TWI853704B - Lpa受體拮抗劑及其用途 - Google Patents

Lpa受體拮抗劑及其用途 Download PDF

Info

Publication number
TWI853704B
TWI853704B TW112134344A TW112134344A TWI853704B TW I853704 B TWI853704 B TW I853704B TW 112134344 A TW112134344 A TW 112134344A TW 112134344 A TW112134344 A TW 112134344A TW I853704 B TWI853704 B TW I853704B
Authority
TW
Taiwan
Prior art keywords
methyl
mmol
inhibitors
compound
pharmaceutically acceptable
Prior art date
Application number
TW112134344A
Other languages
English (en)
Chinese (zh)
Other versions
TW202400561A (zh
Inventor
布萊恩 Ｐ 貝斯維特
約書亞 Ａ 凱佩蘭
梅根 Ｅ 紐比格
堅城 楊
安娜 扎古爾斯卡
Original Assignee
美商基利科學股份有限公司
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 美商基利科學股份有限公司 filed Critical 美商基利科學股份有限公司
Publication of TW202400561A publication Critical patent/TW202400561A/zh
Application granted granted Critical
Publication of TWI853704B publication Critical patent/TWI853704B/zh

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • A61K31/232—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/26—Glucagons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D231/14—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 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
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Zoology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
TW112134344A 2021-05-11 2022-05-10 Lpa受體拮抗劑及其用途 TWI853704B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202163186890P 2021-05-11 2021-05-11
US63/186,890 2021-05-11

Publications (2)

Publication Number Publication Date
TW202400561A TW202400561A (zh) 2024-01-01
TWI853704B true TWI853704B (zh) 2024-08-21

Family

ID=81927511

Family Applications (2)

Application Number Title Priority Date Filing Date
TW112134344A TWI853704B (zh) 2021-05-11 2022-05-10 Lpa受體拮抗劑及其用途
TW111117400A TWI818538B (zh) 2021-05-11 2022-05-10 Ｌｐａ受體拮抗劑及其用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW111117400A TWI818538B (zh) 2021-05-11 2022-05-10 Ｌｐａ受體拮抗劑及其用途

Country Status (9)

Country Link
US (1) US11980609B2 (https=)
EP (1) EP4337641A1 (https=)
JP (1) JP7701473B2 (https=)
KR (1) KR20240005892A (https=)
CN (1) CN117295717A (https=)
AU (1) AU2022273631B2 (https=)
CA (1) CA3218917A1 (https=)
TW (2) TWI853704B (https=)
WO (1) WO2022240879A1 (https=)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4058144A1 (en) 2019-11-15 2022-09-21 Gilead Sciences, Inc. Triazole carbamate pyridyl sulfonamides as lpa receptor antagonists and uses thereof
TWI843503B (zh) 2020-06-03 2024-05-21 美商基利科學股份有限公司 Lpa受體拮抗劑及其用途
EP4161936A1 (en) 2020-06-03 2023-04-12 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
KR20240007233A (ko) 2021-05-13 2024-01-16 길리애드 사이언시즈, 인코포레이티드 Lpa 수용체 길항제 및 이의 용도
WO2023107938A1 (en) 2021-12-08 2023-06-15 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
WO2024157207A1 (en) * 2023-01-25 2024-08-02 Gpcr Therapeutics, Inc. Gpcr inhibitors and uses thereof
EP4731212A1 (en) * 2023-06-20 2026-04-29 Sagimet Biosciences Inc. Combination therapies of fasn inhibitors with thyroid hormone receptor agonists
AU2024317450A1 (en) * 2023-07-28 2026-02-19 Wuhan Createrna Science And Technology Co., Ltd. Compound as lpar1 antagonist, pharmaceutical composition thereof and use thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012138648A1 (en) * 2011-04-06 2012-10-11 Irm Llc Compositions and methods for modulating lpa receptors
WO2014113485A1 (en) * 2013-01-15 2014-07-24 Intermune, Inc. Lysophosphatidic acid receptor antagonists
WO2020060915A1 (en) * 2018-09-18 2020-03-26 Bristol-Myers Squibb Company Cyclopentyl acids as lpa antagonists

