Alla Venkata Rama Rao - Hyderabad, IN Mukund S. Chorghade - Natick MA Amin ul Islam - Hyderabad, IN Vemuri Venkata Kiran Rao - Hyderabad, IN Anegondi Sreenivasa Prasad - Hyderabad, IN Batchu Venkateswara Rao - Nellore, IN Ranga Reddy - Andhra Pradesh, IN Lalata Krishnakanth Reddy - Andhra Pradesh, IN Kotakonda Shailaja - Andhra Pradesh, IN Mukund Keshao Gurjar - Pune, IN Sunil Vyankatesh Mhaskar - Natick MA
Assignee:
Millennium Pharmaceuticals, Inc. - Cambridge MA
International Classification:
C07D30702
US Classification:
549475
Abstract:
A method is provided for synthesizing diaryl-substituted heterocyclic compounds, particularly 2,5-diaryl-substituted tetrahydrofurans and tetrahydrothiophenes. Methods for synthesizing starting materials and intermediates are provided as well. An important application of the invention is in the synthesis of CMI-392, (Â)trans-2-[5-Nâ-methyl-Nâ-hydroxyureidyl-methyl)3-methoxy-4-p-chlorophenylthioethoxyphenyl]-5-(3,4,5-trimethoxyphenyl)-tetrahydrofuran, a highly effective agent in treating inflammatory and immune disorders. The invention also encompasses novel compounds useful as starting materials and intermediates in the synthetic processes disclosed.
Substituted Oxygen Alicyclic Compounds, Including Methods For Synthesis Thereof
Mukund Shankar Chorghade - Natick MA Mukund Keshao Gurjar - Pune, IN Palakodety Radha Krishna - Hyderabad, IN Sista Venkata Sai Lalitha - Sunnyvale CA Kashinath Sadalapure - Dt. Gulbarga, IN Susanta Sekhar Adhikari - West Bengal, IN Andappan Murugaiah Subbaiah Murugaiah - Tamilnadu, IN Batchu Venkateswara Rao - Nellore, IN Levadala Murali Krishna - Hyderabad, IN Sunil Vyankatesh Mhaskar - Natick MA Gangavaram Vasantha Madhava Sharma - Hyderabad, IN Tangallapally Rajendra Prasad - Warandal, IN Punna Sreenivas - Nalgonda, IN Vavilala Goverdhan Reddy - Mahabubnager, IN Aminul Islam - Hyderabad, IN Alla Venkata Rama Rao - Hyderabad, IN Hymavathi Lanka - Hyderabad, IN Bethi Sridhar Reddy - Hyderabad, IN Chittineni Hari Prasad - Hyderabad, IN
Assignee:
Millennium Pharmaceuticals, Inc. - Cambridge MA
International Classification:
C07D30702
US Classification:
549475, 549266, 549273, 549295, 549323, 549324
Abstract:
The invention provides new methods for preparation of cyclic oxygen compounds, including 2,5-disubstituted tetrahydrofurans, 2,6-disubstituted tetrahydropyrans, 2,7-disubstituted oxepanes and 2,8-oxocanes. The invention also provides new cyclic oxygen compounds and pharmaceutical compositions and therapeutic methods that comprise such compounds.
Substituted Oxygen Alicyclic Compounds, Including Methods For Synthesis Thereof
Mukund Shankar Chorghade - Natick MA Mukund Keshao Gurjar - Pune, IN Palakodety Radha Krishna - Hyderabad, IN Sista Venkata Sai Lalitha - Sunnyvale CA Kashinath Sadalapure - Dt. Gulbarga, IN Susanta Sekhar Adhikari - West Bengal, IN Andappan Murugaiah Subbaiah Murugaiah - Tamilnadu, IN Batchu Venkateswara Rao - Nellore, IN Levadala Murali Krishna - Hyderabad, IN Sunil Vyankatesh Mhaskar - Natick MA Gangavaram Vasantha Madhava Sharma - Hyderabad, IN Tangallapally Rajendra Prasad - Warangal, IN Punna Sreenivas - Nalgonda, IN Vavilala Goverdhan Reddy - Mahabubnagar, IN Aminul Islam - Hyderabad, IN Alla Venkata Rama Rao - Hyderabad, IN Hymavathi Lanka - Hyderabad, IN Bethi Sridhar Reddy - Hyderabad, IN Chittineni Hari Prasad - Hyderabad, IN
Assignee:
Millennium Pharmaceuticals, Inc. - Cambridge MA
International Classification:
C07D30512
US Classification:
549323
Abstract:
The invention provides new methods for preparation of cyclic oxygen compounds, including 2,5-disubstituted tetrahydrofurans, 2,6-disubstituted tetrahydropyrans, 2,7-disubstituted oxepanes and 2,8-oxocanes. The invention also provides new cyclic oxygen compounds and pharmaceutical compositions and therapeutic methods that comprise such compounds.
