Patents Assigned to Merck Sharp & Dohme B.V.
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Publication number: 20180079752Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.Type: ApplicationFiled: May 31, 2016Publication date: March 22, 2018Applicants: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME B.V.Inventors: ADRIANUS PETRUS ANTONIUS DE MAN, RONALD KIM, JIAN LIU, JOSEPH A. KOZLOWSKI, SOBHANA BABU BOGA, THIERRY FISCHMANN, DEODIAL Guy GUIADEEN, ILSE HENDRICA MARIA POLS-DE ROOIJ, SHILAN LIU, HAO WU
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Patent number: 9884043Abstract: The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.Type: GrantFiled: March 20, 2017Date of Patent: February 6, 2018Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme B.V.Inventors: Willem Frederik Johan Karstens, Mario Van Der Stelt, Jos Cals, Rita Corte Real Goncalves Azevedo, Kenneth Jay Barr, Hongjun Zhang, Richard Thomas Beresis, Dongshan Zhang, Xiaobang Duan
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Publication number: 20170342053Abstract: The present disclosure relates to forms of a CCR5 inhibitory compound, (4,6-dimethylpyrimidin-5-yl)(4-((3S)-4-((1R)-2-methoxy-1-(4-(trifluoromethyl)phenyl)ethyl)-3-methyl-piperazin-1-yl)-4-methylpiperidin-1-yl)methanone.Type: ApplicationFiled: November 11, 2015Publication date: November 30, 2017Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme B.V.Inventors: Alfred Y. LEE, William De WILDT
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Patent number: 9790226Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to Formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to Formula (I) in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.Type: GrantFiled: February 9, 2016Date of Patent: October 17, 2017Assignee: Merck Sharp & Dohme B.V.Inventors: Tjeerd A. Barf, Christiaan Gerardus Johannes Maria Jans, Adrianus Petrus Antonius de Man, Arthur A. Oubrie, Hans C. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan Gerard Sterrenburg, Jacobus C. H. M. Wijkmans
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Patent number: 9758524Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to Formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to Formula (I) in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.Type: GrantFiled: February 9, 2016Date of Patent: September 12, 2017Assignee: Merck Sharp & Dohme B.V.Inventors: Tjeerd A. Barf, Christiaan Gerardus Johannes Maria Jans, Adrianus Petrus Antonius de Man, Arthur A. Oubrie, Hans C. A. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan Gerard Sterrenburg, Jacobus C. H. M. Wijkmans
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Patent number: 9757552Abstract: The invention pertains to an applicator (1) for inserting an implant, in particular a rod-like implant (2) containing an active substance, under the skin of a human or animal, comprising a housing (3), a cannula (6), a cannula holder (9), an implant (2) accommodated inside the cannula (6) and/or the cannula holder (9), a protective cover (7) for the cannula (6), and a mechanism (22, 23, 7) which, at least after the cover (7) has been removed from the cannula (6), secures the implant (2) inside the cannula (6) and/or cannula holder (9). The mechanism (22, 23, 7) disengages the implant (2) during insertion of the cannula (6) or after the cannula (6) has been inserted. Substantially no lateral force will be exerted during the expelling of the implant from the cannula.Type: GrantFiled: January 20, 2006Date of Patent: September 12, 2017Assignee: MERCK SHARP & DOHME B.V.Inventors: Willem Jansen, Maurice Petrus Wilhelmus Tak, Hendricus Johannes Vertegaal, Iris Epkjen Hobo Van Der Graaf
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Patent number: 9718828Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.Type: GrantFiled: August 30, 2016Date of Patent: August 1, 2017Assignees: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME B.V.Inventors: Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Hans C. A. Raaijmakers, Allard Kaptein, Arthur A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C. H. M. Wijkmans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro
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Publication number: 20170202209Abstract: A mixing apparatus (1) for mixing slaughter offal with a preservative agent, the apparatus comprising an offal collection tank (3) with a bottom (4) provided with a discharge opening (5) connectable to a closable discharge, an agitator (8) extending into the offal collection tank, and a pump unit (9) operatively connectable to the discharge, wherein the apparatus further comprises a preservative reservoir (7) mounted on top of the collection tank (3). A collection and preservation system is provided, wherein the addition of preservation agent can be strictly controlled, can easily and quickly be installed and connected when it is to be used. After use, the system is easily removed and cleaned.Type: ApplicationFiled: February 25, 2016Publication date: July 20, 2017Applicant: Merck Sharp & Dohme B.V.Inventors: Adolph Bartholomeus Gijtenbeek, Harry van Tuijn, Marinus Johannes Gerardus Maria Ploegmakers
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Publication number: 20170157094Abstract: The invention is a pharmaceutical tablet formulation comprising between about 12.5 mg and 100 mg losartan potassium, between about 6.25 mg and about 50 mg chlorthalidone, and sodium bicarbonate in an amount between about 1.0% and about 10.0% by weight.Type: ApplicationFiled: November 24, 2014Publication date: June 8, 2017Applicant: Merck Sharp & Dohme B.V.Inventors: Jan-Piet Wijgergangs, Jocominus Antonius Maria Zwinkels, Albert Falivene Aldea