Family Cites Families (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AP2002002460A0 (en) 2001-03-09 2002-06-30 Pfizer Prod Inc Novel benzimidazole anti-inflammatory compounds.
JP4692281B2 (ja) 2003-08-05 2011-06-01 味の素株式会社 新規アゾール化合物
US7803553B2 (en) 2003-09-04 2010-09-28 Riken Methods of use of antibodies which recognize a protease cleavage site of an LAP fragment of TGF-β
US20070276050A1 (en) 2006-02-27 2007-11-29 Gilead Sciences, Inc. Methods for identifying ASK1 inhibitors useful for preventing and/or treating cardiovascular diseases
PT2303270T (pt) 2008-05-05 2017-08-25 Sanofi Sa Derivados fundidos do ácido ciclopentanocarboxílico substituídos por acilamino e sua utilização como produtos farmacêuticos
US8455499B2 (en) 2008-12-11 2013-06-04 Amira Pharmaceuticals, Inc. Alkyne antagonists of lysophosphatidic acid receptors
GB2466121B (en) 2008-12-15 2010-12-08 Amira Pharmaceuticals Inc Antagonists of lysophosphatidic acid receptors
GB2470833B (en) 2009-06-03 2011-06-01 Amira Pharmaceuticals Inc Polycyclic antagonists of lysophosphatidic acid receptors
TWI598347B (zh) 2009-07-13 2017-09-11 基利科學股份有限公司 調節細胞凋亡信號之激酶的抑制劑
CN102574822A (zh) 2009-08-04 2012-07-11 阿米拉制药公司 作为溶血磷脂酸受体拮抗剂的化合物
KR101678255B1 (ko) 2009-09-25 2016-11-21 아스텔라스세이야쿠 가부시키가이샤 치환 아미드 화합물
GB2474748B (en) 2009-10-01 2011-10-12 Amira Pharmaceuticals Inc Polycyclic compounds as lysophosphatidic acid receptor antagonists
GB2474120B (en) 2009-10-01 2011-12-21 Amira Pharmaceuticals Inc Compounds as Lysophosphatidic acid receptor antagonists
AR079022A1 (es) 2009-11-02 2011-12-21 Sanofi Aventis Derivados de acido carboxilico ciclico sustituidos con acilamino, su uso como productos farmaceuticos, composicion farmaceutica y metodo de preparacion
WO2011159550A2 (en) 2010-06-14 2011-12-22 Amidra Pharmaceuticals, Inc. Lysophosphatidic acid receptor antagonist and uses thereof
WO2011159632A1 (en) 2010-06-15 2011-12-22 Amira Pharmaceuticals, Inc. Lysophosphatidic acid receptor antagonists for the treatment of conditions or diseases of the eye
PH12012500542A1 (en) 2010-09-24 2012-11-12 Astellas Pharma Inc Substituted amide compound
KR20130126659A (ko) 2010-12-07 2013-11-20 아미라 파마슈티칼스 인코포레이티드 리소포스파티드산 수용체 길항제 및 섬유증 치료에서의 그의 용도
DK2648726T3 (da) 2010-12-07 2018-07-16 Amira Pharmaceuticals Inc Polycyklisk lpa1-antagonist og anvendelser deraf
US8785442B2 (en) 2011-01-30 2014-07-22 Curegenix, Inc. Compound as antagonist of lysophosphatidic acid receptor, composition, and use thereof
WO2012138797A1 (en) 2011-04-05 2012-10-11 Amira Pharmaceuticals, Inc. 3- or 5 - bi phenyl - 4 - ylisoxazole - based compounds useful for the treatment of fibrosis, pain, cancer and respiratory, allergic, nervous system or cardiovascular disorders
JP2014525932A (ja) 2011-08-15 2014-10-02 インターミューン， インコーポレイテッド リゾホスファチド酸レセプターアンタゴニスト
RS57157B1 (sr) 2011-11-11 2018-07-31 Gilead Apollo Llc Acc inhibitori i njihove primene
US20140329871A1 (en) 2011-12-04 2014-11-06 Angion Biomedica Corp. Small molecule anti-fibrotic compounds and uses thereof
UY34573A (es) 2012-01-27 2013-06-28 Gilead Sciences Inc Inhibidor de la quinasa que regula la señal de la apoptosis
US9518112B2 (en) 2012-03-08 2016-12-13 Ludwig Institute For Cancer Research Ltd TGF-β1 specific antibodies and methods and uses thereof
SG11201407229UA (en) 2012-06-20 2014-12-30 Hoffmann La Roche Substituted pyrazole compounds as lpar antagonists
IN2014DN09352A (https=) 2012-06-20 2015-07-17 Hoffmann La Roche
JP2015520202A (ja) 2012-06-20 2015-07-16 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｌｐａｒ拮抗薬としてのｎ−アルキルトリアゾール化合物
WO2014037303A1 (en) 2012-09-05 2014-03-13 F. Hoffmann-La Roche Ag Lpar - substituted cyanopyrazole compounds
WO2014072486A1 (en) 2012-11-09 2014-05-15 INSERM (Institut National de la Santé et de la Recherche Médicale) New benzene sulfonamide thiazole compounds
KR102189166B1 (ko) 2012-12-28 2020-12-09 우베 고산 가부시키가이샤 할로겐 치환 헤테로환 화합물
WO2014145873A2 (en) 2013-03-15 2014-09-18 Epigen Biosciences, Inc. Heterocyclic compounds useful in the treatment of disease
EP2994139B1 (en) 2013-05-10 2019-04-10 Gilead Apollo, LLC Acc inhibitors and uses thereof
ES2860952T3 (es) 2013-08-01 2021-10-05 Univ Catholique Louvain Proteína anti-garp y usos de la misma
GB201314926D0 (en) 2013-08-20 2013-10-02 Takeda Pharmaceutical Novel Compounds
US9987381B2 (en) 2013-10-31 2018-06-05 Bristol-Myers Squibb Company Radioligands for imaging the LPA-1 receptor
RU2689315C2 (ru) 2014-06-27 2019-05-27 Убе Индастриз, Лтд. Соль гетероциклического соединения, замещенного галогеном
WO2016115345A1 (en) 2015-01-14 2016-07-21 The Brigham And Women's Hospital, Treatment of cancer with anti-lap monoclonal antibodies