Methods Of Synthesis Of Substituted Tetrahydrofuran Compound
Mukund Shankar Chorghade - Natick MA Mukund Keshao Gurjar - Pune, IN Palakodety Radha Krishna - Hyderabad, IN Sista Venkata Sai Lalitha - Sunnyvale CA Kashinath Sadalapure - Dt. Gulbarga, IN Susanta Sekhar Adhikari - West Bengal, IN Andappan Murugaiah Subbaiah Murugaiah - Tamilnadu, IN Sunil Vyankatesh Mhaskar - Natick MA Gangavaram Vasantha Madhava Sharma - Hyderabad, IN Tangallapally Rajendra Prasad - Warangal, IN Punna Sreenivas - Nalgonda, IN Vavilala Goverdhan Reddy - Mahabubnagar, IN Aminul Islam - Hyderabad, IN Chittineni Hari Prasad - Hyderabad, IN Alla Venkata Rama Rao - Hyderabad, IN
Assignee:
Millennium Pharmaceuticals, Inc. - Cambridge MA
International Classification:
C07D30733
US Classification:
549323, 549497
Abstract:
The invention includes inter alia new methods for preparation of the pharmaceutically active compound 2-(4-fluorophenoxymethyl)-5-(4-N-hydroxyureidyl-1 -butynyl)-tetrahydrofuran and precursors thereof.
Synthesis Of 2-Alkylcysteine Via Substituted Thiazoline Amide
Rayomand H. Gimi - Chelmsford MA Mukund S. Chorghade - Natick MA Sunil V. Mhaskar - Natick MA
Assignee:
Genzyme Corporation - Cambridge MA
International Classification:
C07D27712
US Classification:
548201, 562557
Abstract:
Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. In one embodiment, the present invention relates to a method of preparing 2-alkylcysteine comprising condensing cysteine with an aryl nitrile to form a 2-arylthiazoline-4-carboxylic acid, forming a 2-arylthiazoline-4-amide using an amine group comprising at least one substituted or unsubstituted alkyl group that comprises one or more chiral carbon atoms, and alkylating at the 4-position of the thiazoline ring to form a 2-aryl-4-alkyl-thiazoline-4-amide. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In one embodiment, an aryl nitrile or imidate is condensed with cysteine or a 2-alkyl cysteine.
Synthesis Of 2-Alkylcysteine Via Substituted Thiazoline Ester
Rayomand H. Gimi - Chelmsford MA, US Mukund S. Chorghade - Natick MA, US Sunil V. Mhaskar - Natick MA, US
Assignee:
Genzyme Corporation - Cambridge MA
International Classification:
C07D277/04
US Classification:
548201, 548146, 562553, 562536
Abstract:
Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. In one embodiment, the present invention relates to a method of preparing a 2-alkylcysteine comprising condensing cysteine with an aryl nitrile to form a 2-arylthiazoline-4-carboxylic acid, esterifying the 2-arylthiazoline-4-carboxylic acid using a substituted or unsubstituted alcohol group comprising one or more chiral carbons, and alkylating at the 4-position of the thiazoline ring to form a 2-aryl-4-alkyl-thiazoline-4-carboxylic acid ester. The chiral templates present in the thiazoline carboxylic acid ester can provide face selectivity, and consequently desired stereochemistry, during the delivery of an alkyl group to the 4-position of the thiazoline ring. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In one embodiment, an aryl nitrile is condensed with cysteine or a 2-alkyl cysteine.
Method For Synthesizing Diaryl-Substituted Heterocyclic Compounds, Including Tetrahydrofurans
Alla Venkata Rama Rao - Hyderabad, IN Mukund Chorghade - Natick MA, US Amin ul Islam - Hyderabad, IN Vemuri Venkata Kiran Rao - Hyderabad, IN Anegondi Sreenivasa Prasad - Hyderabad, IN Batchu Venkateswara Rao - Nellore, IN Ranga Reddy - Mahaboobnagar District, IN Lalata Krishnakanth Reddy - Adilbad District, IN Kotakonda Shailaja - Hyderabad, IN Mukund Keshao Gurjar - Pune, IN Sunil Vyankatesh Mhaskar - Natick MA, US
International Classification:
C07D333/02 C 07D 3 7/04
US Classification:
549/029000, 549/059000, 549/429000
Abstract:
A method is provided for synthesizing diaryl-substituted heterocyclic compounds, particularly 2,5-diaryl-substituted tetrahydrofurans and tetrahydrothiophenes. Methods for synthesizing starting materials and intermediates are provided as well. An important application of the invention is in the synthesis of CMI-392, () trans-2-[5-(N′-methyl-N′-hydroxyureidyl-methyl)-3-methoxy-4-p-chlorophenylthioethoxyphenyl]-5-(3,4,5-trimethoxyphenyl)-tetrahydrofuran, a highly effective agent in treating inflammatory and immune disorders. The invention also encompasses novel compounds useful as starting materials and intermediates in the synthetic processes disclosed.
Poly(Potassium And Sodium Styrene Sulfonate), Its Manufacture And Its Uses
Sunil Mhaskar - Natick MA, US Hitesh Bhagat - Wayland MA, US Caroline Bacon Kurtz - Sudbury MA, US Sanjeev Katti - Acton MA, US Toni Chancellor-Adams - Watertown MA, US Mukund Chorghade - Natick MA, US
Assignee:
Genzyme Corporation - Cambridge MA
International Classification:
A61K031/74 C08F008/34
US Classification:
424078100, 525333500
Abstract:
Antibiotic-associated diarrhea, such as that caused by , represents a serious medical complication that can result from administering a broad-spectrum antibiotic to a subject. Such diarrhea leads to significant potassium loss from the subject. The present invention discloses a polymeric therapeutic agent that treats antibiotic-associated diarrhea and is physiologically potassium neutral. This polymer contains polystyrene sodium sulfonate and polystyrene potassium sulfonate repeat units.
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