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Patent number: 9603838Abstract: The present invention relates to compounds according to Formula I or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.Type: GrantFiled: June 26, 2015Date of Patent: March 28, 2017Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme B.V.Inventors: Willem Frederik Johan Karstens, Mario Van Der Stelt, Jos Cals, Rita Corte Real Goncalves Azevedo, Kenneth Jay Barr, Hongjun Zhang, Richard Thomas Beresis, Dongshan Zhang, Xiaobang Duan
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Publication number: 20170008899Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.Type: ApplicationFiled: August 30, 2016Publication date: January 12, 2017Applicants: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME B.V.Inventors: ADRIANUS PETRUS ANTONIUS DE MAN, JAN-GERARD STERRENBURG, HANS C. A. RAAIJMAKERS, ALLARD KAPTEIN, ARTHUR A. OUBRIE, JOHANNES BERNARDUS MARI REWINKEL, CHRISTIAAN GERARDUS JOHANNES MARIA JANS, JACOBUS C.H.M. WIJKMANS, TJEERD A. BARF, ALAN B. COOPER, RONALD M. KIM, SOBHANA BABU BOGA, HUGH Y. ZHU, XIAOLEI GAO, XIN YAO, RAJAN ANAND, HAO WU, SHILAN LIU, CHUNDAO YANG, ABDUL-BASIT ALHASSAN, JAMES WANG, YOUNONG YU, JIAN LIU, HENRY M. VACCARO
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Patent number: 9540361Abstract: The present invention relates to novel N-substituted azetidine derivatives < of the formula (I); wherein SERMF is a Selective Estrogen Receptor Modilator fragment; X is no atom, O, S, CH2, carbonyl, N—R5; R1 is H, (C1-8)alkyl, (C3-8)cycloalkyl, (C3-6)heterocycloalkyl, (C2-6)alkenyl, (C2-6)alkynyl, (C1-4)alkylcarbonyl, (C1-4)alkoxy(C2-4)alkyl, (C3-6)cycloalkyl(C1-3)-alkyl, (C3-6)heterocycloalkyl(C1-3)alkyl, each independently optionally substituted with one or more halogen, nitrile, hydroxyl or (C1-2)alkyl; R5 is H, (C1-3)alkyl, optionally substituted with one or more fluorine; R17, R18 and R19 are independently of each other H, fluorine, nitrile or (C1-3)-alkyl, optionally substituted with one or more fluorine; or a prodrug, isotopically-labelled derivative or pharmaceutically acceptable salt thereof, > to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium canType: GrantFiled: December 16, 2011Date of Patent: January 10, 2017Assignee: Merck Sharp & Dohme B.V.Inventors: Fredericus Antonius Dijcks, Scott James Lusher, Herman Thijs Stock, Arthur Oubrie, Gerrit Herman Veeneman
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Publication number: 20160304606Abstract: Antibodies which block binding of hPD-1 to hPD-L1 or hPD-L2 and their variable region sequences are disclosed. A method of increasing the activity (or reducing downmodulation) of an immune cell through the PD-1 pathway is also disclosed.Type: ApplicationFiled: December 19, 2014Publication date: October 20, 2016Applicant: MERCK SHARP & DOHME B.V.Inventors: Gregory John Carven, Hans Van Eenenneem, Gradus Johannes Dulos
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Patent number: 9464108Abstract: The present invention relates to a synthesis route and to steroid derivatives of general formula VI and VII useful in the synthesis of desogestrel and etonogestrel.Type: GrantFiled: March 13, 2013Date of Patent: October 11, 2016Assignee: Merck Sharp & Dohme B.V.Inventor: Martin Ostendorf
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Patent number: 9290504Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Brutons Tyrosine Kinase (Btk) mediated disorders.Type: GrantFiled: July 11, 2012Date of Patent: March 22, 2016Assignee: Merck Sharp & Dohme B.V.Inventors: Tjeerd A. Barf, Christiaan Gerardus Johannes Maria Jans, Petrus Antonius De Adrianus Man, Arthur A. Oubrie, Hans C. A. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan-Gerard Sterrenburg, Jacobus C. H. M. Wijkmans
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Patent number: 9174940Abstract: The present invention relates the use of a compound, a pharmaceutical composition, compounds and a kit for treating or preventing disorders in a mammal responsive to TSH receptor mediated pathways, including disorders such as hyperthyroidism, Graves' disease, Graves Ophthalmopathy, Graves' associated pretibial dermopathy, nodular goitre and thyroid cancer comprising administering to said mammal an effective amount of a tetrahydroquinoline compound of Formula (I) or an pharmaceutically acceptable salt thereof.Type: GrantFiled: August 28, 2008Date of Patent: November 3, 2015Assignee: Merck Sharp & Dohme B.V.Inventors: Willem Frederik Johan Karstens, Paolo Giovanni Martino Conti, Cornelis Marius Timmers, Ralf Plate, Christianus Johannes Van Koppen
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Patent number: 9127007Abstract: The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.Type: GrantFiled: September 14, 2012Date of Patent: September 8, 2015Assignee: Merck Sharp & Dohme B.V.Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik
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Patent number: 9115126Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: GrantFiled: January 13, 2011Date of Patent: August 25, 2015Assignee: Merck Sharp & Dohme B.V.Inventors: Jiaqiang Cai, David Jonathan Bennett, Philip Stephen Jones
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Publication number: 20150232555Abstract: Antibodies which block binding of hPD-1 to hPD-L1 or hPD-L2 and their variable region sequences are disclosed. A method of increasing the activity (or reducing downmodulation) of an immune cell through the PD-1 pathway is also disclosed.Type: ApplicationFiled: December 19, 2014Publication date: August 20, 2015Applicant: MERCK SHARP & DOHME B.V.Inventors: Gregory John Carven, Hans Van Eenenneem, Gradus Johannes Dulos
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Patent number: 9108939Abstract: The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.Type: GrantFiled: October 26, 2010Date of Patent: August 18, 2015Assignee: Merck Sharp & Dohme B.V.Inventors: Andrew John Cooke, Emma Louise Carswell, David Jonathan Bennett