EP3378491A4 (en) 2015-11-20 2019-07-17 UBE Industries, Ltd. PHARMACEUTICAL COMPOSITION FOR THE TREATMENT AND / OR PREVENTION OF NASH
SG11201807077RA (en) 2016-03-02 2018-09-27 Gilead Apollo Llc Solid forms of a thienopyrimidinedione acc inhibitor and methods for production thereof
AR108185A1 (es) 2016-04-06 2018-07-25 Abbvie Inc Amidas terciarias y método para su uso
AR108838A1 (es) 2016-06-21 2018-10-03 Bristol Myers Squibb Co Ácidos de carbamoiloximetil triazol ciclohexilo como antagonistas de lpa
BR112019013908A2 (pt) 2017-01-06 2020-02-04 Scholar Rock, Inc. inibidores de tgfss1 isoforma-específicos, contexto-permissivos, e seus usos
WO2019041340A1 (en) 2017-09-04 2019-03-07 Eli Lilly And Company LYSOPHOSPHATIDE ACID RECEPTOR 1 RECEPTOR INHIBITORS (LPAR1)
WO2019113123A1 (en) 2017-12-04 2019-06-13 Precithera, Inc. TGF-ß RECEPTOR FUSION PROTEINS AND OTHER TGF-ß ANTAGONISTS FOR REDUCING TGF-ß SIGNALING
EP3720881A1 (en) 2017-12-08 2020-10-14 Elstar Therapeutics, Inc. Multispecific molecules and uses thereof
ES2898364T3 (es) 2017-12-19 2022-03-07 Bristol Myers Squibb Co Acidos carbamoilciclohexílicos ligados a N triazol como antagonistas de LPA
JP7212047B2 (ja) 2017-12-19 2023-01-24 ブリストル－マイヤーズ スクイブ カンパニー Ｌｐａアンタゴニストとしてのシクロヘキシル酸ピラゾールアゾール
CN112041302B (zh) 2017-12-19 2024-11-19 百时美施贵宝公司 作为lpa拮抗剂的吡唑o-连接的氨基甲酰基环己基酸
EP3728216B1 (en) * 2017-12-19 2023-09-06 Bristol-Myers Squibb Company Pyrazole n-linked carbamoyl cyclohexyl acids as lpa antagonists
EP3728209B1 (en) 2017-12-19 2025-12-24 Bristol-Myers Squibb Company Cyclohexyl acid isoxazole azines as lpa antagonists
WO2019126084A1 (en) 2017-12-19 2019-06-27 Bristol-Myers Squibb Company Isoxazole o-linked carbamoyl cyclohexyl acids as lpa antagonists
CN111712492B (zh) 2017-12-19 2024-05-31 百时美施贵宝公司 作为lpa拮抗剂的环己基酸三唑唑类
JP7299892B2 (ja) 2017-12-19 2023-06-28 ブリストル－マイヤーズ スクイブ カンパニー Ｌｐａアンタゴニストとしてのシクロヘキシル酸ピラゾールアジン
JP7208240B2 (ja) 2017-12-19 2023-01-18 ブリストル－マイヤーズ スクイブ カンパニー Ｌｐａアンタゴニストとしてのシクロヘキシル酸トリアゾールアジン
US11447475B2 (en) 2017-12-19 2022-09-20 Bristol-Myers Squibb Company Isoxazole N-linked carbamoyl cyclohexyl acids as LPA antagonists
US11261180B2 (en) 2017-12-19 2022-03-01 Bristol-Myers Squibb Company Cyclohexyl acid isoxazole azoles as LPA antagonists
EP3853232B1 (en) 2018-09-18 2023-03-01 Bristol-Myers Squibb Company Oxabicyclo acids as lpa antagonists
ES2948793T3 (es) 2018-09-18 2023-09-19 Bristol Myers Squibb Co Acidos cicloheptílicos como antagonistas de LPA
US20210379210A1 (en) 2018-10-15 2021-12-09 Bristol-Myers Squibb Company Radioligands for imaging the lpa1 receptor
CN114599640A (zh) 2019-06-18 2022-06-07 百时美施贵宝公司 作为lpa拮抗剂的异噁唑羧酸
WO2020257135A1 (en) 2019-06-18 2020-12-24 Bristol-Myers Squibb Company Triazole carboxylic acids as lpa antagonists
EP3986553B1 (en) 2019-06-18 2026-03-25 Bristol-Myers Squibb Company Cyclobutyl carboxylic acids as lpa antagonists
PH12022550225A1 (en) 2019-07-30 2022-12-19 Taisho Pharmaceutical Co Ltd Urea compound for antagonizing lpa1 receptor
EP4058144A1 (en) 2019-11-15 2022-09-21 Gilead Sciences, Inc. Triazole carbamate pyridyl sulfonamides as lpa receptor antagonists and uses thereof
JP7665619B2 (ja) 2019-12-04 2025-04-21 イドルシア・ファーマシューティカルズ・リミテッド 線維性疾患の治療に使用するためのアゼチジンｌｐａ１受容体アンタゴニストのピルフェニドン及び／又はニンテダニブとの合剤
EP4161936A1 (en) 2020-06-03 2023-04-12 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
TWI843503B (zh) 2020-06-03 2024-05-21 美商基利科學股份有限公司 Lpa受體拮抗劑及其用途
CA3185111A1 (en) * 2020-07-16 2022-01-20 Elisabetta Armani Amido cyclohexane acid derivatives as lpa receptor inhibitors
WO2022034568A1 (en) 2020-08-11 2022-02-17 Viva Star Biosciences Limited Triazole-pyridinyl substituted azacyclohexyl acetic acid compounds as lpa receptor antagonists
CN114456157A (zh) 2020-11-10 2022-05-10 武汉人福创新药物研发中心有限公司 氮取代氨基碳酸酯噻吩类化合物及其用途
CN114456147B (zh) 2020-11-10 2025-07-15 武汉人福创新药物研发中心有限公司 氧取代氨基碳酸酯噻吩类化合物
CN114456159A (zh) 2020-11-10 2022-05-10 武汉人福创新药物研发中心有限公司 氮取代杂环噻吩类化合物及其用途
WO2022174882A1 (en) 2021-02-16 2022-08-25 Chiesi Farmaceutici S.P.A. 5-membered heterocyclyl carbamate derivatives as dual lpa receptor 1 and lpa receptor 2 inhibitors
WO2022174883A1 (en) 2021-02-16 2022-08-25 Chiesi Farmaceutici S.P.A. 5-membered heterocyclyl derivatives as dual lpa receptor 1 and lpa receptor 2 inhibitors
KR20240007233A (ko) 2021-05-13 2024-01-16 길리애드 사이언시즈, 인코포레이티드 Lpa 수용체 길항제 및 이의 용도
WO2023107938A1 (en) 2021-12-08 2023-06-15 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012138648A1 (en) * 2011-04-06 2012-10-11 Irm Llc Compositions and methods for modulating lpa receptors
WO2014113485A1 (en) * 2013-01-15 2014-07-24 Intermune, Inc. Lysophosphatidic acid receptor antagonists
WO2020060915A1 (en) * 2018-09-18 2020-03-26 Bristol-Myers Squibb Company Cyclopentyl acids as lpa antagonists

