公开(公告)号：WO2016199104A1

公开(公告)日：2016-12-15

申请号：PCT/IB2016/053467

申请日：2016-06-13

Applicant: GLENMARK PHARMACEUTICALS S.A.

Inventor： MUTHUKAMAN, Nagarajan ,  GHARAT, Laxmikant Atmaram ,  KADAM, Suresh Mahadev ,  GAVHANE, Sachin ,  KHANDAGALE, Sandeep Bandu ,  NIRGUDE, Sunil Pandurang

IPC: C07D249/12

CPC classification number: C07D249/12 ,  A61P29/00 ,  G01N23/20075 ,  G01N2021/3595

Abstract: The present application relates to solid state forms of a triazolone compound which exhibit mPGES-1 enzyme inhibition activity, specifically N -(4-chloro-3-(5-oxo-1-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1 H -1,2,4-triazol-3-yl)benzyl) pivalamide (Compound of formula II), and process for preparation thereof.

Abstract translation: 本申请涉及具有mPGES-1酶抑制活性的具体的N-（4-氯-3-（5-氧代-1-（4-（三氟甲基）苯基）-4,5 - 二氢-1H-1,2,4-三唑-3-基）苄基）新戊酰胺（式II化合物）及其制备方法。

公开(公告)号：WO2016055947A1

公开(公告)日：2016-04-14

申请号：PCT/IB2015/057661

申请日：2015-10-07

Applicant: GLENMARK PHARMACEUTICALS S.A.

Inventor： GHARAT, Laxmikant Atmaram ,  MUTHUKAMAN, Nagarajan ,  PISAL, Dnyandeo ,  KHAIRATKAR-JOSHI, Neelima ,  SHAH, Daisy Manish ,  KADAM, Sheetal R

IPC: C07C15/54 ,  C07D231/02 ,  C07D259/00 ,  C07C63/00 ,  A61K31/395 ,  A61K31/135 ,  A61K31/192 ,  A61P11/00 ,  A61P11/08 ,  A61P11/04

CPC classification number: C07C65/28 ,  C07D211/34 ,  C07D213/55 ,  C07D213/65 ,  C07D213/68 ,  C07D213/81 ,  C07D213/84 ,  C07D213/87 ,  C07D231/12 ,  C07D233/58 ,  C07D241/18 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D277/24 ,  C07D277/30 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12

Abstract: Provided are compounds of formula (Ia) and pharmaceutically acceptable salts thereof, wherein A, B, R 1 , R 2 , m and n are as defined herein, which are active as inhibitors of S-Nitrosoglutathione reductase (GSNOR). These compounds prevent, inhibit, or suppress the action of GSNOR and are therefore useful in the treatment of GSNOR mediated diseases, disorders, syndromes or conditions such as, e.g., pulmonary hypertension, acute respiratory distress syndrome (ARDS), asthma, bronchospasm, cough, pneumonia, pulmonary fibrosis, interstitial lung diseases, cystic fibrosis and chronic obstructive pulmonary disease (COPD).

Abstract translation: 提供式（Ia）化合物及其药学上可接受的盐，其中A，B，R 1，R 2，m和n如本文所定义，其作为S-亚硝基谷胱甘肽还原酶（GSNOR）的抑制剂是有活性的。 这些化合物预防，抑制或抑制GSNOR的作用，因此可用于治疗GSNOR介导的疾病，病症，综合征或病症，例如肺动脉高压，急性呼吸窘迫综合征（ARDS），哮喘，支气管痉挛，咳嗽 ，肺炎，肺纤维化，间质性肺疾病，囊性纤维化和慢性阻塞性肺疾病（COPD）。

公开(公告)号：WO2013072825A1

公开(公告)日：2013-05-23

申请号：PCT/IB2012/056285

申请日：2012-11-09

Applicant: GLENMARK PHARMACEUTICALS S.A.

Inventor： GHARAT, Laxmikant Atmaram ,  BANERJEE, Abhisek ,  KHAIRATKAR-JOSHI, Neelima ,  KATTIGE, Vidya Ganapati

IPC: C07D237/32 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  A61K31/502 ,  A61P29/00

CPC classification number: C07D237/32 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

Abstract: The present patent application is directed to bicyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (m PGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

Abstract translation: 本专利申请涉及式（I）的双环化合物或其药学上可接受的盐作为mPGES-1抑制剂。 这些化合物是微粒体前列腺素E合酶-1（m PGES-1）酶的抑制剂，因此可用于治疗各种疾病或病症如哮喘，骨关节炎，类风湿性关节炎，急性发作的疼痛和/或炎症 或慢性疼痛和神经退行性疾病。

公开(公告)号：WO2018203298A1

公开(公告)日：2018-11-08

申请号：PCT/IB2018/053121

申请日：2018-05-04

Applicant: GLENMARK PHARMACEUTICALS S.A.

