing Uric Acid. |
Abstract |
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I). The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium Jalciparum-induced inflammation. In Formula I, t, q, r, R6, R7, X and A are as defined herein. |
Applicant(s) |
SHARMA, Shalini et al |
Representative Drug(s) |
D0KD6U |
Drug Info
|
IC50 = 1000 nM |
[1] |
Patent ID |
WO2011159840 |
Title |
Phenylthioacetate Compounds, Compositions and Methods of Use. |
Abstract |
Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid. |
Applicant(s) |
Arcus Biosciences, Inc |
Representative Drug(s) |
D0JM7W |
Drug Info
|
IC50 = 1 to 10000 nM |
[1] |
Patent ID |
WO2011159839 |
Title |
Thioacetate Compounds, Compositions and Methods of Use. |
Abstract |
Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid. |
Applicant(s) |
Arcus Biosciences, Inc |
Representative Drug(s) |
D03QGH |
Drug Info
|
IC50 = 1 to 10000 nM |
[1] |
Patent ID |
WO2015174417 |
Title |
Pyrazine Derivative. |
Abstract |
The present invention relates to: a novel pyrazine derivative that is represented by formula (I) and is useful as a therapeutic agent or preventive agent for diseases involving URAT1, such as gout, hyperuricemia, hypertension, kidney diseases such as interstitial nephritis, diabetes, arteriosclerosis, or Lesch-Nyhan syndrome; or a pharmaceutically acceptable salt of said derivative; or a solvate of said derivative or salt. (The symbols in the formula are as defined in the description.). |
Applicant(s) |
Teijin Pharma Corporation |
Patent ID |
WO2015174411 |
Title |
Novel Crystalline Polymorph of Pyridine Derivative, and Method for Producing Same. |
Abstract |
Disclosed are: a 2-(5-chloropyridine-3-yl)-1-(2,5-dichlorobenzyl)-4-methyl-1H-imidazole-5-carboxylic acid crystal, which is useful as a therapeutic agent or prophylactic agent against gout, hyperuricemia, and the like; and a method for producing the same. |
Applicant(s) |
Teijin Pharma Corporation |
Patent ID |
WO2014077285 |
Title |
Pyridine Derivative. |
Abstract |
Provided is a pyridine derivative represented by formula (I), a prodrug thereof, a pharmaceutically acceptable salt of the pyridine derivative or the prodrug, or a solvate of the pyridine derivative, the prodrug or the pharmaceutically acceptable salt, which is useful for treatment or prophylaxis of diseases associated with URAT1 such as gout, hyperuricemia, hypertension, kidney diseases such as interstitial nephritis, diabetes, arteriosclerosis and Lesch-Nyhan syndrome. |
Applicant(s) |
Teijin Pharma Corporation |
Patent ID |
WO2014017643 |
Title |
Difluoromethylene Compound. |
Abstract |
The present invention relates to: a compound which has URAT1 inhibitory activity; and a URAT1 inhibitor, a blood uric acid level reducing agent and a pharmaceutical composition, each of which contains. |
Applicant(s) |
Sato Pharmaceutical Co., Ltd |
Patent ID |
WO2012102405 |
Title |
Ring-Fused Compound. |
Abstract |
The present invention relates to: a compound having a URAT1 inhibitory activity; and an URAT1 inhibitor, a blood uric acid level reducing agent and a pharmaceutical composition, each of which comprises the compound. More specifically, the present invention relates to a compound represented by formula (I). [In the formula, R1 represents -Q1-A1 or the like; AA represents a double bond or a single bond; W1 represents a nitrogen atom or a group represented by general formula: =C(Ra)- and W2 represents a nitrogen atom or a group represented by general formula: =C(Rb)- when AA represents a double bond; W1 represents a group represented by general formula: -C(Raa)(Rab)- or a group represented by general formula: -(C=O)- and W2 represents a group represented by general formula: -C(Rba)(Rbb)-, a group represented by general formula: -(C=O)- or a group represented by general formula: -N(Rbc)- when AA represents a single bond; W3, W4 and W5 independently represent a nitrogen atom, a methine group which may have a substituentor the like; X represents a single bond, an oxygen atom or the like; Y represents a single bond or (CRYiRYi')n; and Z represents a hydroxy group, COOR2 or the like.]. |
Applicant(s) |
Sato Pharmaceutical Co., Ltd |
Representative Drug(s) |
D07IZC |
Drug Info
|
N.A. |
[1] |
Patent ID |
WO2015095703 |
Title |
Novel Salts and Co-Crystals of Lesinurad. |
Abstract |
Novel salts and cocrystals of lesinurad, processes for their preparation, pharmaceutical compositions comprising these new salt forms and co-crystals, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transport 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties. |
Applicant(s) |
Crystal Pharmatech, Inc |
Patent ID |
WO2015075561 |
Title |
Crystalline forms of Lesinurad and Its Sodium Salt. |
Abstract |
Novel crystalline forms of lesinurad and its sodium salt, processes for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transporter 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties. |
Applicant(s) |
Crystal Pharmatech Co., Ltd |
Patent ID |
WO2013018706 |
Title |
Composition for Regulating Urat1 Activity. |
Abstract |
The present invention provides a composition for regulating a URAT1 activity, characterized by containing taurine, which is a substance that is safe even when ingested on daily basis, as an active ingredient. |
Applicant(s) |
Taisho Pharmaceutical Co., Ltd |
Patent ID |
WO2012092395 |
Title |
Polymorphic forms of 2-(5-Bromo-4-(4-Cyclopropylnaphthalen-1-Yl)-4H-1,2,4-Triazol-3-Ylthio) Acetic Acid and Uses Thereof. |
Abstract |
Crystalline polymorph forms of 2-(5-bromo-4-(4-cyclopropyl naphthalen-l-yl)-4H-l,2,4-triazol- 3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented. |
Applicant(s) |
Arcus Biosciences, Inc |
Patent ID |
WO2011085009 |
Title |
Polymorphic, Crystalline and Mesophase forms of Sodium 2-(5-Bromo-4-(4-Cyclopropylnaphthalen-1-Yl)-4H-1,2,4-Triazol-3-Ylthio)Acetate, and Uses Thereof. |