Also Published As

Publication number Publication date
WO2022240879A1 (en) 2022-11-17
JP7701473B2 (ja) 2025-07-01
US11980609B2 (en) 2024-05-14
AU2022273631A1 (en) 2023-11-02
TW202302537A (zh) 2023-01-16
CN117295717A (zh) 2023-12-26
JP2024517016A (ja) 2024-04-18
TWI818538B (zh) 2023-10-11
EP4337641A1 (en) 2024-03-20
US20220411405A1 (en) 2022-12-29
TW202400561A (zh) 2024-01-01
CA3218917A1 (en) 2022-11-17
AU2022273631B2 (en) 2025-04-17
KR20240005892A (ko) 2024-01-12

Similar Documents

Publication Publication Date Title
TWI853704B (zh) Lpa受體拮抗劑及其用途
KR102866916B1 (ko) Lpa 수용체 길항제 및 이의 용도
TWI767410B (zh) 作為lpa受體拮抗劑之三唑胺基甲酸酯吡啶基磺醯胺及其用途
JP7691522B2 (ja) Ｌｐａ受容体アンタゴニスト及びそれらの使用
AU2022405082B2 (en) Lpa receptor antagonists and uses thereof
HK40105573A (zh) Lpa受体拮抗剂及其用途
HK40105333A (zh) Lpa受体拮抗剂及其用途