Inventor： KUMAR, Sukeerthi ,  CHAUDHARI, Sachin Sundarlal ,  GHARAT, Laxmikant Atmaram ,  KHAIRATKAR-JOSHI, Neelima ,  SHAH, Daisy Manish ,  MUKHOPADHYAY, Indranil

IPC: C07D471/04 ,  C07D491/052 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  A61P11/00 ,  A61P35/00 ,  A61K31/437 ,  A61K31/5377 ,  A61K31/444 ,  A61K31/496 ,  A61K31/4545

Abstract: The present application relates to substituted fused heteroaryl and heterocyclic compounds, useful as nicotinamide adenine dinucleotide phosphate oxidase inhibitors (NADPH oxidase inhibitors), processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment or prevention of various diseases, conditions and/or disorders mediated by NADPH oxidase. (Formula I)

公开(公告)号：WO2017051319A1

公开(公告)日：2017-03-30

申请号：PCT/IB2016/055620

申请日：2016-09-21

Applicant: GLENMARK PHARMACEUTICALS S.A.

Inventor： CHAUDHARI, Sachin Sundarlal ,  DAS, Sanjib ,  GHARAT, Laxmikant Atmaram ,  DHONE, Sachin Vasantrao ,  THOMAS, Abraham ,  KHAIRATKAR-JOSHI, Neelima ,  SHAH, Daisy Manish ,  BAJPAI, Malini

IPC: C07D309/10 ,  C07D213/61 ,  C07D235/12 ,  C07D401/12 ,  A61K31/4184

CPC classification number: C07D213/61 ,  C07D213/64 ,  C07D235/12 ,  C07D309/10 ,  C07D401/04 ,  C07D405/04

Abstract: Provided are compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring B, L, R 1 , R 2 , R a , R b , n, x, y and z are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORyt).

Abstract translation: 本发明提供了式（I）化合物及其药学上可接受的盐，其中环A，环B，L，R 1，R 2，R a，R b，n，x，y和z如本文所定义， 作为类视黄醇相关孤儿受体γt（RORyt）的调节剂。

公开(公告)号：WO2017021879A1

公开(公告)日：2017-02-09

申请号：PCT/IB2016/054639

申请日：2016-08-02

Applicant: GLENMARK PHARMACEUTICALS S.A.

Inventor： DAS, Sanjib ,  GHARAT, Laxmikant Atmaram ,  HARDE, Rajendra Laxman ,  SHELKE, Sandeep Yadunath ,  PARDESHI, Shailesh Ramesh ,  THOMAS, Abraham ,  KHAIRATKAR-JOSHI, Neelima ,  SHAH, Daisy Manish ,  BAJPAI, Malini

IPC: C07D231/12 ,  C07D401/04 ,  C07D403/04 ,  C07D239/26 ,  C07D239/36 ,  C07D239/42 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D213/40 ,  A61K31/506 ,  A61P37/00

CPC classification number: C07D417/12 ,  C07D213/40 ,  C07D231/12 ,  C07D239/26 ,  C07D239/36 ,  C07D239/42 ,  C07D241/12 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12

Abstract: The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring B, L, R 1 , R 2 , R 3 , R 4 , R 5 , R a , R b , n, m, p and q are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.

Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐，其中环A，环B，L，R 1，R 2，R 3，R 4，R 5，R a，R b，n，m，p和q为 其定义为作为类视黄醇相关孤儿受体γt（RORγt）的调节剂的活性。 这些化合物预防，抑制或抑制RORγt的作用，因此可用于治疗RORγt介导的疾病，病症，综合征或病症，例如疼痛，炎症，COPD，哮喘，类风湿性关节炎，结肠炎，多发性硬化， 牛皮癣，神经退行性疾病和癌症。

公开(公告)号：WO2008081282A2

公开(公告)日：2008-07-10

申请号：PCT/IB2007/004045

申请日：2007-12-19

Applicant: GLENMARK PHARMACEUTICALS S.A. ,  GHARAT, Laxmikant Atmaram ,  GAJERA, Jitendra, Maganbhai ,  FARANDE, Aniket, Vijaykumar ,  KADAM, Suresh, M. ,  CHAPALA, Kasturaiah ,  BHADANE, Shailendra

Inventor： GHARAT, Laxmikant Atmaram ,  GAJERA, Jitendra, Maganbhai ,  FARANDE, Aniket, Vijaykumar ,  KADAM, Suresh, M. ,  CHAPALA, Kasturaiah ,  BHADANE, Shailendra

IPC: C07D307/86 ,  C07D491/04

CPC classification number: C07D307/80 ,  C07D307/85 ,  C07D491/04

Abstract: The present invention relates to a process for the synthesis of N9-(3,5- dichloro-4-pyridyl)-6-difluoromethoxybenzo[4,5]furo[3,2-c]pyridine-9-carboxamide and salts thereof which are useful as a PDE4 inhibitor. The invention also relates to a process for the synthesis of methyl-2-formyl-7-cyclopentyloxybenzo[b]furan-4-carboxylate and salts thereof, which are useful as intermediates in preparing compounds with PDE4 inhibitory activity.