Abstract |
Crystalline polymorphs and solid mesophase forms of sodium 2-(5-bromo-4- (4-cyclopropylnaphthalen-l-yl)-4H-l,2,4-triazol-3-ylthio)acetate are described. In addition, pharmaceutical compositions and uses of such compositions for the treatment of a variety of diseases and conditions are provided. |
Applicant(s) |
Arcus Biosciences, Inc |
United States Patent and Trademark Office (USPTO) |
Patent ID |
US8236488 |
Title |
Method of Screening for Therapeutic Compounds for Vascular Disorders and Hypertension Based On Urat1 Activity Modulation. |
Applicant(s) |
Human Cell Systems, Inc |
Japan Patent Office (JPO) |
Patent ID |
JP2015214527 |
Title |
Preparation of Imidazole Derivatives As Urate Transporter 1 (Urat1) Inhibitors. |
Applicant(s) |
Teijin Pharma Co., Ltd |
Patent ID |
JP2015214523 |
Title |
Preparation of Pyrazine-Substituted Imidazoles As Urate Transporter 1 (Urat1) Inhibitors. |
Applicant(s) |
Teijin Pharma Co., Ltd |
China National Intellectual Property Administration (CNIPA) |
Patent ID |
CN104370843 |
Title |
Halotriazolesulfinylmalonic Acid Compounds As Well As Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104370841 |
Title |
Triazolesulfinylmalonic Acid Compounds As Well As Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104341367 |
Title |
Tetrazoleacetic Acid Compound, As Well As Preparation Method and Applications Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0FX9D |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104341365 |
Title |
Halogenated Triazole Malonic Acid Compounds As Well As Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104341364 |
Title |
Triazole Malonic Acid Compounds As Well As Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104341363 |
Title |
Nitro-Substituted Triazolesulfonylmalonic Acid Compounds As Well As Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104341362 |
Title |
Triazolesulfonylmalonic Acid Compounds As Well As Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104341361 |
Title |
Cyano-Substituted Triazolesulfonylmalonic Acid Compounds As Well As Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104327000 |
Title |
Phenyl-Substituted Triazole Sulfinyl Malonate Type Compound, and Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104326999 |
Title |
Alkoxy-Substituted Triazole Sulfinyl Malonate Type Compound, and Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104326998 |
Title |
Phenyl-Substituted Triazole Malonate Type Compound, and Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104326997 |
Title |
Alkoxy-Substituted Triazole Malonate Type Compound, and Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104326996 |
Title |
Nitro-Substituted Triazole Malonate Type Compound, and Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104326995 |
Title |
Nitrile-Substituted Triazole Malonate Type Compound, and Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104326994 |
Title |
Nitrile-Substituted Triazole Sulfonyl Malonate Type Compound, and Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104326993 |
Title |
Nitro-Substituted Triazole Sulfinyl Malonate Type Compound, and Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0R5DH |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104292178 |
Title |
Compounds Containing Tetrazoleacetic Acids As Well As Preparation Method and Application of Compounds. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0FX9D |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104292177 |
Title |
Tetrazoleacetic Acid Compounds Containing Cyano and Halobenzene Substituent As Well As Preparation Method and Application of Tetrazoleacetic Acid Compounds. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0FX9D |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104292176 |
Title |
Tetrazoleacetic Acid Compounds Containing Halogenobenzene As Well As Preparation Method and Application of Tetrazoleacetic Acid Compounds. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0FX9D |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104292175 |
Title |
Nitro-Containing Tetrazoleacetic Acid Compounds As Well As Preparation Method and Application of Nitro-Containing Tetrazoleacetic Acid Compounds. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0FX9D |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104292124 |
Title |
Succinic Acid Amide Derivatives Containing Nitrophenyl-Substituted Naphthalene Rings As Well As Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D04ULX |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104292123 |
Title |
Succinic Acid Amide Derivatives Containing Phenylnaphthalene Rings As Well As Preparation Method and Application Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D04ULX |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104262277 |
Title |
Nitro Containing and Halogen Benzene Substituted 1H-Tetrazole-1-Acetic Acid Structure, and Preparation Method and Use Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0FX9D |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN104230833 |
Title |
H-Tetrazole-1-Acetic Acid Compound Containing Nitrile Grouping and Preparation Method and Purpose Thereof. |
Applicant(s) |
Yuanqiang Z |
Representative Drug(s) |
D0FX9D |
Drug Info
|
IC50 < 20 nM |
[1] |
Patent ID |
CN102718735 |
Title |
2-Ethyl-3-(4-Hydroxy) Benzoyl Benzofuran Compounds and Compositions and Preparation Methods of Compounds. |
Applicant(s) |
Santa (Zhangjiakou) Pharmaceutical Co., Ltd |
Representative Drug(s) |
D03PZX |
Drug Info
|
N.A. |
[1] |
Patent ID |
CN101181345 |
Title |
Application of Huaimi Flavonoids Extract In The Preparation of Medicament for Uric Acid Transporter Urat1 Inhibitor. |
Applicant(s) |
Nanjing University |
Patent ID |
CN100571692 |
Title |
Application of Curcumin In The Preparation of Medicament for Uric Acid Transportor Urat1 Inhibitor. |
Applicant(s) |
Nanjing University |