Abstract translation: 本发明涉及合成N9-（3,5-二氯-4-吡啶基）-6-二氟甲氧基苯并[4,5]呋喃并[3,2-c]吡啶-9-甲酰胺及其盐的方法，其中 可用作PDE4抑制剂。 本发明还涉及一种合成甲基-2-甲酰基-7-环戊氧基苯并[b]呋喃-4-羧酸甲酯及其盐的方法，其可用作制备具有PDE4抑制活性的化合物的中间体。

公开(公告)号：WO2018215668A1

公开(公告)日：2018-11-29

申请号：PCT/EP2018/063957

申请日：2018-05-28

Applicant: GLENMARK PHARMACEUTICALS S.A.

Inventor： PATEL, Vinod ,  REDDY, Venkateshwar ,  GHARAT, Laxmikant Atmaram ,  CHAUDHARI, Sachin Sundarlal ,  DAS, Sanjib ,  VELGALETI, Ranganadh ,  SHAH, Daisy Manish ,  BAJPAI, Malini

IPC: C07D498/04 ,  A61K31/4375 ,  A61K31/519 ,  A61P35/00

Abstract: The invention relates to novel inhibitors of MAP4K1 (HPK1) useful for the treatment of diseases or disorders characterised by dysregulation of the signal transduction pathways associated with MAPK activation, including hyperproliferative diseases, diseases of immune system dysfunction, inflammatory disorders, neurological diseases, and cardiovascular diseases. The invention further relates to pharmaceutical compositions comprising the same and methods of treatment of said diseases and disorders. The inhibitors are of formula (I) wherein the definitions for A, D, E, F, R 5 , R 6 , R 7 , Z, ring Q, n, x and y are as given in the application.

公开(公告)号：WO2018116285A1

公开(公告)日：2018-06-28

申请号：PCT/IB2017/058391

申请日：2017-12-23

Applicant: GLENMARK PHARMACEUTICALS S.A.

Inventor： LINGAM, V. S. Prasada Rao ,  GHARAT, Laxmikant Atmaram ,  KHAIRATKAR-JOSHI, Neelima ,  SHAH, Daisy Manish ,  BAJPAI, Malini

IPC: C07D295/155 ,  C07D413/04 ,  C07D417/04 ,  A61K31/5375 ,  A61K31/5377 ,  A61P3/10 ,  A61P11/06 ,  A61P17/06 ,  A61P17/00 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D417/04 ,  A61P3/10 ,  A61P11/06 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  C07D295/155 ,  C07D413/04

Abstract: The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, X1, X2, m and n are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORyt). These compounds prevent, inhibit, or suppress the action of RORyt and are therefore useful in the treatment of RORyt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer. (I)

公开(公告)号：WO2017037595A1

公开(公告)日：2017-03-09

申请号：PCT/IB2016/055104

申请日：2016-08-26

Applicant: GLENMARK PHARMACEUTICALS S.A.

Inventor： DAS, Sanjib ,  GHARAT, Laxmikant Atmaram ,  HARDE, Rajendra Laxman ,  SHELKE, Dnyaneshwar Eknath ,  PARDESHI, Shailesh Ramesh ,  THOMAS, Abraham ,  KHAIRATKAR-JOSHI, Neelima ,  SHAH, Daisy Manish ,  BAJPAI, Malini

IPC: C07C311/16 ,  A61K31/167 ,  A61P35/00

CPC classification number: C07C237/42 ,  C07B2200/07 ,  C07C2601/02

Abstract: The present disclosure is directed to novel carbocyclic compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R a , R b , n, m and p are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.

Abstract translation: 本公开涉及式（I）的新型碳环化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，R a，R b，n，m和p如本文所定义， 作为类视黄醇相关孤儿受体γt（RORγt）的调节剂。 这些化合物预防，抑制或抑制RORγt的作用，因此可用于治疗RORγt介导的疾病，病症，综合征或病症，例如疼痛，炎症，COPD，哮喘，类风湿性关节炎，结肠炎，多发性硬化， 牛皮癣，神经退行性疾病和癌症。